Compounds > celecoxib
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celecoxib

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Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that selectively inhibits the cyclooxygenase-2 (COX-2) enzyme. It is used to treat pain and inflammation in conditions such as osteoarthritis, rheumatoid arthritis, and acute pain. Celecoxib was first synthesized by scientists at Searle (now part of Pfizer) in the 1990s. It was approved by the U.S. Food and Drug Administration (FDA) in 1999. Celecoxib is a selective COX-2 inhibitor, meaning that it primarily targets COX-2, an enzyme that is involved in the production of prostaglandins, which are chemicals that cause pain and inflammation. COX-2 is also involved in the regulation of fever and blood clotting. By inhibiting COX-2, celecoxib reduces the production of prostaglandins, which helps to relieve pain and inflammation. Celecoxib is also studied for its potential to prevent colon cancer, as COX-2 is known to play a role in the development of this type of cancer. Celecoxib has been shown to be effective in treating pain and inflammation in a variety of conditions. However, it is important to note that celecoxib, like other NSAIDs, can cause side effects, such as stomach ulcers, heart attack, and stroke. It is important to talk to your doctor about the risks and benefits of celecoxib before taking it.'

Cross-References

ID SourceID
PubMed CID2662
CHEMBL ID118
CHEBI ID41423
SCHEMBL ID3708
MeSH IDM0276185

Synonyms (213)

Synonym
AC-4228
BIDD:GT0408
HY-14398
AB00052396-07
AB00052396-08
BRD-K02637541-001-02-4
AKOS015842517
benzenesulfonamide, 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]-
nsc-719627
ym177
sc58635
DIVK1C_000893
KBIO1_000893
NCI60_041049
tpi-336
solexa
onsenal
ai-525
celecox
cep-33222
ym-177
sc-58635 ,
SPECTRUM_000432
benzenesulfonamide, 4-(5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)-
celecoxib [usan]
IDI1_000893
BSPBIO_003596
SPECTRUM5_001324
MLS001304708
4-(5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide
p-(5-p-tolyl-3-(trifluoromethyl)pyrazol-1-yl)benzenesulfonamide
celebra
sc 58635
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]benzenesulfonamide
celocoxib
celebrex
ym 177
hsdb 7038
NCGC00091455-01
C07589
celecoxib ,
169590-42-5
184007-95-2
celecoxibum
CHEBI:41423 ,
bdbm11639
cid_2662
us8741944, comparative compound
1OQ5
chembl118 ,
DB00482
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]benzene-1-sulfonamide
nsc719627
celebrex (tn)
celecoxib (jan/usp/inn)
onsenal (tn)
D00567
CMAP_000027
NCGC00091455-02
NCGC00091455-03
KBIOGR_000723
KBIOSS_000912
KBIO3_002830
KBIO2_000912
KBIOSS_002354
KBIO2_007487
KBIOGR_002351
KBIO2_004919
KBIO2_002351
KBIO2_006048
KBIO2_003480
KBIO3_003037
SPECTRUM2_001576
SPECTRUM3_001996
SPECTRUM4_000182
SPBIO_001512
NINDS_000893
SPECTRUM1503678
NCGC00091455-04
MLS001165684
MLS001195656
smr000550473
UNM-0000305813
HMS2089L18
HMS2093I07
dfn15
dfn-15
nsc-758624
HMS502M15
HMS1922G14
4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-pyrazol-1-yl]benzenesulfonamide;4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]benzenesulfonamide
A25046
NCGC00091455-05
NCGC00091455-06
NCGC00091455-07
HMS3261A14
HMS3259L08
194044-54-7
NCGC00254540-01
tox21_201964
tox21_300599
NCGC00259513-01
pharmakon1600-01503678
BCP9000507
nsc758624
tox21_111135
cas-169590-42-5
dtxcid502777
dtxsid0022777 ,
HMS2234N18
CCG-39354
nsc 719627
unii-jcx84q7j1l
xilebao
jcx84q7j1l ,
celecoxib [usan:inn:ban]
nsc 758624
ccris 9330
4-[5-(p-tolyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
BCPP000290
FT-0623536
FT-0601628
NCGC00091455-08
STL373576
elyxyb
celecoxib [jan]
celecoxib [who-dd]
celecoxib [mi]
celecoxib [inn]
celecoxib component of consensi
consensi component celecoxib
celecoxib [usp monograph]
celecoxib [mart.]
celecoxib [orange book]
celecoxib [usp-rs]
celecoxib [hsdb]
celecoxib [ep monograph]
celecoxib [ema epar]
celecoxib [vandf]
AM84588
CS-0570
S1261
gtpl2892
HMS3373A09
BP-30217
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]-benzenesulfonamide
NC00708
BBL029086
SCHEMBL3708
tox21_111135_1
NCGC00091455-09
KS-1041
AB00052396-09
NCGC00261091-01
tox21_500406
4-(5-p-tolyl-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide
MLS006011862
Q-200816
4-(5-(p-tolyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide
5-(4-methylphenyl)-1-(4-sulfamoylphenyl)-3-(trifluoromethyl)pyrazole
C2816
AB00052396_11
AB00052396_10
mfcd00941298
J-520011
544686-20-6
EX-A175
SR-01000837528-3
sr-01000837528
SR-01000837528-2
celecoxib, united states pharmacopeia (usp) reference standard
HMS3654H09
celecoxib, european pharmacopoeia (ep) reference standard
celecoxib, >=98% (hplc)
celecoxib, pharmaceutical secondary standard; certified reference material
celecoxib 1.0 mg/ml in acetonitrile
J-010566
SBI-0051875.P002
HMS3715F11
NCGC00091455-13
SW199611-3
Q408801
4-[5-(p-tolyl)-3-(trifluoromethyl)-1-pyrazolyl]benzenesulfonamide
SY064976
FT-0700357
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-pyrazol-1-yl]benzenesulfonamide
celebcoxib
BCP02156
BRD-K02637541-001-06-5
EN300-119504
SB19318
HMS3867I03
HMS3884M07
benzenesulfonamide,4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl]-
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1h-pyazol-1-yl]benezenesulfonamide
4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonami de
celecoxib- bio-x
BC164295
Z1258938406
celecoxib (mart.)
l01xx33
celecoxib (usp monograph)
generic drug
celecoxib 400 mg
celecoxib 200 mg
celecoxib (usp-rs)
celecoxib 100 mg
celecoxib (ep monograph)
celecoxib 50 mg
elyxyb-celecoxib
m01ah01
celecixib

Research Excerpts

Overview

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) designed to be a selective cyclooxygenase-2 (COX-2) inhibitor. Celecoxib analogue 4f is a promising multi-targeted lead for the design and synthesis of potent anticancer agents.

ExcerptReferenceRelevance
"Celecoxib analogue 4f is a promising multi-targeted lead for the design and synthesis of potent anticancer agents."( Design and Synthesis of Novel Celecoxib Analogues with Potential Cytotoxic and Pro-apoptotic Activity against Breast Cancer Cell Line MCF-7.
Abdelhaleem, EF; El-Nassan, HB; Kassab, AE; Khalil, OM, 2022)		2.45
"Celecoxib is a selective inhibitor of COX-2."( The Importance of Drug Concentration at the Site of Action: Celecoxib and Colon Polyp Prevention as a Case Study.
Martinez, JA; Thompson, PA, 2022)		1.68
"Celecoxib is a commonly used nonsteroidal anti-inflammatory drug that selectively inhibits cyclooxygenase-2."( Improvement After Celecoxib Treatment in Patients with Thalamic Hemorrhage - A Case Report.
Jeng, JS; Lin, YW; Tang, SC; Tsai, LK; Yeh, SJ, 2022)		1.78
"Celecoxib (CLB) is a highly hydrophobic selective cyclo-oxygenase inhibitor with high plasma protein binding and undergoes extensive hepatic metabolism. "( Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation.
Alqahtani, A; Ather, H; Atiya, A; Begum, MY; Ghazwani, M; Hani, U; M Osmani, RA; Rahamathulla, M; Siddiqua, A, 2022)		2.42
"Celecoxib is a relatively safe, inexpensive, and widely available drug with non-steroidal anti-inflammatory properties. "( Short-term celecoxib (celebrex) adjuvant therapy: a clinical trial study on COVID-19 patients.
Abedipour, F; Ataee, M; Ghaznavi, H; Gorgani, F; Khorashad, ARS; Metanat, M; Mohammadghasemipour, Z; Mohammadi, M; Momeni, MK; Sargazi, S; Sartipi, M; Shahraki, O; Sheervalilou, R; Shirvaliloo, M, 2022)		2.55
"Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) designed to be a selective cyclooxygenase-2 (COX-2) inhibitor. "( Recent advances in the development of celecoxib analogs as anticancer agents: A review.
Abdelhaleem, EF; El-Nassan, HB; Kassab, AE; Khalil, OM, 2022)		2.44
"Celecoxib is a well-known selective cyclooxygenase-2 inhibitor for treating arthritis and relieving pain."( Celecoxib activates autophagy by inhibiting the mTOR signaling pathway and prevents apoptosis in nucleus pulposus cells.
Chen, W; Jiang, L; Lin, H; Lu, S; Wang, H; Wang, Z; Yasen, M; Zhuang, C, 2022)		2.89
"Celecoxib is a sulfanilamide nonsteroidal anti-inflammatory drug that can selectively inhibit cyclooxygenase-2 to inhibit prostaglandin production, achieving anti-inflammatory and analgesic effects. "( Bioequivalence of Celecoxib Capsules in Chinese Healthy Volunteers.
Chen, J; Dong, L; Fan, Y; Feng, J; Guan, R; He, J; Huang, H; Li, R; Long, S; Zhang, J; Zhao, M; Zou, W, 2023)		2.69
"Celecoxib is a selective cyclooxygenase-2 inhibitor widely used in patients with osteoarthritis and rheumatoid arthritis. "( Effects of Celecoxib on the QTc Interval: A Thorough QT/QTc Study.
Kim, JR; Kim, S; Ko, JW; Lee, H, 2019)		2.35
"Celecoxib is a selective cyclooxygenase (COX)-2 inhibitor that is commonly used to reduce the incidence of gastrointestinal (GI) complications in patients with rheumatoid arthritis (RA). "( Comparison of the efficacy and safety of CELBESTA® versus CELEBREX® in patients with rheumatoid arthritis: a 6-week, multicenter, double-blind, double-dummy, active-controlled, randomized, parallel-group, non-inferiority phase 4 clinical trial.
Choi, SJ; Choi, WH; Hong, SJ; Hur, JW; Kim, BY; Kim, GT; Kim, HS; Kim, SH; Kim, SS; Kim, YS; Lee, MS; Lee, SI, 2020)		2
"Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that can selectively target COX-2, suppress downstream pathways, and finally lead to anticancer potentiality."( MicroRNAs in the anticancer effects of celecoxib: A systematic review.
Bagheri, A; Khazeei Tabari, MA; Mishan, MA; Zargari, M, 2020)		1.55
"Celecoxib is a selective inhibitor of inducible cyclooxygenase-2 (COX-2) and is prescribed for the management of pain and other inflammatory disorders."( Lipid-based nanocarrier-mediated targeted delivery of celecoxib attenuate severity of ulcerative colitis.
Ahmad, A; Khan, R; Kumar, A; Mishra, RK; Raza, SS; Vyawahare, A, 2020)		1.53
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase-2 (COX-2) inhibitor. "( Tablet Formulation of a Synthesized Celecoxib Potassium Salt and Development of a Validated Method for Its Analysis.
Abualhasan, M; Shehab, KA; Shraim, N; Zatar, N, )		1.85
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) and a representative selective cyclooxygenase (COX)-2 inhibitor, which is commonly prescribed for osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute pain, and primary dysmenorrhea. "( Physiologically based pharmacokinetic (PBPK) modeling for prediction of celecoxib pharmacokinetics according to CYP2C9 genetic polymorphism.
Bae, JW; Cho, CK; Jang, CG; Jung, EH; Kang, P; Kim, YH; Lee, SY; Lee, YJ; Park, HJ, 2021)		2.3
"Celecoxib is a selective non-steroidal anti-inflammatory drug (NSAID)."( Celecoxib for osteoarthritis.
Marin, A; Markotic, F; Puljak, L; Tugwell, P; Utrobicic, A; Vrdoljak, D, 2017)		2.62
"Celecoxib is a selective non-steroidal anti-inflammatory drug (NSAID) used for treatment of people with rheumatoid arthritis."( Celecoxib for rheumatoid arthritis.
Fidahic, M; Jelicic Kadic, A; Puljak, L; Radic, M, 2017)		2.62
"Celecoxib (Cel) is a COX-2-selective nonsteroidal anti-inflammatory drug and its antitumoral effect has been shown widely in a variety of cancers including OS cells in vitro."( The potential combinational effect of miR-34a with celecoxib in osteosarcoma.
Chen, X; Huang, J; Liu, B; Peng, D; Shen, Y; Tao, H; Zhou, H, 2017)		1.43
"Celecoxib is a widely prescribed nonsteroidal anti-inflammatory drug, and has been associated with rare instances of idiosyncratic drug-induced liver injury (DILI). "( Celecoxib-induced Liver Injury: Analysis of Published Case Reports and Cases Reported to the Food and Drug Administration.
Chalasani, N; Fontana, RJ; Ghabril, M; Mukthinuthalapati, PK; Vuppalanchi, R, 2018)		3.37
"Celecoxib is an anti-inflammatory drug with antibacterial activity whose fate in surface water is unknown. "( Photochemical, thermal, biological and long-term degradation of celecoxib in river water. Degradation products and adsorption to sediment.
Jiménez, JJ; Muñoz, BE; Pardo, R; Sánchez, MI, 2018)		2.16
"Celecoxib (CXB) is a widely used anti-inflammatory drug that also acts as a chemopreventive agent against several types of cancer, including skin cancer. "( Liquid Crystalline Systems Based on Glyceryl Monooleate and Penetration Enhancers for Skin Delivery of Celecoxib: Characterization, In Vitro Drug Release, and In Vivo Studies.
Borgheti-Cardoso, LN; Dante, MCL; Fantini, MCA; Lara, MG; Medina, WSG; Pierre, MBR; Praça, FSG, 2018)		2.14
"Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX‑2), an enzyme of which the expression is induced by various stimuli, such as inflammation."( Cyclooxygenase-2 expression is induced by celecoxib treatment in lung cancer cells and is transferred to neighbor cells via exosomes.
Hong, SW; Hur, DY; Jin, DH; Kim, B; Kim, D; Kim, J; Kim, S; Kim, YS, 2018)		1.47
"Celecoxib is a non-steroidal anti-inflammatory drug that selectively inhibits cyclooxygenase-2 and is prescribed for severe pain and inflammation. "( Evaluation of the toxic effects of celecoxib on Xenopus embryo development.
Bae, YC; Cho, HJ; Chung, HY; Kim, JY; Lee, HS; Lee, S; Nam, SW; Park, MJ; Yoon, YH, 2018)		2.2
"Celecoxib is an inhibitor of cyclooxygenase-2, a gene that is often aberrantly expressed in the lung squamous cell carcinoma (LSQCC). "( Identification of key genes and long non‑coding RNAs in celecoxib‑treated lung squamous cell carcinoma cell line by RNA‑sequencing.
Gan, C; Li, G; Luo, Q; Wang, X, 2018)		2.17
"Celecoxib is an effective inhibitor of COX-2, used in anti-inflammation."( Celecoxib Conjugated Fluorescent Probe for Identification and Discrimination of Cyclooxygenase-2 Enzyme in Cancer Cells.
Cui, H; Du, J; Fan, J; Gurram, B; Li, H; Li, M; Peng, X; Wang, J; Xie, Y; Zhang, S, 2018)		2.64
"Celecoxib is a selective COX-2 inhibitor and has a lower effect of platelet aggregation compared with conventional non-steroidal anti-inflammatory drugs (NSAIDs)."( A Comparison of Analgesic Effect between Loxoprofen and Celecoxib and the Frequency of the Hemorrhage Following Tonsillectomy.
Ariki, M; Fukushima, N; Hirai, T; Miyahara, N; Yoshiga, A, 2016)		1.4
"Celecoxib (CEL) is a selective cyclooxygenase-2 (COX-2) inhibitor therapeutically indicated for the treatment of rheumatoid arthritis, osteoarthritis, acute pain, and inflammation. "( Preparation, characterization, and evaluation of celecoxib eutectic mixtures with adipic acid/saccharin for improvement of wettability and dissolution rate.
Abuzar, SM; Hong, SH; Hwang, SJ; Hyun, SM; Joo, Y; Kang, H; Kwon, KA; Lee, BJ; Lee, S; Velaga, S, 2019)		2.21
"Celecoxib has proven to be a very prominent member of this group with cytostatic activities."( Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.
Buzharevski, A; Hey-Hawkins, E; Laube, M; Lönnecke, P; Maksimovic-Ivanic, D; Mijatovic, S; Neumann, W; Paskas, S; Pietzsch, J; Sárosi, MB, 2019)		1.54
"Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat pain conditions in humans. "( Implication of K
Lopez-Garcia, JA; Rivera-Arconada, I; Vicente-Baz, J, 2019)		1.96
"Celecoxib is a COX-2 inhibitor drug that can be used to reduce the risk of colorectal adenocarcinoma. "( A nitrophenyl-based prodrug type for colorectal targeting of prednisolone, budesonide and celecoxib.
Gavin, J; Gilmer, JF; Kedziora, K; Kelleher, DP; Keogh, B; Marquez Ruiz, JF; Pigott, M; Windle, H, 2013)		2.05
"Celecoxib (Celebrex®) is a selective cyclooxygenase-2 (COX-2) inhibitor which exhibits antitumor effects in human HCC cells."( Novel combination of sorafenib and celecoxib provides synergistic anti-proliferative and pro-apoptotic effects in human liver cancer cells.
Azzolina, A; Bachvarov, D; Cervello, M; Cusimano, A; Lampiasi, N; McCubrey, JA; Montalto, G, 2013)		1.39
"Celecoxib is an anti-inflammatory drug that induces intracellular ROS generation."( Synergistic effects of 5-aminolevulinic acid based photodynamic therapy and celecoxib via oxidative stress in human cholangiocarcinoma cells.
Chung, CW; Jeong, YI; Kang, DH; Kim, CH; Kim, DH; Kwak, TW; Lee, HM, 2013)		1.34
"Celecoxib (CLX) is a highly hydrophobic cyclooxygenase-2 inhibitor that can reduce the incidence of colorectal polyps; however, the adverse cardiovascular effects limit its applicability."( In vitro characterization of a liposomal formulation of celecoxib containing 1,2-distearoyl-sn-glycero-3-phosphocholine, cholesterol, and polyethylene glycol and its functional effects against colorectal cancer cell lines.
Banerjee, S; Erdoğ, A; Keskin, D; Putra Limasale, YD; Tezcaner, A, 2013)		1.36
"Celecoxib is a selective Cox-2 inhibitor and has been widely used for treatment of several diseases."( Enhanced inhibition of urinary bladder cancer growth and muscle invasion by allyl isothiocyanate and celecoxib in combination.
Bhattacharya, A; Li, Y; Shi, Y; Zhang, Y, 2013)		1.33
"Celecoxib is an anti-inflammatory drug, specific inhibitor of COX-2, classified as a BCS class II compound due to its very low aqueous solubility (3 μg/mL) and good permeability."( Development of a chitosan-derivative micellar formulation to improve celecoxib solubility and bioavailability.
Bragagni, M; Di Cesare Mannelli, L; Furlanetto, S; Ghelardini, C; Mennini, N; Mura, P, 2014)		2.08
"Celecoxib is a widely used anti-inflammatory agent, with special use in rheumatoid arthritis."( Design and characterization of microcrystals for enhanced dissolution rate of celecoxib.
Kaza, R; Lakshmi, K; Reddy, MP, 2013)		1.34
"Celecoxib is a selective cyclo-oxygenase-2 (COX-2) inhibitor usually prescribed for the relief of chronic pain in osteoarthritis and rheumatoid arthritis."( Single dose oral celecoxib for acute postoperative pain in adults.
Derry, S; Moore, RA, 2013)		1.45
"Celecoxib (CEL), which is a BCS class II drug, was used as a model drug and loaded into FMS with different pore sizes by the solvent deposition method at a drug-silica ratio of 1:4."( Exploitation of 3D face-centered cubic mesoporous silica as a carrier for a poorly water soluble drug: influence of pore size on release rate.
Gao, Y; Jiang, T; Wan, L; Wang, S; Zhang, C; Zheng, X; Zhu, W, 2014)		1.12
"Celecoxib is a poorly water-soluble non-steroidal anti-inflammatory drug."( Impact of surfactants on the crystal growth of amorphous celecoxib.
Mosquera-Giraldo, LI; Taylor, LS; Trasi, NS, 2014)		1.37
"Celecoxib is a selective cyclooxygenase-2 (COX2) inhibitor. "( A trifluoromethyl analogue of celecoxib exerts beneficial effects in neuroinflammation.
Alloza, I; Chiba, A; Di Penta, A; Miyake, S; Vandenbroeck, K; Villoslada, P; Wyssenbach, A; Yamamura, T, 2013)		2.12
"Celecoxib is a selective COX-2 inhibitor and reported to prevent the progression of prostate cancer."( EP2 signaling mediates suppressive effects of celecoxib on androgen receptor expression and cell proliferation in prostate cancer.
Inokuchi, J; Kashiwagi, E; Naito, S; Shiota, M; Uchiumi, T; Yokomizo, A, 2014)		1.38
"Celecoxib is a selective inhibitor of COX-2, whose connection with the development and progression of human tumors has been extensively studied. "( Cyclooxygenase-2 inhibitor celecoxib suppresses invasion and migration of nasopharyngeal carcinoma cell lines through a decrease in matrix metalloproteinase-2 and -9 activity.
Gan, L; Hu, GQ; Hu, GY; Jiang, JZ; Li, WW; Liu, DB; Long, GX; Mei, Q; Sun, W; Wang, JF, 2014)		2.14
"Celecoxib is a well known non-steroidal anti-inflammatory drug (NSAID) and extensively employed for the treatment of arthritis. "( Three levels face centered central composite design of colon targeted micro-particulates system of celecoxib: screening of formulations variables and in vivo studies.
Dey, S; Mazumder, B; Nandy, BC; Verma, V, 2014)		2.06
"Celecoxib (CLX) is a poorly water soluble drug with its bioavailability being limited by its poor dissolution."( Comparing various techniques to produce micro/nanoparticles for enhancing the dissolution of celecoxib containing PVP.
Garekani, HA; Homayouni, A; Nokhodchi, A; Sadeghi, F; Varshosaz, J, 2014)		1.34
"Celecoxib is a potent nonsteroidal anti-inflammatory drug that has demonstrated promise in cancer chemoprevention and treatment. "( Celecoxib induces apoptosis via a mitochondria‑dependent pathway in the H22 mouse hepatoma cell line.
Chen, L; Kan, M; Li, J; Pan, Y; Qiao, P; Shao, D; Wang, Z; Xiao, X, 2014)		3.29
"Celecoxib is an effective analgesic in adult surgery patients; however, its analgesic efficacy on pain and functional recovery in pediatric A&T patients is unknown."( Celecoxib pharmacogenetics and pediatric adenotonsillectomy: a double-blinded randomized controlled study.
Aglipay, M; Lamontagne, C; MacCormick, J; McFaul, C; Murto, K; Ramakko, KA; Rosen, D; Vaillancourt, R, 2015)		2.58
"Celecoxib is a safe and effective treatment for depression due to brucellosis when compared with placebo."( Celecoxib for the treatment of mild-to-moderate depression due to acute brucellosis: a double-blind, placebo-controlled, randomized trial.
Akhondzadeh, S; Ashrafizadeh, SG; Entezari, P; Jafari, S; Rasoulinejad, M; Seddighi, S; Zeinoddini, A, 2015)		3.3
"Celecoxib is an effective adjuvant therapy in the treatment of manic episodes (without psychotic features) of bipolar mood disorder. "( Celecoxib adjunctive therapy for acute bipolar mania: a randomized, double-blind, placebo-controlled trial.
Akhondzadeh, S; Ameli, N; Arabzadeh, S; Farokhnia, M; Ghaleiha, A; Mohammadinejad, P; Rezaei, F; Zeinoddini, A, 2015)		3.3
"Celecoxib is a selective cyclooxygenase-2 inhibitor used extensively for the treatment of rheumatism and osteoarthritis. "( Influence of genetic polymorphisms on the pharmacokinetics of celecoxib and its two main metabolites in healthy Chinese subjects.
Ding, L; Gong, C; Liu, R; Ma, P; Tao, L; Yang, W; Zheng, X, 2015)		2.1
"Celecoxib is a cyclooxygenase 2 (COX2) inhibitor."( Celecoxib reduces glucocorticoids in vitro and in a mouse model with adrenocortical hyperplasia.
Berthon, A; Faucz, FR; Liu, S; Martinez, A; Sahut-Barnola, I; Saloustros, E; Salpea, P; Starost, MF; Stratakis, CA; Szarek, E, 2016)		2.6
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) that can decrease inflammation responses."( Release of celecoxib from a bi-layer biomimetic tendon sheath to prevent tissue adhesion.
Cui, W; Fan, C; Fan, D; Li, L; Ruan, H; Wu, D; Yu, S; Zheng, X, 2016)		1.55
"Celecoxib (CXB) is a Biopharmaceutical Classification System class II drug in which its oral bioavailability is limited by poor aqueous solubility. "( Solid Phospholipid Dispersions for Oral Delivery of Poorly Soluble Drugs: Investigation Into Celecoxib Incorporation and Solubility-In Vitro Permeability Enhancement.
Bauer-Brandl, A; Brandl, M; Fong, SY; Martins, SM, 2016)		2.1
"Celecoxib is a cyclooxygenase-2-specific inhibitor indicated to treat acute pain and pain secondary to osteoarthritis and rheumatoid arthritis. "( Celecoxib Versus Placebo in Tonsillectomy: A Prospective, Randomized, Double-Blind Placebo-Controlled Trial.
Bodeker, KL; Trask, DK; Van Daele, DJ, 2016)		3.32
"Celecoxib is a cyclooxygenase-2 (COX2) inhibitor."( Celecoxib treatment of fibrous dysplasia (FD) in a human FD cell line and FD-like lesions in mice with protein kinase A (PKA) defects.
Bhattacharyya, N; Collins, M; Leikin, S; Liu, S; Mertz, EL; Nesterova, M; Saloustros, E; Salpea, P; Starost, MF; Stratakis, CA, 2017)		2.62
"Celecoxib (CEL) is a nonsteroidal anti-inflammatory drug (NSAID) showing selective cycloxygenase-2 inhibition. "( Assessment of celecoxib poly(lactic-co-glycolic) acid nanoformulation on drug pharmacodynamics and pharmacokinetics in rats.
Denham, JW; Hanley, GA; Harirforoosh, S; Murrell, DE; Panus, PC; West, KO, 2016)		2.24
"Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). "( Formulation Optimization and Ex Vivo and In Vivo Evaluation of Celecoxib Microemulsion-Based Gel for Transdermal Delivery.
Cao, M; Chen, G; Ren, L, 2017)		2.14
"Celecoxib is a nonsteroidal anti-inflammatory drug inhibiting enzyme cyclooxygenase-2 (COX-2). "( Celecoxib is an inhibitor of enzyme acetylcholinesterase.
Pohanka, M, 2016)		3.32
"Celecoxib is a cyclooxygenase 2-selective nonsteroidal anti-inflammatory drug (NSAID) that exhibited therapeutic activity in cancer. "( TRAIL-mediated apoptosis in malignant glioma cells is augmented by celecoxib through proteasomal degradation of survivin.
Becker, MR; Ehemann, V; Gaiser, T; Habel, A; Rami, A; Reuss, DE; Siegelin, MD, 2008)		2.02
"Celecoxib is a specific inhibitor of cyclooxygenase 2 (COX2). "( Celecoxib potently inhibits TNFalpha-induced nuclear translocation and activation of NF-kappaB.
Funakoshi-Tago, M; Itoh, H; Kasahara, T; Nakamura, M; Shimizu, T; Sonoda, Y; Tago, K, 2008)		3.23
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used in the therapy of inflammatory and painful conditions. "( Celecoxib inhibits 5-lipoxygenase.
Angioni, C; Coste, O; Geisslinger, G; Groesch, S; Hoernig, M; Maier, TJ; Metzner, J; Pergola, C; Schmidt, R; Steinhilber, D; Tausch, L; Werz, O, 2008)		3.23
"Celecoxib is a selective cyclo-oxygenase-2 (COX-2) inhibitor prescribed for the relief of chronic pain in osteoarthritis and rheumatoid arthritis."( Single dose oral celecoxib for acute postoperative pain in adults.
Barden, J; Derry, S; McQuay, HJ; Moore, RA, 2008)		1.41
"Celecoxib (Celebrex) is a cyclooxygenase-2 (COX-2) selective inhibitor and gefitinib (Iressa(R), ZD1839) is a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor for human non-small cell lung cancer (NSCLC). "( The role of celecoxib in Rad51 expression and cell survival affected by gefitinib in human non-small cell lung cancer cells.
Ciou, SC; Hong, JH; Jhan, JY; Ko, JC; Lin, ST; Lin, YW; Wang, LH, 2009)		2.17
"Celecoxib is a potent anti-inflammatory drug with a safety profile that has been well-demonstrated in several human diseases and is reported to have beneficial effects in a rat model of intracerebral hemorrhage (ICH). "( Effects of celecoxib on volumes of hematoma and edema in patients with primary intracerebral hemorrhage.
Chu, K; Lee, SH; Park, HK; Roh, JK, 2009)		2.19
"Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) and blocks prostaglandin (PG) biosynthesis associated with inflammatory conditions. "( The analgesic actions of centrally administered celecoxib are mediated by endogenous opioids.
Bakhle, YS; de Francischi, JN; Dos Reis, WG; Duarte, ID; Lima, PP; Rezende, RM, 2009)		2.05
"Celecoxib is a selective cyclooxygenase-2-(COX-2)-inhibitor used to treat inflammation and pain and prevents colorectal cancer in patients at high doses by affecting several non-COX-2 proteins. "( Cellular membranes function as a storage compartment for celecoxib.
Angioni, C; Birod, K; Geisslinger, G; Glaubitz, C; Grösch, S; Hoffmann, M; Lopez, JJ; Maier, TJ; Schiffmann, S; Steinhilber, D; Wobst, I, 2009)		2.04
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) developed as a selective inhibitor of cyclooxygenase-2 (COX-2). "( Novel nitro-oxy derivatives of celecoxib for the regulation of colon cancer cell growth.
Bassignana, A; Bocca, C; Boschi, D; Bozzo, F; Gasco, A; Lazzarato, L; Miglietta, A, 2009)		2.08
"CLX (celecoxib) is a highly hydrophobic non-steroidal anti-inflammatory drug with high plasma protein binding. "( Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics.
Banerjee, S; Deniz, A; Keskin, D; Sade, A; Severcan, F; Tezcaner, A, 2010)		2.32
"Celecoxib is a nonsteroidal anti-inflammatory drug that selectively inhibits COX-2."( Cyclooxygenase-2 inhibition for the prophylaxis and treatment of preinvasive breast cancer in a her-2/neu mouse model.
Buttars, S; Done, SJ; Tran-Thanh, D; Wen, Y; Wilson, C, 2010)		1.08
"Celecoxib is an orally administered coxib."( [Selective inhibitors of cyclooxygenase-2 (COX-2), celecoxib and parecoxib: a systematic review].
Mateos, JL, 2010)		1.33
"Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX-2). "( The inhibitory effect of celecoxib on mouse hepatoma H22 cell line on the arachidonic acid metabolic pathway.
Chen, L; Lv, X; Xiang, D; Xu, Z; Zhang, M; Zhang, X, 2010)		2.11
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits cyclooxygenase-2 (COX-2). "( Celecoxib induces tolerance in a model of peripheral inflammatory pain in rats.
Bakhle, YS; Camêlo, VM; de Francischi, JN; Dos Reis, WG; Paiva-Lima, P; Rezende, RM, 2010)		3.25
"Celecoxib is a COX-2 inhibitor that has been related to an increased cardiovascular risk and that exerts several actions on different targets. "( Celecoxib blocks cardiac Kv1.5, Kv4.3 and Kv7.1 (KCNQ1) channels: effects on cardiac action potentials.
Alemanni, M; Cogolludo, A; David, M; González, T; Macías, A; Moral-Sanz, J; Moreno, C; Pérez-Vizcaíno, F; Valenzuela, C; Zaza, A, 2010)		3.25
"Celecoxib is a selective cyclooxygenase (COX)-2 inhibitor used to treat inflammation, while selenium is known to down-regulate the transcription of COX-2 and other pro-inflammatory genes. "( Synthesis and evaluation of the anti-inflammatory properties of selenium-derivatives of celecoxib.
Amin, S; Arner, RJ; Chen, G; D'Souza, C; Desai, D; El-Bayoumy, K; Gandhi, UH; Kaushal, N; Prabhu, KS; Vunta, H, 2010)		2.03
"Celecoxib is a drug designed to selectively inhibit COX-2, an inflammation-inducible cyclooxygenase isoform, over the constitutively expressed COX-1 isoform. "( Induction of a fast inactivation gating on delayed rectifier Shab K(+) channels by the anti-inflammatory drug celecoxib.
Arias-Olguin, II; Balleza, D; Barriga-Montoya, C; Carrillo, E; Gomez-Lagunas, F; Meza-Torres, B, )		1.79
"Celecoxib is a paradigmatic selective inhibitor of cyclooxygenase-2 (COX-2). "( Targeting apoptosis pathways by Celecoxib in cancer.
Jendrossek, V, 2013)		2.12
"Celecoxib is a potent nonsteroid anti-inflammatory drug (NSAID) that has demonstrated great promise in cancer chemoprevention and treatment. "( Inhibitory effect of celecoxib in lung carcinoma by regulation of cyclooxygenase-2/cytosolic phospholipase A₂ and peroxisome proliferator-activated receptor gamma.
Chen, L; Li, O; Li, W; Li, ZJ; Shao, D; Shi, Z; Wang, KZ; Xu, ZG; Zhang, M, 2011)		2.13
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used for the treatment of pain and inflammation. "( Characteristics and molecular basis of celecoxib modulation on K(v)7 potassium channels.
An, HL; Du, XN; Fu, Y; Gao, HX; Gao, ZB; Li, JW; Qi, JL; Wan, YM; Zhan, Y; Zhang, HL; Zhang, X, 2011)		2.08
"Celecoxib is a COX-2 inhibitor that reduces the risk of colon cancer. "( Celecoxib promotes c-FLIP degradation through Akt-independent inhibition of GSK3.
Cao, W; Chen, S; Hao, C; Khuri, FR; Sun, SY; Yue, P, 2011)		3.25
"Celecoxib would appear to be a useful option for therapy in patients at high risk for NSAID-induced GI toxicity, or in those responding suboptimally to or intolerant of NSAIDs."( Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
McCormack, PL, 2011)		2.53
"Celecoxib is a multifaceted drug with promising anticancer properties. "( Celecoxib and Bcl-2: emerging possibilities for anticancer drug design.
Payton-Stewart, F; Winfield, LL, 2012)		3.26
"Celecoxib is a cyclooxygenase-2 (COX-2)-specific inhibitor that downregulates ataxia telangiectasia and rad3-related (ATR) protein, an upstream kinase of Chk1."( Celecoxib enhances the radiosensitizing effect of 7-hydroxystaurosporine (UCN-01) in human lung cancer cell lines.
Jeong, IH; Kim, YM; Pyo, H, 2012)		2.54
"Celecoxib is a selective cyclo-oxygenase-2 (COX-2) inhibitor usually prescribed for the relief of chronic pain in osteoarthritis and rheumatoid arthritis."( Single dose oral celecoxib for acute postoperative pain in adults.
Derry, S; Moore, RA, 2012)		1.44
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor that has been reported to elicit anti-proliferative response in various tumors. "( Down-regulation of glucose-regulated protein (GRP) 78 potentiates cytotoxic effect of celecoxib in human urothelial carcinoma cells.
Chen, SC; Chiang, CK; Chuang, YT; Huang, KH; Kuo, KL; Liu, SH; Pu, YS; Tsai, YC; Weng, TI, 2012)		2.04
"Celecoxib is a clinically available COX-2 inhibitor that has been reported to have antineoplastic activity. "( Selective COX-2 inhibitor (celecoxib) decreases cellular growth in prostate cancer cell lines independent of p53.
Abdulkadir, SA; Chatla, C; Grizzle, WE; Katkoori, VR; Manne, K; Manne, U; Rodríguez-Burford, C; Shanmugam, C; Sthanam, M; Vital-Reyes, VS, 2013)		2.13
"Celecoxib (CXB) is a widely prescribed COX-2 inhibitor used clinically to treat pain and inflammation. "( The role of potassium channel activation in celecoxib-induced analgesic action.
Du, X; Gao, H; Huang, D; Li, L; Mi, Y; Qi, J; Zhang, F; Zhang, H; Zhang, X, 2013)		2.09
"Celecoxib is a newly developed cyclo-oxygenase (COX)-2 inhibitor with significantly less toxicity."( Antiangiogenic and chemopreventive activities of celecoxib in oral carcinoma cell.
Fuentes, CF; Shapshay, SM; Wang, Z, 2002)		1.29
"Celecoxib is a novel cyclooxygenase-2-specific inhibitor for the management of acute pain, primary dysmenorrhea, and the signs and symptoms of arthritis. "( Celecoxib does not affect the antiplatelet activity of aspirin in healthy volunteers.
Adler, R; Eskra, J; Noveck, R; Rushing, M; Vargas, R; Walden, C; Wilner, KD, 2002)		3.2
"Celecoxib is a novel selective cyclooxygenase-2 inhibitor, which is subject to extensive hepatic metabolism. "( Oxidation of celecoxib by polymorphic cytochrome P450 2C9 and alcohol dehydrogenase.
Eliasson, E; Höög, JO; Sandberg, M; Strömberg, P; Yasar, U, 2002)		2.13
"Celecoxib itself seems to be a valuable alternative drug in NSAID-sensitive patients."( Positive patch test reactions to celecoxib may be due to irritation and do not correlate with the results of oral provocation.
Boehncke, WH; Kaufmann, R; Kleinhans, M; Linzbach, L; Zedlitz, S, 2002)		1.32
"Celecoxib is a member of a novel group of agents that selectively inhibit cyclooxygenase 2 (COX-2). "( Single-dose and steady-state pharmacokinetics of celecoxib in children.
Baruchel, S; Gammon, J; Klein, J; Koren, G; Stempak, D, 2002)		2.01
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used to treat pain. "( A randomized, clinical trial comparing oral celecoxib 200 mg, celecoxib 400 mg, and ibuprofen 600 mg for acute pain.
Goldberg, J; Kenwood, A; Lavery, R; Salo, DF; Shapiro, T; Varma, V, 2003)		2.02
"Celecoxib is a safe alternative in subjects with previous adverse reactions to NSAIDs."( [The selective cyclooxygenase-2 inhibitor celecoxib is a safe alternative in patients with pseudo-allergic reactions to nonsteroidal anti-inflammatory drugs].
Ahlbach, S; Boehncke, WH; Kaufmann, R; Usadel, KH, 2003)		1.3
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor, COX-2 has been shown to be upregulated by convulsive nerve activity. "( Anticonvulsant action of celecoxib (alone and in combination with sub-threshold dose of phenytoin) in electroshock induced convulsion.
Malhotra, S; Pandhi, P; Shafiq, N, 2003)		2.07
"Celecoxib (Celebrex) is a COX-2 enzyme inhibitor and has emerged as a preferred therapeutic agent for the treatment of rheumatoid arthritis as compared to other NSAIDs."( The cox-2-specific inhibitor celecoxib inhibits adenylyl cyclase.
Gessell-Lee, DL; Peterson, JW; Saini, SS, 2003)		1.33
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor prescribed for the relief of chronic pain in osteoarthritis and rheumatoid arthritis. "( Single dose oral celecoxib for postoperative pain.
Barden, J; Edwards, JE; McQuay, HJ; Moore, RA, 2003)		2.1
"Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) which acts via specific inhibition of cyclooxygenase-2 (synthesis of prostaglandins mediating pathological inflammation) but which preserves the homeostatic action of cyclooxygenase-1. "( [Hypersensitivity to celecoxib].
Chiffoleau, A; Fradet, G; Huguenin, H; Robin-Le Nechet, A, 2003)		2.08
"Celecoxib (Celebrex) is a Cox 2 selective non steroidal anti-inflammatory agent. "( [Severe cutaneous drug reactions to celecoxib (Celebrex)].
Barbarot, S; Cassagnau, E; Foulc, P; Marquès, S; Milpied, B; Stalder, JF, 2003)		2.04
"Celecoxib may prove to be a very efficient component in the prevention and treatment of gastrointestinal tumors because it inhibits the growth of cancerous cells without affecting the growth of normal cells."( Celecoxib but not rofecoxib inhibits the growth of transformed cells in vitro.
Arber, N; Choen-Noyman, E; Deutsch, V; Dvory-Sobol, H; Kazanov, D; Kunik, T; Liberman, E; Pick, M; Strier, L, 2004)		3.21
"Celecoxib is a potent COX-2 inhibitor being developed for the treatment of rheumatoid arthritis and osteoarthritis."( Celecoxib: a potent cyclooxygenase-2 inhibitor in cancer prevention.
Abbasoglu, O; Akay, MT; Ercan, A; Kismet, K, 2004)		2.49
"Celecoxib is a new generation non-steroidal anti-inflammatory drug and sulfonamide derivative."( Celecoxib-induced photoallergic drug eruption.
Baz, K; Ikizoglu, G; Kokturk, A; Tataroglu, C; Uzumlu, H; Yazici, AC, 2004)		2.49
"Celecoxib, however, is a weak PDK-1 inhibitor (IC(50), 48 microM), requiring at least 30 microM to exhibit discernable effects on the growth of tumor cells in vitro."( From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors.
Chen, CS; Fowble, J; Huang, JW; Kulp, SK; Shaw, YJ; Shiau, CW; Tseng, PH; Yang, YT; Zhu, J, 2004)		1.32
"Celecoxib is a potential inhibitor of neointimal formation by blocking injury-induced Akt activation. "( Celecoxib, a cyclooxygenase-2 inhibitor, reduces neointimal hyperplasia through inhibition of Akt signaling.
Jeon, SI; Kim, HS; Kim, SH; Lee, MM; Oh, BH; Park, KW; Park, YB; Walsh, K; Yang, HM; You, HJ; Youn, SW, 2004)		3.21
"Celecoxib is a nonsteroidal antiinflammatory drug that selectively inhibits cyclooxygenase-2. "( Celecoxib-induced methemoglobinemia.
Banda, VR; Campo, NJ; Hayes, SD; Kaushik, P; Kaushik, R; Zuckerman, SJ, 2004)		3.21
"Celecoxib is a potent nonsteroid antiinflammatory drug (NSAID) that has shown great promise in cancer chemoprevention and treatment. "( Celecoxib derivatives induce apoptosis via the disruption of mitochondrial membrane potential and activation of caspase 9.
Chen, CS; D'Ambrosio, SM; Ding, H; Han, C; Zhu, J, 2005)		3.21
"Celecoxib is a hydrophobic and highly permeable drug belonging to class II of biopharmaceutics classification system. "( Formulation design of self-microemulsifying drug delivery systems for improved oral bioavailability of celecoxib.
Bhadra, R; Ghosal, SK; Moulik, SP; Ray, S; Subramanian, N, 2004)		1.98
"Celecoxib is a potent selective COX-2 inhibitor."( [A case report of disseminated malignant mesothelioma of peritoneum responding remarkably to thalidomide, celecoxib, vinorelbine and CDDP].
Hada, M; Kazuhiro, M, 2004)		1.26
"Celecoxib (CE) is a novel drug, with high selectivity and affinity for COX-2 enzyme."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.
D'Amato, G; D'Amato, M; Liccardi, G; Piccolo, A; Piscitelli, E; Salzillo, A; Senna, G, 2005)		1.45
"Celecoxib appears to be an alternative to traditional NSAIDs in the patient populations studied."( Assessing the cost-effectiveness of COX-2 specific inhibitors for arthritis in the Veterans Health Administration.
Botteman, M; DeLattre, M; Gao, X; Morreale, A; Schaefer, M; Stephens, J, 2005)		1.05
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor."( Gemcitabine plus celecoxib (GECO) in advanced pancreatic cancer: a phase II trial.
Amoroso, V; Ferrari, V; Grisanti, S; Marini, G; Marpicati, P; Nodari, F; Rangoni, G; Simoncini, E; Strina, C; Tiberio, GA; Valcamonico, F; Vassalli, L, 2006)		1.39
"Celecoxib is a potent inhibitor of tumor growth of secondary bone tumors in vivo which can be explained by its anti-angiogenic and pro-apoptotic effects. "( The selective Cox-2 inhibitor Celecoxib suppresses angiogenesis and growth of secondary bone tumors: an intravital microscopy study in mice.
Abdollahi, A; Ewerbeck, V; Gebhard, MM; Huber, PE; Klenke, FM; Sckell, A, 2006)		2.07
"Celecoxib (CE) is a novel drug, with high selectivity and affinity for COX-2 enzyme."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and other non-steroidal anti-inflammatory drugs.
Cazzola, M; D'Amato, G; D'Amato, M; De Giglio, C; Liccardi, G; Manfredi, D; Piscitelli, E, 2005)		1.45
"Celecoxib appears to be a more expensive therapeutic option than rofecoxib due to a relatively higher daily dose and tablet consumption."( Retrospective analysis of utilization patterns and cost implications of coxibs among seniors in Quebec, Canada: what is the potential impact of the withdrawal of rofecoxib?
Chabot, I; Hunsche, E; Rahme, E; Toubouti, Y, 2006)		1.78
"Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). "( Celecoxib inhibits interleukin-12 alphabeta and beta2 folding and secretion by a novel COX2-independent mechanism involving chaperones of the endoplasmic reticulum.
Alloza, I; Baxter, A; Chen, Q; Matthiesen, R; Vandenbroeck, K, 2006)		3.22
"Celecoxib is a potent selective COX-2 inhibitor."( [A case report of unresectable gallbladder cancer that responded remarkably to the combination of thalidomide, celecoxib, and gemcitabine].
Hada, M; Horiuchi, T; Shinji, H, 2006)		1.27
"Celecoxib is a cyclooxygenase-2 (COX-2) selective non-steroidal anti-inflammatory drug (NSAID) which has been shown to be capable of inhibiting the growth of various cancer cell lines. "( Celecoxib induces dose dependent growth inhibition in nasopharyngeal carcinoma cell lines independent of cyclooxygenase-2 expression.
Chan, AT; Chan, CM; Ma, BB; Wong, SC, 2005)		3.21
"Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) that is a critical factor in carcinogenesis, but precise mechanism of its action remains to be elucidated. "( Heterogeneous nuclear ribonuclear protein C is increased in the celecoxib-induced growth inhibition of human oral squamous cell carcinoma.
Kim, J; Kim, SH; Kwark, YE; Lee, EJ, 2006)		2.02
"Celecoxib is a cyclooxygenase-2 inhibitor with significantly less toxicity."( Chemopreventive effect of celecoxib in oral precancers and cancers.
Feng, L; Wang, Z, 2006)		1.36
"Celecoxib is a selective cyclooxygenase-2 inhibitor with antitumor and antiangiogenic activity. "( Celecoxib reduces microvessel density in patients treated with nasopharyngeal carcinoma and induces changes in gene expression.
Aggarwal, A; Goh, BC; Hsieh, W; Hsu, S; Lai, YF; Loh, KS; Low, JS; Mow, B; Putti, T; Soo, RA; Soon, WL; Tan, KB; Tan, L; Tan, P; Tao, Q; Wu, J, 2006)		3.22
"Celecoxib is an anti-cyclooxygenase-2 drug with anti-neoplastic properties."( Phase II study of an optimized 5-fluorouracil-oxaliplatin strategy (OPTIMOX2) with celecoxib in metastatic colorectal cancer: a GERCOR study.
André, T; Bidard, FC; de Gramont, A; Fellague-Chebra, R; Flesch, M; Hebbar, M; Louvet, C; Mabro, M; Mineur, L; Postel Vinay, S; Tournigand, C, 2007)		1.29
"Celecoxib is a highly selective inhibitor of cyclooxygenase-2 (COX-2), and inhibits osteoclastogenesis in vitro."( The selective cyclooxygenase-2 inhibitor celecoxib reduces bone resorption, but not bone formation, in ovariectomized mice in vivo.
Baylink, DJ; Itoi, E; Kasukawa, Y; Maekawa, S; Miyakoshi, N; Mohan, S; Nozaka, K; Srivastava, AK, 2007)		1.33
"Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used in the treatment of osteoarthritis and rheumatoid arthritis with fewer gastrointestinal toxicities compared to traditional non-steroidal anti-inflammatory drugs. "( Celecoxib inhibits Na+ currents in rat dorsal root ganglion neurons.
Kim, HI; Kim, TH; Lee, CS; Park, M; Park, SY; Shin, YK; Song, JH, 2007)		3.23
"Celecoxib is a non-steroidal anti-inflammatory drug that has been demonstrated to induce apoptosis in some cellular systems."( Apoptosis is not the major death mechanism induced by celecoxib on rheumatoid arthritis synovial fibroblasts.
Audo, R; Combe, B; Deschamps, V; Hahne, M; Morel, J, 2007)		1.31
"Celecoxib was found to be a moderately potent competitive inhibitor of CYP1A2 in vitro with a K(i) (inhibitor constant) of 25.4 microM. "( Celecoxib is a CYP1A2 inhibitor in vitro but not in vivo.
Backman, JT; Karjalainen, MJ; Neuvonen, PJ, 2008)		3.23
"Celecoxib is an NSAID that was developed as a selective inhibitor of COX-2 and approved by the FDA for the treatment of various forms of arthritis and the management of acute or chronic pain. "( Celecoxib analogs that lack COX-2 inhibitory function: preclinical development of novel anticancer drugs.
Chen, TC; Hofman, FM; Louie, SG; Petasis, NA; Schönthal, AH, 2008)		3.23
"Celecoxib is a frequently used nonsteroidal anti-inflammatory drug (NSAID) in the treatment of rheumatoid arthritis and osteoarthritis. "( The effects of some nonsteroidal anti-inflammatory drugs on experimental induced gastric ulcers in rats.
Batu, OS; Erol, K, 2007)		1.78
"Celecoxib is a cyclo-oxygenase (COX) inhibitor that exhibits relative in vitro and ex vivo selectivity for COX-2 over COX-1. "( Celecoxib: a review of its use in osteoarthritis, rheumatoid arthritis and acute pain.
Clemett, D; Goa, KL, 2000)		3.19
"Celecoxib (CEL) is a relatively new cyclooxygenase-2 specific inhibitor nonsteroidal anti-inflammatory drug with low incidents of the toxic side effects. "( Pharmacokinetics of celecoxib in the presence and absence of interferon-induced acute inflammation in the rat: application of a novel HPLC assay.
Guirguis, MS; Jamali, F; Sattari , S, )		1.9
"Celecoxib is a cyclooxygenase- (COX)-1-sparing inhibitor of COX-2 that is indicated for the treatment of osteoarthritis and rheumatoid arthritis. "( The hepatic safety and tolerability of the novel cyclooxygenase-2 inhibitor celecoxib.
Geis, GS; Maddrey, WC; Maurath, CJ; Verburg, KM, 2000)		1.98
"Celecoxib is a cyclooxygenase-2 specific inhibitor, that has been recently and intensively prescribed as an anti-inflammatory drug in rheumatic osteoarthritis. "( Liquid chromatographic-mass spectrometric determination of celecoxib in plasma using single-ion monitoring and its use in clinical pharmacokinetics.
Abdel-Hamid, M; Hamza, H; Novotny, L, 2001)		2
"Celecoxib is an effective anti-inflammatory, analgesic and antipyretic agent therapeutically utilised in the management of osteoarthritis and rheumatoid arthritis."( Celecoxib: a new option in the treatment of arthropathies and familial adenomatous polyposis.
Davies, NM; de Leeuw, MA; Gudde, TW, 2001)		2.47
"Celecoxib is a new cyclo-oxygenase-2 inhibitor recently approved for arthritis."( Celecoxib-induced Sweet's syndrome.
Berger, TG; Connolly, MK; Crowley, E; Fye, KH; LeBoit, PE, 2001)		2.47
"Celecoxib (Celebrex(R)) is a new generation non-steroidal anti-inflammatory drug, recently introduced in France. "( [Celecoxib induced toxiderma with positive patch-test].
Ajebbar, K; Caron, J; Charlanne, H; Modiano, P; Morant, C; Verbeiren, S, 2002)		2.67
"Celecoxib is an effective and safe chemopreventive agent in UV carcinogenesis. "( Celecoxib, a cyclooxygenase 2 inhibitor as a potential chemopreventive to UV-induced skin cancer: a study in the hairless mouse model.
Black, HS; Gerguis, J; Guevara, A; Lewis, AT; Orengo, IF; Phillips, R, 2002)		3.2

Effects

Celecoxib (CXB) has a good analgesic effect on postoperative acute pain, but clinically its compliance is compromised because of frequent administration. Celecoxib has a positive effect on human osteoarthritic cartilage, but the mechanisms remain unclear.

Celecoxib 200 mg has been reported to reduce pain following dental extraction but to offer poorer pain relief than active comparators. Celecoxib has also a possible involvement with redox homeostasis, because its administration caused changes in the activity of oxidative enzymes.

ExcerptReferenceRelevance
"Celecoxib (CXB) has a good analgesic effect on postoperative acute pain, but clinically its compliance is compromised because of frequent administration. "( Comparison of in vivo behaviors of intramuscularly long-acting celecoxib nanosuspensions with different particle sizes for the postoperative pain treatment.
Fu, Q; He, Z; Li, M; Qin, M; Sui, X; Sun, Y; Xin, J; Ye, G, 2023)		2.59
"Celecoxib has a significant inhibitory effect on postoperative aseptic inflammation."( Effect of Celecoxib on Surgical Site Inflammation after Total Knee Arthroplasty: A Randomized Controlled Study.
Liu, Y; Lu, H; Ma, J; Sang, W; Xu, X; Zhu, L, 2018)		2.33
"Celecoxib has a greater potency for AGI than diclofenac and its use is associated with a significantly higher AIX%. "( Aldosterone glucuronidation inhibition as a potential mechanism for arterial dysfunction associated with chronic celecoxib and diclofenac use in patients with rheumatoid arthritis.
Crilly, MA; Knights, KM; Mangoni, AA, )		1.78
"Celecoxib has a good therapeutic potential for MTC to prevent metastasis growth, and its anti-tumoral effect is, at least in part, independent of PGE(2)."( Anti-tumoral effect of a celecoxib low dose on a model of human medullary thyroid cancer in nude mice.
Cohen, R; Jullienne, A; Lausson, S; Lepoivre, M; Quidville, V; Segond, N; Tebbi, A, 2009)		2.1
"Celecoxib has a positive effect on human osteoarthritic cartilage, but the mechanisms remain unclear. "( Selective COX-2 inhibitor ameliorates osteoarthritis by repressing apoptosis of chondrocyte.
An, H; Jiang, D; Luo, X; Ou, Y; Quan, Z; Tan, C; Tang, K, 2012)		1.82
"Celecoxib has a potential role for oral cancer chemoprevention but its systemic side effects are a concern. "( Topical inhibition of oral carcinoma cell with polymer delivered celecoxib.
Polavaram, R; Shapshay, SM; Wang, Z, 2003)		2
"Celecoxib has a superior upper-gastrointestinal (GI) safety profile compared with nonselective nonsteroidal antiinflammatory drugs (NS-NSAIDs). "( Do proton-pump inhibitors confer additional gastrointestinal protection in patients given celecoxib?
Barkun, AN; Lelorier, J; Rahme, E; Rochon, S; Scalera, A; Toubouti, Y, 2007)		2
"Celecoxib has been reported to reduce the incidence of colorectal adenomas and CRC but is also associated with an increased risk of cardiovascular events."( Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Bachman, KE; Bonnette, WG; Chen, H; Connolly, PJ; Dallas, S; Diloreto, KA; Dong, Y; Edwards, JP; Evans, DC; Ghosh, A; King, P; Li, X; Liao, D; Pande, V; Patel, S; Pietrak, B; Sensenhauser, C; Shi, Y; Suarez, J; Szewczuk, L; Tian, G; Wang, J; Wilde, T; Zhang, Z, 2021)		1.34
"Oral celecoxib has been proved to be the best pharmacological intervention to ameliorate the skin lesions."( Pharmaceutical and clinical studies of celecoxib topical hydrogel for management of chemotherapy-induced hand-foot syndrome.
Afshar, M; Gharib, B; Jafariazar, Z; Ramezannia, F; Rezaeilaal, A; Shahi, F; Shayeganmehr, D, 2023)		1.63
"Celecoxib (CXB) has a good analgesic effect on postoperative acute pain, but clinically its compliance is compromised because of frequent administration. "( Comparison of in vivo behaviors of intramuscularly long-acting celecoxib nanosuspensions with different particle sizes for the postoperative pain treatment.
Fu, Q; He, Z; Li, M; Qin, M; Sui, X; Sun, Y; Xin, J; Ye, G, 2023)		2.59
"Celecoxib has been accounted to be an effective antitumor drug, but may exhibit significant side effects. "( ADT-OH synergistically enhanced the antitumor activity of celecoxib in human colorectal cancer cells.
Cai, F; Hua, ZC; Li, P; Ma, H; Sun, H; Tan, Y; Wang, X; Xu, H; Xu, J; Zhuang, H, 2023)		2.6
"Celecoxib has been effective in the prevention and treatment of chronic inflammatory disorders through inhibition of altered cyclooxygenase-2 (COX-2) pathways. "( Short-term supplementation of celecoxib-shifted butyrate production on a simulated model of the gut microbial ecosystem and ameliorated in vitro inflammation.
Calatayud Arroyo, M; Heiremans, E; Hernandez-Sanabria, E; Leclercq, L; Props, R; Snoeys, J; Van de Wiele, T, 2020)		2.29
"Celecoxib has low systemic bioavailability due to its low water solubility."( Tablet Formulation of a Synthesized Celecoxib Potassium Salt and Development of a Validated Method for Its Analysis.
Abualhasan, M; Shehab, KA; Shraim, N; Zatar, N, )		1.13
"Celecoxib has properties that should be evaluated in randomized controlled studies and is also available for off-label use."( COX2 inhibition in the treatment of COVID-19: Review of literature to propose repositioning of celecoxib for randomized controlled studies.
Aydin, SY; Baghaki, HS; Baghaki, S; Daghan, B; Yalcin, CE; Yavuz, E, 2020)		1.5
"Celecoxib has shown antitumor effects in preclinical models of human breast cancer, but clinical evidence is lacking."( Effect of Celecoxib vs Placebo as Adjuvant Therapy on Disease-Free Survival Among Patients With Breast Cancer: The REACT Randomized Clinical Trial.
Bartlett, J; Bliss, JM; Borley, A; Coleman, R; Coombes, RC; Denkert, C; Dibble, T; Evans, A; Grieve, R; Hicks, J; Kilburn, L; Kunze, CA; Loibl, S; Lu, XL; Makris, A; Mansi, J; Mehta, K; Mousa, K; Murray, E; Palmieri, C; Rautenberg, B; Rhein, U; Schmidt, M; Tovey, H; von Minckwitz, G, 2021)		1.75
"Celecoxib has been explored as a possible treatment of liver fibrosis with contradictory results, depending on the model."( Celecoxib Does Not Protect against Fibrosis and Inflammation in a Carbon Tetrachloride-Induced Model of Liver Injury.
Hammock, BD; Harris, TR; Hwang, SH; Imai, DM; Kodani, S; Rand, AA; Yang, J, 2018)		2.64
"Celecoxib has a significant inhibitory effect on postoperative aseptic inflammation."( Effect of Celecoxib on Surgical Site Inflammation after Total Knee Arthroplasty: A Randomized Controlled Study.
Liu, Y; Lu, H; Ma, J; Sang, W; Xu, X; Zhu, L, 2018)		2.33
"Celecoxib has proven to be a very prominent member of this group with cytostatic activities."( Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.
Buzharevski, A; Hey-Hawkins, E; Laube, M; Lönnecke, P; Maksimovic-Ivanic, D; Mijatovic, S; Neumann, W; Paskas, S; Pietzsch, J; Sárosi, MB, 2019)		1.54
"Celecoxib has low aqueous solubility, which may limit its tumor inhibiting effect."( Cyclooxgenase-2 inhibiting perfluoropoly (ethylene glycol) ether theranostic nanoemulsions-in vitro study.
Janjic, JM; Patel, SK; Pollock, JA; Zhang, Y, 2013)		1.11
"Celecoxib has a greater potency for AGI than diclofenac and its use is associated with a significantly higher AIX%. "( Aldosterone glucuronidation inhibition as a potential mechanism for arterial dysfunction associated with chronic celecoxib and diclofenac use in patients with rheumatoid arthritis.
Crilly, MA; Knights, KM; Mangoni, AA, )		1.78
"Celecoxib has also been evaluated in bladder cancer patients, but its efficacy against bladder cancer as a single agent remains unclear."( Enhanced inhibition of urinary bladder cancer growth and muscle invasion by allyl isothiocyanate and celecoxib in combination.
Bhattacharya, A; Li, Y; Shi, Y; Zhang, Y, 2013)		1.33
"Celecoxib has been shown to have antitumor effect in previous studies but the mechanisms are unclear. "( Celecoxib-induced increase in cytosolic Ca(2+) levels and apoptosis in HA59T human hepatoma cells.
Cheng, HH; Cheng, JS; Chi, CC; Chou, CT; Jan, CR; Kuo, CC; Liang, WZ; Liu, SI; Lu, T; Lu, YC; Tseng, LL, 2014)		3.29
"Celecoxib has been reported to switch the human SULT2A1-catalyzed sulfonation of 17β-estradiol (17β-E2) from the 3- to the 17-position. "( Celecoxib influences steroid sulfonation catalyzed by human recombinant sulfotransferase 2A1.
Ambadapadi, S; James, MO; Palii, SP; Wang, PL, 2015)		3.3
"Celecoxib and citrate have been shown to possess antitumor activity in a variety of cancer cells. "( Citrate and celecoxib induce apoptosis and decrease necrosis in synergistic manner in canine mammary tumor cells.
Farsinejad, A; Panahi, N; Safi, S; Vahidi, R, 2015)		2.24
"Celecoxib has been utilized with success in the treatment of several types of cancer, including gliomas."( Celecoxib and LLW-3-6 Reduce Survival of Human Glioma Cells Independently and Synergistically with Sulfasalazine.
Winfield, LL; Yerokun, T, 2015)		2.58
"Celecoxib has been found to be effective in cancer prevention and treatment. "( In-vitro and in-vivo inhibition of melanoma growth and metastasis by the drug combination of celecoxib and dacarbazine.
Averineni, RK; Guan, X; Sadhu, SS; Seefeldt, T; Wang, S; Yang, Y, 2016)		2.1
"Celecoxib has protective effects on sepsis due to its preservative effects on mesenteric perfusion, aortic function and its anti-inflammatory and antioxidative effects."( Celecoxib administration reduced mortality, mesenteric hypoperfusion, aortic dysfunction and multiple organ injury in septic rats.
Bariskaner, H; Goktas, MT; Iskit, AB; Kilinc, I; Ozer, EK; Ugurluoglu, C, 2017)		3.34
"Celecoxib (CXB) has been explored as an anti-inflammatory or chemopreventive drug for topical treatment of skin diseases and cancer."( In Vitro and In Vivo Evaluation of DMSO and Azone as Penetration Enhancers for Cutaneous Application of Celecoxib.
de Padula, M; Kibwila, DM; Lara, MG; Leitao, AC; Mata Dos Santos, HA; Padua, TA; Riemma Pierre, MB; Rosas, EC; Santos Pyrrho, AD; Senna, TD, 2017)		2.11
"Celecoxib has been shown to have antiangiogenic and antiproliferative properties."( uPA is upregulated by high dose celecoxib in women at increased risk of developing breast cancer.
Chen, YC; Flynn, JT; Hewett, JE; Kliethermes, B; Mannello, F; Qin, W; Rottinghaus, G; Sauter, ER; Zhu, W, 2008)		1.35
"Celecoxib has been associated with decreased gastrointestinal toxicity and improved chemotherapy tolerance in preclinical in vivo models, resulting in its investigation in CRC clinical trials."( Does celecoxib have a role in the treatment of patients with colorectal cancer?
Fakih, MG; Rustum, YM, 2009)		1.59
"Celecoxib has a good therapeutic potential for MTC to prevent metastasis growth, and its anti-tumoral effect is, at least in part, independent of PGE(2)."( Anti-tumoral effect of a celecoxib low dose on a model of human medullary thyroid cancer in nude mice.
Cohen, R; Jullienne, A; Lausson, S; Lepoivre, M; Quidville, V; Segond, N; Tebbi, A, 2009)		2.1
"Celecoxib has also a possible involvement with redox homeostasis, because its administration caused significant changes in the activity of oxidative enzymes, such as catalase and superoxide dismutase."( Celecoxib prevents tumor growth in an animal model by a COX-2 independent mechanism.
Acco, A; Ávila, TV; Bastos-Pereira, AL; Cadena, SM; Cristina da Silva de Assis, H; Donatti, L; Lugarini, D; Muscará, MN; Oliveira-Christoff, Ad; Pires, Ado R; Teixeira, S, 2010)		2.52
"Celecoxib has demonstrated an outstanding inhibitory effect on bladder cancer chemoprevention, which might be due to its expected anti-inflammatory actions, as well as by anti-proliferatory and antioxidant actions. "( Anti-inflammatory, anti-proliferative and antioxidant profiles of selective cyclooxygenase-2 inhibition as chemoprevention for rat bladder carcinogenesis.
Cunha, MF; Figueiredo, A; Garrido, P; Mota, A; Parada, B; Pinto, AF; Pinto, R; Reis, F; Sereno, J; Teixeira, F; Teixeira-Lemos, E, 2009)		1.8
"Celecoxib has now been shown to affect cellular physiology via an unexpected, COX-independent, pathway - by inhibiting K(v)2.1 and other ion channels."( Mechanisms of Kv2.1 channel inhibition by celecoxib--modification of gating and channel block.
Bondarenko, VE; Frolov, RV; Singh, S, 2010)		1.35
"Celecoxib has shown potential anticancer activity against most carcinomas, especially in patients with familial adenomatous polyposis and precancerous disease of the colon. "( The potential of celecoxib-loaded hydroxyapatite-chitosan nanocomposite for the treatment of colon cancer.
Azab, B; Dash, R; Fisher, PB; Kundu, SC; Mandal, M; Pathak, A; Prashanth Kumar, BN; Puvvada, N; Sarkar, D; Venkatesan, P, 2011)		2.15
"Celecoxib has been shown, by computer modeling, to bind STAT3 at the SH2 domain and competitively inhibit native peptide binding necessary for phosphorylation and subsequent propagation of the STAT3 signaling cascade."( Celecoxib inhibits STAT3 phosphorylation and suppresses cell migration and colony forming ability in rhabdomyosarcoma cells.
Li, C; Li, H; Lin, J; Reed, S, 2011)		2.53
"Celecoxib has reversal effect on MDR in MCF-7/Taxol cells, it's possible mechanism might be related to reduce the protein expression of COX-2, the inhibition of P-gp, BCRP mRNA and protein overexpression."( [Effect of combination of taxol and celecoxib on reversing multidrug resistance human breast cancer cells (MCF-7/ Taxol) and explore its underlying mechanism].
Chen, YJ; Liu, Q; Liu, XJ; Wang, J, 2011)		2.09
"Celecoxib has been shown to have an antitumor effect in previous studies, but the mechanisms are unclear. "( Effect of celecoxib on Ca(2+) handling and viability in human prostate cancer cells (PC3).
Chang, HT; Chen, IS; Cheng, JS; Chou, CT; Hsu, SS; Jan, CR; Kuo, CC; Liao, WC; Lin, KL; Liu, SI; Lu, YC; Tsai, JY; Wang, JL, 2012)		2.22
"Celecoxib has a positive effect on human osteoarthritic cartilage, but the mechanisms remain unclear. "( Selective COX-2 inhibitor ameliorates osteoarthritis by repressing apoptosis of chondrocyte.
An, H; Jiang, D; Luo, X; Ou, Y; Quan, Z; Tan, C; Tang, K, 2012)		1.82
"Celecoxib has recently been the subject of criticism for its side effects, mainly arterial thrombosis and renal hemorrhage, although it is considered a superior drug in protecting the gastrointestinal tract."( The cox-2-specific inhibitor celecoxib inhibits adenylyl cyclase.
Gessell-Lee, DL; Peterson, JW; Saini, SS, 2003)		1.33
"Celecoxib has a potential role for oral cancer chemoprevention but its systemic side effects are a concern. "( Topical inhibition of oral carcinoma cell with polymer delivered celecoxib.
Polavaram, R; Shapshay, SM; Wang, Z, 2003)		2
"Celecoxib has no effect on postoperative pain scores and PCA piritramide requirements. "( Effect of celecoxib and dexamethasone on postoperative pain after lumbar disc surgery.
Hussein, S; Karst, M; Kegel, T; Lüdemann, W; Lukas, A; Piepenbrock, S, 2003)		2.16
"Celecoxib has very low water solubility. "( Solubility enhancement of celecoxib using beta-cyclodextrin inclusion complexes.
Jain, SK; Rawat, S, 2004)		2.07
"Celecoxib has been shown to have antitumor effects that may be mediated through the cyclooxygenase-independent inhibition of Akt signaling. "( Celecoxib, a cyclooxygenase-2 inhibitor, reduces neointimal hyperplasia through inhibition of Akt signaling.
Jeon, SI; Kim, HS; Kim, SH; Lee, MM; Oh, BH; Park, KW; Park, YB; Walsh, K; Yang, HM; You, HJ; Youn, SW, 2004)		3.21
"Celecoxib has shown promising antitumor efficacy in lung cancer and a large variety of solid tumors that rely on COX-2-related mechanisms for growth and survival."( Celecoxib: a novel treatment for lung cancer.
Abou-Issa, H; Alshafie, G, 2004)		2.49
"Celecoxib has retarded COX-2 expression and delayed ulcer healing."( Cyclo-oxygenase-2 expression and prostaglandin E2 production in experimental chronic gastric ulcer healing.
Gautam, P; Poonam, D; Vinay, CS, 2005)		1.05
"Celecoxib has a superior upper-gastrointestinal (GI) safety profile compared with nonselective nonsteroidal antiinflammatory drugs (NS-NSAIDs). "( Do proton-pump inhibitors confer additional gastrointestinal protection in patients given celecoxib?
Barkun, AN; Lelorier, J; Rahme, E; Rochon, S; Scalera, A; Toubouti, Y, 2007)		2
"Celecoxib has been shown to reduce human colorectal cancers."( Activation of p38 mitogen-activated protein kinase by celecoxib oppositely regulates survivin and gamma-H2AX in human colorectal cancer cells.
Chang, CC; Chao, JI; Chiu, TH; Hsiao, PW; Liu, HF; Tsai, CM, 2007)		1.31
"Celecoxib has shown benefit in regressing colorectal adenomas and appears to have some duodenal activity as well."( Chemoprevention with special reference to inherited colorectal cancer.
Lynch, PM, 2008)		1.07
"Free celecoxib was found to have been extensively distributed to organs of the reticuloendothelial system such as the liver, lungs and spleen."( Enhanced retention of celecoxib-loaded solid lipid nanoparticles after intra-articular administration.
Kumar Sharma, R; Murthy, RS; Thakkar, H, 2007)		1.11
"Celecoxib has inhibitory effects on MMP-1, MMP-3 and NO productions, suggesting the protective roles directly on articular chondrocytes."( Celecoxib inhibits production of MMP and NO via down-regulation of NF-kappaB and JNK in a PGE2 independent manner in human articular chondrocytes.
Akiyoshi, M; Hiramitsu, T; Ito, H; Kitaori, T; Nakamura, T; Nishitani, K; Tsutsumi, R; Yasuda, T, 2008)		2.51
"Celecoxib 200 mg has been reported to reduce pain following dental extraction but to offer poorer pain relief than active comparators."( Analgesic efficacy of celecoxib in postoperative oral surgery pain: a single-dose, two-center, randomized, double-blind, active- and placebo-controlled study.
Cheung, R; Kowalski, K; Krishnaswami, S, 2007)		2.1
"Celecoxib has extremely poor aqueous wettability and dispersibility. "( Development of a rapidly dispersing tablet of a poorly wettable compound: formulation DOE and mechanistic study of effect of formulation excipients on wetting of celecoxib.
Barone, MR; He, X; Marsac, PJ; Sperry, DC, 2008)		1.98
"Celecoxib has been shown to be well tolerated, with incidences of adverse events similar to placebo in most instances."( Celecoxib, a COX-2--specific inhibitor: the clinical data.
Fort, J, 1999)		2.47
"Celecoxib also has been shown to be as effective as traditional NSAIDs in the treatment of rheumatoid arthritis, but it may cause fewer adverse effects, including endoscopically documented ulcers."( Selective cyclooxygenase-2 inhibitors for the treatment of arthritis.
Fung, HB; Kirschenbaum, HL, 1999)		1.02
"Celecoxib has shown significant equivalent anti-inflammatory and analgesic efficacy and has produced less endoscopically apparent gastrointestinal (GI) ulceration or erosion than have 3 classic NSAIDs."( Celecoxib, a selective cyclooxygenase-2 inhibitor for the treatment of rheumatoid arthritis and osteoarthritis.
Goldenberg, MM, 1999)		2.47
"Celecoxib has no significant effect on the pharmacokinetics or renal clearance of MTX in patients with RA, although these results should be confirmed in prospective studies of elderly and renally impaired patients."( Celecoxib, a specific COX-2 inhibitor, has no significant effect on methotrexate pharmacokinetics in patients with rheumatoid arthritis.
Geis, GS; Harper, KM; Hubbard, RC; Hunt, TL; Karim, A; Tolbert, DS, 1999)		3.19
"Celecoxib also has efficacy in treating the signs and symptoms of osteoarthritis of the hip."( Celecoxib: a review of its use in osteoarthritis, rheumatoid arthritis and acute pain.
Clemett, D; Goa, KL, 2000)		2.47
"Celecoxib has demonstrated interactions with fluconazole, lithium and warfarin."( Celecoxib: a new option in the treatment of arthropathies and familial adenomatous polyposis.
Davies, NM; de Leeuw, MA; Gudde, TW, 2001)		2.47
"Celecoxib has recently been approved for this indication and offers the potential for equivalent or greater efficacy than that seen with nonselective COX inhibitors but without the gastrointestinal mucosal toxicity and the inhibition of platelet function associated with those agents."( Approach to angiogenesis inhibition based on cyclooxygenase-2.
Masferrer, J, )		0.85
"Celecoxib and rofecoxib have been used in Norway since 2000. "( [A critical evaluation of side effect data on COX-2 inhibitors].
Pomp, E, 2002)		1.76
"Celecoxib has been approved for the management of familial adenomatous polyposis and is under investigation for the management of sporadic colorectal polyps and for its potential as a chemopreventive agent for other cancers."( Reducing the risk of colorectal cancer by intervening in the process of carcinogenesis: a status report.
Alberts, DS, )		0.85

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Celecoxib could inhibit tumor growth and enhance the antitumor effects of oxaliplatin through their synergistic role in inhibiting different targets. Celecoxib did not inhibit the progression of initiated HO in the patients in whom HO was diagnosed. Those who received celecoxib after surgery had lower morbidity.

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"Celecoxib did not inhibit the progression of initiated HO in the patients in whom HO was diagnosed, whereas those who received celecoxib after surgery had lower morbidity. "( Celecoxib cannot inhibit the progression of initiated traumatic heterotopic ossification.
Li, F; Mao, D; Mi, J; Pan, X; Rui, Y; Zhang, X, 2019)		3.4
"Celecoxib was shown to inhibit recombinant SULT1A1-catalyzed sulfonation of 10nM estrone and 4μM p-nitrophenol with IC"( Celecoxib affects estrogen sulfonation catalyzed by several human hepatic sulfotransferases, but does not stimulate 17-sulfonation in rat liver.
Ambadapadi, S; James, MO; Palii, SP; Wang, PL, 2017)		2.62
"Celecoxib did not increase cumulative WBA of standard TB drugs (mean cumulative WBA -0.10 ± 0.13ΔlogCFU versus -0.10 ± 0.12ΔlogCFU for TB drugs alone versus TB drugs and celecoxib; mean difference -0.01, 95% CI -0.02 to 0.00; p = 0.16)."( Adjunctive use of celecoxib with anti-tuberculosis drugs: evaluation in a whole-blood bactericidal activity model.
Gurumurthy, M; Hee, KH; Lee, LS; Lin, W; Lu, Q; Naftalin, CM; Paton, NI; Seng, KY; Tan, KH; Verma, R; Yeo, BCM; Yu, B, 2018)		1.54
"Celecoxib can enhance the antitumor effect of capecitabine by inhibiting the expressions of COX-2 and NF-ΚB p65 in mice bearing H22 implanted tumor."( [Inhibitory effects of celecoxib combined with capecitabine on H22 hepatoma mice and its mechanism].
Guo, HQ; Liu, YY; Yang, SJ; Yao, SN; Yao, ZH; Yuan, YD; Zhao, Y, 2013)		2.14
"Celecoxib could enhance the toxicity of VCR against KB/VCR cells. "( [Celecoxib enhances the chemotherapy sensitivity of KB/VCR cell lines to vincristine].
Li, W; Yan, Y, 2013)		2.74
"Celecoxib can inhibit proliferation and induce apoptosis in a dose- and time-dependent manner, repress telomerase activity, decrease hTERT mRNA and Bcl-2 protein expression and increase Bax protein expression, PGE2 had no effect on telomerase."( Antiproliferative effects of celecoxib in Hep-2 cells through telomerase inhibition and induction of apoptosis.
Chen, XM; Fan, XL; Feng, HW; Jia, T; Xu, AT; Zhang, H; Zhang, HL; Zhao, YQ, 2014)		2.14
"Celecoxib plays antitumor roles via multiple mechanisms in a variety of human cancers. "( Celecoxib exerts antitumor effects in canine mammary tumor cells via COX‑2‑independent mechanisms.
Asano, R; Kawashima, M; Murata, K; Saito, T; Tamura, D, 2015)		3.3
"Celecoxib can produce an anaphylactic reaction in patients who have previously tolerated sulfonamide antibiotics and who have previously tolerated celecoxib. "( Celecoxib-associated anaphylaxis.
Chamberlin, KW; Silverman, AR, 2009)		3.24
"Celecoxib could inhibit tumor growth and enhance the antitumor effects of oxaliplatin through their synergistic role in inhibiting different targets."( Synergistic inhibition effect of tumor growth by using celecoxib in combination with oxaliplatin.
Bian, H; Cai, J; Gui, L; Zhao, F; Zhao, S, 2009)		2.04
"Celecoxib could notably enhance the inhibitory effect of bleomycin on Tca8113 cells by blocking cell cycle progress and thus resulting in the increasing G(0)/G(1) cells [(60.93 +/- 0.32)%] distribution and inducing apoptosis [(1.87 +/- 0.11)%]."( [Celecoxib enhances the lethal effects of bleomycin in human tongue squamous carcinoma cell line Tca8113].
Ding, YQ; Li, WZ; Li, ZG; Wang, XY; Zhang, JH, 2009)		1.98
"Celecoxib can inhibit cell proliferation, regulate cell cycle and induce apoptosis, but the underlying mechanisms are still unclear. "( [Celecoxib promotes apoptosis of breast cancer cell line MDA-MB-231 through down-regulation of the NF-kappaB pathway].
Li, J; Liu, LH; Sang, MX; Shan, BE; Wang, L; Zhang, C, 2009)		2.71
"Celecoxib could inhibit MDA-MB-231 cell proliferation and promote cell apoptosis by down-regulating the NF-kappaB signaling pathway."( [Celecoxib promotes apoptosis of breast cancer cell line MDA-MB-231 through down-regulation of the NF-kappaB pathway].
Li, J; Liu, LH; Sang, MX; Shan, BE; Wang, L; Zhang, C, 2009)		2.71
"Celecoxib can inhibit the growth of human nasopharyngeal carcinoma cell line CNE-2 and induce the cell apoptosis, which may be related to blocking the cell cycle progress of CNE-2 cells."( [Effects of celecoxib on the proliferation and apoptosis of human nasopharyngeal carcinoma cell line CNE-2].
Du, J; Fu, X; Huang, Q; Li, D; Xu, X; Yi, F, 2009)		2.17
"Celecoxib can enhance apoptosis of GC cell by induction of NAG-1 gene transcription in human."( [Celecoxib inhibits gastric adenocarcinoma growth via inducing expression of human nonsteroidal anti-inflammatory drug activated gene].
Chen, JP; Ciren, YJ; Tang, CW; Wang, R; Yang, JL; Zhang, B, 2009)		2.71
"Celecoxib was found to inhibit the proliferation of H22 cells in a dose- and time-dependent manner."( The inhibitory effect of celecoxib on mouse hepatoma H22 cell line on the arachidonic acid metabolic pathway.
Chen, L; Lv, X; Xiang, D; Xu, Z; Zhang, M; Zhang, X, 2010)		1.39
"Celecoxib could inhibit PGE2 production of Tca8113 cell in a dose-dependent manner, down-regulate MMP-2 secretion of Tca8113 cell, and at the same time significantly inhibit invasion and adhesion ability of these cells."( Inhibitive effect of celecoxib on the adhesion and invasion of human tongue squamous carcinoma cells to extracellular matrix via down regulation of MMP-2 expression.
Huo, QJ; Li, WZ; Wang, XY; Xu, F, 2010)		1.4
"Celecoxib can inhibit the proliferation of Raji cells in a dose-dependent and time-dependent manner. "( [Effect of celecoxib and adriamycin on proliferation and apoptosis of Raji cells and its mechanism].
Fu, B; Huang, R; Huang, X; Li, X; Yang, X, 2010)		2.19
"Celecoxib did not inhibit proliferation of Y79 or Weri-RB1 cells, even at concentrations far exceeding clinically achievable levels. "( Effects of celecoxib in human retinoblastoma cell lines and in a transgenic murine model of retinoblastoma.
Grossniklaus, HE; Howard, SA; Lin, ET; O'Brien, JM; Shah, HR; Tong, CT; Van Quill, KR, 2005)		2.16
"Celecoxib can enhance the anti-proliferative effect of hydroxyurea on K562 cells, which is associated with the down-regulation of both COX-2 protein and COX-2 mRNA on K562 cells."( [Effect of celecoxib on enhancing the chemotherapic sensitivity of hydroxyurea to K562 cells and its mechanism].
Liu, DS; Zhang, GS, 2004)		2.16
"Celecoxib can inhibit proliferation and induce apoptosis of hepatoma cell strains in a dose- and time-dependent manner."( Overexpression of cyclooxygenase-2 in human HepG2, Bel-7402 and SMMC-7721 hepatoma cell lines and mechanism of cyclooxygenase-2 selective inhibitor celecoxib-induced cell growth inhibition and apoptosis.
Leng, J; Liu, NB; Pan, C; Peng, T; Shen, B; Yao, YY, 2005)		1.25
"Celecoxib could inhibit MR2 cell proliferation by inducing apoptosis, which might be mediated by the caspase-3 and 9 activation and PARP cleavage. "( [Celecoxib-induced apoptosis in acute promyelocytic leukemia cell line MR2 and its mechanism].
Huang, H; Xu, Y; Zhao, YM, 2007)		2.69
"Celecoxib can inhibit the proliferation of different liver cancer cell lines both in vitro and in vivo, and therefore may serve as an important candidate drug for prevention and treatment of hepatocellular carcinoma."( [Inhibitory effects of cyclooxygenase-2 inhibitor celecoxib on the proliferation of hepatocellular carcinoma cells].
Lin, QH; Liu, SC; Tang, BD; Zhou, Q, 2007)		2.04
"Celecoxib does not increase perioperative blood loss but reduces pain during the postoperative period after TKR. "( Effects of celecoxib on blood loss, pain, and recovery of function after total knee replacement: a randomized placebo-controlled trial.
Good, L; Lisander, B; Meunier, A, 2007)		2.17
"Celecoxib displays classic competitive kinetics on COX-1 (Ki=10-16 microM)."( Kinetic basis for selective inhibition of cyclo-oxygenases.
Gierse, JK; Isakson, PC; Koboldt, CM; Seibert, K; Walker, MC, 1999)		1.02

Treatment

Celecoxib/STZ treatments produced a significant loss of learning and memory. Celecoxib treatment led to significant improvement in the signs and symptoms of osteoarthritis. In celecoxib-treated animals, vasodilation in response to arachidonic acid was reduced.

ExcerptReferenceRelevance
"Celecoxib treatment can prevent inflamm-aging-induced TDSC senescence, which holds potential for alleviating the development of degenerative RCT."( Celecoxib, Beyond Anti-inflammation, Alleviates Tendon-Derived Stem Cell Senescence in Degenerative Rotator Cuff Tendinopathy.
Cai, Z; Liu, S; Liu, X; Zhang, Y, 2022)		3.61
"Celecoxib treatment was also associated with reduced phosphorylation of ribosomal protein S6 in myoblasts, and reduced phosphorylation of AKT, p70S6K, S6, and ERK in myotubes."( Celecoxib impairs primary human myoblast proliferation and differentiation independent of cyclooxygenase 2 inhibition.
Geddis, AV; Kolb, AL; Matheny, RW; Roberts, BM, 2022)		2.89
"Celecoxib treatment (100 mg/day) was initiated for local pain management."( Celecoxib as a Potential Treatment for Intractable Lymphatic Malformation.
Imamura, M; Kawamura, J; Kawano, Y; Nishikawa, T; Okamoto, Y; Yamasaki, Y; Yoneyama, T, 2019)		2.68
"The celecoxib treatment decreased such rats to 0, 0, 0, and 13.33%, respectively (p<0.05 compared to model group)."( Effect of celecoxib on protein expression of FAK and Cx43 in DMBA induced rat tongue carcinoma cells.
Guo, B; Li, YS; Shan, BZ; Sun, XF, 2019)		1.4
"Celecoxib treatment produces a 2.8-fold increase in calcification in ex vivo porcine aortic valve leaflets and a more than 2-fold increase in calcification in porcine aortic valve interstitial cells cultured in osteogenic media. "( Induction of aortic valve calcification by celecoxib and its COX-2 independent derivatives is glucocorticoid-dependent.
Butcher, JT; Byers, S; Donnelly, MP; Gee, TW; Ibrahim Aibo, MA; Vaidya, KA, )		1.84
"Celecoxib treatment decreased polyubiquitinated protein load and ER stress marker expression such as glucose-related protein 78 (GRP78), C/EBP (CCAAT/enhancer-binding protein) homologous protein (CHOP), and caspase 12 after 48 h of reperfusion."( Celecoxib-Dependent Neuroprotection in a Rat Model of Transient Middle Cerebral Artery Occlusion (tMCAO) Involves Modifications in Unfolded Protein Response (UPR) and Proteasome.
Anuncibay-Soto, B; Fernández-López, A; Font-Belmonte, E; González-Rodríguez, P; Pérez-Rodríguez, D; Santos-Galdiano, M; Ugidos, IF, 2021)		2.79
"Celecoxib treatment reduced osteoclast formation in apical periodontitis, regardless of the period of treatment (P < 0.0001 for 7 days and P = 0.026 for 14 days)."( Celecoxib treatment dampens LPS-induced periapical bone resorption in a mouse model.
Almeida-Junior, LA; Arnez, MFM; Faccioli, LH; Paula-Silva, FWG; Petean, IBF; Queiroz, AM; Silva, LAB; Silva, RAB, 2021)		2.79
"Celecoxib treatment resulted in delayed bone fracture healing, alterations in growth plate development and progression of mineralisation."( Impairment of the chondrogenic phase of endochondral ossification in vivo by inhibition of cyclooxygenase-2.
Caron, MM; Emans, PJ; Janssen, MP; Surtel, DA; van Rhijn, LW; van Rietbergen, B; Welting, TJ, 2017)		1.18
"Celecoxib treatment decreased the WDA incidence in the late response group."( Steroidal hormone and morphological responses in the prostate anterior lobe in different cancer grades after Celecoxib and Goniothalamin treatments in TRAMP mice.
Cagnon, VHA; Kido, LA; Montico, F; Pilli, RA; Silva, RS; Vendramini-Costa, DB, 2018)		1.41
"Celecoxib treatment also induced increases in utrophin A expression ranging from ∼1.5- to 2-fold in tibialis anterior diaphragm and heart muscles."( Celecoxib treatment improves muscle function in mdx mice and increases utrophin A expression.
Adam, NJ; Jasmin, BJ; Péladeau, C, 2018)		2.64
"Celecoxib treatment improved the neurologic deficit, reduced the infarct volume by 50% after 48 hours of reperfusion, and resulted in a reduced percentage of SNL areas and microglia and astroglia reactivity after 48 hours of reperfusion."( Celecoxib Treatment Improves Neurologic Deficit and Reduces Selective Neuronal Loss and Glial Response in Rats after Transient Middle Cerebral Artery Occlusion.
Anuncibay-Soto, B; Fernández-López, A; Font-Belmonte, E; Pérez-García, CC; Pérez-Rodríguez, D; Santos-Galdiano, M; Ugidos, IF, 2018)		2.64
"Celecoxib and anti-Gr1 treatment may be useful for blockade of these processes, thereby preventing brain metastasis in patients with breast cancer."( Premetastatic soil and prevention of breast cancer brain metastasis.
Fellows-Mayle, W; Ikeura, M; Kohanbash, G; Kosaka, A; Liu, Y; Okada, H; Snyder, LA, 2013)		1.11
"Celecoxib treatment greatly reduced the tortuous hepatic portal venules."( Celecoxib ameliorates portal hypertension of the cirrhotic rats through the dual inhibitory effects on the intrahepatic fibrosis and angiogenesis.
Gao, JH; Huang, ZY; Liu, ZX; Lu, YY; Tang, CW; Tong, H; Wen, SL; Yang, WJ, 2013)		2.55
"Celecoxib-IOL/PA-treated eyes had significantly less flare than PA-treated eyes, which had significantly less flare than bromfenac-treated eyes 24 h postoperatively. "( Efficacy of COX-2 inhibitors in controlling inflammation and capsular opacification after phacoemulsification cataract removal.
Brookshire, HL; English, RV; Gift, BW; Gilger, BC; Nadelstein, B; Weigt, AK, 2015)		1.86
"Celecoxib-IOL/PA-treated eyes showed better initial control of PCO (up to 12 weeks), while eyes receiving bromfenac had better long-term control of PCO (56 weeks)."( Efficacy of COX-2 inhibitors in controlling inflammation and capsular opacification after phacoemulsification cataract removal.
Brookshire, HL; English, RV; Gift, BW; Gilger, BC; Nadelstein, B; Weigt, AK, 2015)		1.14
"Celecoxib for the treatment of pain resulting from osteoarthritis (OA) was reviewed by the Tandvårds- och läkemedelsförmånsverket-Dental and Pharmaceutical Benefits Board (TLV) in Sweden in late 2010. "( A cost-effectiveness analysis of celecoxib compared with diclofenac in the treatment of pain in osteoarthritis (OA) within the Swedish health system using an adaptation of the NICE OA model.
Akehurst, R; Brereton, N; Ekelund, M; Pennington, B, 2014)		2.13
"Celecoxib treatment significantly increased the IC50 of carboplatin, suppressed carboplatin-induced caspase-3 and PARP cleavage and caspase-3 activity in EC109 and EC109/CDDP cells. "( [Celecoxib antagonizes the cytotoxic effect of carboplatin in human esophageal cancer cells].
Gu, C; Shi, L; Yu, L; Zhong, D, 2014)		2.76
"Celecoxib treatment prevented the losses in body mass and mass of retroperitoneal adipose tissue, gastrocnemius, and extensor digitorum longus muscles in tumor-bearing rats."( Effects of celecoxib and ibuprofen on metabolic disorders induced by Walker-256 tumor in rats.
Borba-Murad, GR; de Andrade, FG; de Fatima Silva, F; de Morais, H; de Souza, CO; de Souza, HM; Kurauti, MA, 2015)		1.53
"Celecoxib and ibuprofen treatment reversed the reduced production of glucose, pyruvate, lactate and urea from alanine as well as the reduced production of glucose from pyruvate and lactate in perfused liver from tumor-bearing rats. "( Celecoxib and Ibuprofen Restore the ATP Content and the Gluconeogenesis Activity in the Liver of Walker-256 Tumor-Bearing Rats.
Curi, R; de Morais, H; de Souza, CO; de Souza, HM; Hirabara, SM; Kurauti, MA; Rosa Neto, JC; Silva, Fde F, 2015)		3.3
"Celecoxib- treated OIR mice reduced the retinal neovascular tufts and the levels of VEGF and HIF-1α."( Celecoxib attenuates retinal angiogenesis in a mouse model of oxygen-induced retinopathy.
Cai, N; Chen, L; Liu, N, 2015)		2.58
"Celecoxib treatment improved social affiliation in the AlCl3‑induced neurotoxicity group, the results of which were superior to piroxicam."( Cyclooxygenase I and II inhibitors distinctly enhance hippocampal- and cortex-dependent cognitive functions in mice.
Ahmed, T; Ikram, MF; Syed, H; Yaqinuddin, A, 2015)		1.14
"Celecoxib treatment led to decreased PGE2 and corticosterone levels, reduced proliferation and increased apoptosis of adrenocortical cells, and decreased steroidogenic gene expression."( Celecoxib reduces glucocorticoids in vitro and in a mouse model with adrenocortical hyperplasia.
Berthon, A; Faucz, FR; Liu, S; Martinez, A; Sahut-Barnola, I; Saloustros, E; Salpea, P; Starost, MF; Stratakis, CA; Szarek, E, 2016)		2.6
"Celecoxib treatment may be a favorable treatment option for NASH."( Suppressing cyclooxygenase-2 prevents nonalcoholic and inhibits apoptosis of hepatocytes that are involved in the Akt/p53 signal pathway.
Cai, B; Cai, X; Chen, C; Chen, X; Guan, Y; Hu, H; Hu, X; Jing, X; Wang, Q; Wu, J, 2016)		1.16
"Celecoxib treatment was efficient in the regulation of COX2 in the TRAMP mice, mainly in the advanced disease grade."( Anti-inflammatory therapies in TRAMP mice: delay in PCa progression.
Cagnon, VH; Carvalho, JE; Costa, DB; Kido, LA; Macedo, AB; Minatel, E; Montico, F; Pilli, RA; Sauce, R, 2016)		1.16
"Celecoxib and SC19220 treatment did not modify the altered lumen diameter and wall : lumen ratio in mesenteric resistance arteries from SHR-infused and/or AngII-infused animals. "( Role of COX-2-derived PGE2 on vascular stiffness and function in hypertension.
Aguado, A; Alonso, MJ; Avendaño, MS; Beltrán, LM; Briones, AM; Cachofeiro, MV; García-Puig, J; González-Amor, M; Guillem-Llobat, P; Martínez-Revelles, S; Palacios, R; Salaices, M; Simões, MR; Vassallo, DV; Vila, L, 2016)		1.88
"Both celecoxib treatment groups were non-inferior to diclofenac."( Celecoxib versus diclofenac for the treatment of ankylosing spondylitis: 12-week randomized study in Norwegian patients.
Essex, MN; Li, C; Park, PW; Walker, C, 2016)		2.33
"Celecoxib treatment suppressed FGF-2 and FGFR-2 expression and decreased MMP-2, MMP-9 and p-ERK expression in the PANC-1 cells."( Celecoxib suppresses fibroblast growth factor-2 expression in pancreatic ductal adenocarcinoma PANC-1 cells.
Dong, L; Li, J; Luo, M; Shang, B; Wang, Y, 2016)		2.6
"The celecoxib-treated group experienced significantly more vomiting (celecoxib vs placebo p < 0.001 (Mann-Whitney test), confidence interval = 0.57 to 0.76)."( Is celecoxib a useful adjunct in the treatment of post-tonsillectomy pain in the adult population? A randomised, double-blind, placebo-controlled study.
De Silva, N; Diamantaras, D; Mahanta, V; Ng, TT; Priestley, J; Redman, J, 2017)		1.56
"The celecoxib pre-treated samples showed decreased expression levels in multiple genes involved in cellular lipid and glutathione metabolism; changes associated with diminished cellular proliferation."( Celecoxib pre-treatment in human colorectal adenocarcinoma patients is associated with gene expression alterations suggestive of diminished cellular proliferation.
Auman, JT; Church, R; Fleshman, JW; Lee, SY; Mcleod, HL; Watson, MA, 2008)		2.27
"Celecoxib treatment resulted in significantly altered expression levels of over 1,000 to 3,000 transcripts in these cell lines, respectively."( Altered gene expression profiles define pathways in colorectal cancer cell lines affected by celecoxib.
Ajaz, S; Ali, IU; Fatima, N; Greenwald, P; Munroe, DJ; Stauffer, S; Stephens, RM; Yi, M, 2008)		1.29
"Celecoxib treatment significantly reduced MPO activity, TBARS levels and the incidence of gastric cancer."( Celecoxib inhibits apurinic/apyrimidinic endonuclease-1 expression and prevents gastric cancer in Helicobacter pylori-infected mongolian gerbils.
Crowe, SE; Futagami, S; Gudis, K; Hamamoto, T; Horie, A; Kawagoe, T; Kusunoki, M; Miyake, K; Sakamoto, C; Shindo, T; Suzuki, K; Tsukui, T, 2008)		2.51
"Celecoxib treatment significantly reduced the volumes of edema noted on follow-up brain CT scans as compared with the volumes in the control group (30.2+/-17.7 vs."( Effects of celecoxib on volumes of hematoma and edema in patients with primary intracerebral hemorrhage.
Chu, K; Lee, SH; Park, HK; Roh, JK, 2009)		1.46
"Celecoxib treatment significantly decreased mRNA expression of COX-2, alpha-SMA, transforming growth factor beta1 (TGFbeta1) and collagen alpha1(I) in both models."( Celecoxib induces hepatic stellate cell apoptosis through inhibition of Akt activation and suppresses hepatic fibrosis in rats.
An, SH; Brenner, DA; Chon, CY; Han, KH; Kang, SH; Kim, DY; Kim, JK; Lee, DK; Lee, JI; Lee, KS; Lee, SI; Lee, SJ; Paik, YH, 2009)		2.52
"Celecoxib pretreatment before radiation caused strongly inhibited G(2) arrest."( Modulation of ionizing radiation-induced G2 arrest by cyclooxygenase-2 and its inhibitor celecoxib.
Choi, SA; Jun, HJ; Kim, YM; Lee, EJ; Park, JS; Park, SY; Pyo, H, 2009)		1.3
"Celecoxib treatment resulted in significant increase in apoptosis and early apoptotic rate."( [Effect of Celecoxib on cycloxygenase-2 expression and inducing apoptosis in Tca8113 cell lines].
Ding, YQ; Li, WZ; Wang, XY, 2009)		1.46
"Celecoxib treatment resulted in a significant reduction in the proliferation of H."( Short-term celecoxib intervention is a safe and effective chemopreventive for gastric carcinogenesis based on a Mongolian gerbil model.
Chang, LL; Hu, HM; Jan, CM; Kuo, CH; Tsai, PY; Wang, JY; Wang, WM; Wu, DC; Wu, IC; Yang, SF, 2009)		1.46
"Celecoxib treatment for 24 h also resulted in significantly decreased adhesion of Tca8113 cells on Fn-coated surface in a dose-dependent manner."( [Inhibitory effects of COX-2 inhibitor on migration of human tongue squamous cell carcinoma Tca8113 cells].
Huo, QJ; Li, WZ, 2009)		1.07
"Celecoxib treatment down-regulated the expression of vascular endothelial growth factor receptor (VEGFR)-3 in stromal tissues by 73.9%, and attenuated expression of podoplanin, a marker for lymphatic endothelial cells."( Host prostaglandin EP3 receptor signaling relevant to tumor-associated lymphangiogenesis.
Amano, H; Hayashi, I; Hosono, K; Ito, Y; Kamata, H; Kato, H; Kato, T; Kubo, H; Majima, M; Narumiya, S; Ogawa, Y; Sakagami, H; Sugimoto, Y; Suzuki, T; Watanabe, M, 2010)		1.08
"Oral celecoxib treatment inhibited BCC carcinogenesis in PTCH1(+/-) mice and had a significant anti-BCC effect in humans with less severe disease."( Basal cell carcinoma chemoprevention with nonsteroidal anti-inflammatory drugs in genetically predisposed PTCH1+/- humans and mice.
Aszterbaum, M; Athar, M; Barsanti, F; Bickers, DR; Cappola, C; Epstein, EH; Estevez, N; Hebert, J; Hwang, J; Khaimskiy, Y; Kim, A; Kohn, MA; Kopelovich, L; Lu, Y; McCulloch, CE; So, PL; Tang, JY; Tang, X, 2010)		0.82
"Celecoxib treatment significantly reduced CD133-positive cell migration and CCR2 expression levels."( Celecoxib inhibits CD133-positive cell migration via reduction of CCR2 in Helicobacter pylori-infected Mongolian gerbils.
Futagami, S; Gudis, K; Hamamoto, T; Horie, A; Kawagoe, T; Nagoya, H; Sakamoto, C; Shimpuku, M; Shindo, T, 2010)		2.52
"Celecoxib-treated rats had statistically significant decreases of cholesterol, total bilirubin, total protein, urea, globulin, blood urea nitrogen, phosphorus, and calcium."( Pathological and biochemical effects of therapeutic and supratherapeutic doses of celecoxib in Wistar albino male rats.
Akay, MT; Kismet, K; Koçkaya, EA; Selmanoğlu, G, 2010)		1.31
"Celecoxib treatment inhibited urinary excretion of PGEM by 50% or more in subjects with asthma and healthy controls, whereas there was no significant change in the excretion of PGDM. "( Effects of celecoxib on major prostaglandins in asthma.
Daham, K; Dahlén, B; Dahlén, SE; FitzGerald, GA; Gülich, A; Kupczyk, M; Lawson, JA; Song, WL, 2011)		2.2
"Celecoxib treatment had no effect on prostaglandin E(2) levels in the culture supernatants."( Expression and possible role of non-steroidal anti-inflammatory drug-activated gene-1 (NAG-1) in the human endometrium and endometriosis.
Cho, S; Choi, YS; Jeon, YE; Lee, BS; Nam, A; Seo, SK, 2010)		1.08
"Celecoxib-treated groups showed significantly fewer mice with lung metastases than non-celecoxib-treated groups."( Selective inhibition of cyclooxygenase-2 suppresses metastatic disease without affecting primary tumor growth in a murine model of Ewing sarcoma.
Edelman, M; Gendy, AS; Glick, RD; Lipskar, A; Soffer, SZ; Steinberg, BM, 2011)		1.09
"Celecoxib treatment decreased the incidence of EA in rats undergoing EJA with H."( Effect of Helicobacter pylori infection on Barrett's esophagus and esophageal adenocarcinoma formation in a rat model of chronic gastroesophageal reflux.
Gao, PP; Li, J; Liu, FX; Wang, J; Wang, WH, 2011)		1.09
"In celecoxib-treated zebrafish embryos, the heart failed to undergo normal looping and the heart valve was absent, causing serious blood regurgitation. "( Celecoxib impairs heart development via inhibiting cyclooxygenase-2 activity in zebrafish embryos.
Bu, JW; Du, JL; Gu, SY; Wang, YW; Xia, YM; Xu, DJ, 2011)		2.43
"Five celecoxib-treated patients experienced 6 serious adverse events with one of these events (rash) considered related to celecoxib."( Clinical characteristics and outcomes in familial adenomatous polyposis patients with a long-term treatment of celecoxib: a matched cohort study.
Bülow, S; Castells, A; Church, JM; Eagle, CJ; Gallinger, S; Gutierrez, LP; Huang, K, 2011)		1.04
"Celecoxib treatment resulted in significantly altered expression levels of 240 and 403 transcripts in Huh7 and HepG2 cells, respectively."( COX-2-dependent and COX-2-independent mode of action of celecoxib in human liver cancer cells.
Azzolina, A; Bachvarov, D; Cervello, M; Cusimano, A; Giannitrapani, L; Lampiasi, N; McCubrey, JA; Montalto, G; Sardina, F, 2011)		1.34
"Celecoxib treatment significantly down-regulated TNF-α induced NF-κB nuclear translocation, NF-κB DNA binding activity, and NF-κB-dependent reporter gene expression in U373 and T98G cells in a dose-dependent manner."( The nonsteroidal anti-inflammatory drug celecoxib suppresses the growth and induces apoptosis of human glioblastoma cells via the NF-κB pathway.
Babu, PP; Geeviman, K; Ramulu, C; Sareddy, GR, 2012)		1.37
"Celecoxib pretreatment radiosensitizes HeLa cells via a mechanism dependent on down-regulation of COX-2 and VEGF-C."( Celecoxib radiosensitizes the human cervical cancer HeLa cell line via a mechanism dependent on reduced cyclo-oxygenase-2 and vascular endothelial growth factor C expression.
Liu, H; Mi, JQ; Tian, XY; Wang, AH; Wang, RF; Yu, JJ, 2012)		3.26
"The celecoxib treatment also protected the mice from aortic rupture and death."( Effectiveness of cyclooxygenase-2 inhibition in limiting abdominal aortic aneurysm progression in mice correlates with a differentiated smooth muscle cell phenotype.
Gitlin, JM; Loftin, CD; Mukherjee, K, 2012)		0.86
"Celecoxib treatment was not statistically different than placebo for these latter two parameters."( A phase 2 study evaluating the efficacy and safety of a novel, proprietary, nano-formulated, lower dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012)		1.1
"Celecoxib was the only treatment to significantly reduce the number of lesions established per mouse, their size and vascularized area."( Anastrozole and celecoxib for endometriosis treatment, good to keep them apart?
Barañao, RI; Bilotas, MA; Meresman, GF; Olivares, CN; Ricci, AG, 2013)		1.46
"Celecoxib treatment activated Cdc25C and inhibited p21 expression in both unirradiated and irradiated cells, regardless of COX-2 expression."( Different cell cycle modulation by celecoxib at different concentrations.
Kim, YM; Pyo, H, 2013)		1.39
"Celecoxib-treated tumors showed reduced proliferation and increased apoptosis of both tumor and stromal cells compared with vehicle controls."( Direct evidence for a role of cyclooxygenase 2-derived prostaglandin E2 in human head and neck xenograft tumors.
Davis, TW; Masferrer, JL; Ornberg, RL; Zweifel, BS, 2002)		1.04
"Celecoxib treatment significantly delayed the onset of weakness and weight loss and prolonged survival by 25%."( Cyclooxygenase 2 inhibition protects motor neurons and prolongs survival in a transgenic mouse model of ALS.
Almer, G; Drachman, DB; Dykes-Hoberg, M; Frank, K; Przedborski, S; Rothstein, JD; Teismann, P, 2002)		1.04
"celecoxib-treated group, and 1500 p.p.m."( Chemopreventive effect of celecoxib and expression of cyclooxygenase-1 and cyclooxygenase-2 on chemically-induced rat mammary tumours.
Jang, TJ; Jung, HG; Jung, KH; O, MK, 2002)		1.34
"Celecoxib treatment inhibited VEGF mRNA expression without any significant reduction in cyclooxygenase-2 mRNA."( Celecoxib, a selective cyclooxygenase-2 inhibitor, inhibits retinal vascular endothelial growth factor expression and vascular leakage in a streptozotocin-induced diabetic rat model.
Ayalasomayajula, SP; Kompella, UB, 2003)		2.48
"Celecoxib treatment had no significant effect on the urinary concentrations of F2 isoprostane or thromboxane metabolites."( Short- and long-term COX-2 inhibition reverses endothelial dysfunction in patients with hypertension.
Duffy, SJ; Eberhardt, RT; Gokce, N; Holbrook, M; Keaney, JF; Maxwell, C; Morrow, JD; Palmisano, J; Price, DT; Vita, JA; Widlansky, ME, 2003)		1.04
"Celecoxib-treated A549 tumors had marginal reduction of total and perfused blood vessels compared with untreated controls."( Combination of radiation and celebrex (celecoxib) reduce mammary and lung tumor growth.
Chen, Y; Ding, I; Fenton, B; Finkelstein, J; Guo, M; Hu, D; Keng, P; Liang, L; Liu, W; Okunieff, P; Wang, W, 2003)		1.31
"Celecoxib-treated animals had less inflammation of the dermis compared with saline-treated controls."( Celecoxib reduces skin damage after radiation: selective reduction of chemokine and receptor mRNA expression in irradiated skin but not in irradiated mammary tumor.
Ding, I; Hu, D; Liang, L; Liu, W; Okunieff, P; Williams, JP, 2003)		2.48
"In celecoxib-treated PHN rats (group D) the mRNA expression of the EP3 and EP4 receptors was significantly reduced to 1.0-fold and 0.7-fold induction, respectively."( COX-2 inhibition and prostaglandin receptors in experimental nephritis.
Heering, P; Heise, G; Schrör, K; Waldner, C, 2003)		0.83
"Celecoxib-treated mice also developed fewer tumors (1.3 +/- 1.1 SD; P = 0.039 versus control) than the control mice (2.2 +/- 1.2) or the SC560 treated mice (2.3 +/- 1.3)."( The cyclooxygenase-2 inhibitor, celecoxib, prevents the development of mammary tumors in Her-2/neu mice.
Daskalakis, C; Flynn, J; Gallatig, K; Lanza-Jacoby, S; Masferrer, JL; Miller, S; Russo, IH; Sembhi, H; Zweifel, BS, 2003)		1.32
"In celecoxib-treated subjects, 2.6% developed ulcers compared with 17.9% of those treated with ibuprofen (P = 0.056). "( A randomized, controlled comparison of ibuprofen at the maximal over-the-counter dose compared with prescription-dose celecoxib on upper gastrointestinal mucosal injury.
Cryer, B; Kimmey, MB; Riff, DS; Rothstein, RI; Scheiman, JM; Wolfe, MM, 2004)		1.15
"Celecoxib treatment results in a reasonable cost-effectiveness ratio for patients with OA of the knee. "( Cost-effectiveness of treatment strategies for osteoarthritis of the knee in Taiwan.
Chen, LS; Chen, SC; Chen, WJ; Hou, SM; Lai, MS; Wang, CT; Yen, ZS, 2004)		1.77
"Celecoxib-treated rats recovered better by the behavioral tests at 7 days after ICH throughout the 28-day period, and the earlier the drug was administered, the better the functional recovery."( Celecoxib induces functional recovery after intracerebral hemorrhage with reduction of brain edema and perihematomal cell death.
Chu, K; Han, SY; Jeong, SW; Jung, KH; Kim, M; Lee, ST; Roh, JK, 2004)		2.49
"Celecoxib treatment initiating before polyposis (3.5-10 months) led to a dramatic reduction in tumor burden (86%) and was associated with decreased vascularity of the polyps."( Suppression of Peutz-Jeghers polyposis by inhibition of cyclooxygenase-2.
Järvinen, HJ; Katajisto, P; Lahesmaa, AM; Lepistö, A; Mäkelä, TP; Ristimäki, AP; Rossi, DJ; Udd, L; Ylikorkala, A, 2004)		1.04
"Celecoxib treatment decreased cell survival, activated caspase cascades, and increased DNA fragmentation, all of which were abrogated when caspase 8 expression was silenced with caspase 8 siRNA. "( Death receptor regulation and celecoxib-induced apoptosis in human lung cancer cells.
Khuri, FR; Liu, X; Sun, SY; Yue, P; Zhou, Z, 2004)		2.05
"Celecoxib treatment significantly decreased MCP-1 expression (P < 0.01)."( Celecoxib, a selective cyclooxygenase-2 inhibitor, decreases monocyte chemoattractant protein-1 expression and neointimal hyperplasia in the rabbit atherosclerotic balloon injury model.
Forudi, F; Keller, BT; Koki, AT; Lincoff, AM; Penn, MS; Smith, ME; Tarakji, K; Topol, EJ; Wang, K; Zhang, M; Zhou, X; Zhou, Z, 2005)		2.49
"One celecoxib-treated patient and 6 ketoprofen-treated patients ( P = 0.013) needed electrocautery to stop postoperative bleeding."( Celecoxib and ketoprofen for pain management during tonsillectomy: a placebo-controlled clinical trial.
Kokki, H; Linna, TJ; Nikanne, E; Salo, J, 2005)		2.25
"Celecoxib treatment improved the efficiency of the locomotor mechanism significantly. "( Celecoxib improves the efficiency of the locomotor mechanism in patients with knee osteoarthritis. A randomised, placebo, double-blind and cross-over trial.
De Nayer, J; Detrembleur, C; van den Hecke, A, 2005)		3.21
"Celecoxib treatment significantly suppressed viral reactivation when given prophylactically by the gastrointestinal route."( Inhibition of cyclooxygenase 2 synthesis suppresses Herpes simplex virus type 1 reactivation.
Gebhardt, BM; Kaufman, HE; Varnell, ED, 2005)		1.05
"Celecoxib-treated patients had significant decrease in nitrite levels (p = 0.043), whereas SOD, XO, GSH-Px enzyme activities, and MDA levels did not change significantly compared to baseline."( In vivo effect of celecoxib and tenoxicam on oxidant/ anti-oxidant status of patients with knee osteoarthritis.
Ardicoglu, O; Erdogan, H; Fadillioglu, E; Gudul, H; Ozgocmen, S, 2005)		1.38
"Celecoxib treatment inhibited COX-2 activity, indicated by prostaglandin E2 secretion, and caused significant growth arrest in both breast cancer cell lines."( Mechanisms underlying the growth inhibitory effects of the cyclo-oxygenase-2 inhibitor celecoxib in human breast cancer cells.
Basu, GD; Gendler, SJ; Mukherjee, P; Pathangey, LB; Tinder, TL, 2005)		1.27
"Celecoxib treatment significantly delayed the seizure attack and also reduced COX-2 expression."( Cyclooxygenase-2 expression and effect of celecoxib in flurothyl-induced neonatal seizure.
Jang, TJ; Kim, DK, 2006)		1.32
"Celecoxib treatment induced Bak expression, whereas cell transfected with siGADD153 showed lower levels of celecoxib-induced Bak upregulation."( GADD153 mediates celecoxib-induced apoptosis in cervical cancer cells.
Hwang, CI; Kim, SH; Lee, JH; Park, WY; Song, YS, 2006)		1.39
"Celecoxib treatment was started at tumor induction."( Cutaneous and intra-abdominal abscess formation in rats following radio frequency [corrected] ablation of liver tumors in combination with celecoxib treatment.
De Heer, P; Ensink, GN; Koudijs, MM; Kuppen, PJ; Putter, H; Sandel, MH; Speetjens, FM; Van de Velde, CJ, )		1.05
"Celecoxib treatment initially suppressed COX-2 and prostaglandin E2 (PGE2) expression, but long-term use produced significantly higher levels of these molecules and reactivated PGE2-associated growth factor signaling pathways in tumor and normal tissues."( Changes in antitumor response in C57BL/6J-Min/+ mice during long-term administration of a selective cyclooxygenase-2 inhibitor.
Bertagnolli, MM; Carothers, AM; Cho, NL; Moran, AE; Redston, M, 2006)		1.06
"In celecoxib-treated mice, interferon-gamma (IFN-gamma) production from MOG-specific T cells was reduced and MOG-specific IgG1 was elevated compared with vehicle-treated mice."( Selective COX-2 inhibitor celecoxib prevents experimental autoimmune encephalomyelitis through COX-2-independent pathway.
Kusunoki, S; Miyake, S; Miyamoto, K; Mizuno, M; Oka, N; Yamamura, T, 2006)		1.15
"Celecoxib treatment inhibited the development of large intestinal cancers in mice sacrificed at 26 or 35 weeks after the first injection of the carcinogen."( Inhibition of large intestinal cancers by celecoxib using a serial sacrifice technique.
Coles, M; Toth, B, )		1.12
"Also celecoxib treatment brought about an increase in glycolipid content."( Effects of non steroidal anti-inflammatory drugs on the antioxidant defense system and the membrane functions in the rat intestine.
Kanwar, SS; Nair, P; Sanyal, SN, )		0.59
"Celecoxib treatment induced Bak expression, whereas cell treated with siGADD153 or TPCK showed lower levels of celecoxib-induced Bak up-regulation."( GADD153 mediates celecoxib-induced apoptosis in cervical cancer cells.
Hwang, CI; Juhnn, YS; Kim, SH; Lee, JH; Park, WY; Song, YS, 2007)		1.4
"Celecoxib-treated tumors were less vascular with increased apoptosis."( Celecoxib inhibits meningioma tumor growth in a mouse xenograft model.
Couldwell, WT; Gillespie, DL; Jensen, RL; Prescott, SM; Ragel, BT, 2007)		2.5
"Celecoxib treatment at a dose of 4 mg/kg/day reduced fracture callus prostaglandin E2 and F(2alpha) levels by >60%."( Dose and time-dependent effects of cyclooxygenase-2 inhibition on fracture-healing.
O'Connor, JP; Simon, AM, 2007)		1.06
"Celecoxib treatment decreased angiopoietin-2 and VEGF levels as well as germinal matrix endothelial proliferation."( Angiogenic inhibition reduces germinal matrix hemorrhage.
Ballabh, P; Braun, A; Csiszar, A; Goldman, SA; Hu, F; Lou, N; Nedergaard, M; Rivera, A; Smith, K; Ungvari, Z; Xu, H, 2007)		1.06
"Celecoxib treatment did not increase intracellular oxidation of 2',7'-dichlorofluorescin in myocytes, which suggested that its cytotoxicity was not due to reactive oxygen species generation."( The cytotoxicity of celecoxib towards cardiac myocytes is cyclooxygenase-2 independent.
Hasinoff, BB; Patel, D; Wu, X, 2007)		1.38
"Celecoxib treatment induced apoptosis of murine lupus T cells in vitro, which was inhibited by z-VAD-fmk, a pan-caspase inhibitor."( Apoptosis of murine lupus T cells induced by the selective cyclooxygenase-2 inhibitor celecoxib: molecular mechanisms and therapeutic potential.
Gao, XM; Ping, L; Yang, P; Zhang, Y, 2007)		1.28
"Celecoxib treatment resulted in a pronounced radiosensitization of A549, HCT116, and HSF7 cells, whereas FaDu and HH4dd cells were not radiosensitized. "( Celecoxib induced tumor cell radiosensitization by inhibiting radiation induced nuclear EGFR transport and DNA-repair: a COX-2 independent mechanism.
Andratschke, NH; Dittmann, KH; Mayer, C; Milas, L; Ohneseit, PA; Raju, U; Rodemann, HP, 2008)		3.23
"Celecoxib treatment resulted in highly significant increases in the mRNA expression of the smooth muscle component desmin, the detoxification enzyme glutathione S-transferase pi (GSTpi), and nonsteroidal anti-inflammatory response gene (NAG-1) in the LNCaPCOX-2 cell line compared with LNCaPneo cells."( The effects of cyclooxygenase-2 expression in prostate cancer cells: modulation of response to cytotoxic agents.
Coley, HM; Kass, GE; Macanas-Pirard, P; Mehar, A; Mizokami, A; Takahashi, Y, 2008)		1.07
"Celecoxib/STZ treatments produced a significant loss of learning and memory."( Modulation of celecoxib- and streptozotocin-induced experimental dementia of Alzheimer's disease by pitavastatin and donepezil.
Sharma, B; Singh, M; Singh, N, 2008)		1.43
"Celecoxib treatment led to significant improvement in the signs and symptoms of osteoarthritis as determined by all efficacy measures. "( Treatment of osteoarthritis with celecoxib, a cyclooxygenase-2 inhibitor: a randomized controlled trial.
Bensen, WG; Fiechtner, JJ; Geis, GS; Hubbard, RC; Isakson, PC; McMillen, JI; Verburg, KM; Woods, EM; Yu, SS; Zhao, WW, 1999)		2.03
"Celecoxib-treated patients were also found to experience safety and tolerability similar to that of the placebo-treated patients."( Functional status and health-related quality of life of elderly osteoarthritic patients treated with celecoxib.
Dedhiya, SD; Espinoza, L; Lisse, J; Osterhaus, JT; Zhao, SZ, 2001)		1.25
"In celecoxib-treated animals, vasodilation in response to arachidonic acid was reduced significantly compared with controls."( Effects of selective cyclooxygenase-2 inhibition on vascular responses and thrombosis in canine coronary arteries.
Barrett, TD; Crofford, LJ; Driscoll, EM; Hennan, JK; Huang, J; Lucchesi, BR; Park, AM; Willens, DE, 2001)		0.82
"Celecoxib-treated/injured ligaments were found to have a 32% lower load to failure than untreated/injured ligaments."( A cyclooxygenase-2 inhibitor impairs ligament healing in the rat.
Dahners, LE; Elder, CL; Weinhold, PS, )		0.85
"Treatment of Celecoxib decreased DON-induced translocation of Protein Kinase C isozymes (α,ε,γ), demonstrating the role of PKC in DON-mediated biochemical and molecular alterations responsible for its dermal toxicity."( Celecoxib reduces Deoxynivalenol induced proliferation, inflammation and protein kinase C translocation via modulating downstream targets in mouse skin.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mandal, P; Mishra, S; Rath, SK; Srivastava, S; Tripathi, A; Wahajuddin, M, 2020)		2.35
"Treatment with celecoxib after DMH induced significant increase in apoptotic cell numbers by 47% after 16 weeks, but these numbers had not changed after 32 weeks compared with the corresponding group treated DMH only."( Celecoxib Targeted Therapy Attenuates Mouse Colon Carcinogenesis through Modulation of Expression Patterns of Cancer Stem Cells.
Eltonouby, EA; Hegazi, MM; Helmy, HM; Kang, JS; Mahfouz, ME; Salim, EI, 2019)		2.3
"Treatment with celecoxib-loaded NLCs alleviated severity of colitis as demonstrated by disease activity index, colon length, fecal occult blood test, and histopathological analysis."( Lipid-based nanocarrier-mediated targeted delivery of celecoxib attenuate severity of ulcerative colitis.
Ahmad, A; Khan, R; Kumar, A; Mishra, RK; Raza, SS; Vyawahare, A, 2020)		1.15
"Treatment with celecoxib alone promoted the membrane translocation of phosphatase and tensin homolog (PTEN), indicating PTEN activation, and consequently led to protein kinase B (AKT) dephosphorylation (inactivation)."( Synergistic antitumor effects of the combined treatment with an HDAC6 inhibitor and a COX-2 inhibitor through activation of PTEN.
Gan, YH; Zhang, G, 2017)		0.79
"Treatment with celecoxib at approved dosages conferred a similar or lower risk of CV, GI, and renal adverse events compared with treatment with ibuprofen or naproxen in patients with OA and patients with RA."( Differences in Safety of Nonsteroidal Antiinflammatory Drugs in Patients With Osteoarthritis and Patients With Rheumatoid Arthritis: A Randomized Clinical Trial.
Bao, W; Berger, MF; Borer, JS; Graham, DY; Husni, ME; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wang, Q; Wisniewski, LM; Wolski, KE; Yeomans, ND, 2018)		0.83
"Treatment with celecoxib in the postoperative setting was associated with decreased mean use of opioids in oral (mean difference, 9.9 mg/d; 95% CI, -1.2 to 21.1), IV (mean difference, 3.9 mg/d; 95% CI, 1.0-6.8), and total (mean difference, 14 mg/d; 95% CI, 2.6-25.4) amount of morphine equivalents per day."( Association of Celecoxib Use With Decreased Opioid Requirements After Head and Neck Cancer Surgery With Free Tissue Reconstruction.
Buchmann, LO; Cannon, RB; Carpenter, PS; Hunt, JP; Kull, A; McCrary, H; Monroe, MM; Shepherd, HM; Torrecillas, V, 2018)		1.17
"Co-treatment with celecoxib and doxorubicin significantly inhibited cell growth and induced cell apoptosis in the acute leukemia cell line HL60 and primary AML cells."( Combination of celecoxib and doxorubicin increases growth inhibition and apoptosis in acute myeloid leukemia cells.
Chen, C; Wang, CM; Xu, W, 2013)		1.07
"Treatment with Celecoxib, a non-steroidal anti-inflammatory drug (NSAID), is shown to downregulate Mcl-1 expression, and enhances PDT-induced apoptosis both in vitro and in vivo."( Enhanced apoptotic effects by downregulating Mcl-1: evidence for the improvement of photodynamic therapy with Celecoxib.
Chen, Q; Song, J; Xing, D, 2013)		0.94
"Treatment with celecoxib significantly reduced LPS-induced sensorimotor behavioral disturbances and dopaminergic neuronal dysfunction."( Celecoxib reduces brain dopaminergic neuronaldysfunction, and improves sensorimotor behavioral performance in neonatal rats exposed to systemic lipopolysaccharide.
Bhatt, AJ; Cai, Z; Fan, LW; Kaizaki, A; Numazawa, S; Pang, Y; Tanaka, S; Tien, LT, 2013)		2.17
"Treatment with celecoxib and triamcinolone significantly reduced total leukocyte count by 40% (P = 0.02) and 31% (P = 0.01), respectively."( The safety, pharmacokinetics, and efficacy of intraocular celecoxib.
Kim, SJ; Kompella, UB; Shah, R; Sheng, J; Toma, H; Vooturi, SK, 2014)		0.99
"Treatment with celecoxib and IFN-α synergistically inhibited cell proliferation in a dose- and time-dependent manner."( Interferon-α and cyclooxygenase-2 inhibitor cooperatively mediates TRAIL-induced apoptosis in hepatocellular carcinoma.
Burns, M; Dan, H; Li, Q; Liu, C; Liu, J; Liu, N; Qiu, X; Wang, X; Wu, Q; Xia, M; Xie, H; Yang, D; Zhu, H; Zuo, C, 2015)		0.76
"Treatment with celecoxib alone dephosphorylated phosphatase and tensin homolog deleted on chromosome ten (PTEN), promoted PTEN membrane translocation or activation, and correspondingly dephosphorylated or inactivated protein kinase B (AKT)."( Activating PTEN by COX-2 inhibitors antagonizes radiation-induced AKT activation contributing to radiosensitization.
Gan, YH; Meng, Z, 2015)		0.76
"Treatment of celecoxib with a proton pump inhibitor is safer than treatment with nonselective NSAID and a proton pump inhibitor in high risk gastrointestinal and cardiovascular patients who mostly also take acetylsalicylic acid."( [Gastrointestinal bleeding].
Lanas, Á, 2015)		0.77
"Treatment with celecoxib significantly decreased the induced tumor size and metastasis of the PyMT/Col1a1 tumors, such that their size was not different from the smaller PyMT tumors."( COX-2 modulates mammary tumor progression in response to collagen density.
Esbona, K; Inman, D; Jeffery, J; Keely, P; Saha, S; Schedin, P; Wilke, L, 2016)		0.77
"Treatment with celecoxib lowered the numbers of ACF, as well as the tumor volumes and multiplicities after 32 weeks."( Expression Patterns of Cancer Stem Cell Markers During Specific Celecoxib Therapy in Multistep Rat Colon Carcinogenesis Bioassays.
Hegazi, MM; Helmy, HM; Kang, JS; Salim, EI, 2016)		1.01
"Treatment with celecoxib resulted in G1 cell cycle arrest, induction of apoptosis, inhibition of cellular adhesion and invasion and reduction of expression of hTERT mRNA and COX-2 protein in all of the ovarian cancer cell lines."( The effect of celecoxib on tumor growth in ovarian cancer cells and a genetically engineered mouse model of serous ovarian cancer.
Bae-Jump, VL; Gehrig, PA; Han, X; Jones, HM; Schuler, KM; Sheng, X; Suri, A; Zhong, Y; Zhou, C, 2016)		1.13
"Treatment with celecoxib, a selective COX-2 inhibitor, reduces formation of premalignant adenomatous polyps in the gastrointestinal tracts of humans and mice. "( Celecoxib Alters the Intestinal Microbiota and Metabolome in Association with Reducing Polyp Burden.
Benezra, R; Dannenberg, AJ; Gross, SS; Karoly, ED; Leve, ND; Ling, L; McNally, EM; Montrose, DC; Pamer, EG; Sue, E; Suen, CS; Yantiss, RK; Zhou, XK, 2016)		2.23
"Cotreatment with celecoxib and 5-FU partially blocked AKT phosphorylation, although no significant changes in total AKT protein levels were detected."( Celecoxib enhances the inhibitory effect of 5-FU on human squamous cell carcinoma proliferation by ROS production.
Ahn, SH; Choi, JJ; Kim, YH; Kwon, SK; Lee, DY; Oh, SM; Park, SW; Shin, ES; Sung, MW, 2017)		2.23
"Treatment with celecoxib also restored GSK3β function and led to down-regulation of β-catenin activity through transcriptional and post-translational mechanisms, two effects likely to contribute to Ph+ cell growth suppression by celecoxib.Celecoxib inhibited colony formation of TKI-resistant Ph+ cell lines including those with the T315I BCR-ABL mutation and acted synergistically with imatinib in suppressing colony formation of TKI-sensitive Ph+ cell lines."( Celecoxib inhibits proliferation and survival of chronic myelogeous leukemia (CML) cells via AMPK-dependent regulation of β-catenin and mTORC1/2.
Calabretta, B; Canonico, PL; Condorelli, F; De Dominici, M; Genazzani, AA; Gnemmi, I; Mariani, SA; Minassi, A; Minieri, V; Riva, B; Salomoni, P, 2016)		2.22
"Pretreatment with celecoxib showed protection against pilocarpine-induced seizures. "( Cyclooxygenase-2 inhibitor inhibits hippocampal synaptic reorganization in pilocarpine-induced status epilepticus rats.
Lei, GF; Liu, CX; Sun, RP; Yang, L; Zhang, HJ, 2008)		0.68
"Treatment with celecoxib in subjects with OPLs favorably modulates the primary mediator of cyclooxygenase-2 activity, PGE(2), after 12 weeks."( A pilot surrogate endpoint biomarker study of celecoxib in oral premalignant lesions.
Bertagnolli, MM; Dorfman, DM; Goguen, L; Haddad, RI; Krane, JF; Li, Y; Moran, AE; Norris, CM; Othus, M; Posner, MR; Wirth, LJ, 2008)		0.94
"Treatment with celecoxib alone has no effect on the ERK1/2 activation, Rad51 mRNA and protein levels, however, combined treatment with gefitinib results in a significant reduction of phospho-ERK1/2 and Rad51 protein levels, and triggers the degradation of Rad51 via a 26S proteasome-dependent pathway."( The role of celecoxib in Rad51 expression and cell survival affected by gefitinib in human non-small cell lung cancer cells.
Ciou, SC; Hong, JH; Jhan, JY; Ko, JC; Lin, ST; Lin, YW; Wang, LH, 2009)		1.07
"Treatment with celecoxib 200 mg once daily and diclofenac 50 mg twice daily resulted in similar rates of AE-related study discontinuation in elderly patients with OA. "( A randomized, multicentre, double-blind, parallel-group study to assess the adverse event-related discontinuation rate with celecoxib and diclofenac in elderly patients with osteoarthritis.
Dahlberg, LE; Holme, I; Høye, K; Ringertz, B, )		0.69
"Pre-treatment with celecoxib completely abolished rosuvastatin's protective effect (FMD pre-IR: 8.0 +/- 2.2%; FMD post-IR: 1.4 +/- 2.0%, [p < 0.001] compared with pre-IR, [p = NS] vs."( Rosuvastatin prevents conduit artery endothelial dysfunction induced by ischemia and reperfusion by a cyclooxygenase-2-dependent mechanism.
Gori, T; Liuni, A; Luca, MC; Parker, JD, 2010)		0.68
"Treatment with celecoxib (50 mg/kg ip) or saline (0.9% NaCl ip) began at 60 days of age."( Cox-2 inhibition attenuates cardiovascular and inflammatory aspects in monosodium glutamate-induced obese rats.
Cecchini, R; Cunha, NV; de Abreu, SB; Grassiolli, S; Guarnier, FA; Martins-Pinge, MC; Mazzuco, TL; Panis, C; Pinge-Filho, P, 2010)		0.7
"Treatment with celecoxib in a dose of 5 mg/kg was effective in decreasing the elevated levels of IL-6, IL-1β, TNF-α, PGE₂ whereas it lacked any effect on TXB₂ level since it had hardly any effect on COX-1 enzyme."( Effect of selective COX-2 inhibitor, celecoxib on adjuvant-induced arthritis model in irradiated rats.
El-Ghazaly, MA; El-Hazek, RM; Khayyal, MT; Nada, AS, 2010)		0.97
"Pretreatment with celecoxib and fish oil in DMBA-treated animals led to normal histology, increase in DNA fragmentation, and decrease in TSA and LASA levels with reduced oxidative stress, and the effect was more pronounced than animals pretreated with either celecoxib/fish oil alone suggesting a synergistic effect of the two regimens."( Evaluation of the role of oxidative stress in chemopreventive action of fish oil and celecoxib in the initiation phase of 7,12-dimethyl benz(α)anthracene-induced mammary carcinogenesis.
Aggarwal, R; Agnihotri, N; Kansal, S; Kaur, R; Negi, AK; Sarotra, P; Sharma, G, 2011)		0.92
"Pretreatment with celecoxib (2.5 and 5 mg per kg) or L-NAME (50 mg per kg) induced anticonvulsant effect on the PTZ-induced clonic seizures."( Anticonvulsant effect of celecoxib on pentylenetetrazole-induced convulsion: Modulation by NO pathway.
Dehpour, AR; Hajimirzabeigi, A; Khalilzadeh, O; Maleki, F; Zandieh, A; Zandieh, B, 2010)		0.99
"Co-treatment with celecoxib restored the normal histoarchitechture in hepatic tissues of CS inhaling mice."( Celecoxib mitigates cigarette smoke induced oxidative stress in mice.
Arora, N; Koul, A, 2010)		2.13
"Treatment with celecoxib or naproxen did not improve depressive symptoms over time compared with placebo. "( Celecoxib or naproxen treatment does not benefit depressive symptoms in persons age 70 and older: findings from a randomized controlled trial.
Drye, L; Fields, C; Lyketsos, C; Vaidya, V, 2012)		2.17
"Treatment with celecoxib, a selective COX-2 inhibitor, caused a 45% reduction in mammary PGE(2) levels, attenuated the influx of mast cells and reduced vascularization in Tg glands."( Transgenic insulin-like growth factor-1 stimulates activation of COX-2 signaling in mammary glands.
Berton, TR; Conti, CJ; Digiovanni, J; Fischer, SM; Fuchs-Young, R; Kiguchi, K; Lambertz, I; Rundhaug, JE; Shirley, SH; Tian, J, 2012)		0.72
"Co-treatment of celecoxib and NPC-16 could induce colorectal cancer cell apoptosis via COX-2-independent and caspase-dependent mechanisms. "( COX-2-independent induction of apoptosis by celecoxib and polyamine naphthalimide conjugate mediated by polyamine depression in colorectal cancer cell lines.
Li, JH; Li, Q; Wang, CJ; Wang, JH; Xie, SQ; Zhang, YH; Zhao, J, 2012)		0.99
"Pretreatment with celecoxib resulted in a significant reduction in TNF-α levels and an increase in NO(x) and NOS levels compared with the AMI group."( Low-dose celecoxib improves coronary function after acute myocardial ischaemia in rabbits.
Bi, XY; He, X; Li, DL; Liu, JJ; Ma, X; Yu, XJ; Zang, WJ; Zhang, HL; Zhao, M, 2012)		1.12
"Treatment with celecoxib had effects on inflammation response and reduced cancer metastasis."( Primary tumor regulates the pulmonary microenvironment in melanoma carcinoma model and facilitates lung metastasis.
Bi, Y; Han, M; Jia, J; Jiang, M; Liu, Q; Xu, J; Xu, X, 2013)		0.73
"Treatment with celecoxib had no effect on tumor volume, despite the fact that we found a dose-dependent inhibitory effect on cell cultures and there was a sufficiently high celecoxib concentration in blood plasma and brain tissue. "( Effect of systemic celecoxib on human meningioma after intracranial transplantation into nude mice.
Friedrich, S; Grote, M; Krauss, JK; Nakamura, M; Schwabe, K, 2013)		1.07
"Treatment with celecoxib for 6 months, with before-treatment and after-treatment videos posted to an intranet with an interactive site for scoring."( Global quantitative assessment of the colorectal polyp burden in familial adenomatous polyposis by using a web-based tool.
Khalaf, R; Levin, B; Lynch, PM; Morris, JS; Posadas, J; Rodriguez-Bigas, MA; Ross, WA; Sepeda, VO; Shureiqi, I; Weber, DM, 2013)		0.74
"The treatment with celecoxib did not modify substantially the histological alterations and the number of active osteoclasts after activation of orthodontic appliance."( Celecoxib treatment does not alter recruitment and activation of osteoclasts in the initial phase of experimental tooth movement.
Carvalho-Filho, EP; Ervolino, E; Iyomasa, MM; Rocha, MJ; Stabile, AC; Stuani, MB, 2012)		2.14
"Pretreatment with celecoxib inhibited nicotine-induced change in the expression of VEGF and COX-2."( Change in nicotine-induced VEGF, PGE2 AND COX-2 expression following COX inhibition in human oral squamous cancer.
Amanzadeh, A; Aslani, HR; Bidgoli, SA; Esfahani, M; Esfandiary, M; Ghahremani, MH; Habibzadeh, N; Salimi, M; Sedaghati, B, 2012)		0.7
"Treatment with celecoxib (500 ppm) significantly reduced the incidence of mammary tumors in MMTV/neu mice (P = 0.003) and caused about a 50% reduction in mammary prostaglandin E2 (PGE2) levels."( Celecoxib, a selective cyclooxygenase 2 inhibitor, protects against human epidermal growth factor receptor 2 (HER-2)/neu-induced breast cancer.
Brown, AM; Dannenberg, AJ; Deora, A; Du, B; Howe, LR; Hudis, C; Masferrer, JL; Muller, WJ; Patel, J; Subbaramaiah, K; Thaler, HT, 2002)		2.1
"Treatment with celecoxib increased insulin release from these cells in a dose-dependent manner in glucose concentrations ranging from 5 to 17 mM."( Cellular distribution and contribution of cyclooxygenase COX-2 to diabetogenesis in NOD mouse.
Gross, R; Kallajoki, M; Laine, J; Luo, C; Mäkinen, M; Mulari, M; Simell, O; Teros, T; Ylinen, L, 2002)		0.65
"Treatment with celecoxib increased cortical alpha(v) integrin mRNA expression 2.2-fold (p < 0.05) in healthy animals and 4.0-fold (p < 0.05) in rats with PHN, but lowered COX-2 mRNA expression in rats with PHN to 0.8-fold (p < 0.05)."( Selective cyclooxygenase-2 inhibition upregulates renal cortical alpha V integrin expression.
Grabensee, B; Heering, P; Heise, G; Meyer-Kirchrath, J; Schrör, K; Waldner, C, 2003)		0.66
"Treatment with celecoxib produced dose- and time-dependent decrease in ODC activity."( Do altering in ornithine decarboxylase activity and gene expression contribute to antiproliferative properties of COX inhibitors?
Bartnik, W; Ostrowski, J; Skurzak, H; Wocial, T, 2003)		0.66
"Treatment with celecoxib significantly reduced calcium ionophore-stimulated PGE2 production from AMs recovered from smokers. "( Celecoxib modulates the capacity for prostaglandin E2 and interleukin-10 production in alveolar macrophages from active smokers.
Baratelli, F; Dubinett, SM; Holmes, EC; Mao, JT; Roth, MD; Serio, KJ; Strieter, RM; Zhu, L, 2003)		2.11
"Treatment with celecoxib also led to dose-dependent inhibition of PC3 xenograft growth without causing a reduction in intratumor prostaglandin E(2)."( Celecoxib inhibits prostate cancer growth: evidence of a cyclooxygenase-2-independent mechanism.
Chang, M; Cordon-Cardo, C; Dannenberg, AJ; Du, B; Newman, RA; Patel, MI; Subbaramaiah, K; Thaler, HT; Yang, P, 2005)		2.11
"Pretreatment with celecoxib, a selective COX-2 inhibitor, attenuated Abeta-induced cell death, which was aggravated by addition of the COX-2 product PGE(2)."( Beta-amyloid-induced apoptosis is associated with cyclooxygenase-2 up-regulation via the mitogen-activated protein kinase-NF-kappaB signaling pathway.
Jang, JH; Surh, YJ, 2005)		0.65
"Cotreatment with celecoxib abrogated the increase in levels of PGE(2) but not COX-2 induced by chemotherapy."( Chemotherapy induces the expression of cyclooxygenase-2 in non-small cell lung cancer.
Altorki, NK; Dannenberg, AJ; Duffield-Lillico, AJ; Golijanin, D; Port, JL; Subbaramaiah, K; Thaler, HT; Zhang, F, 2005)		0.66
"Treatment with celecoxib was associated with no side effects apart from allergic exanthema in two patients."( Celecoxib, a selective inhibitor of cyclooxygenase 2 for therapy of diffuse anterior scleritis.
Bauer, AM; Becker, MD; Fiehn, C, 2005)		2.11
"Treatment with celecoxib only or combined with gemcitabine altered the cell cycle phase distribution in SW1990, cells were mainly arrested in G(0)/G(1) phase, S phase and G(2)/M phase development were greatly inhibited."( [Enhancing effects of celecoxib on the growth inhibition of pancreatic carcinoma by gemcitabine treatment].
Wang, XP; Wu, K; Xu, G; Zhao, S, 2005)		0.98
"The treatment of celecoxib (40 micromol/L) combined with hydroxyurea (10 mmol/L) could significantly inhibit the K562 cell viability and induce the K562 cell apoptosis than those treatments of celecoxib or hydroxyurea alone. "( [Effect of celecoxib on enhancing the chemotherapic sensitivity of hydroxyurea to K562 cells and its mechanism].
Liu, DS; Zhang, GS, 2004)		1.05
"With treatment with celecoxib, PGE(2) levels, the gastric mucosal thickness, and the number of total gastric cells per gastric gland of ACT-GAS mice were significantly decreased."( Involvement of cyclooxygenase-2 in gastric mucosal hypertrophy in gastrin transgenic mice.
Chiba, T; Fukui, H; Kanda, N; Kawada, M; Konda, Y; Nakajima, T; Sawabu, T; Seno, H; Takeuchi, T; Uenoyoma, Y, 2006)		0.65
"Treatment with Celecoxib significantly reduced Ki-67 LI in smokers by 35% (P = 0.016), and increased the expression of nuclear survivin by 23% (P = 0.036) without significantly changing that of cytoplasmic survivin."( Celecoxib decreases Ki-67 proliferative index in active smokers.
Adams, B; Burdick, M; Dubinett, SM; Fishbein, MC; Goodglick, L; Holmes, C; Hong, L; Mao, JT; Roth, MD; Strieter, ER; Tashkin, DP, 2006)		2.13
"Treatment with Celecoxib reduced both microvessel density and tumor growth. "( The selective Cox-2 inhibitor Celecoxib suppresses angiogenesis and growth of secondary bone tumors: an intravital microscopy study in mice.
Abdollahi, A; Ewerbeck, V; Gebhard, MM; Huber, PE; Klenke, FM; Sckell, A, 2006)		0.98
"Treatment with celecoxib alone or in combination with IR led to a dose-dependent increase in COX-2 protein expression."( Inhibition of cyclooxygenase-2 activity by celecoxib does not lead to radiosensitization of human prostate cancer cells in vitro.
Dittmann, K; Kehlbach, R; Krebiehl, G; Ohneseit, PA; Rodemann, HP, 2007)		0.94
"The treatment with celecoxib or vehicle was started immediately after the sham operation or ovariectomy, and lasted for 4 weeks."( The selective cyclooxygenase-2 inhibitor celecoxib reduces bone resorption, but not bone formation, in ovariectomized mice in vivo.
Baylink, DJ; Itoi, E; Kasukawa, Y; Maekawa, S; Miyakoshi, N; Mohan, S; Nozaka, K; Srivastava, AK, 2007)		0.92
"Treatment with celecoxib 200 and 400 mg qd was statistically superior to placebo treatment at weeks 2 and 6 for Patient's Assessment of Arthritis Pain."( A comparison of the efficacy and safety of celecoxib 200 mg and celecoxib 400 mg once daily in treating the signs and symptoms of psoriatic arthritis.
Espinoza, LR; Kivitz, AJ; Liu-Dumaw, M; Sherrer, YR; West, CR, 2007)		0.94
"Treatment with celecoxib increased the cellular radiosensitivity in the DNA-PKcs-deficient cell line V3 with a dose-enhancement ratio of 1.3 for a surviving fraction of 0.5. "( DNA-PKcs-dependent modulation of cellular radiosensitivity by a selective cyclooxygenase-2 inhibitor.
Chen, BP; Chen, DJ; Choy, H; Kodym, E; Kodym, R; Morotomi-Yano, K; Saha, D, 2007)		0.69
"Treatment with celecoxib for 24 h resulted in the activation of caspase-3 and 9, cleavage of PARP."( [Celecoxib-induced apoptosis in acute promyelocytic leukemia cell line MR2 and its mechanism].
Huang, H; Xu, Y; Zhao, YM, 2007)		1.59
"Treatment with Celecoxib was associated with activation of Bax, decreased expression of Mcl-1, loss of the mitochondrial membrane potential and caspase-9-dependent apoptosis."( Celecoxib disrupts the canonical apoptotic network in HTLV-I cells through activation of Bax and inhibition of PKB/Akt.
Brown, M; Nicot, C; Sinha-Datta, U; Taylor, JM, 2008)		2.13
"Treatment with celecoxib was associated with the lowest number of GI side effects and related deaths."( Costs and effects of various analgesic treatments for patients with rheumatoid arthritis and osteoarthritis in the Netherlands.
Al, MJ; Grijseels, EW; Janssen, M; Maniadakis, N, )		0.47
"Treatment with celecoxib, but not rapamycin, increased apoptosis in the two cell lines."( Antiproliferative and proapoptotic effects of rapamycin and celecoxib in malignant melanoma cell lines.
Becker, B; Bundscherer, A; Hafner, C; Landthaler, M; Maisch, T; Vogt, T, 2008)		0.93
"Rats treated with celecoxib exhibited significant increases in weight gain (20%), plasma arginine-vasopressin levels (148%) and plasma urea (69%) relative to vehicle-treated controls."( Selective cyclo-oxygenase-2 inhibition with celecoxib elevates blood pressure and promotes leukocyte adherence.
Asfaha, S; Elliott, SN; Lovren, F; Muscará, MN; Triggle, CR; Vergnolle, N; Wallace, JL, 2000)		0.89
"Treatment with celecoxib was examined and compared to treatment with the general NSAID, ibuprofen, and to a control group receiving only dimethylbenz(a)anthracene."( Chemoprevention of breast cancer in rats by celecoxib, a cyclooxygenase 2 inhibitor.
Abou-Issa, H; Alshafie, GA; Harris, RE; Seibert, K, 2000)		0.91
"Treatment with celecoxib significantly delayed esophageal ulcer healing and suppressed ulceration-triggered increases in esophageal epithelial cell proliferation, c-Met mRNA and protein expression, and ERK2 activity."( Selective cyclooxygenase-2 blocker delays healing of esophageal ulcers in rats and inhibits ulceration-triggered c-Met/hepatocyte growth factor receptor induction and extracellular signal-regulated kinase 2 activation.
Baatar, D; Jones, MK; Kawanaka, H; Kitano, S; Moon, WS; Pai, R; Szabo, IL; Tarnawski, AS, 2002)		0.65

Toxicity

Diacerein and celecoxib combination therapy is as safe and effective as corresponding monotherapies. Patients at highest baseline risk demonstrated disproportionately greater risk of cele Coxib-related adverse events.

ExcerptReferenceRelevance
"SC-58635 achieves analgesic and antiinflammatory efficacy in arthritis through selective COX-2 inhibition, without showing any evidence of 2 of the toxic effects of COX-1 inhibition associated with nonsteroidal antiinflammatory drugs."( Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects.
Geis, GS; Hubbard, RC; Isakson, PC; Lanza, FL; Lipsky, PE; Schwartz, BD; Simon, LS; Talwalker, S, 1998)		0.3
"Conventional nonsteroidal anti-inflammatory drugs (NSAIDs) are associated with a spectrum of toxic effects, notably gastrointestinal (GI) effects, because of inhibition of cyclooxygenase (COX)-1."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000)		0.59
"To determine whether celecoxib, a COX-2-specific inhibitor, is associated with a lower incidence of significant upper GI toxic effects and other adverse effects compared with conventional NSAIDs."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000)		0.91
"Incidence of prospectively defined symptomatic upper GI ulcers and ulcer complications (bleeding, perforation, and obstruction) and other adverse effects during the 6-month treatment period."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000)		0.59
"In this study, celecoxib, at dosages greater than those indicated clinically, was associated with a lower incidence of symptomatic ulcers and ulcer complications combined, as well as other clinically important toxic effects, compared with NSAIDs at standard dosages."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000)		0.95
" However, NSAIDs cause significant adverse upper gastrointestinal effects, including increased mortality from serious ulcer complications."( Selective inhibitors of COX-2--are they safe for the stomach?
Giercksky, KE; Haglund, U; Rask-Madsen, J, 2000)		0.31
" This article critically reviews the data on gastrointestinal toxic side effects for conventional NSAIDs without as well as with prevention therapy."( Gastrointestinal toxic side effects of nonsteroidal anti-inflammatory drugs and cyclooxygenase-2-specific inhibitors.
Burmester, GR; Buttgereit, F; Simon, LS, 2001)		0.31
" The overall incidence of hepatic adverse events in arthritis patients receiving celecoxib was similar to that for placebo but significantly lower than in the combined group of patients receiving nonsteroidal anti-inflammatory drugs (NSAIDs)."( The hepatic safety and tolerability of the novel cyclooxygenase-2 inhibitor celecoxib.
Geis, GS; Maddrey, WC; Maurath, CJ; Verburg, KM, 2000)		0.76
" The overall incidence of renal adverse events after celecoxib was greater than that after placebo but similar to that after NSAIDs."( Renal safety and tolerability of celecoxib, a novel cyclooxygenase-2 inhibitor.
Geis, GS; Maurath, CJ; Verburg, KM; Whelton, A, 2000)		0.84
" We therefore investigated whether combination of a COX-2 inhibitor with an angiotensin II subtype 1 (AT1) receptor blocker is safe with regard to preservation of normal renal function in a state of slight volume contraction."( Renal safety of combined cyclooxygenase 2 (COX-2) inhibitor and angiotensin II receptor blocker administration in mild volume depletion.
Ambühl, PM; Kistler, T, 2001)		0.31
"Selective COX-2 inhibition by celecoxib in combination with an AT1 receptor blocker (irbesartan) has no acute adverse effects on renal haemodynamics and renal salt handling in slightly volume-depleted subjects with normal renal function."( Renal safety of combined cyclooxygenase 2 (COX-2) inhibitor and angiotensin II receptor blocker administration in mild volume depletion.
Ambühl, PM; Kistler, T, 2001)		0.6
" Inhibition of COX-2 has been associated with the therapeutic effects of NSAIDs, whereas inhibition of COX-1 is believed to be the cause of the adverse gastrointestinal effects associated with NSAID therapy."( A comparison of renal-related adverse drug reactions between rofecoxib and celecoxib, based on the World Health Organization/Uppsala Monitoring Centre safety database.
Arellano, FM; Lejkowith, J; Reynolds, MW; Whelton, A; Zhao, SZ, 2001)		0.54
"This study sought to compare renal safety signals between the COX-2-specific inhibitors rofecoxib and celecoxib, based on spontaneous reports of adverse drug reactions (ADRs) in the World Health Organization/Uppsala Monitoring Centre (WHO/UMC) safety database through the end of the second quarter 2000."( A comparison of renal-related adverse drug reactions between rofecoxib and celecoxib, based on the World Health Organization/Uppsala Monitoring Centre safety database.
Arellano, FM; Lejkowith, J; Reynolds, MW; Whelton, A; Zhao, SZ, 2001)		0.76
" However, the adverse renal impact of rofecoxib was significantly greater than that of celecoxib."( A comparison of renal-related adverse drug reactions between rofecoxib and celecoxib, based on the World Health Organization/Uppsala Monitoring Centre safety database.
Arellano, FM; Lejkowith, J; Reynolds, MW; Whelton, A; Zhao, SZ, 2001)		0.76
" Three patients (11%) had other adverse events (renal insufficiency, rash, and asymptomatic colonic ulceration)."( Safety of selective cyclooxygenase-2 inhibitors in inflammatory bowel disease.
Loftus, EV; Mahadevan, U; Sandborn, WJ; Tremaine, WJ, 2002)		0.31
"Our preliminary results suggest that cyclooxygenase-2 inhibitors may be safe and beneficial in most patients with IBD."( Safety of selective cyclooxygenase-2 inhibitors in inflammatory bowel disease.
Loftus, EV; Mahadevan, U; Sandborn, WJ; Tremaine, WJ, 2002)		0.31
" Patients prescribed CSIs (or NSAIDs) should be reviewed within the first few weeks of therapy to assess effectiveness, identify adverse effects and determine the need for ongoing therapy."( Considerations for the safe prescribing and use of COX-2-specific inhibitors.
, 2002)		0.31
" There were no significant maternal or neonatal adverse events."( A prospective randomized safety trial of celecoxib for treatment of preterm labor.
Bernhard, LM; Gerber, S; Gross, GA; Leguizamon, G; Levy, R; Mathur, A; Nelson, DM; Sadovsky, Y; Stika, CS, 2002)		0.58
" Tolerability: withdrawal rates for adverse effects."( Efficacy, tolerability, and upper gastrointestinal safety of celecoxib for treatment of osteoarthritis and rheumatoid arthritis: systematic review of randomised controlled trials.
Bradley, MD; Deeks, JJ; Smith, LA, 2002)		0.56
" Compared with those taking other NSAIDs, in patients taking celecoxib the rate of withdrawals due to adverse gastrointestinal events was 46% lower (95% confidence interval 29% to 58%; NNT 35 at three months), the incidence of ulcers detectable by endoscopy was 71% lower (59% to 79%; NNT 6 at three months), and the incidence of symptoms of ulcers, perforations, bleeds, and obstructions was 39% lower (4% to 61%; NNT 208 at six months)."( Efficacy, tolerability, and upper gastrointestinal safety of celecoxib for treatment of osteoarthritis and rheumatoid arthritis: systematic review of randomised controlled trials.
Bradley, MD; Deeks, JJ; Smith, LA, 2002)		0.8
" All other adverse effects of celecoxib are comparable with NSAIDs adverse reactions."( [Safety of celecoxib administration].
Babić-Naglić, D, 2002)		0.99
"Among the most widely prescribed drugs worldwide, non-steroidal anti-inflammatory drugs (NSAIDs) are effective for relieving pain, but they are also associated with a high incidence of gastrointestinal (GI) adverse events."( Do selective cyclo-oxygenase inhibitors eliminate the adverse events associated with nonsteroidal anti-inflammatory drug therapy?
Devière, J, 2002)		0.31
" Phone call follow up in 25 patients disclosed that 15 patients continued to take celecoxib, while five patients did not take celecoxib following the oral challenge, and five discontinued celecoxib due to adverse effects, lack of drug efficacy or physician preference."( Safety of celecoxib in individuals allergic to sulfonamide: a pilot study.
Knowles, SR; Neuman, MG; Shapiro, LE; Shear, NH; Weber, E, 2003)		0.95
"Adverse reactions to nonsteroidal anti-inflammatory drugs (NSAIDs) are frequent, and the need to identify a safe alternative drug is a common problem in clinical practice."( [The selective cyclooxygenase-2 inhibitor celecoxib is a safe alternative in patients with pseudo-allergic reactions to nonsteroidal anti-inflammatory drugs].
Ahlbach, S; Boehncke, WH; Kaufmann, R; Usadel, KH, 2003)		0.58
"77 patients (24 males, 53 females, age 31-80 years) with a history of adverse reactions to NSAIDs underwent standardized skin prick, scratch and patch tests along with oral, placebo-controlled blinded exposure to celecoxib (maximum single dose 200 mg, cumulative daily dose 350 mg)."( [The selective cyclooxygenase-2 inhibitor celecoxib is a safe alternative in patients with pseudo-allergic reactions to nonsteroidal anti-inflammatory drugs].
Ahlbach, S; Boehncke, WH; Kaufmann, R; Usadel, KH, 2003)		0.77
" Oral challenge with celecoxib was tolerated by all 77 patients without adverse effects."( [The selective cyclooxygenase-2 inhibitor celecoxib is a safe alternative in patients with pseudo-allergic reactions to nonsteroidal anti-inflammatory drugs].
Ahlbach, S; Boehncke, WH; Kaufmann, R; Usadel, KH, 2003)		0.9
" Celecoxib is a safe alternative in subjects with previous adverse reactions to NSAIDs."( [The selective cyclooxygenase-2 inhibitor celecoxib is a safe alternative in patients with pseudo-allergic reactions to nonsteroidal anti-inflammatory drugs].
Ahlbach, S; Boehncke, WH; Kaufmann, R; Usadel, KH, 2003)		1.49
"With the extensive use of COX-2 inhibitors to treat inflammatory and pain syndromes, gastrointestinal adverse effects are being increasingly observed."( Celecoxib associated esophagitis: review of gastrointestinal side effects from cox-2 inhibitors.
Mantry, P; Shah, A; Sundaram, U, 2003)		1.76
"Because recent studies have shown that COX-2 inhibitors are similar to NSAIDs with regards to absorption, in contrast to premarketing trials, extensive use of COX-2 inhibitors is likely to demonstrate gastrointestinal adverse effects similar to those caused by traditional NSAIDs."( Celecoxib associated esophagitis: review of gastrointestinal side effects from cox-2 inhibitors.
Mantry, P; Shah, A; Sundaram, U, 2003)		1.76
" Pregnancy and lactation require precise monitoring of adverse effects on the fetus, neonate and infant, or discontinuation of therapy with the drug."( [Coxibs: highly selective cyclooxygenase-2 inhibitors. Part II. Side effects].
Burdan, F; Korobowicz, A, 2003)		0.32
"COX-2 inhibitors provide a potentially safe alternative for treatment of inflammatory conditions in patients with AERD."( Safety of COX-2 inhibitors in asthma patients with aspirin hypersensitivity.
Fernández, C; West, PM, 2003)		0.32
" The most common treatment-related adverse events for tramadol/APAP were somnolence (6."( Efficacy and safety of tramadol/acetaminophen tablets (Ultracet) as add-on therapy for osteoarthritis pain in subjects receiving a COX-2 nonsteroidal antiinflammatory drug: a multicenter, randomized, double-blind, placebo-controlled trial.
Emkey, R; Jordan, D; Kamin, M; Rosenthal, N; Wu, SC, 2004)		0.32
"5 mg/APAP 325 mg combination tablets were effective and safe as add-on therapy with COX-2 NSAID for treatment of OA pain."( Efficacy and safety of tramadol/acetaminophen tablets (Ultracet) as add-on therapy for osteoarthritis pain in subjects receiving a COX-2 nonsteroidal antiinflammatory drug: a multicenter, randomized, double-blind, placebo-controlled trial.
Emkey, R; Jordan, D; Kamin, M; Rosenthal, N; Wu, SC, 2004)		0.32
" Information on suspected adverse drug reactions (ADRs), reasons for stopping treatment, outcome of pregnancies and cause of death were also requested."( Safety profile of celecoxib as used in general practice in England: results of a prescription-event monitoring study.
Layton, D; Shakir, SA; Wilton, LV, 2004)		0.66
"Frequently reported adverse events were those GI events commonly associated with treatment with other NSAIDS."( Safety profile of celecoxib as used in general practice in England: results of a prescription-event monitoring study.
Layton, D; Shakir, SA; Wilton, LV, 2004)		0.66
" Frequencies of adverse events were also recorded."( Gastroduodenal safety and tolerability of lumiracoxib compared with Ibuprofen and celecoxib in patients with osteoarthritis.
Cousin, M; Fiedorowicz-Fabrycy, IF; Gitton, X; Hawkey, CC; Hoexter, G; Nasonov, EL; Pikhlak, EG; Svoboda, P, 2004)		0.55
" A greater number of patients in the ibuprofen group discontinued treatment due to an adverse event compared with both lumiracoxib groups and the celecoxib group."( Gastroduodenal safety and tolerability of lumiracoxib compared with Ibuprofen and celecoxib in patients with osteoarthritis.
Cousin, M; Fiedorowicz-Fabrycy, IF; Gitton, X; Hawkey, CC; Hoexter, G; Nasonov, EL; Pikhlak, EG; Svoboda, P, 2004)		0.75
"Controlled oral challenge with nonsteroidal anti-inflammatory drugs (NSAIDs) is the only definite way to detect safe NSAIDs in patients with NSAID-induced anaphylactoid reactions."( Safety of the new selective cyclooxygenase type 2 inhibitors rofecoxib and celecoxib in patients with anaphylactoid reactions to nonsteroidal anti-inflammatory drugs.
Conde, J; Delgado, J; Florido, JF; López-Pascual, E; Nieto, MA; Ortega, N; Quiralte, J; Sáenz de San Pedro, B, 2004)		0.55
"The SBPCOCs with highly selective COX-2 inhibitors were safe in patients with single-reactive, NSAID-induced anaphylactoid reactions, even in cases that involved pyrazole derivatives."( Safety of the new selective cyclooxygenase type 2 inhibitors rofecoxib and celecoxib in patients with anaphylactoid reactions to nonsteroidal anti-inflammatory drugs.
Conde, J; Delgado, J; Florido, JF; López-Pascual, E; Nieto, MA; Ortega, N; Quiralte, J; Sáenz de San Pedro, B, 2004)		0.55
" The rate of adverse hypersensitivity reactions to these agents is generally low."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.
D'Amato, G; D'Amato, M; Liccardi, G; Piccolo, A; Piscitelli, E; Salzillo, A; Senna, G, 2005)		0.73
"We evaluated the tolerability of CE in a group of patients with documented history of adverse cutaneous reactions to P and N associated or not to classic NSAIDs."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.
D'Amato, G; D'Amato, M; Liccardi, G; Piccolo, A; Piscitelli, E; Salzillo, A; Senna, G, 2005)		0.73
"The objective was to improve understanding of adverse events occurring with celecoxib in the treatment of osteoarthritis and rheumatoid arthritis."( Tolerability and adverse events in clinical trials of celecoxib in osteoarthritis and rheumatoid arthritis: systematic review and meta-analysis of information from company clinical trial reports.
Derry, S; Makinson, GT; McQuay, HJ; Moore, RA, 2005)		0.81
"Cyclooxygenase (COX-2) inhibitors were developed with the hope that they will cause fewer gastrointestinal adverse effects."( Comparative gastrointestinal toxicity of selective cyclooxygenase (COX-2) inhibitors.
Malhotra, S; Nada, R; Pandhi, P; Shafiq, N, 2005)		0.33
"Combination of celecoxib and weekly paclitaxel is safe and active new regimen in pretreated non-small cell lung cancer."( The combination of the selective cyclooxygenase-2 inhibitor celecoxib with weekly paclitaxel is a safe and active second-line therapy for non-small cell lung cancer: a phase II study with biological correlates.
Avallone, A; Bonginelli, P; Comella, G; Gamucci, T; Gasparini, G; Gattuso, D; Gion, M; Lo Vullo, S; Mansueto, G; Mariani, L; Meo, S; Stani, SC, )		0.73
" With celecoxib, studies have shown that a 50% lower dosage is effective and causes fewer adverse effects."( How celecoxib could be safer, how valdecoxib might have been.
Cohen, JS, 2005)		1.37
"The use of selective inhibitors of cyclooxygenase 2 (COX-2) has been shown to be safe in patients with aspirin-induced asthma."( Safety of etoricoxib, a new cyclooxygenase 2 inhibitor, in patients with nonsteroidal anti-inflammatory drug-induced urticaria and angioedema.
Caballero-Fonseca, F; Capriles-Hulett, A; Sánchez-Borges, M, 2005)		0.33
" Adverse experiences (AEs) were recorded and combined from the two studies for analysis."( Efficacy and safety of rofecoxib 12.5 mg and celecoxib 200 mg in two similarly designed osteoarthritis studies.
Birbara, C; Chang, DJ; Petruschke, RA; Rodgers, A; Ruoff, G; Sheldon, E; Tershakovec, AM; Valenzuela, C, 2006)		0.59
" Assessment of safety was performed by upper GI endoscopy, gastrointestinal symptoms evaluation, electrocardiography, blood and urine laboratory tests, adverse events recording."( Gastrointestinal safety of amtolmetin guacyl in comparison with celecoxib in patients with rheumatoid arthritis.
Dankó, K; Jajić, Z; Koó, E; Kovacs, M; Malaise, M; Nekam, K; Scarpignato, C, )		0.37
"Acetaminophen (paracetamol-P) is a widely used analgesic-antipyretic drug with no anti inflammatory effects and its rate of adverse hypersensitivity reactions is very low."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and other non-steroidal anti-inflammatory drugs.
Cazzola, M; D'Amato, G; D'Amato, M; De Giglio, C; Liccardi, G; Manfredi, D; Piscitelli, E, 2005)		0.73
"We evaluated the tolerability of CE in a group of patients with documented history of adverse cutaneous reactions to P and to classic NSAIDs."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and other non-steroidal anti-inflammatory drugs.
Cazzola, M; D'Amato, G; D'Amato, M; De Giglio, C; Liccardi, G; Manfredi, D; Piscitelli, E, 2005)		0.73
" Eleven percent of patients in each group experienced a bowel-related adverse event (P > ."( Safety of celecoxib in patients with ulcerative colitis in remission: a randomized, placebo-controlled, pilot study.
Bloom, BJ; Brynskov, J; Kent, JD; Lorenz, RG; Robbins, JL; Sandborn, WJ; Steidle, GM; Stenson, WF, 2006)		0.74
" The factors that predispose to adverse events by NSAIDs are unknown."( Nitric oxide deficiency promotes vascular side effects of cyclooxygenase inhibitors.
Anning, PB; Coles, B; Dey, SK; Marnett, LJ; Morrow, JD; Morton, J; O'Donnell, VB; Uddin, J; Wang, H, 2006)		0.33
" Adverse experiences were collected for safety assessment."( Efficacy and safety of etoricoxib 30 mg and celecoxib 200 mg in the treatment of osteoarthritis in two identically designed, randomized, placebo-controlled, non-inferiority studies.
Bingham, CO; Bird, S; Fitzgerald, BJ; Kremer, J; O'Brien, K; Rubin, BR; Ruoff, GE; Sebba, AI; Smugar, SS; Tershakovec, AM, 2007)		0.6
"Celecoxib 200 mg bid did not slow the progression of AD in this study, and the occurrence of adverse events was as expected for an elderly population with a complex chronic medical condition."( Long-term efficacy and safety of celecoxib in Alzheimer's disease.
Niculescu, L; Robbins, J; Soininen, H; West, C, 2007)		2.06
" No significant side effect was reported by the 2 groups of patients."( Safety and efficacy of short-term celecoxib before elective percutaneous coronary intervention for stable angina pectoris.
Cianfrocca, C; Granatelli, A; Mercuro, G; Pasceri, V; Pelliccia, F; Pristipino, C; Richichi, G; Roncella, A; Speciale, G, 2006)		0.61
" Gastrointestinal adverse events for IDEA-033 were similar to placebo."( Efficacy and safety of epicutaneous ketoprofen in Transfersome (IDEA-033) versus oral celecoxib and placebo in osteoarthritis of the knee: multicentre randomised controlled trial.
Kneer, W; Lavins, BJ; Lehnhardt, K; Mazgareanu, S; Rother, M; Seidel, EJ, 2007)		0.56
"The cyclooxygenase (COX)-2 inhibitors celecoxib and rofecoxib were studied for their effects on neonatal rat cardiac myocytes as a possible model for the adverse cardiovascular effects that this class of compounds have shown in their clinical use."( The cytotoxicity of celecoxib towards cardiac myocytes is cyclooxygenase-2 independent.
Hasinoff, BB; Patel, D; Wu, X, 2007)		0.93
" Patients at highest baseline risk demonstrated disproportionately greater risk of celecoxib-related adverse events (P for interaction=0."( Cardiovascular risk of celecoxib in 6 randomized placebo-controlled trials: the cross trial safety analysis.
Arber, N; Arndt, G; Bertagnolli, MM; Chew, EY; Finn, PV; Fowler, R; Goss, PE; Hawk, E; Kim, J; Lance, P; Levin, B; Martin, B; Meinert, CL; Obara, S; Pater, JL; Solomon, SD; Viner, J; Wittes, J, 2008)		0.88
" Randomized clinical trials had demonstrated fewer adverse gastrointestinal events with COX-2 inhibitors, but no difference with other adverse events, including adverse renal events."( NSAID use in individuals at risk of renal adverse events: an observational study to investigate trends in Australian veterans.
Gilbert, AL; Pratt, N; Ramsay, E; Roughead, EE, 2008)		0.35
"Despite the increased vulnerability of veterans receiving ACEI-ARB/furosemide or diabetes medicines to adverse events of NSAIDs, uptake rates of COX inhibitors were equivalent to the rest of the veteran population."( NSAID use in individuals at risk of renal adverse events: an observational study to investigate trends in Australian veterans.
Gilbert, AL; Pratt, N; Ramsay, E; Roughead, EE, 2008)		0.35
"To compare the adverse event (AE)-related discontinuation rate with celecoxib vs."( A randomized, multicentre, double-blind, parallel-group study to assess the adverse event-related discontinuation rate with celecoxib and diclofenac in elderly patients with osteoarthritis.
Dahlberg, LE; Holme, I; Høye, K; Ringertz, B, )		0.57
" The results showed significant antitumor effect but also indicated increased cardiovascular adverse events in patients treated with celecoxib compared with placebo."( Five-year efficacy and safety analysis of the Adenoma Prevention with Celecoxib Trial.
Bagheri, D; Bertagnolli, MM; Breazna, A; Burn, J; Chung, DC; Collins, NT; Dewar, T; Eagle, CJ; Foley, TR; Hawk, ET; Hoffman, N; Kim, K; Macrae, F; Pruitt, RE; Redston, M; Rosenstein, RB; Saltzman, JR; Salzberg, B; Sylwestrowicz, T; Tang, J; Umar, A; Zauber, AG, 2009)		0.79
" Selective cyclooxygenase (COX)-2 inhibitors have been developed to avoid the adverse drug reaction of traditional NSAIDs."( Pattern recognition analysis for the prediction of adverse effects by nonsteroidal anti-inflammatory drugs using 1H NMR-based metabolomics in rats.
Choi, KH; Chung, MW; Kim, KB; Kim, SH; Lee, HJ; Oh, HY; Oh, JS; Um, SY, 2009)		0.35
" Treatment-emergent hepatobiliary adverse events (AEs) were compared for celecoxib <200 mg/day (943 patients), 200 mg/day (12 008 patients), 400 mg/day (7380 patients), and 800 mg/day (4602 patients); placebo (4057 patients); diclofenac 100-150 mg/day (7639 patients); naproxen 1000 mg/day (2953 patients); and ibuprofen 2400 mg/day (2484 patients)."( The hepatic safety and tolerability of the cyclooxygenase-2 selective NSAID celecoxib: pooled analysis of 41 randomized controlled trials.
Cawkwell, G; Li, C; Ma, H; Shell, B; Soni, P, 2009)		0.81
"Juvenile toxicology studies in animals provide useful information to guide monitoring of potential adverse effects in children especially on growth and development."( Essentials for starting a pediatric clinical study (4): Clinical pediatric safety planning based on preclinical toxicity studies and pediatric pharmacovigilance guidance.
Sheth, N, 2009)		0.35
"Cyclooxygenase inhibitors represented extremely promising novel anti-inflammatory drugs until one of them, rofecoxib (Vioxx), was found to be associated with increased cardiovascular morbidity; however, another such drug, celecoxib (Celebrex), suffers far less from this side effect for unknown reasons and is still widely used."( An ion channel hypothesis to explain divergent cardiovascular safety of cyclooxygenase-2 inhibitors: the answer to a hotly debated puzzle?
Shapiro, MS, 2009)		0.54
" Adherence and adverse event (AE) monitoring was conducted at 2-week intervals during drug administration."( The safety and efficacy of celecoxib in children with familial adenomatous polyposis.
Ayers, GD; Burke, CA; Church, J; Eagle, C; Half, E; Hasson, H; Hawk, E; Lynch, PM; Patterson, S; Richmond, E; Woloj, M, 2010)		0.66
" Adverse reactions were similar among treatment groups and serious adverse events were rare for all treatments."( Clinical efficacy and safety of glucosamine, chondroitin sulphate, their combination, celecoxib or placebo taken to treat osteoarthritis of the knee: 2-year results from GAIT.
Bingham, CO; Bradley, JD; Clegg, DO; Dunlop, DD; Finco, MF; Furst, DE; Harris, CL; Jackson, CG; Lane, NE; Lisse, J; Moskowitz, RW; Oddis, CV; Reda, DJ; Sawitzke, AD; Shi, H; Silver, D; Singer, NG; Williams, HJ; Wolfe, F, 2010)		0.58
" This may offer a novel therapeutic target for management of the adverse effect of cisplatin chemotherapy."( Amelioration of cisplatin nephrotoxicity by genetic or pharmacologic blockade of prostaglandin synthesis.
Aoyagi, T; Jia, Z; Liu, H; Wang, H; Wang, N; Yang, T, 2011)		0.37
"Gastrointestinal (GI) disorders are common adverse reactions of nonsteroidal anti-inflammatory drugs (NSAIDs)."( Efficacy and safety of the selective cyclooxygenase-2 inhibitor celecoxib in the treatment of rheumatoid arthritis and osteoarthritis in Japan.
Sakamoto, C; Soen, S, 2011)		0.61
"Nephrotic syndrome, with or without concomitant tubulointerstitial nephritis, is a rare renal adverse effect of NSAIDs."( Safe administration of celecoxib to a patient with repeated episodes of nephrotic syndrome induced by NSAIDs.
Knotek, M; Ljubanovic, D; Mihovilovic, K, 2011)		0.68
"This study aimed to evaluate the risks of upper gastrointestinal (GI) adverse events across a variety of oral and parenteral coxibs and nonselective nonsteroidal anti-inflammatory drugs (nsNSAIDs) in the general population of Taiwan."( Risk of hospitalization for upper gastrointestinal adverse events associated with nonsteroidal anti-inflammatory drugs: a nationwide case-crossover study in Taiwan.
Chang, CH; Chen, HC; Kuo, CW; Lai, MS; Lin, JW; Shau, WY, 2011)		0.37
"In a case-crossover study, all patients aged ≥20 years who were hospitalized for upper GI adverse events (peptic ulcer and bleeding; gastritis and duodenitis) in 2006 were identified using the International Classification of Diseases, 9th Revision, Clinical Modification diagnosis codes from inpatient claims from the Taiwan National Health Insurance Database."( Risk of hospitalization for upper gastrointestinal adverse events associated with nonsteroidal anti-inflammatory drugs: a nationwide case-crossover study in Taiwan.
Chang, CH; Chen, HC; Kuo, CW; Lai, MS; Lin, JW; Shau, WY, 2011)		0.37
"A total of 40,635 patients hospitalized for upper GI adverse events were included."( Risk of hospitalization for upper gastrointestinal adverse events associated with nonsteroidal anti-inflammatory drugs: a nationwide case-crossover study in Taiwan.
Chang, CH; Chen, HC; Kuo, CW; Lai, MS; Lin, JW; Shau, WY, 2011)		0.37
" The objective of this study was to evaluate the risk of upper GI adverse events associated with celecoxib and oral and parenteral non-selective NSAIDs in cirrhotic patients."( Non-steroidal anti-inflammatory drugs use and risk of upper gastrointestinal adverse events in cirrhotic patients.
Chang, CH; Chen, HC; Lai, MS; Lee, YC; Lin, JW; Lin, MS, 2012)		0.6
"All the patients aged ≥ 20 years with a diagnosis of cirrhosis hospitalized for variceal bleeding and non-variceal upper GI adverse events (oesophageal, gastric, duodenal ulcer, bleeding; gastritis and duodenitis) in 2006 were identified using ICD-9-CM diagnosis codes from inpatient claims from the Taiwan National Health Insurance Database."( Non-steroidal anti-inflammatory drugs use and risk of upper gastrointestinal adverse events in cirrhotic patients.
Chang, CH; Chen, HC; Lai, MS; Lee, YC; Lin, JW; Lin, MS, 2012)		0.38
" The incidence of treatment-related, all-cause adverse events was slightly lower in patients receiving celecoxib 200 mg (20."( Efficacy and safety of additional 200-mg dose of celecoxib in adult patients with postoperative pain following extraction of impacted third mandibular molar: a multicenter, randomized, double-blind, placebo-controlled, phase II study in Japan.
Kaneko, A; Machii, K; Ohkura, M; Ohta, H; Saito, K; Suzuki, M, 2012)		0.85
" Incidence of moderate-to-severe abdominal symptoms and discontinuation of treatment due to GI adverse events (AEs) were lower in the celecoxib group."( Efficacy and safety of celecoxib versus diclofenac and omeprazole in elderly arthritis patients: a subgroup analysis of the CONDOR trial.
Essex, MN; Kellner, HL; Li, C, 2012)		0.89
" Furthermore, the panel agreed there is substantial evidence to indicate that cost savings can be achieved by using celecoxib in patients at moderate to high risk of gastrointestinal adverse events, even in countries with moderate healthcare expenditures."( A review of the efficacy, safety, and cost-effectiveness of COX-2 inhibitors for Africa and the Middle East region.
Al Sayed, B; Bargaoui, N; Djebbar, M; Djennane, M; Donald, R; El Deeb, K; Joudeh, RA; Nabhan, A; Schug, SA; Zeidan, AZ, 2013)		0.6
"COX-2 inhibitors are safe alternatives in patients with cross-reactive non-steroidal anti-inflammatory drug (NSAID) hypersensitivity."( Are drug provocation tests still necessary to test the safety of COX-2 inhibitors in patients with cross-reactive NSAID hypersensitivity?
Aydın, Ö; Çelik, GE; Demirel, YS; Erkekol, FÖ; Mısırlıgil, Z, )		0.13
"This study included the retrospective analysis of cases with cross-reactive NSAID hypersensitivity who underwent DPTs with COX-2 inhibitors in order to find safe alternatives."( Are drug provocation tests still necessary to test the safety of COX-2 inhibitors in patients with cross-reactive NSAID hypersensitivity?
Aydın, Ö; Çelik, GE; Demirel, YS; Erkekol, FÖ; Mısırlıgil, Z, )		0.13
"Our results suggest to follow the traditional DPT method to introduce COX-2 inhibitors for finding safe alternatives in all patients with cross-reactive NSAID hypersensitivity before prescription as uncertainty of any predictive factor for a positive response continues."( Are drug provocation tests still necessary to test the safety of COX-2 inhibitors in patients with cross-reactive NSAID hypersensitivity?
Aydın, Ö; Çelik, GE; Demirel, YS; Erkekol, FÖ; Mısırlıgil, Z, )		0.13
" Safety concerns associated with nonsteroidal anti-inflammatory drugs (NSAIDs) have prompted the development of new formulations that minimize adverse events (AEs) and maintain efficacy."( A phase 2 study evaluating the efficacy and safety of a novel, proprietary, nano-formulated, lower dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012)		0.38
" The relevance of the gathered results will be discussed in terms of the reported celecoxib therapeutic and toxic effects."( Interaction of celecoxib with membranes: the role of membrane biophysics on its therapeutic and toxic effects.
Lima, JL; Lúcio, M; Nunes, C; Pereira-Leite, C; Reis, S, 2012)		0.96
" For older adult patients at higher risk for NSAID-related adverse effects, such as those who have gastrointestinal or cardiovascular disease, diabetes mellitus, or who are taking low-dose aspirin, opioids are recommended instead."( Opioids for chronic pain: new evidence, new strategies, safe prescribing.
de Leon-Casasola, OA, 2013)		0.39
"To study the adverse effects of Celecoxib and compare them with those of other non-steroidal anti-inflammatory drugs (NSAIDs) in an Asian Indian cohort."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013)		1.05
" All the recorded adverse events were noted and compared between the Celecoxib and non-selective NSAID users."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013)		1
" Multiple NSAID users had higher adverse events (6."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013)		0.77
" The adverse events were mild (gastric, grade 1; and hematologic, grade 1 or 2)."( Safety and therapeutic effect of metronomic chemotherapy with cyclophosphamide and celecoxib in advanced breast cancer patients.
Alasino, CM; Mainetti, LE; Perroud, HA; Pezzotto, SM; Queralt, F; Rico, MJ; Rozados, VR; Scharovsky, OG, 2013)		0.61
"Further understand the safety profile of celecoxib and provide safety information for important adverse events (AEs)."( Safety of celecoxib compared with placebo and non-selective NSAIDs: cumulative meta-analysis of 89 randomized controlled trials.
Berger, MF; Essex, MN; Park, PW; Upadhyay, S; Zhang, RY, 2013)		1.06
" The most frequent types of treatment-related adverse events reported were gastrointestinal for oral (15."( A multicentre, randomized, placebo- and active-controlled trial comparing the efficacy and safety of topical ketoprofen in Transfersome gel (IDEA-033) with ketoprofen-free vehicle (TDT 064) and oral celecoxib for knee pain associated with osteoarthritis.
Bolten, W; Cevc, G; Conaghan, PG; Dickson, J; Rother, M, 2013)		0.58
" Adverse drug reactions (ADRs) were carefully investigated."( A prospective, randomized, double-blind, multicenter comparative study on the safety and efficacy of Celecoxib and GCSB-5, dried extracts of six herbs, for the treatment of osteoarthritis of knee joint.
Bin, SI; Ha, CW; Han, CD; Jung, YB; Kim, HC; Lim, HC; Park, YG, 2013)		0.61
"Use of nonsteroidal anti-inflammatory drugs (NSAIDs) is primarily limited by renal and gastrointestinal adverse effects."( Effects of rebamipide on nephrotoxicity associated with selected NSAIDs in rats.
Bullins, KW; Denham, JW; Hanley, AV; Hanley, GA; Harirforoosh, S; Panus, PC; Wood, RC; Wyatt, JE, 2013)		0.39
" For safety assessment, adverse events were recorded at each clinical visit."( Efficacy and safety of PG201 (Layla(®)) and celecoxib in the treatment of symptomatic knee osteoarthritis: a double-blinded, randomized, multi-center, active drug comparative, parallel-group, non-inferiority, phase III study.
Baek, HJ; Choi, SJ; Kang, SW; Kim, HA; Ko, HS; Lee, YJ; Park, SH; Shim, SC; Song, JS; Song, YW; Suh, CH; Tae, DN; Yoo, HG; Yoo, WH; Yoon, BY, 2014)		0.66
" Safety assessments included adverse events, physical and neurological examinations, laboratory tests and vital signs."( Efficacy and safety of tanezumab monotherapy or combined with non-steroidal anti-inflammatory drugs in the treatment of knee or hip osteoarthritis pain.
Brown, MT; Ekman, EF; Greenberg, HS; Schnitzer, TJ; Smith, MD; Spierings, EL; Verburg, KM; West, CR, 2015)		0.42
" Adverse event frequency was higher with tanezumab than with NSAIDs and highest with combination therapy."( Efficacy and safety of tanezumab monotherapy or combined with non-steroidal anti-inflammatory drugs in the treatment of knee or hip osteoarthritis pain.
Brown, MT; Ekman, EF; Greenberg, HS; Schnitzer, TJ; Smith, MD; Spierings, EL; Verburg, KM; West, CR, 2015)		0.42
" All adverse events (AEs) regardless of severity were captured in the database."( Safety of celecoxib and nonselective nonsteroidal anti-inflammatory drugs in juvenile idiopathic arthritis: results of the Phase 4 registry.
Abramsky, S; Brunner, HI; Chalom, EC; Giannini, EH; Goldsmith, DP; Gottlieb, BS; Jung, LK; Lovell, DJ; Morris, PW; Nanda, K; Onel, KB; Petiniot, L; Shishov, M; Sobel, RE; Weiss, JE; Young, JP, 2014)		0.8
"6% patients in the celecoxib group experienced an adverse drug reaction (ADR)."( Comparison of the efficacy and safety profiles of a pelubiprofen versus celecoxib in patients with rheumatoid arthritis: a 6-week, multicenter, randomized, double-blind, phase III, non-inferiority clinical trial.
Baek, HJ; Cho, CS; Choi, IA; Chung, WT; Kang, SW; Kim, HA; Lee, J; Lee, SS; Lee, YA; Lee, YJ; Park, YB; Park, YE; Song, JS; Song, YW; Yoo, WH, 2014)		0.96
" Our objective was to estimate and compare rates of gastrointestinal, renovascular, and cardiovascular adverse events in patients exposed to etoricoxib, celecoxib, or nonselective NSAIDs or totally unexposed to NSAIDs."( Safety of Etoricoxib, Celecoxib, and Nonselective Nonsteroidal Antiinflammatory Drugs in Ankylosing Spondylitis and Other Spondyloarthritis Patients: A Swedish National Population-Based Cohort Study.
Askling, J; Jacobsson, LT; Jakobsen, AK; Kristensen, LE; Nilsson, F, 2015)		0.93
" No major risk differences for serious cardiovascular, gastrointestinal, or renal adverse events were seen among the 3 exposure groups."( Safety of Etoricoxib, Celecoxib, and Nonselective Nonsteroidal Antiinflammatory Drugs in Ankylosing Spondylitis and Other Spondyloarthritis Patients: A Swedish National Population-Based Cohort Study.
Askling, J; Jacobsson, LT; Jakobsen, AK; Kristensen, LE; Nilsson, F, 2015)		0.73
"Overall, serious adverse events related to nonselective NSAIDs, etoricoxib, and celecoxib were similar and in the range of what would be expected in a group of SpA patients."( Safety of Etoricoxib, Celecoxib, and Nonselective Nonsteroidal Antiinflammatory Drugs in Ankylosing Spondylitis and Other Spondyloarthritis Patients: A Swedish National Population-Based Cohort Study.
Askling, J; Jacobsson, LT; Jakobsen, AK; Kristensen, LE; Nilsson, F, 2015)		0.96
" Secondary endpoints, including Patient's and Physician's Global Assessments of Arthritis, Western Ontario and McMaster Universities OA Index (WOMAC), use of complementary and alternative medicines, incidence of treatment-emergent adverse events (TEAEs) and measurements of upper gastrointestinal tolerability, were also assessed."( Efficacy and safety of nonsteroidal anti-inflammatory drugs in Asian patients with knee osteoarthritis: summary of a randomized, placebo-controlled study.
Bao, W; Behar, R; Essex, MN; O'Connell, MA, 2016)		0.43
" Celecoxib was shown to be safe and well tolerated in this patient population."( Efficacy and safety of nonsteroidal anti-inflammatory drugs in Asian patients with knee osteoarthritis: summary of a randomized, placebo-controlled study.
Bao, W; Behar, R; Essex, MN; O'Connell, MA, 2016)		1.34
" Although no significant difference was observed among the five options with respect to the three major adverse effects (withdrawal due to adverse events, serious adverse events and the number of patients with adverse events), the additional classical meta-analysis showed that celecoxib exhibited a higher rate of gastrointestinal adverse effect comparing with the placebo group."( Effectiveness and safety of Glucosamine, chondroitin, the two in combination, or celecoxib in the treatment of osteoarthritis of the knee.
Gao, SG; Lei, GH; Li, H; Li, YS; Luo, W; Wang, YL; Wei, J; Xie, DX; Yang, T; Zeng, C, 2015)		0.82
" These results indicate GCSB-5 is safe for a long-term treatment of knee OA patients."( Gastrointestinal safety and efficacy of long-term GCSB-5 use in patients with osteoarthritis: A 24-week, multicenter study.
Bae, KC; Bin, SI; Cho, SD; Choi, ES; Ha, CW; Han, CS; Kang, JS; Kim, CW; Kim, JG; Kyung, HS; Lee, DC; Lee, JH; Lee, MC; Lee, WS; Lim, HC; Park, SE; Park, YB; Seon, JK; Won, YY, 2016)		0.43
" There was no significant difference in the incidence of adverse events (AEs), SAEs, and discontinuations due to AEs; however, the incidence of gastrointestinal AEs in OA patients treatment with celecoxib is significantly higher than that with placebo."( Efficacy and Safety of Celecoxib Therapy in Osteoarthritis: A Meta-Analysis of Randomized Controlled Trials.
Gu, K; Hou, Y; Xu, C; Yasen, Y, 2016)		0.93
"Nonsteroidal anti-inflammatory drugs (NSAIDs), which are globally prescribed, exhibit mainly anti-inflammatory and analgesic effects but also can cause adverse effects including gastrointestinal erosions, ulceration, bleeding, and perforation."( (1)H-Nuclear magnetic resonance-based metabolic profiling of nonsteroidal anti-inflammatory drug-induced adverse effects in rats.
Choi, KH; Chung, MW; Lee, HJ; Park, JH; Um, SY, 2016)		0.43
" The hypothesis is that compared to placebo with opioids as rescue treatment, sequential use of parecoxib and celecoxib can achieve less morphine consumption over the postoperative 2 weeks, as well as better pain control, quicker functional recovery in the postoperative 6 weeks and less opioid-related adverse events during the 12-week recovery phase."( Efficacy and safety of Postoperative Intravenous Parecoxib sodium Followed by ORal CElecoxib (PIPFORCE) post-total knee arthroplasty in patients with osteoarthritis: a study protocol for a multicentre, double-blind, parallel-group trial.
Bian, Y; Feng, B; Jiang, J; Lin, J; Pei, F; Shen, B; Sun, T; Wang, W; Weng, X; Yan, S; Zhang, M; Zhuang, Q, 2016)		0.87
" No serious adverse event was reported."( A Randomized, Double-Blind Placebo-Controlled Trial on Effectiveness and Safety of Celecoxib Adjunctive Therapy in Adolescents with Acute Bipolar Mania.
Akhondzadeh, S; Gholamian, F; Karkhaneh-Yousefi, MA; Khezri, R; Mohammadi, MR; Mohammadinejad, P; Mousavi, SY; Zeinoddini, A, 2017)		0.68
" Excluding patients who reached study endpoints, 21 (8%) patients in the celecoxib group and 17 (7%) patients in the naproxen group had adverse events leading to discontinuation of treatment."( Gastrointestinal safety of celecoxib versus naproxen in patients with cardiothrombotic diseases and arthritis after upper gastrointestinal bleeding (CONCERN): an industry-independent, double-blind, double-dummy, randomised trial.
Au, KWL; Chan, FKL; Chan, H; Cheong, PK; Ching, JYL; Kee, KM; Kyaw, MH; Lam, K; Lee, V; Lo, A; Ng, SC; Suen, BY; Tse, YK; Wong, GLH; Wong, VWS; Wu, JCY, 2017)		0.98
" The outcome was major nonsteroidal anti-inflammatory drug toxicity, including time to first occurrence of major adverse cardiovascular events, important gastrointestinal events, renal events, and all-cause mortality."( The Risk of Major NSAID Toxicity with Celecoxib, Ibuprofen, or Naproxen: A Secondary Analysis of the PRECISION Trial.
Borer, JS; Brennan, DM; Husni, ME; Libby, PA; Lincoff, AM; Lϋscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wisniewski, LM; Yeomans, ND, 2017)		0.73
" No difference in adverse events was observed between the two groups."( Efficacy and safety of adalimumab by intra-articular injection for moderate to severe knee osteoarthritis: An open-label randomized controlled trial.
Wang, J, 2018)		0.48
"Non-steroidal anti-inflammatory drugs (NSAIDs), both non-selective and selective cyclooxygenase-2 (COX-2) inhibitors, are among the most widely prescribed drugs worldwide, but associate with increased blood pressure (BP) and adverse cardiovascular (CV) events."( Differential blood pressure effects of ibuprofen, naproxen, and celecoxib in patients with arthritis: the PRECISION-ABPM (Prospective Randomized Evaluation of Celecoxib Integrated Safety Versus Ibuprofen or Naproxen Ambulatory Blood Pressure Measurement)
Beckerman, B; Borer, JS; Davey, DA; Fayyad, R; Flammer, AJ; Graham, DY; Husni, ME; Iorga, D; Krum, H; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Ruschitzka, F; Solomon, DH; Wisniewski, LM; Yeomans, ND, 2017)		0.69
" Pain visual analog scale (VAS) scores (at rest and at 90 flexion) and patient global assessment (PGA) score were evaluated before and after operation, and also pethidine consumption and adverse events (AEs)."( The efficacy and safety of early initiation of preoperative analgesia with celecoxib in patients underwent arthroscopic knee surgery: A randomized, controlled study.
Du, Y; Huang, W; Shan, J; Xu, G; Zhou, F, 2017)		0.69
" Other outcome measures included adverse events (AEs), laboratory tests, vital signs, electrocardiograms, and physical examinations."( A Randomized, Multicenter, Phase III Trial to Evaluate the Efficacy and Safety of Polmacoxib Compared with Celecoxib and Placebo for Patients with Osteoarthritis.
Bin, SI; Cho, S; Choi, CH; Han, SB; In, Y; Kang, SB; Kim, J; Kim, JG; Kim, YM; Kyung, HS; Lee, BK; Lee, M; Moon, YW; Yoo, J, 2017)		0.67
" The results obtained during the 18-week trial extension with polmacoxib 2 mg were consistent with those observed during the 6-week treatment period, indicating that polmacoxib can be considered safe for long-term use based on this relatively small scale of study in a Korean population."( A Randomized, Multicenter, Phase III Trial to Evaluate the Efficacy and Safety of Polmacoxib Compared with Celecoxib and Placebo for Patients with Osteoarthritis.
Bin, SI; Cho, S; Choi, CH; Han, SB; In, Y; Kang, SB; Kim, J; Kim, JG; Kim, YM; Kyung, HS; Lee, BK; Lee, M; Moon, YW; Yoo, J, 2017)		0.67
"To determine the relative risks of cardiovascular (CV), gastrointestinal (GI), and renal adverse events during long-term treatment with celecoxib, compared with ibuprofen and naproxen, in patients with osteoarthritis (OA) and patients with rheumatoid arthritis (RA)."( Differences in Safety of Nonsteroidal Antiinflammatory Drugs in Patients With Osteoarthritis and Patients With Rheumatoid Arthritis: A Randomized Clinical Trial.
Bao, W; Berger, MF; Borer, JS; Graham, DY; Husni, ME; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wang, Q; Wisniewski, LM; Wolski, KE; Yeomans, ND, 2018)		0.68
" The main outcomes were the first occurrence of a major adverse CV event, GI event, or renal event, and mortality."( Differences in Safety of Nonsteroidal Antiinflammatory Drugs in Patients With Osteoarthritis and Patients With Rheumatoid Arthritis: A Randomized Clinical Trial.
Bao, W; Berger, MF; Borer, JS; Graham, DY; Husni, ME; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wang, Q; Wisniewski, LM; Wolski, KE; Yeomans, ND, 2018)		0.48
"Treatment with celecoxib at approved dosages conferred a similar or lower risk of CV, GI, and renal adverse events compared with treatment with ibuprofen or naproxen in patients with OA and patients with RA."( Differences in Safety of Nonsteroidal Antiinflammatory Drugs in Patients With Osteoarthritis and Patients With Rheumatoid Arthritis: A Randomized Clinical Trial.
Bao, W; Berger, MF; Borer, JS; Graham, DY; Husni, ME; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wang, Q; Wisniewski, LM; Wolski, KE; Yeomans, ND, 2018)		0.83
"Celecoxib combined with chemotherapy yields clinical benefits for gastric cancer patients with positive COX-2, which not only enhances the OS, DFS, PFS, QOL, and short-term clinical efficacy, but also does not increase the risk of adverse events."( Comprehensive evaluation of clinical efficacy and safety of celecoxib combined with chemotherapy in management of gastric cancer.
Chen, Z; Guo, Q; Ji, R; Liu, X; Lu, L; Wang, Y; Yuan, H; Zhou, Y, 2017)		2.14
" In conclusion, celecoxib was both toxic and teratogenic in Xenopus embryos, where it produced serious heart and vessel malformation by inhibiting vascular wall maturation and vascular network formation."( Evaluation of the toxic effects of celecoxib on Xenopus embryo development.
Bae, YC; Cho, HJ; Chung, HY; Kim, JY; Lee, HS; Lee, S; Nam, SW; Park, MJ; Yoon, YH, 2018)		1.1
" In addition, the rate of adverse reaction of research group was also lower than that of control group, P<0."( Clinical therapeutic effect and safety of celecoxib in treating knee osteoarthritis.
Bi, J; Yu, C; Yu, X; Yu, Z; Zhao, L, 2018)		0.75
" The risk score was designed to predict the 1-year occurrence of major toxicity among NSAID users, including major adverse cardiovascular events, acute kidney injury, significant gastrointestinal events, and mortality."( Derivation and Validation of a Major Toxicity Risk Score Among Nonsteroidal Antiinflammatory Drug Users Based on Data From a Randomized Controlled Trial.
Husni, ME; Nissen, S; Paynter, N; Shao, M; Solomon, DH; Wolski, K, 2019)		0.51
"To perform an international comparison and analysis of celecoxib spontaneous adverse event reports (AERs) from Canada, Australia and the United States, focusing on gastrointestinal, renal and cardiovascular events."( Potentially inappropriate concomitant medicine use with the selective COX-2 inhibitor celecoxib: Analysis and comparison of spontaneous adverse event reports from Australia, Canada and the USA.
Ahmed, R; Baselyous, Y; De Cocinis, M; Ibrahim, M; Kalra, A; Yacoub, R, 2019)		0.98
" Gastrointestinal disorders were the most frequently reported adverse events at the system organ class (SOC) level in the AERs."( Potentially inappropriate concomitant medicine use with the selective COX-2 inhibitor celecoxib: Analysis and comparison of spontaneous adverse event reports from Australia, Canada and the USA.
Ahmed, R; Baselyous, Y; De Cocinis, M; Ibrahim, M; Kalra, A; Yacoub, R, 2019)		0.74
"The large number of reports that involved a concomitant medicine that was in contravention with prescribing guidelines indicates an increased need for efforts to support the safe prescribing of celecoxib."( Potentially inappropriate concomitant medicine use with the selective COX-2 inhibitor celecoxib: Analysis and comparison of spontaneous adverse event reports from Australia, Canada and the USA.
Ahmed, R; Baselyous, Y; De Cocinis, M; Ibrahim, M; Kalra, A; Yacoub, R, 2019)		0.93
"9% (25/282) of placebo-treated subjects reported a treatment-emergent adverse event (TEAE)."( Efficacy, Tolerability, and Safety of DFN-15 (Celecoxib Oral Solution, 25 mg/mL) in the Acute Treatment of Episodic Migraine: A Randomized, Double-Blind, Placebo-Controlled Study.
Brand-Schieber, E; Dodick, DW; Lipton, RB; Munjal, S; Tepper, SJ, 2020)		0.82
" Since then, many coxibs have been discontinued one by one due to adverse cardiovascular events."( Structural investigation on the selective COX-2 inhibitors mediated cardiotoxicity: A review.
Arora, M; Choudhary, S; Sapra, B; Silakari, O; Singh, PK, 2020)		0.56
" CDDP-induced nephrotoxicity (CIN) is one of the most severe adverse events associated with the use of CDDP."( Comparison of the nephroprotective effects of non-steroidal anti-inflammatory drugs on cisplatin-induced nephrotoxicity in vitro and in vivo.
Furugen, A; Iseki, K; Kobayashi, M; Narumi, K; Okamoto, K; Saito, Y, 2020)		0.56
" As for adverse events, the incidences of nausea, vomiting, constipation, drowsiness and dizziness were similar between PRE group and POST group."( Efficiency and safety: comparison between preoperative analgesia and postoperative analgesia using non-steroidal anti-inflammatory drugs in patients receiving arthroscopic knee surgery in a multicenter, randomized, controlled study.
Jiang, C; Ma, L; Wang, H; Zhang, L, 2021)		0.62
" Pain at rest/motion (based on pain visual analog scale (VAS) score), rescue analgesia consumption, satisfaction level and adverse events were assessed after AKS."( Oxycodone-paracetamol tablet exhibits increased analgesic efficacy for acute postoperative pain, higher satisfaction and comparable safety profiles compared with celecoxib in patients underwent arthroscopic knee surgery.
Di, J; Liu, J; Xing, E; Zhang, Y, 2021)		0.82
"The aim of this meta-analysis was to assess the analgesic efficacy and adverse effects of celecoxib compared to non-opioid drugs after third molar surgery."( Analgesic effectiveness and safety of celecoxib versus non-opioid active controls after third molar surgery: A meta-analytical evaluation.
Alonso-Castro, ÁJ; Franco-de la Torre, L; Franco-González, MA; Isiordia-Espinoza, MA, 2022)		1.21
" DFN-15 was similar to placebo in the incidence of adverse events with no apparent dose-related effects."( Efficacy and safety of single-dose DFN-15 for treatment of acute postsurgical dental pain: a randomized, double-blind, placebo-controlled study.
Bertoch, T; Munjal, S; Shenoy, S; Singla, N, 2022)		0.72
"The main GI and CV adverse events associated with NSAID use are reviewed."( Gastrointestinal and cardiovascular adverse events associated with NSAIDs.
Domper Arnal, MJ; Hijos-Mallada, G; Lanas, A, 2022)		0.72
" In this study, we focused on an analysis of celecoxib toxic effects on isolated mitochondria."( Celecoxib decreases mitochondrial complex IV activity and induces oxidative stress in isolated rat heart mitochondria: An analysis for its cardiotoxic adverse effect.
Atashbar, S; Jamali, Z; Khezri, S; Salimi, A, 2022)		2.42
"Mitochondria are the main target organelles through which drugs and chemicals exert their toxic effect on cardiomyocytes."( Gallic acid inhibits celecoxib-induced mitochondrial permeability transition and reduces its toxicity in isolated cardiomyocytes and mitochondria.
Atashbar, S; Salimi, A; Shabani, M, 2021)		0.94
" No severe adverse events were observed."( Efficacy and safety of treating chronic nonspecific low back pain with radial extracorporeal shock wave therapy (rESWT), rESWT combined with celecoxib and eperisone (C + E) or C + E alone: a prospective, randomized trial.
Feng, Z; Guo, X; Li, L; Li, Y; Peng, Z; Schmitz, C; Yan, Z; Yang, Y; Zhang, Y, 2021)		0.82
"Celecoxib is relatively safe in rheumatoid arthritis and osteoarthritis patients, independent of dose or duration."( Cardiovascular safety of celecoxib in rheumatoid arthritis and osteoarthritis patients: A systematic review and meta-analysis.
Chen, JQ; Cheng, BR; Gao, QY; Li, WH; Liu, JP; Wu, CJ; Xing, JL; Yan, LJ; Zhang, XW; Zhang, YQ, 2021)		2.37
" The pain visual analog scale (VAS) score at rest or flexion, salvage consumption of pethidine, patient's satisfaction score, modified University of California at Los Angeles (UCLA) score and adverse events were evaluated."( The analgesic effect and safety of preoperative versus postoperative administration of celecoxib in patients who underwent arthroscopic rotator cuff repair: a randomized, controlled study.
Liu, L; Shao, Y; Wang, J; Wang, S; Yang, J, 2022)		0.94
" However, no difference of modified UCLA scores at D7 or M3, or the occurrences of adverse events were found between the two groups."( The analgesic effect and safety of preoperative versus postoperative administration of celecoxib in patients who underwent arthroscopic rotator cuff repair: a randomized, controlled study.
Liu, L; Shao, Y; Wang, J; Wang, S; Yang, J, 2022)		0.94
", celecoxib) are believed to have fewer gastrointestinal (GI) adverse effects than nonselective NSAIDS."( Meloxicam versus Celecoxib for Postoperative Analgesia after Total Knee Arthroplasty: Safety, Efficacy and Cost.
Breckenridge, L; Fillingham, YA; Gursay, D; Haffar, A; Lonner, JH, 2022)		1.78
" Although superiority to tramadol was not reached, CTC 200 mg BID exposed patients to lower cumulative opioid (tramadol) doses than tramadol (100 mg QID) alone, with fewer treatment-emergent adverse events."( Efficacy and safety of co-crystal of tramadol-celecoxib (CTC) in acute moderate-to-severe pain after abdominal hysterectomy: A randomized, double-blind, phase 3 trial (STARDOM2).
Adeyemi, S; But-Husaim, L; Cebrecos, J; Fettiplace, J; Gascón, N; Langford, R; Morte, A; Ortiz, E; Plata-Salamán, C; Raba, G; Sust, M; Vaqué, A, 2022)		0.98
" Adverse drug reactions may be renal, gastrointestinal, hematological, or immunologic."( Efficacy and Safety of NSAIDs in Infants: A Comprehensive Review of the Literature of the Past 20 Years.
Gorenflo, M; Saur, P; van den Anker, JN; van Dyk, M; Welzel, T; Ziesenitz, VC, 2022)		0.72
" The endpoints were overall survival (OS), progression-free survival (PFS), disease-free survival (DFS), objective response rate (ORR), disease control rate (DCR), pathological complete response (pCR), and adverse events (AEs)."( The Efficacy and Safety of Celecoxib in Addition to Standard Cancer Therapy: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Chen, XW; Gao, P; Huang, XZ; Li, JY; Li, TH; Li, Y; Song, YX; Sun, JX; Wu, ZH; Ye, SY; Zhao, JH, 2022)		1.02
" The results showed that celecoxib (20 µg/ml) induced a significant increase in cytotoxicity, reactive oxygen species (ROS) formation, mitochondria membrane potential (ΔΨm) collapse, lipid peroxidation, oxidative stress and mitochondrial swelling while CuCsSLN and curcumin reverted the above toxic effect of celecoxib."( Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and Mitochondria.
Ebrahimi, HA; Esmaeli, S; Khezri, S; Salimi, A, 2023)		1.44
" Safety indexes will be recorded before and after treatment, and adverse events (AEs) will be recorded throughout this trial."( Efficacy and safety of Yaobitong capsule for acute lumbar disc herniation: A protocol for a multi-center randomized controlled trial.
Gu, M; Lei, Q; Li, S; Li, Z; Shi, M; Tang, B; Wang, S; Yang, K; Yin, H; Zhang, X; Zhao, C; Zhou, G, 2022)		0.72
"Selective COX-2 inhibitor NSAIDs are safe in patients with N-ERD."( Which non-steroidal anti-inflammatory drug (NSAID) is safer in patients with Non-steroids Exacerbated Respiratory Disease (N-ERD)? A single-center retrospective study.
Çakmak, ME, 2022)		0.72
" Besides, the incidences of all adverse events were not different between imrecoxib and celecoxib groups (all P > 0."( Postoperative analgesic efficacy and safety of imrecoxib versus celecoxib in hip osteoarthritis patients undergoing total hip arthroplasty: a multi-center, randomized, controlled, non-inferiority study.
Cui, S; Jiang, L; Liu, Z; Miao, X; Wang, Z; Zhang, K, 2023)		1.37
" The obtained results indicate that CLX bioavailability has been considerably improved without being toxic to the heart with the aid of NE and advocate the use of PDL NE for developing oral formulations for poorly soluble drugs."( Attenuation of celecoxib cardiac toxicity using Poly(δ-decalactone) based nanoemulsion via oral route.
Bansal, KK; Maru, S; Rosenholm, JM; Verma, J; Wilen, CE, 2023)		1.26
" Additionally, no serious adverse events occurred following combination therapy, with most adverse events being mild and resolving without specific treatment."( Efficacy and safety of diacerein and celecoxib combination therapy for knee osteoarthritis: A double-blind, randomized, placebo-controlled prospective study.
Choi, JH; Choi, WS; Kim, C; Kim, SM; Youn, S, 2023)		1.18
"Diacerein and celecoxib combination therapy is as safe and effective as corresponding monotherapies."( Efficacy and safety of diacerein and celecoxib combination therapy for knee osteoarthritis: A double-blind, randomized, placebo-controlled prospective study.
Choi, JH; Choi, WS; Kim, C; Kim, SM; Youn, S, 2023)		1.54

Pharmacokinetics

Polymorphisms in the CYP2C9 gene have been associated with decreased enzyme activity and alteration of celecoxib pharmacokinetic parameters. In this study, in vitro dissolution testing using biorelevant media was applied to the prediction of food effects on the absorption of a poorly soluble drug.

ExcerptReferenceRelevance
"To determine the effects of celecoxib, a specific inhibitor of cyclooxygenase 2 (COX-2) on the renal clearance and plasma pharmacokinetic profile of stable methotrexate (MTX) doses in patients with rheumatoid arthritis (RA)."( Celecoxib, a specific COX-2 inhibitor, has no significant effect on methotrexate pharmacokinetics in patients with rheumatoid arthritis.
Geis, GS; Harper, KM; Hubbard, RC; Hunt, TL; Karim, A; Tolbert, DS, 1999)		2.04
"The plasma pharmacokinetic profile of MTX did not change significantly when celecoxib or a placebo was coadministered."( Celecoxib, a specific COX-2 inhibitor, has no significant effect on methotrexate pharmacokinetics in patients with rheumatoid arthritis.
Geis, GS; Harper, KM; Hubbard, RC; Hunt, TL; Karim, A; Tolbert, DS, 1999)		1.98
" Celecoxib is metabolised primarily by the cytochrome P450 (CYP) 2C9 isoenzyme and has an elimination half-life of about 11 hours in healthy individuals."( Clinical pharmacokinetics and pharmacodynamics of celecoxib: a selective cyclo-oxygenase-2 inhibitor.
Davies, NM; Day, RO; McLachlan, AJ; Williams, KM, 2000)		1.47
" Maximal concentration of radioactivity was reached in most all tissues between 1 and 3 h postdose with the half-life paralleling that of plasma, with the exception of the gastrointestinal tract tissues."( Pharmacokinetics, tissue distribution, metabolism, and excretion of celecoxib in rats.
Breau, AP; Burton, EG; Cogburn, JN; Gresk, CJ; Hribar, JD; Jessen, SM; Lawal, YM; Liu, NW; Markos, CS; Maziasz, TJ; Paulson, SK; Schoenhard, GL; Zhang, JY, 2000)		0.54
"The objective of this study was to determine the effects of celecoxib, an anti-inflammatory/analgesic agent that primarily inhibits COX-2 and not COX-1 at therapeutic doses, on the steady-state pharmacokinetic profile and hypoprothrombinemic effect of racemic warfarin in healthy volunteers."( Celecoxib does not significantly alter the pharmacokinetics or hypoprothrombinemic effect of warfarin in healthy subjects.
Geis, GS; Harper, K; Hubbard, RC; Karim, A; Piergies, A; Slater, M; Tolbert, D; Wallemark, CB, 2000)		1.99
"The validated assay has sufficient accuracy and precision for pharmacokinetic studies of CEL in the rat."( Pharmacokinetics of celecoxib in the presence and absence of interferon-induced acute inflammation in the rat: application of a novel HPLC assay.
Guirguis, MS; Jamali, F; Sattari , S, )		0.45
" The validated LC-MS method has been utilized to establish various pharmacokinetic parameters of celecoxib following a single oral dose administration of celecoxib capsules in two selected volunteers."( Liquid chromatographic-mass spectrometric determination of celecoxib in plasma using single-ion monitoring and its use in clinical pharmacokinetics.
Abdel-Hamid, M; Hamza, H; Novotny, L, 2001)		0.77
" After validation, the method was used to study the pharmacokinetic profile of celecoxib following administration of a single oral dose (200 mg) in 12 healthy volunteers."( Investigation of the pharmacokinetics of celecoxib by liquid chromatography-mass spectrometry.
Brune, K; Gillich, M; Mundkowski, R; Pahl, A; Werner, D; Werner, U, 2002)		0.81
" As an initial screening step, a comparative single oral dose pharmacokinetic study was conducted in rats for CBX and its three aliphatic acyl water-soluble prodrugs viz."( Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats.
Bhamidipati, R; Datla, S; Katneni, K; Khan, AA; Kota, J; Mamidi, RN; Mullangi, R; Rajagopalan, R; Rao, CS; Rao, KY; Singh, SK; Srinivas, NR, 2002)		0.57
" Decreased concentrations of carboxy- and hydroxy-celecoxib in heterozygous and homozygous carriers of CYP2C9*3 were detected which supported the influence of CYP2C9 polymorphisms on celecoxib pharmacokinetic variability."( Influence of CYP2C9 genetic polymorphisms on pharmacokinetics of celecoxib and its metabolites.
Brockmöller, J; Kirchheiner, J; Meisel, C; Roots, I; Steinbach, N; Störmer, E, 2003)		0.81
" Pharmacokinetic parameters were determined based on non-compartmental model analysis using the computer program KINETICA."( Influence of rifampicin pretreatment on the pharmacokinetics of celecoxib in healthy male volunteers.
Chandrasekhar, K; Jayasagar, G; Krishna Kumar, M; Madhusudan Rao, Y, 2003)		0.56
"We studied the toxicities, potential pharmacokinetic interactions, and preliminary antitumor activity of the combination of docetaxel and irinotecan with celecoxib, a selective cyclooxygenase-2 inhibitor."( Phase I and pharmacokinetic study of docetaxel, irinotecan, and celecoxib in patients with advanced non-small cell lung cancer.
Argiris, A; Avram, MJ; Kut, V; Luong, L, 2006)		0.77
" The alteration of irinotecan pharmacokinetic parameters observed may not be clinically relevant."( Phase I and pharmacokinetic study of docetaxel, irinotecan, and celecoxib in patients with advanced non-small cell lung cancer.
Argiris, A; Avram, MJ; Kut, V; Luong, L, 2006)		0.57
"To elucidate clinical pharmacokinetic of celecoxib following an oral dose administration."( Clinical pharmacokinetic of celecoxib in healthy Thai volunteers.
Chompootaweep, S; Itthipanichpong, C; Kemsri, W; Lilitkarntrakul, P; Parikamsil, S; Thaworn, N; Wittayalertpanya, S, 2005)		0.89
"22 hrs by average with the mean peak concentration (Cmax) of 686."( Clinical pharmacokinetic of celecoxib in healthy Thai volunteers.
Chompootaweep, S; Itthipanichpong, C; Kemsri, W; Lilitkarntrakul, P; Parikamsil, S; Thaworn, N; Wittayalertpanya, S, 2005)		0.62
" Pharmacokinetic parameters were determined by use of noncompartmental analysis."( Plasma pharmacokinetics and synovial fluid concentrations after oral administration of single and multiple doses of celecoxib in greyhounds.
Corse, M; Halstead, J; Hunter, RP; Koch, DE; Pellerin, MA; Radlinsky, M, 2005)		0.54
" Although the exact mechanism for the decreases in AUC and Cmax is not known, results suggested that the plasma pharmacokinetics of celecoxib are different after administration of multiple doses in Greyhounds."( Plasma pharmacokinetics and synovial fluid concentrations after oral administration of single and multiple doses of celecoxib in greyhounds.
Corse, M; Halstead, J; Hunter, RP; Koch, DE; Pellerin, MA; Radlinsky, M, 2005)		0.74
"Four separate studies investigated the pharmacokinetic interaction between single oral doses of aliskiren and lovastatin, atenolol, celecoxib or cimetidine, respectively."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005)		0.75
" Aliskiren mean Cmax was not affected by either lovastatin or atenolol, although a non-significant 36% increase was observed with celecoxib."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005)		0.75
"Overall, single doses of aliskiren showed no evidence of clinically important pharmacokinetic interactions with lovastatin, atenolol, celecoxib or cimetidine."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005)		0.75
" We also demonstrate the applicability of this method for pharmacokinetic studies in humans."( Simple and rapid high-performance liquid chromatographic method for determination of celecoxib in plasma using UV detection: application in pharmacokinetic studies.
Foroutan, SM; Khoddam, A; Shafaati, A; Zarghi, A, 2006)		0.56
" This multiple-dose study investigated the potential for pharmacokinetic interactions between aliskiren and three drugs, each predominantly eliminated by a different clearance/metabolic pathway: allopurinol (glomerular filtration), celecoxib (cytochrome P450 metabolism) and cimetidine (P-glycoprotein and organic anion/cation transporters)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008)		0.74
"Three open-label, multiple-dose studies in healthy subjects investigated possible pharmacokinetic interactions between aliskiren 300 mg od and allopurinol 300 mg od (n = 20), celecoxib 200 mg bid (n = 22), or cimetidine 800 mg od (n = 22)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008)		0.75
"In this multiple-dose study, aliskiren showed no clinically relevant pharmacokinetic interactions when co-administered with allopurinol, celecoxib or cimetidine in healthy subjects."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008)		0.76
" There were no significant differences in any celecoxib pharmacokinetic parameters between 15 +EIASD and 12 -EIASD patients."( Effect of phenytoin on celecoxib pharmacokinetics in patients with glioblastoma.
Batchelor, T; Desideri, S; Grossman, SA; Hammour, T; Lesser, G; Olson, J; Peereboom, D; Supko, JG; Ye, X, 2008)		0.91
" Potential pharmacokinetic interactions and Topo-1 and DT-diaphorase (NQ01) gene expressions in peripheral-mononuclear cells were evaluated."( Phase I and pharmacokinetic study of mitomycin C and celecoxib as potential modulators of tumor resistance to irinotecan in patients with solid malignancies.
Drengler, R; Duan, W; Kolesar, JM; Kuhn, J; Otterson, G; Schaaf, LJ; Shapiro, C; Villalona-Calero, MA; Xu, Y, 2009)		0.6
" No relevant pharmacokinetic interactions occurred between irinotecan and MMC, and mean increases in Topo-1, were observed."( Phase I and pharmacokinetic study of mitomycin C and celecoxib as potential modulators of tumor resistance to irinotecan in patients with solid malignancies.
Drengler, R; Duan, W; Kolesar, JM; Kuhn, J; Otterson, G; Schaaf, LJ; Shapiro, C; Villalona-Calero, MA; Xu, Y, 2009)		0.6
" In this study, in vitro dissolution testing using biorelevant media coupled with in silico physiologically based pharmacokinetic (PBPK) modeling was applied to the prediction of food effects on the absorption of a poorly soluble drug, celecoxib, from 200mg capsules."( Prediction of food effects on the absorption of celecoxib based on biorelevant dissolution testing coupled with physiologically based pharmacokinetic modeling.
Dressman, JB; Janssen, N; Jantratid, E; Kesisoglou, F; Mao, Y; Reppas, C; Shono, Y; Vertzoni, M, 2009)		0.79
" VE-C gene expression and VEGF levels represent potentially useful pharmacodynamic markers for the clinical response."( Clinical and pharmacodynamic evaluation of metronomic cyclophosphamide, celecoxib, and dexamethasone in advanced hormone-refractory prostate cancer.
Allegrini, G; Antonuzzo, A; Bocci, G; Bursi, S; D'Arcangelo, M; Danesi, R; Del Tacca, M; Di Marsico, R; Falcone, A; Fioravanti, A; Fontana, A; Fontana, E; Galli, C; Galli, L; Landi, L; Orlandi, P, 2009)		0.59
" Pharmacokinetic parameters and their between animal variability were obtained using standard non-compartmental analysis as well as a compartmental analysis using nonlinear mixed effects modeling."( Pharmacokinetics of a combination of Δ9-tetrahydro-cannabinol and celecoxib in a porcine model of hemorrhagic shock.
Mehrotra, N; Meibohm, B; Moore, BM; Vaddady, PK; Yates, CR; Zhang, X, 2011)		0.61
" Potential predictive pharmacokinetic parameters and pharmacodynamic biomarkers have been found."( Clinical, pharmacokinetic and pharmacodynamic evaluations of metronomic UFT and cyclophosphamide plus celecoxib in patients with advanced refractory gastrointestinal cancers.
Allegrini, G; Arrighi, G; Barletta, MT; Bocci, G; Brandi, G; Canu, B; Chericoni, S; Ciarlo, A; Danesi, R; Di Desidero, T; Di Paolo, A; Falcone, A; Fioravanti, A; Fontana, A; Giusiani, M; Kerbel, RS; Loupakis, F; Lucchesi, S; Masi, G; Orlandi, P, 2012)		0.59
"The development of a novel class of pharmacodynamic hybrids that inhibits COX-2 isoform is reported."( Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
Alfonso, S; Anzini, M; Battilocchio, C; Biava, M; Calderone, V; Consalvi, S; Di Cesare Mannelli, L; Ghelardini, C; Giordani, A; Martelli, A; Patrignani, P; Poce, G; Porretta, GC; Rossi, A; Sautebin, L; Schenone, S; Testai, L, 2012)		0.38
" Polymorphisms in the CYP2C9 gene have been associated with decreased enzyme activity and alteration of celecoxib pharmacokinetic parameters."( Evaluation of the relationship between polymorphisms in CYP2C8 and CYP2C9 and the pharmacokinetics of celecoxib.
Abad-Santos, F; Cabaleiro, T; Ochoa, D; Prieto-Pérez, R; Román, M; Sánchez-Rojas, SD; Talegón, M, 2013)		0.82
" We conducted a phase I and pharmacokinetic study with the erlotinib and celecoxib combination in patients with advanced premalignant lesions."( Chemoprevention of head and neck cancer with celecoxib and erlotinib: results of a phase ib and pharmacokinetic study.
Beitler, JJ; Chen, AY; Chen, Z; Chen, ZG; Grandis, JR; Grist, W; Hurwitz, SJ; Khuri, FR; Kono, SA; Lewis, M; Moore, CE; Moreno-Williams, R; Müller, S; Nannapaneni, S; Owonikoko, TK; Ramalingam, S; Saba, NF; Shin, DM; Shin, HJ; Sica, G; Yang, CS; Zhao, Y, 2014)		0.89
" In this study, we investigated the pharmacokinetic drug interactions of rebamipide with two selected NSAIDs, celecoxib or diclofenac."( Pharmacokinetic interactions between rebamipide and selected nonsteroidal anti-inflammatory drugs in rats.
Cooper, DL; Harirforoosh, S; Wood, RC; Wyatt, JE, 2014)		0.61
"We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties."( Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
Alfonso, S; Anzini, M; Battilocchio, C; Biava, M; Calderone, V; Colovic, M; Consalvi, S; Di Capua, A; Di Cesare Mannelli, L; Dovizio, M; Ghelardini, C; Giordani, A; Martelli, A; Patrignani, P; Persiani, S; Poce, G; Rossi, A; Sautebin, L; Testai, L, 2014)		0.4
"We designed a series of specifically deuterated benzopyran analogues as new COX-2 inhibitors with the aim of improving their pharmacokinetic properties."( Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
Bai, Y; Liu, J; Liu, X; Lu, X; Lu, Y; Talley, JJ; Tortorella, MD; Tu, Z; Wang, Y; Wen, D; Zhang, Y, 2014)		0.4
" In conclusion, our results showed that our validated LC-MS/MS method can be successfully used for the pharmacokinetic studies of celecoxib and that the blood cells are a very important compartment for this drug such that profiles of celecoxib and its metabolites in whole blood will be more comprehensive and accurate representation of their profiles in vivo than the plasma."( Quantitation of celecoxib and four of its metabolites in rat blood by UPLC-MS/MS clarifies their blood distribution patterns and provides more accurate pharmacokinetics profiles.
Gao, S; Hu, M; Ma, Y, 2015)		0.97
" Compared with CYP2C9*1/*1 group, pharmacokinetic parameters of celecoxib such as AUC0-48 and Cmax was increased by 90."( Influence of genetic polymorphisms on the pharmacokinetics of celecoxib and its two main metabolites in healthy Chinese subjects.
Ding, L; Gong, C; Liu, R; Ma, P; Tao, L; Yang, W; Zheng, X, 2015)		0.9
"We compared the pharmacokinetic (PK) profiles of co-crystal of tramadol-celecoxib (CTC) vs."( Pharmacokinetics of multiple doses of co-crystal of tramadol-celecoxib: findings from a four-way randomized open-label phase I clinical trial.
Encina, G; Escriche, M; Gascón, N; Lahjou, M; Plata-Salamán, C; Sans, A; Sicard, E; Soler, L; Sust, M; Vaqué, A; Videla, S, 2018)		0.95
" Although commonly used in avian medicine, limited pharmacokinetic (PK) data in domestic and companion birds are available."( Comparative population pharmacokinetics and absolute oral bioavailability of COX-2 selective inhibitors celecoxib, mavacoxib and meloxicam in cockatiels (Nymphicus hollandicus).
Antonissen, G; Croubels, S; De Backer, P; De Baere, S; Devreese, M; Dhondt, L; Gehring, R; Goessens, T; Haesendonck, R, 2017)		0.67
" The prostate tissue penetration and related pharmacokinetic parameters were evaluated by non-compartmental analysis."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018)		0.48
" A two-factor analysis of variance (ANOVA) with replication indicated an overall statistically significant difference in the pharmacokinetic parameters for celecoxib, diclofenac, ibuprofen, and naproxen."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018)		0.68
" The pharmacokinetic data indicated that celecoxib has the highest penetration and retention in rat prostate tissues."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018)		0.75
" The blood samples for pharmacokinetic evaluation were collected for up to 48 hr after the administration of celecoxib in each study period."( Effects of Ojeok-san on the Pharmacokinetics of Celecoxib at Steady-state in Healthy Volunteers.
Kim, BH; Park, JY; Park, MJ; Park, SI; Yim, SV, 2018)		0.95
" Tramadol's pharmacokinetic exposure was comparable between cohorts after adjusting for body weight; the pharmacokinetic exposure of O-desmethyltramadol and celecoxib was increased in Japanese subjects."( Pharmacokinetics of Tramadol and Celecoxib in Japanese and Caucasian Subjects Following Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label Study.
Bennett, C; Dooner, H; Encabo, M; Encina, G; Escriche, M; Lorch, U; Mersmann, S; Mundin, G; Smith, K, 2019)		0.99
" Celecoxib half-life in blood increased from 5 h for the bolus injection of celecoxib to more than 10 days for the slowest releasing gel formulation."( In vivo pharmacokinetics of celecoxib loaded endcapped PCLA-PEG-PCLA thermogels in rats after subcutaneous administration.
Chan, A; de Leede, LGJ; Hennink, WE; Sandker, M; van Midwoud, PM; Weinans, H, 2018)		1.69
" The primary aim of this study was to determine the pharmacokinetic profile of celecoxib-a selective cyclooxygenase-2 (COX-2) inhibitor in horses."( Pharmacokinetics, metabolism and excretion of celecoxib, a selective cyclooxygenase-2 inhibitor, in horses.
Albert, PH; Kadry, AM; Singh, J; Subhahar, MB, 2019)		1
"This study investigated the time course and magnitude of the pharmacokinetic interaction between capecitabine and the cytochrome P450 (CYP) 2C9 substrate celecoxib, with implications for coadministration of fluoropyrimidines with CYP2C9 substrates such as warfarin."( Prolonged Pharmacokinetic Interaction Between Capecitabine and a CYP2C9 Substrate, Celecoxib.
House, LK; Janisch, LA; Karrison, TG; Ramírez, J; Ratain, MJ; Salgia, R; Sharma, MR; Turcich, M, 2019)		0.94
" Corresponding pharmacokinetic studies were performed in which twelve healthy male subjects from two bioequivalence studies received either one immediate release (IR) dose of the test (test 1 or test 2) or the reference formulation (Celebrex®, 200 mg)."( Development of a Two-Compartment System In vitro Dissolution Test and Correlation with In vivo Pharmacokinetic Studies for Celecoxib.
Cheng, Z; Jiang, S; Liu, W; Wang, L; Zeng, Y; Zhang, G, 2020)		0.77
" The aim of this study was to develop a physiologically based pharmacokinetic (PBPK) model of celecoxib according to CYP2C9 genetic polymorphism for personalized pharmacotherapy."( Physiologically based pharmacokinetic (PBPK) modeling for prediction of celecoxib pharmacokinetics according to CYP2C9 genetic polymorphism.
Bae, JW; Cho, CK; Jang, CG; Jung, EH; Kang, P; Kim, YH; Lee, SY; Lee, YJ; Park, HJ, 2021)		1.07
" The aim of this study was to evaluate the pharmacokinetic interaction between tegoprazan and commonly used NSAIDS, namely, naproxen, aceclofenac, and celecoxib."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022)		1.15
" Pharmacokinetic blood samples were collected up to 24 hours after the last dose."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022)		0.95
"Seventeen subjects from cohort 1, sixteen subjects from cohort 2, and thirteen subjects from cohort 3 were included in the pharmacokinetic analysis."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022)		0.95
"Changes in the maximum aceclofenac or celecoxib concentrations were detected after concurrent administration with tegoprazan, which were considered mainly due to the pharmacodynamic effect of tegoprazan."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022)		1.22
" post-surgery celecoxib/etoricoxib/etodolac pharmacokinetic (PK) profiles."( Selective COX-2 inhibitors after bariatric surgery: Celecoxib, etoricoxib and etodolac post-bariatric solubility/dissolution and pharmacokinetics.
Cvijić, S; Dahan, A; Dukhno, O; Partook-Maccabi, M; Porat, D; Vainer, E, 2023)		1.52

Compound-Compound Interactions

Cetuximab in combination with celecoxib also induced G1 phase arrest and downregulated the expression of KDR and AQP1 in A549 cells. Combined atorvastatin with Celecoxib and tipifarnib synergistically decreased the sphere forming ability of Panc-1 cells.

ExcerptReferenceRelevance
" Experiments were designed to assess the potential chemopreventive properties of highly selective iNOS inhibitors, administered individually and in combination with a selective COX-2 inhibitor, on the development of AOM-induced colonic aberrant crypt foci (ACF)."( Chemopreventive properties of a selective inducible nitric oxide synthase inhibitor in colon carcinogenesis, administered alone or in combination with celecoxib, a selective cyclooxygenase-2 inhibitor.
Connor, JR; Indranie, C; Manning, PT; Rao, CV; Reddy, BS; Simi, B, 2002)		0.51
" This study investigates the effect of pretreatment with celecoxib alone, or in combination with phenytoin, on electroshock-induced convulsions."( Anticonvulsant action of celecoxib (alone and in combination with sub-threshold dose of phenytoin) in electroshock induced convulsion.
Malhotra, S; Pandhi, P; Shafiq, N, 2003)		0.87
" This study was to investigate inhibitory effects of COX-2 inhibitor celecoxib alone, and celecoxib combined with octreotide on growth of multidrug resistant human gastric cancer cell line SGC7901/ADR."( [Inhibitory effects of celecoxib combined with octreotide on growth of multidrug resistant human gastric cancer cell line SGC7901/ADR].
Qiang, O; Tang, CW; Wang, CH; Zheng, WB, 2004)		0.87
"Experimental groups:(1)celecoxib (1 x 10(-4)-1 x 10(-8) mol/L); (2)octreotide (1 x 10(-5)-1 x 10(-9) mol/L); (3)celecoxib (1 x 10(-4)-1 x 10(-8) mol/L) combined with octreotide (1 x 10-6 mol/L);(4)control group (RPMI-1640 medium without serum)."( [Inhibitory effects of celecoxib combined with octreotide on growth of multidrug resistant human gastric cancer cell line SGC7901/ADR].
Qiang, O; Tang, CW; Wang, CH; Zheng, WB, 2004)		0.94
" When combined with octreotide, celecoxib presented lower (3)H-thymidine incorporation [(220."( [Inhibitory effects of celecoxib combined with octreotide on growth of multidrug resistant human gastric cancer cell line SGC7901/ADR].
Qiang, O; Tang, CW; Wang, CH; Zheng, WB, 2004)		0.92
"Celecoxib combined with octreotide may enhance inhibition of growth of multidrug resistant human gastric cancer cells."( [Inhibitory effects of celecoxib combined with octreotide on growth of multidrug resistant human gastric cancer cell line SGC7901/ADR].
Qiang, O; Tang, CW; Wang, CH; Zheng, WB, 2004)		2.08
"Patients with solid tumors received one of three escalating dose levels of daily celecoxib in combination with docetaxel and irinotecan administered on days 1 and 8 of an every 21-day cycle."( A phase I trial of celecoxib in combination with docetaxel and irinotecan in patients with advanced cancer.
Adjei, AA; Croghan, GC; Dy, GK; Furth, A; Hanson, LJ; Mandrekar, S; Okuno, SH; Peethambaram, PP, 2005)		0.88
" However, the tumors administered with a initial dose of CX at 24-h post-PDT had no tumor control."( Anti-angiogenic effects of Hypericin-photodynamic therapy in combination with Celebrex in the treatment of human nasopharyngeal carcinoma.
Olivo, M; Soo, KC; Yee, KK, 2005)		0.33
" There is increasing interest in using COX-2 inhibitors in combination with other chemopreventive agents to overcome the issue of toxicity."( Docosahexaenoic acid in combination with celecoxib modulates HSP70 and p53 proteins in prostate cancer cells.
Bosland, M; Condon, MS; Narayanan, BA; Narayanan, NK; Nargi, D, 2006)		0.6
"The present study evaluated the safety of treatment of colorectal liver metastases with radio frequency ablation (RFA) in combination with high doses of the selective cyclooxygenase-2 inhibitor celecoxib."( Cutaneous and intra-abdominal abscess formation in rats following radio frequency [corrected] ablation of liver tumors in combination with celecoxib treatment.
De Heer, P; Ensink, GN; Koudijs, MM; Kuppen, PJ; Putter, H; Sandel, MH; Speetjens, FM; Van de Velde, CJ, )		0.52
" Primary end points included evaluation of toxicity and determination of the OBD of celecoxib when combined with erlotinib."( A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer.
Dubinett, SM; Elashoff, RM; Figlin, RA; Krysan, K; Milne, GL; Morrow, JD; Newman, RA; Reckamp, KL; Tucker, C, 2006)		0.8
"This study defines the OBD of celecoxib when combined with a fixed dose of EGFR TKI."( A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer.
Dubinett, SM; Elashoff, RM; Figlin, RA; Krysan, K; Milne, GL; Morrow, JD; Newman, RA; Reckamp, KL; Tucker, C, 2006)		0.86
" Randomized studies are needed to explore the role of celecoxib in combination with chemotherapy or as maintenance treatment in these patients."( Temozolomide in combination with celecoxib in patients with advanced melanoma. A phase II study of the Hellenic Cooperative Oncology Group.
Fountzilas, G; Frangia, K; Gogas, H; Mantzourani, M; Markopoulos, C; Middleton, M; Panagiotou, P; Papadopoulos, O; Pectasides, D; Polyzos, A; Stavrinidis, I; Tsoutsos, D; Vaiopoulos, G, 2006)		0.86
" This study was to evaluate the chemopreventive effect of tamoxifen combined with celecoxib, a COX-2 selective inhibitor, on 7,12-dimethylbenz anthracene (DMBA)-induced breast cancer in rats."( [Chemopreventive effect of tamoxifen combined with celecoxib on DMBA-induced breast cancer in rats].
Dai, ZJ; Kang, HF; Liu, XX; Wang, XJ; Xue, FJ; Xue, XH, 2006)		0.81
"To investigated if cyclooxygenase-2 (COX-2) inhibitor celecoxib in combination with somatostatin (SST) analog octreotide is able to inhibit the metastasis of human gastric cancer (GC) in vivo."( [The inhibitive effects of celecoxib combined with octreotide on the metastasis of human gastric cancer in vivo].
Chen, ZX; Huang, MH; Huang, MT; Tang, CW; Wang, CH; Wei, B; Zhang, B, 2006)		0.88
" Aspirin in combination with a coxib retarded the healing of experimentally induced gastric ulcers, whereas healing rates of rats treated with celecoxib in combination with aspirin/PC were comparable to controls."( Surface phospholipids in gastric injury and protection when a selective cyclooxygenase-2 inhibitor (Coxib) is used in combination with aspirin.
Dial, EJ; Lichtenberger, LM; Romero, JJ, 2007)		0.54
"Aspirin's gastric toxicity in combination with a coxib can be dissociated from its ability to inhibit COX-1 and appears to be dependent, in part, on its ability to attenuate the stomach's surface hydrophobic barrier."( Surface phospholipids in gastric injury and protection when a selective cyclooxygenase-2 inhibitor (Coxib) is used in combination with aspirin.
Dial, EJ; Lichtenberger, LM; Romero, JJ, 2007)		0.34
"To study the effects of two specific cyclooxygenase inhibitors (SCI), rofecoxib and celecoxib, combined with chemotherapeutic drugs 5-Fu, DDP and VP-16 on gastric cancer cell line BGC-823, and to evaluate whether specific cyclooxygenase inhibitors can be used as a synergetic agent in chemotherapy."( [Antitumor effects of specific cyclooxygenase inhibitors combined with chemotherapeutic agents on gastric cancer cells in vitro].
Chen, XM; Feng, JX; Wang, YJ; Zhang, X; Zhu, FS, 2007)		0.56
"Both rofecoxib and celecoxib have an ability to suppress gastric cancer cells in vitro, and the synergetic role becomes evident when rofecoxib and celecoxib are combined with chemotherapeutic agents at different concentrations, which indicate that the two specific cyclooxygenase inhibitors may be used as a chemotherapeutic sensitizer."( [Antitumor effects of specific cyclooxygenase inhibitors combined with chemotherapeutic agents on gastric cancer cells in vitro].
Chen, XM; Feng, JX; Wang, YJ; Zhang, X; Zhu, FS, 2007)		0.67
"The rats that received celecoxib in combination with exisulind at low doses showed a significant decrease in prostatic intraepithelial neoplasia and adenocarcinomas as well as an enhanced rate of apoptosis."( Exisulind in combination with celecoxib modulates epidermal growth factor receptor, cyclooxygenase-2, and cyclin D1 against prostate carcinogenesis: in vivo evidence.
Bosland, MC; Horton, L; Narayanan, BA; Narayanan, NK; Nargi, D; Randolph, C; Reddy, BS, 2007)		0.94
" The objective of this study was to determine the maximum tolerated dose and dose-limiting toxicities of bortezomib in combination with celecoxib in patients with advanced solid tumors."( Bortezomib in combination with celecoxib in patients with advanced solid tumors: a phase I trial.
Chaudhary, U; Dunder, S; Green, M; Hayslip, J; Kraft, A; Meyer, M; Montero, AJ; Salzer, S; Sherman, C, 2007)		0.83
"Patients received escalating doses of bortezomib either on a weekly schedule (days 1, 8, 15, 22, and 29 repeated every 42 days) or on a twice-weekly administration schedule (days 1, 4, 8, and 11 repeated every 21 days), in combination with escalating doses of celecoxib twice daily throughout the study period from 200 mg to 400 mg twice daily."( Bortezomib in combination with celecoxib in patients with advanced solid tumors: a phase I trial.
Chaudhary, U; Dunder, S; Green, M; Hayslip, J; Kraft, A; Meyer, M; Montero, AJ; Salzer, S; Sherman, C, 2007)		0.81
" We carried out the in vitro study using selective COX-2 inhibitor celecoxib combined with EGFR-tyrosine kinase inhibitor (EGFR-TKI) ZD1839 on NSCLC cell lines to investigate the anti proliferation effect and the cell molecular mechanism."( Selective COX-2 inhibitor celecoxib combined with EGFR-TKI ZD1839 on non-small cell lung cancer cell lines: in vitro toxicity and mechanism study.
Chen, L; He, Y; Huang, H; Liao, H; Wei, W, 2008)		0.88
" We propose that this novel drug combination should receive further evaluation as a potentially effective anticancer therapy."( Aggravated endoplasmic reticulum stress as a basis for enhanced glioblastoma cell killing by bortezomib in combination with celecoxib or its non-coxib analogue, 2,5-dimethyl-celecoxib.
Chen, TC; Golden, EB; Hofman, FM; Kardosh, A; Louie, SG; Petasis, NA; Pyrko, P; Schönthal, AH; Uddin, J, 2008)		0.55
" There was significant difference between rats with EA combined with 5 mg/(kg."( [Analgesic effects of electroacupuncture combined with Celebrex on rats with tibial cancer pain].
Liu, Q; Mao-Ying, QL; Mi, WL; Ren, DH; Wang, YQ, 2008)		0.35
" The objective of this study was to evaluate the effect of various SPI, both alone and in combination with cisplatin, on three different non-small cell lung cancer (NSCLC) cell lines."( Efficacy of signal pathway inhibitors alone and in combination with Cisplatin varies between human non-small cell lung cancer lines.
El-Hefnawy, T; Kilic, A; Landreneau, RJ; Luketich, JD; Schuchert, MJ, 2009)		0.35
" Louis, MO), Cox-2 (NS-398 [Sigma-Aldrich] or Celecoxib [Pfizer]), MAPK (U0126 [Sigma-Aldrich]), and EGFR (Iressa; AstraZeneca, Macclesfield, United Kingdom) both alone and in combination with 10 or 30 mum cisplatin (Sigma-Aldrich) (18 possible regimens for each cell line)."( Efficacy of signal pathway inhibitors alone and in combination with Cisplatin varies between human non-small cell lung cancer lines.
El-Hefnawy, T; Kilic, A; Landreneau, RJ; Luketich, JD; Schuchert, MJ, 2009)		0.61
"There is a substantial degree of variability between NSCLC cell lines in response to SPI, both alone and in combination with cisplatin."( Efficacy of signal pathway inhibitors alone and in combination with Cisplatin varies between human non-small cell lung cancer lines.
El-Hefnawy, T; Kilic, A; Landreneau, RJ; Luketich, JD; Schuchert, MJ, 2009)		0.35
"In a single-institution phase II study, we sought to determine the effectiveness of concurrent chemoradiation given with celecoxib and examined biomarkers to predict response to COX-2 inhibition."( A phase II study of celecoxib in combination with paclitaxel, carboplatin, and radiotherapy for patients with inoperable stage IIIA/B non-small cell lung cancer.
Carbone, DP; Choy, H; Csiki, I; Johnson, DH; Lu, B; Moretti, L; Morrow, JD; Mutter, R; Sandler, AB; Shyr, Y; Ye, F, 2009)		0.88
"To evaluate the effects of celecoxib, in combination with oxaliplatin, on tumour growth, cell apoptosis and angiogenesis in nude mice models."( Synergistic inhibition effect of tumor growth by using celecoxib in combination with oxaliplatin.
Bian, H; Cai, J; Gui, L; Zhao, F; Zhao, S, 2009)		0.9
" Celecoxib in combination with oxaliplatin could further promote cell apoptosis and reduce beta-catenin protein expression."( Synergistic inhibition effect of tumor growth by using celecoxib in combination with oxaliplatin.
Bian, H; Cai, J; Gui, L; Zhao, F; Zhao, S, 2009)		1.51
" The present study explores the effects of p53-modulating agent CP-31398 alone and combined with celecoxib on azoxymethane-induced aberrant crypt foci (ACF) and colon adenocarcinomas in F344 rats."( Inhibition of azoxymethane-induced colorectal cancer by CP-31398, a TP53 modulator, alone or in combination with low doses of celecoxib in male F344 rats.
Guruswamy, S; Kopelovich, L; Patlolla, JM; Rao, CV; Steele, VE; Swamy, MV, 2009)		0.78
" Herein, we investigated the therapeutic efficacy of metronomic Cy combined with celecoxib (Cel) in two murine mammary adenocarcinoma models."( Antitumoral and antimetastatic effects of metronomic chemotherapy with cyclophosphamide combined with celecoxib on murine mammary adenocarcinomas.
Bonfil, RD; Mainetti, LE; Rossa, A; Rozados, VR; Scharovsky, OG, 2011)		0.81
" MCT with Cy combined with Cel was more effective than each monotherapy."( Antitumoral and antimetastatic effects of metronomic chemotherapy with cyclophosphamide combined with celecoxib on murine mammary adenocarcinomas.
Bonfil, RD; Mainetti, LE; Rossa, A; Rozados, VR; Scharovsky, OG, 2011)		0.58
" Celecoxib, a cyclooxygenase (COX) 2 inhibitor, has not been reported to interact with methotrexate, but the mechanisms are unclear why the interaction did not occur."( Drug interaction between celecoxib and methotrexate in organic anion transporter 3-transfected renal cells and in rats in vivo.
Endou, H; Fujimura, A; Kanai, Y; Maeda, A; Miyamoto, E; Saito, K; Tsuruoka, S; Ushijima, K, 2010)		1.57
" We investigated the potential benefits of oral celecoxib on postoperative analgesia combined with thoracic epidural analgesia (TEA)."( Effect of celecoxib combined with thoracic epidural analgesia on pain after thoracotomy.
Deflandre, EP; Hubert, BM; Joris, JL; Ledoux, D; Libbrecht, D; Radermecker, M; Roediger, L; Senard, M, 2010)		1.02
" This factorial design phase I/II protocol tested dose-dense temozolomide alone and combined with cytostatic agents."( A phase I factorial design study of dose-dense temozolomide alone and in combination with thalidomide, isotretinoin, and/or celecoxib as postchemoradiation adjuvant therapy for newly diagnosed glioblastoma.
Chang, E; Colman, H; Conrad, C; de Groot, J; Giglio, P; Gilbert, MR; Gonzalez, J; Groves, MD; Hess, K; Hunter, K; Levin, V; Mahajan, A; Puduvalli, V; Woo, S; Yung, WK, 2010)		0.57
"To investigate whether EGFR inhibitor AG1478 combined with celecoxib could enhance the inhibitive effects on the growth of gastric cancer cells."( [Effects of EGFR inhibitor AG1478 in combination with celecoxib on the growth of gastric cancer cells].
Li, RK; Liao, J; Qiang, O; Wang, CH, 2010)		0.85
"AG1478 combined with celecoxib results in enhanced inhibitive effect on the growth of SGC-7901, which may partly due to the suppression of ERK phospholation."( [Effects of EGFR inhibitor AG1478 in combination with celecoxib on the growth of gastric cancer cells].
Li, RK; Liao, J; Qiang, O; Wang, CH, 2010)		0.93
"To investigate the efficacy and toxicity of a short intensive Uracil/Tegafur (UFT) based chemoradiotherapy scheme combined with celecoxib in locally advanced pancreatic cancer."( Phase II trial of Uracil/Tegafur plus leucovorin and celecoxib combined with radiotherapy in locally advanced pancreatic cancer.
Busch, OR; Morak, MJ; Nuyttens, JJ; Padmos, EE; Richel, DJ; Schaake, EE; van der Gaast, A; van Eijck, CH; van Tienhoven, G; Vervenne, WL, 2011)		0.82
"5 Gy radiotherapy combined with UFT 300 mg/m(2) per day, leucovorin (folinic acid) 30 mg and celecoxib 80 0mg for 28 days concomitant with radiotherapy."( Phase II trial of Uracil/Tegafur plus leucovorin and celecoxib combined with radiotherapy in locally advanced pancreatic cancer.
Busch, OR; Morak, MJ; Nuyttens, JJ; Padmos, EE; Richel, DJ; Schaake, EE; van der Gaast, A; van Eijck, CH; van Tienhoven, G; Vervenne, WL, 2011)		0.84
"Based on the lack of response, the substantial toxicity of mainly gastro-intestinal origin and the reported mediocre overall and progression free survival, we cannot advise our short intensive chemoradiotherapy schedule combined with celecoxib as the standard treatment."( Phase II trial of Uracil/Tegafur plus leucovorin and celecoxib combined with radiotherapy in locally advanced pancreatic cancer.
Busch, OR; Morak, MJ; Nuyttens, JJ; Padmos, EE; Richel, DJ; Schaake, EE; van der Gaast, A; van Eijck, CH; van Tienhoven, G; Vervenne, WL, 2011)		0.8
"The present study provided evidence that treatment with celecoxib in combination with fluvastatin resulted in the inhibition of HCC tumour growth in an in vivo mouse model."( [Effects of celecoxib combined with fluvastatin on tumor growth and cell apoptosis in a xenograft model of hepatocellular carcinoma].
Gao, J; Ge, YS; Jia, WD; Li, JS; Ma, JL; Xu, GL; Yu, JH, 2010)		0.99
"A new non-cytotoxic therapy that SOM230 (pasireotide)，a somatostatin analogue (SSTA) combined with celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor was tested in nude mice bearing HepG2 xenografts."( SOM230 combined with celecoxib prolongs the survival in nude mice with HepG-2 xenografts.
Chen, S; Tang, CW; Wang, CH; Xie, Y, 2011)		0.9
" Phase II recommended dose of celecoxib combined with accelerated radiotherapy in advanced H&N cancer was 600mg bid."( Plasma levels of vascular endothelial growth factor during and after radiotherapy in combination with celecoxib in patients with advanced head and neck cancer.
Cvek, J; Dusek, L; Feltl, D; Halamka, M; Horacek, J; Kominek, P; Kubes, J; Zavadova, E, 2011)		0.87
"To investigate the effects of celecoxib combined with radiotherapy on apoptosis of CNE-2Z cell lines and the potential mechanisms."( [Effects of celecoxib combined with radiotherapy on apoptosis of CNE-2Z cell lines].
Gui, P; Peng, P; Wei, LZ; Xiang, YZ; Xiong, ZJ; Yu, L, 2011)		1.04
" Celecoxib combined with radiotherapy up-regulation the expression of Bax."( [Effects of celecoxib combined with radiotherapy on apoptosis of CNE-2Z cell lines].
Gui, P; Peng, P; Wei, LZ; Xiang, YZ; Xiong, ZJ; Yu, L, 2011)		1.66
"Celecoxib combined with radiotherapy could induce apoptosis and enhance the radiosensitivity of human nasopharyngeal carcinoma CNE-2Z cell lines."( [Effects of celecoxib combined with radiotherapy on apoptosis of CNE-2Z cell lines].
Gui, P; Peng, P; Wei, LZ; Xiang, YZ; Xiong, ZJ; Yu, L, 2011)		2.19
" Possible further antitumor efficacy of lower-dose and longer-term CPT-11 combined with simultaneous low-dose celecoxib was investigated for chemosensitive TNB9 and multi-drug resistant TS-N-2nu neuroblastoma xenografts."( Enhanced antitumor effect of lower-dose and longer-term CPT-11 treatment in combination with low-dose celecoxib against neuroblastoma xenografts.
Fukushima, T; Kaneko, M; Kaneko, S, 2013)		0.82
"Our findings demonstrate that lower-dose and longer-term CPT-11 treatment in combination with simultaneous low-dose celecoxib enhances antitumor activity and can successfully eradicate most of the neuroblastoma xenografts."( Enhanced antitumor effect of lower-dose and longer-term CPT-11 treatment in combination with low-dose celecoxib against neuroblastoma xenografts.
Fukushima, T; Kaneko, M; Kaneko, S, 2013)		0.81
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012)		0.38
"The present study was designed to investigate the effects of cyclooxygenase (COX) inhibitors in combination with taxol on the expression of cyclin D1 and Ki-67 in human ovarian SKOV-3 carcinoma cells xenograft-bearing mice."( Effects of cyclooxygenase inhibitors in combination with taxol on expression of cyclin D1 and Ki-67 in a xenograft model of ovarian carcinoma.
Cai, JH; Li, W; Tang, YX; Wan, L; Zhang, J, 2012)		0.38
"The present study was designed to investigate whether taxol in combination with cyclooxygenase (COX) inhibitors could be superior on inhibitory effect of ovarian cancer growth than taxol alone as drug therapy of mice implanted with human ovarian carcinoma cell line SKOV-3."( Antitumor properties of taxol in combination with cyclooxygenase-1 and cyclooxygenase-2 selective inhibitors on ovarian tumor growth in vivo.
Cai, J; Li, W; Liu, M; Tang, Y; Zhai, L; Zhang, J, 2012)		0.38
"The purpose of this study was to investigate the anti-tumor effect and explore the mechanisms of celecoxib (a selective cyclooxygenase-2 inhibitor) combined with 5-fluorouracil (5-FU) on the treatment of human colorectal cancer in a BALB/C nude mouse subcutaneous xenograft model."( Increase of cyclooxygenase-2 inhibition with celecoxib combined with 5-FU enhances tumor cell apoptosis and antitumor efficacy in a subcutaneous implantation tumor model of human colon cancer.
Chen, WC; Guo, Q; Zhang, DQ; Zhu, JH, 2013)		0.87
"Effects of celecoxib combined with 5-FU on the proliferation of xenograft carcinoma induced by HT-29 were investigated."( Increase of cyclooxygenase-2 inhibition with celecoxib combined with 5-FU enhances tumor cell apoptosis and antitumor efficacy in a subcutaneous implantation tumor model of human colon cancer.
Chen, WC; Guo, Q; Zhang, DQ; Zhu, JH, 2013)		1.04
" More apoptotic cells existed after treatment with celecoxib combined with 5-FU."( Increase of cyclooxygenase-2 inhibition with celecoxib combined with 5-FU enhances tumor cell apoptosis and antitumor efficacy in a subcutaneous implantation tumor model of human colon cancer.
Chen, WC; Guo, Q; Zhang, DQ; Zhu, JH, 2013)		0.9
"Celecoxib combined with 5-FU could inhibit the growth of tumors in vivo by inducing apoptosis and activation of the cytochrome C dependency apoptosis signal pathway."( Increase of cyclooxygenase-2 inhibition with celecoxib combined with 5-FU enhances tumor cell apoptosis and antitumor efficacy in a subcutaneous implantation tumor model of human colon cancer.
Chen, WC; Guo, Q; Zhang, DQ; Zhu, JH, 2013)		2.09
"Evaluation of in-vivo anticancer activity of aerosolized Celecoxib encapsulated Nanolipidcarriers (Cxb-NLC) as a single therapeutic agent and combined with intravenously administered Docetaxel (Doc) against non-small cell lung cancer."( Efficacy of aerosolized celecoxib encapsulated nanostructured lipid carrier in non-small cell lung cancer in combination with docetaxel.
Chougule, MB; I, T; Patel, AR; Patlolla, R; Singh, M; Wang, G, 2013)		0.94
"To investigate the anti-tumor effect of celecoxib combined with tegafur gimeracil oteracil potassium on subcutaneous xenograft tumor of gastric cancer in nude mice and analyze the possible mechanism."( [Inhibitive effect of celecoxib combined with tegafur gimeracil oteracil potassium on the growth of xenograft tumor of gastric cancer in nude mice].
Chen, X; Luo, Z; Meng, C, 2013)		0.97
"To evaluate the inhibitory effect and its mechanism of celecoxib combined with capecitabine on the growth of implanted H22 hepatoma in mice."( [Inhibitory effects of celecoxib combined with capecitabine on H22 hepatoma mice and its mechanism].
Guo, HQ; Liu, YY; Yang, SJ; Yao, SN; Yao, ZH; Yuan, YD; Zhao, Y, 2013)		0.95
" This study aims to explore the effect of cetuximab combined with celecoxib on apoptosis and KDR and AQP1 expression in lung cancer A549 cells."( [Effects of cetuximab combined with celecoxib on apoptosis and KDR and AQP1 expression in lung cancer].
Bai, H; Wang, C; Xia, H; Ye, J, 2013)		0.9
" Cetuximab in combination with celecoxib also induced G1 phase arrest and downregulated the expression of KDR and AQP1 in A549 cells (P<0."( [Effects of cetuximab combined with celecoxib on apoptosis and KDR and AQP1 expression in lung cancer].
Bai, H; Wang, C; Xia, H; Ye, J, 2013)		0.95
"Cetuximab in combination with celecoxib can synergistically inhibit the growth of A549 cells and downregulate the expression of KDR and AQP1 in A549 cells."( [Effects of cetuximab combined with celecoxib on apoptosis and KDR and AQP1 expression in lung cancer].
Bai, H; Wang, C; Xia, H; Ye, J, 2013)		0.95
" Therefore, we examined the effect of rapamycin combined with celecoxib on K562 cells in vitro."( Rapamycin combined with celecoxib enhanced antitumor effects of mono treatment on chronic myelogenous leukemia cells through downregulating mTOR pathway.
Hao, H; Li, J; Li, R; Luo, J; Xue, L, 2014)		0.95
"We recently demonstrated that both murine and human carcinomas grow significantly slower in mice on low carbohydrate (CHO), high protein diets than on isocaloric Western diets and that a further reduction in tumor growth rates occur when the low CHO diets are combined with the cyclooxygenase-2 inhibitor, celecoxib."( A low carbohydrate, high protein diet combined with celecoxib markedly reduces metastasis.
Adomat, HH; Bennewith, KL; Dang, NH; Guns, ES; Hamilton, MJ; Ho, VW; Hsu, BE; Krystal, G; Samudio, I; Weljie, A, 2014)		0.83
" In some tumor models, the combination of celecoxib with chemotherapy agents has shown synergistic antitumor effect; however, the effect of celecoxib combination with tegafur/gimeracil/oteracil potassium on the malignant biological behaviors of gastric cancer in nude mice is unclear."( Effect of celecoxib combined with chemotherapy drug on malignant biological behaviors of gastric cancer.
Dai, K; Fang, M; Lu, Z; Luo, J; Luo, Z; Meng, C; Zhang, S; Zhou, X, 2014)		1.07
" In the present study, we aimed to evaluate the treatment effect of celecoxib (CLX) combined with diacerein (DC) on OA and delineate the underlying molecular mechanism."( Celecoxib Combined with Diacerein Effectively Alleviates Osteoarthritis in Rats via Regulating JNK and p38MAPK Signaling Pathways.
Li, G; Li, Y; Li, Z; Meng, D; Tian, K; Xu, J, 2015)		2.1
" We investigated if arsenic sulfide (As4S4) in combination with other distinct agents could enhance its cytotoxic activity."( Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.
Chen, S; Pan, M; Tong, Y; Zhang, L; Zhang, X, 2015)		0.66
"We used gastric and colon cancer cell lines to study the synergistic effect of As4S4 in combination with BRD4 inhibitor JQ1, or with chemotherapy drug cisplatin and irinotecan or with COX2 inhibitor celecoxib."( Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.
Chen, S; Pan, M; Tong, Y; Zhang, L; Zhang, X, 2015)		0.85
"We found that when As4S4 was combined with JQ1, cisplatin, irinotecan or celecoxib, its cytotoxic activity was dramatically enhanced in both gastric and colon cancer cell lines."( Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.
Chen, S; Pan, M; Tong, Y; Zhang, L; Zhang, X, 2015)		0.89
"As4S4 in combination with JQ1, cisplatin, irinotecan or celecoxib showed enhanced cytotoxic effect on gastric and colon cancer cells, indicating the potential application of these novel drug combinations as part of treatment strategy that warrants further investigation."( Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.
Chen, S; Pan, M; Tong, Y; Zhang, L; Zhang, X, 2015)		0.91
" The objective of this study is to investigate the effect of FLP alone or in combination with celecoxib in the prevention of lung cancer progression by Cyclooxygenase (Cox)-2 mediated tumor inflammatory microenvironment in vivo."( Anti-tumor enhancement of Fei-Liu-Ping ointment in combination with celecoxib via cyclooxygenase-2-mediated lung metastatic inflammatory microenvironment in Lewis lung carcinoma xenograft mouse model.
Bao, Y; Gao, Y; Guo, Q; He, S; Hirasaki, Y; Hou, W; Hua, B; Li, C; Li, W; Liu, R; Pei, Y; Qi, X; Zhang, Y; Zheng, H, 2015)		0.87
" Treatment of FLP in combination with celecoxib was more effective than FLP or celecoxib alone in inhibiting vascular endothelial growth factor, platelet-derived growth factor receptors β, microsomal Prostaglandin E synthase-1, MMP-2, MMP-9, N-cadherin, and Vimentin expression, but increased E-cadherin expression."( Anti-tumor enhancement of Fei-Liu-Ping ointment in combination with celecoxib via cyclooxygenase-2-mediated lung metastatic inflammatory microenvironment in Lewis lung carcinoma xenograft mouse model.
Bao, Y; Gao, Y; Guo, Q; He, S; Hirasaki, Y; Hou, W; Hua, B; Li, C; Li, W; Liu, R; Pei, Y; Qi, X; Zhang, Y; Zheng, H, 2015)		0.92
" FLP in combination with celecoxib enhanced the antitumor growth and anti-metastasis effects."( Anti-tumor enhancement of Fei-Liu-Ping ointment in combination with celecoxib via cyclooxygenase-2-mediated lung metastatic inflammatory microenvironment in Lewis lung carcinoma xenograft mouse model.
Bao, Y; Gao, Y; Guo, Q; He, S; Hirasaki, Y; Hou, W; Hua, B; Li, C; Li, W; Liu, R; Pei, Y; Qi, X; Zhang, Y; Zheng, H, 2015)		0.96
"The multiple drug interactions in which CAIs are involved should be carefully considered when such drugs are used in combination with the drug classes mentioned above, as the risks of developing toxicity and serious side effects if the dosages are not adjusted are high."( Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors.
Supuran, CT, 2016)		0.43
" In this study, we investigated the effectiveness of CX and its combination with anticancer agent IM on human colorectal cancer HT-29 cell and their probable molecular targets."( The effect of celecoxib and its combination with imatinib on human HT-29 colorectal cancer cells: Involvement of COX-2, Caspase-3, VEGF and NF-κB genes expression.
Atari-Hajipirloo, S; Heydari, A; Kheradmand, F; Nikanfar, S; Noori, F, 2016)		0.79
" This study aimed to evaluate the efficacy and safety of Zhuanggu joint capsules combined with celecoxib and the benefit of treatment with Zhuanggu alone for KOA."( Efficacy and Safety of Zhuanggu Joint Capsules in Combination with Celecoxib in Knee Osteoarthritis: A Multi-center, Randomized, Double-blind, Double-dummy, and Parallel Controlled Trial.
Cai, XY; Fan, WM; Liu, JG; Ma, JZ; Weng, XS; Yang, J; Yang, L; Yun, XQ; Zhang, XL, 2016)		0.89
" The groups were treated, respectively, with Zhuanggu joint capsules combined with celecoxib capsule simulants, Zhuanggu joint capsules combined with celecoxib capsules, and celecoxib capsules combined with Zhuanggu joint capsule simulants for 4 weeks consecutively."( Efficacy and Safety of Zhuanggu Joint Capsules in Combination with Celecoxib in Knee Osteoarthritis: A Multi-center, Randomized, Double-blind, Double-dummy, and Parallel Controlled Trial.
Cai, XY; Fan, WM; Liu, JG; Ma, JZ; Weng, XS; Yang, J; Yang, L; Yun, XQ; Zhang, XL, 2016)		0.9
"Zhuanggu joint capsules alone or combined with celecoxib showed clinical efficacy in the treatment of KOA."( Efficacy and Safety of Zhuanggu Joint Capsules in Combination with Celecoxib in Knee Osteoarthritis: A Multi-center, Randomized, Double-blind, Double-dummy, and Parallel Controlled Trial.
Cai, XY; Fan, WM; Liu, JG; Ma, JZ; Weng, XS; Yang, J; Yang, L; Yun, XQ; Zhang, XL, 2016)		0.93
" Preclinical studies of GTx-024 supported the evaluation of several potential drug-drug interactions in a clinical setting."( Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin.
Coss, CC; Dalton, JT; Jones, A, 2016)		0.64
" The results obtained at concentrations higher than the therapeutic level of drugs and reflect that Metformin in combination with Celecoxib synergistically inhibits the cell proliferation in a concentration dependent pattern."( Enhancement of anti-proliferative activities of Metformin, when combined with Celecoxib, without increasing DNA damage.
Ali, S; Anjum, AA; Ashraf, M; Attiq, A; Javeed, A; Ullah, A, 2016)		0.87
" Its combination with other chemotherapeutic agents was reported to produce synergistic/additive effects on various cancers."( In-vitro and in-vivo inhibition of melanoma growth and metastasis by the drug combination of celecoxib and dacarbazine.
Averineni, RK; Guan, X; Sadhu, SS; Seefeldt, T; Wang, S; Yang, Y, 2016)		0.65
"This study was aimed to evaluate the efficacy of preemptive analgesia (PA) by using celecoxib combined with low-dose tramadol/acetaminophen (tramadol/APAP) in treating post-operative pain of patients undergoing unilateral total knee arthroplasty (TKA)."( Preemptive analgesia by using celecoxib combined with tramadol/APAP alleviates post-operative pain of patients undergoing total knee arthroplasty.
Luo, J; Xu, Z; Zhang, H; Zhang, J; Zhou, A, 2017)		0.97
" Hence, this study was conducted to investigate the comparative pharmacokinetics of anastrozole after single administration and combination with celecoxib."( Comparative pharmacokinetics study of anastrozole after single administration and combination with celecoxib.
Chen, X; Gu, L; Guo, P; Lv, M; Sun, X; Wang, B; Wang, S; Zhao, S, 2018)		0.9
"To evaluate the clinical efficacy and safety of celecoxib combined with chemotherapy in the treatment of gastric cancer."( Comprehensive evaluation of clinical efficacy and safety of celecoxib combined with chemotherapy in management of gastric cancer.
Chen, Z; Guo, Q; Ji, R; Liu, X; Lu, L; Wang, Y; Yuan, H; Zhou, Y, 2017)		0.95
" In the experimental group (n = 120), patients were administered with celecoxib-based chemotherapy, and chemotherapy alone was performed in the control group."( Comprehensive evaluation of clinical efficacy and safety of celecoxib combined with chemotherapy in management of gastric cancer.
Chen, Z; Guo, Q; Ji, R; Liu, X; Lu, L; Wang, Y; Yuan, H; Zhou, Y, 2017)		0.93
"Celecoxib combined with chemotherapy yields clinical benefits for gastric cancer patients with positive COX-2, which not only enhances the OS, DFS, PFS, QOL, and short-term clinical efficacy, but also does not increase the risk of adverse events."( Comprehensive evaluation of clinical efficacy and safety of celecoxib combined with chemotherapy in management of gastric cancer.
Chen, Z; Guo, Q; Ji, R; Liu, X; Lu, L; Wang, Y; Yuan, H; Zhou, Y, 2017)		2.14
"To evaluate the efficacy and safety of celecoxib combined with chemotherapy in the treatment of metastatic or postoperative recurrent gastric cancer."( A comprehensive evaluation of clinical efficacy and safety of celecoxib in combination with chemotherapy in metastatic or postoperative recurrent gastric cancer patients: A preliminary, three-center, clinical trial study.
Chen, Z; Guan, Q; Guo, Q; Li, Q; Liu, M; Wang, J; Wang, Y; Ye, Y; Zhou, Y, 2019)		1.02
" In the experimental group (n = 100), patients were treated with celecoxib combined with chemotherapy, and chemotherapy alone was used in the control group."( A comprehensive evaluation of clinical efficacy and safety of celecoxib in combination with chemotherapy in metastatic or postoperative recurrent gastric cancer patients: A preliminary, three-center, clinical trial study.
Chen, Z; Guan, Q; Guo, Q; Li, Q; Liu, M; Wang, J; Wang, Y; Ye, Y; Zhou, Y, 2019)		0.99
"Celecoxib combined with chemotherapy offers more clinical benefits for COX-2 positive advanced gastric cancer patients."( A comprehensive evaluation of clinical efficacy and safety of celecoxib in combination with chemotherapy in metastatic or postoperative recurrent gastric cancer patients: A preliminary, three-center, clinical trial study.
Chen, Z; Guan, Q; Guo, Q; Li, Q; Liu, M; Wang, J; Wang, Y; Ye, Y; Zhou, Y, 2019)		2.2
"To determine the maximum tolerated dose, toxicities, and response of sirolimus combined with oral metronomic therapy in pediatric patients with recurrent and refractory solid and brain tumors."( A phase I study of sirolimus in combination with metronomic therapy (CHOAnome) in children with recurrent or refractory solid and brain tumors.
Cash, T; Goldsmith, KC; Katzenstein, HM; Kean, L; MacDonald, TJ; Qayed, M; Suessmuth, Y; Tanos, R; Tighiouart, M; Watkins, B; Wetmore, C, 2020)		0.56
" Further NAC in combination with Celecoxib (CXB) inhibits tumor growth by altering antioxidant status and increasing autophagy in DON initiated Swiss mice."( N-acetyl-cysteine in combination with celecoxib inhibits Deoxynivalenol induced skin tumor initiation via induction of autophagic pathways in swiss mice.
Asthana, S; Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Sharma, D; Srivastava, S; Wahajuddin, M, 2020)		1.11
" Combined atorvastatin with celecoxib and tipifarnib synergistically decreased the sphere forming ability of Panc-1 cells and the drug combination also strongly inhibited cell proliferation and promoted apoptosis in the sphere-forming cells."( Effects of atorvastatin in combination with celecoxib and tipifarnib on proliferation and apoptosis in pancreatic cancer sphere-forming cells.
Chen, J; Goodin, S; Li, DL; Ma, YR; Ma, YY; Ren, X; Wang, X; Xu, XT; Zhang, K; Zhao, DG; Zheng, X; Zhou, RP, 2021)		1.18
"This study was designed to evaluate the clinical efficacy of controlled-release morphine tablets combined with celecoxib in relieving osteocarcinoma-related pain and the effects of the combination on WNK1 expression."( Clinical Efficacy of Controlled-Release Morphine Tablets Combined with Celecoxib in Pain Management and the Effects on WNK1 Expression.
Dong, J; Li, J; Luan, F; Shang, M; Song, J, 2021)		1.07
" This study aimed to investigate the anti-cancer potential of PPAR-γ agonist Pioglitazone combined with COX-2 inhibitor Celelcoxib in NSCLC."( Preliminary evaluation of anticancer efficacy of pioglitazone combined with celecoxib for the treatment of non-small cell lung cancer.
Kiran, AVVVR; Krishnamurthy, PT; Kumari, GK, 2022)		0.95
"The significant tumor reducing potential of pioglitazone combined with celecoxib was observed (p < 0."( Preliminary evaluation of anticancer efficacy of pioglitazone combined with celecoxib for the treatment of non-small cell lung cancer.
Kiran, AVVVR; Krishnamurthy, PT; Kumari, GK, 2022)		1.18
" Altogether 128 patients with knee osteoarthritis in the middle and early stage admitted to our hospital from January 2018 to July 2019 were selected and grouped into the control group (CG) (celecoxib tablet therapy) and the combination group (ComG) (celecoxib combined with glucosamine hydrochloride therapy)."( Effect of celecoxib combined with glucosamine hydrochloride in promoting the functional recovery and decreasing the inflammatory factor levels in patients with knee osteoarthritis.
Ge, R; Yang, Z; Zhang, J, 2021)		1.21
" Herein, we assessed a combination of chidamide plus celecoxib (called CC-01) combined with programmed cell death protein 1 (PD-1) blockade in a CT26 model as potent tumor microenvironment (TME) regulator."( CC-01 (chidamide plus celecoxib) modifies the tumor immune microenvironment and reduces tumor progression combined with immune checkpoint inhibitor.
Chao, YS; Chen, CN; Chen, JS; Chou, CH; Chu, SH; Wu, YH; Yang, MH, 2022)		1.29
"To investigate the effects of different nonsteroidal anti-inflammatory drugs combined with platelet-rich plasma on inflammatory factor levels in patients with osteoarthritis."( Effects of Different Nonsteroidal Anti-Inflammatory Drugs Combined with Platelet-Rich Plasma on Inflammatory Factor Levels in Patients with Osteoarthritis.
Cheng, Y; Huang, Y; Jiang, W; Zhang, Y, 2022)		0.72
" This open-label study (NCT03974932) evaluated the efficacy and safety of HTX-011 combined with an MMA regimen in patients undergoing TKA under spinal anesthesia."( HTX-011 in Combination with Multimodal Analgesic Regimen Minimized Severe Pain and Opioid Use after Total Knee Arthroplasty in an Open-Label Study.
Berkowitz, R; Hacker, S; Hu, J; Lee, GC; Rechter, A, 2023)		0.91
" However, the traditional drug combination approaches are restricted with high-cost apparatus, complex and numerous unit operations."( Enabling the drug combination of celecoxib through a spherical co-agglomeration strategy with controllable and stable drug content and good powder properties.
Chen, M; Feng, S; Gao, Y; Gong, J; Guo, S; Han, D; Li, K; Li, T; Tong, L; Wei, J; Yu, C; Zhao, P, 2022)		1
" In the present study, liposomal celecoxib (Lip-CLX) was combined with ex vivo generated DC vaccines pulsed with gp100 peptide (in liposomal and non-liposomal forms) for prophylactic and therapeutic evaluation in the B16F10 melanoma model."( Liposomal celecoxib combined with dendritic cell therapy enhances antitumor efficacy in melanoma.
Arabi, L; Badiee, A; Jaafari, MR; Jahani, V; Yazdani, M, 2023)		1.59
"The purpose of the present study (a randomized clinical trial) was to evaluate the preemptive analgesic effects of pregabalin combined with celecoxib in total knee arthroplasty (TKA)."( Positive Preemptive Analgesia Effectiveness of Pregabalin Combined with Celecoxib in Total Knee Arthroplasty: A Prospective Controlled Randomized Study.
Ding, C; Liu, X; Xiang, B; Yan, L; Zhou, Y, 2023)		1.34
"The preemptive analgesia regimen of pregabalin combined with celecoxib had positive effects on improving acute pain and reducing the cumulative dose of opioids after TKA."( Positive Preemptive Analgesia Effectiveness of Pregabalin Combined with Celecoxib in Total Knee Arthroplasty: A Prospective Controlled Randomized Study.
Ding, C; Liu, X; Xiang, B; Yan, L; Zhou, Y, 2023)		1.38
"We investigated the effects of celecoxib combined with (-)-epigallocatechin-3-gallate (EGCG) or polyphenon E in a cisplatin-induced lung tumorigenesis model."( Effect of a Cyclooxygenase-2 Inhibitor in Combination with (-)-Epigallocatechin Gallate or Polyphenon E on Cisplatin-Induced Lung Tumorigenesis in A/J Mice.
Hisamoto, A; Katayama, H; Kishino, D; Kiura, K; Kubo, T; Maeda, Y; Mimoto, J; Ochi, N; Okada, T; Sato, K; Takigawa, N; Tanimoto, M; Ueoka, H; Yoshino, T, 2023)		1.2

Bioavailability

Curcumin (CUR) and celecoxib (CLX) are two highly hydrophobic drugs which show bioavailability problems. Low solubility and bioavailability issues related with cele Coxib lead to the development and advancement in the discovery and research of some possible formulation administered either orally, topically or via transdermal route.

ExcerptReferenceRelevance
" Both exhibit good oral bioavailability and are potent in standard models of pain, fever, and inflammation yet have a much reduced effect on the GI integrity of rats compared to standard nonsteroidal antiflammatory drugs."( 2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
Black, WC; Brideau, C; Chan, CC; Charleson, S; Chauret, N; Claveau, D; Ethier, D; Gordon, R; Greig, G; Guay, J; Hughes, G; Jolicoeur, P; Leblanc, Y; Nicoll-Griffith, D; Ouimet, N; Prasit, P; Riendeau, D; Visco, D; Wang, Z; Xu, L, 1999)		0.3
" The rate of absorption of celexocib is moderate when given orally (peak plasma drug concentration occurs after 2 to 4 hours), although the extent of absorption is not known."( Clinical pharmacokinetics and pharmacodynamics of celecoxib: a selective cyclo-oxygenase-2 inhibitor.
Davies, NM; Day, RO; McLachlan, AJ; Williams, KM, 2000)		0.56
" The absolute bioavailability of celecoxib was higher when given as a solution (64--88%) compared with capsule (22--40%)."( Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption.
Cook, CS; Gresk, CJ; Jessen, SM; Karim, A; Lawal, Y; Maziasz, TJ; Paulson, SK; Vaughn, MB; Yan, B, 2001)		0.92
" Dose proportionality in pharmacokinetic studies of CBX-BU and CBX at equimolar oral doses confirmed that relative oral bioavailability of CBX was improved following CBX-BU administration and there was linearity in pharmacokinetics of CBX over a wide dose range (10-100 mg/kg), whereas CBX in its conventional form showed poor bioavailability and lack of dose linearity in pharmacokinetics."( Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats.
Bhamidipati, R; Datla, S; Katneni, K; Khan, AA; Kota, J; Mamidi, RN; Mullangi, R; Rajagopalan, R; Rao, CS; Rao, KY; Singh, SK; Srinivas, NR, 2002)		0.57
" Colon-targeted tablets showed decreased AUC(0-infinity), Cmax and absorption rate constant, prolonged absorption time (ta), and increased t1/2 in comparison with the immediate release capsules."( In vivo evaluation of guargum-based colon-targeted oral drug delivery systems of celecoxib in human volunteers.
Bhaskar, P; Dinesh Kumar, B; Karthikeyan, RS; Krishnaiah, YS; Satyanarayana, V, )		0.36
" Under these conditions, enhanced expression of cyclooxygenase-2 might lead to increased production of vasoconstrictor prostanoids and reactive oxygen species that reduce the bioavailability of endothelium-derived nitric oxide."( Short- and long-term COX-2 inhibition reverses endothelial dysfunction in patients with hypertension.
Duffy, SJ; Eberhardt, RT; Gokce, N; Holbrook, M; Keaney, JF; Maxwell, C; Morrow, JD; Palmisano, J; Price, DT; Vita, JA; Widlansky, ME, 2003)		0.32
" The aim of this study was to quantify the relative retinal bioavailability of celecoxib from the subconjunctival route compared to a systemic route."( Retinal delivery of celecoxib is several-fold higher following subconjunctival administration compared to systemic administration.
Ayalasomayajula, SP; Kompella, UB, 2004)		0.87
" The relative bioavailability was estimated as the AUC(0-infinity) ratio between subconjunctival and intraperitoneal groups."( Retinal delivery of celecoxib is several-fold higher following subconjunctival administration compared to systemic administration.
Ayalasomayajula, SP; Kompella, UB, 2004)		0.65
" To improve the solubility and bioavailability and to get faster onset of action of celecoxib, the self-microemulsifying drug delivery system (SMEDDS) was developed."( Formulation design of self-microemulsifying drug delivery systems for improved oral bioavailability of celecoxib.
Bhadra, R; Ghosal, SK; Moulik, SP; Ray, S; Subramanian, N, 2004)		0.76
" Thus, the structural modification of the celecoxib analogues increased P-Akt inhibition and enhanced the bioavailability of the drugs in vitro."( Celecoxib analogues disrupt Akt signaling, which is commonly activated in primary breast tumours.
Cheang, M; Chen, CS; Dunn, SE; Emerman, J; Gilks, CB; Huntsman, D; Kucab, JE; Lee, C; Pollak, M; Yorida, E; Zhu, J, 2005)		2.04
" A celecoxib suspension containing the Form IV had significantly higher bioavailability (>4 times) in dogs than the marketed capsules and the suspension containing bulk drug powders (Form III)."( Characterization of a novel polymorphic form of celecoxib.
Geiger, BM; Hawley, M; Lu, GW; Pfund, W; Smith, M, 2006)		1.21
"The objective of the present study is to develop microspheres for celecoxib to enhance its bioavailability by increasing its gastric residence time."( Development and evaluation of a gastroretentive drug delivery system for the low-absorption-window drug celecoxib.
Ahuja, A; Ali, J; Baboota, S; Hasan, S; Tyagi, P, )		0.58
" In contrast, 5 mg/kg celecoxib in the form of Celebrex(R) showed approximately 40% absolute bioavailability in a cross-over experiment."( Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of celecoxib from solid oral formulations.
Almarsson, O; Chen, H; Gardner, CR; Guzmán, HR; Moreau, JP; Ratanabanangkoon, P; Remenar, JF; Shaw, P; Tawa, M; Zhang, Z, 2007)		0.87
" Relative bioavailability of celecoxib was below 20% in all cases and was probably the consequence of a slow in vivo release of celecoxib from microparticles or low wettability in the case of Celebrex and physical mixture."( Influence of polymers on the bioavailability of microencapsulated celecoxib.
El Ghazouani, F; Homar, M; Kerc, J; Kristl, J; Maincent, P; Ubrich, N, 2007)		0.87
" Following oral administration, the less lipophilic celecoxib has a lower bioavailability (20-40%) than the other two coxibs (74-100%)."( Clinical use and pharmacological properties of selective COX-2 inhibitors.
Klotz, U; Shi, S, 2008)		0.6
" In the present study, we determined the effects of 3,3'-diindolylmethane (Bioresponse BR-DIM referred to as B-DIM), a formulated DIM with greater bioavailability on cell viability and apoptosis with erlotinib in vitro and in vivo using an orthotopic animal tumor model."( Apoptosis-inducing effect of erlotinib is potentiated by 3,3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer.
Ahmad, A; Ali, S; Banerjee, S; El-Rayes, BF; Philip, PA; Sarkar, FH, 2008)		0.35
"The aim of the present study was to assess the skin permeation mechanism and bioavailability of celecoxib (CXB) using novel nanoemulsion formulation."( Celecoxib nanoemulsion: skin permeation mechanism and bioavailability assessment.
Ahuja, A; Ali, J; Baboota, S; Shafiq, S; Shakeel, F, 2008)		2.01
" Specifically, the fasted-state bioavailability (F) was statistically higher (p<0."( Silica-lipid hybrid (SLH) microcapsules: a novel oral delivery system for poorly soluble drugs.
Davey, AK; Prestidge, CA; Rades, T; Simovic, S; Tan, A, 2009)		0.35
"Since the rate-determining step to the intestinal absorption of poorly soluble drugs is the dissolution in the gastrointestinal (GI) tract, postprandial changes in GI physiology, in addition to any specific interactions between drug and food, are expected to affect the pharmacokinetics and bioavailability of such drugs."( Prediction of food effects on the absorption of celecoxib based on biorelevant dissolution testing coupled with physiologically based pharmacokinetic modeling.
Dressman, JB; Janssen, N; Jantratid, E; Kesisoglou, F; Mao, Y; Reppas, C; Shono, Y; Vertzoni, M, 2009)		0.61
"Perifosine is an orally bioavailable alkylphospholipid currently being tested in phase II clinical trials as a potential anticancer drug."( Celecoxib antagonizes perifosine's anticancer activity involving a cyclooxygenase-2-dependent mechanism.
Elrod, HA; Khuri, FR; Sun, SY; Yue, P, 2009)		1.8
" This method of drug delivery may be used to circumvent the low bioavailability and systemic side effects of oral CLX formulations."( Celecoxib-loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics.
Banerjee, S; Deniz, A; Keskin, D; Sade, A; Severcan, F; Tezcaner, A, 2010)		1.8
"The objectives of this research were to prepare celecoxib proniosomes and evaluate the influence of proniosomal formulation on the oral bioavailability of the drug in human volunteers."( In vitro and in vivo evaluation of proniosomes containing celecoxib for oral administration.
Nasr, M, 2010)		0.86
" Aerosolization of Cxb-NLC improved the Cxb pulmonary bioavailability compared to solution formulation which will potentially lead to better patient compliance with minimal dosing intervals."( Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers.
Chougule, M; Jackson, T; Patel, AR; Patlolla, RR; Singh, M; Tata, PN, 2010)		0.6
"Celecoxib mixed with the matrix (final concentration of 6%) was smeared on the surface of the tongue mucosa of hamsters, and the concentration and absorption rate of celecoxib in the tongue tissue were determined by HPLC at 5, 10, 15, 30, 60, 90, 120 min after the application."( [High-performance liquid chromatography for determining celecoxib concentration in hamster tongue tissue after oral local application].
Diao, JX; Li, WZ; Xu, F, 2010)		2.05
" The aim of the present work was to enhance dissolution and oral bioavailability of poorly water-soluble celecoxib (CXB) by preparing stable CXB nanoparticles using a promising method, meanwhile, investigate the mechanism of increasing dissolution of CXB."( Mechanism of dissolution enhancement and bioavailability of poorly water soluble celecoxib by preparing stable amorphous nanoparticles.
Hao, Y; Jiang, T; Liu, Y; Sun, C; Wang, S; Zheng, L, 2010)		0.8
" Additionally, the studies of in-vitro drug dissolution and oral bioavailability in beagle dogs of nanoparticles were performed."( Mechanism of dissolution enhancement and bioavailability of poorly water soluble celecoxib by preparing stable amorphous nanoparticles.
Hao, Y; Jiang, T; Liu, Y; Sun, C; Wang, S; Zheng, L, 2010)		0.59
"The process by combining the antisolvent precipitation under sonication and HPH was a promising method to produce small, uniform and stable CXB nanoparticles with markedly enhanced dissolution rate and oral bioavailability due to an increased solubility that is attributed to a combination of amorphization and nanonization with increased surface area, improved wettability and reduced diffusion pathway."( Mechanism of dissolution enhancement and bioavailability of poorly water soluble celecoxib by preparing stable amorphous nanoparticles.
Hao, Y; Jiang, T; Liu, Y; Sun, C; Wang, S; Zheng, L, 2010)		0.59
"Micro- and nanoparticle formulations are widely used to improve the bioavailability of low solubility drugs."( Preparation of microspheres containing low solubility drug compound by electrohydrodynamic spraying.
Bohr, A; Dyas, M; Edirisinghe, M; Kristensen, J; Stride, E, 2011)		0.37
"CEL-SLH formulations and Celebrex® consistently produced a 2-fold higher maximum plasma concentration (C(max)) and bioavailability (AUC(0→∞)) than pure CEL in a dose-linear manner within the dose range of 5-50 mg/kg CEL (R² > 0."( Silica-lipid hybrid (SLH) versus non-lipid formulations for optimising the dose-dependent oral absorption of celecoxib.
Davey, AK; Prestidge, CA; Tan, A, 2011)		0.58
"Collectively, the results highlight the potential of the SLH microparticles in enhancing the bioavailability of CEL in a dose-linear manner as facilitated by supersaturated solubilisation of CEL in the intestinal milieu."( Silica-lipid hybrid (SLH) versus non-lipid formulations for optimising the dose-dependent oral absorption of celecoxib.
Davey, AK; Prestidge, CA; Tan, A, 2011)		0.58
"Celecoxib suffers from low and variable bioavailability following oral administration of solutions or capsules."( Colon-targeted celecoxib-loaded Eudragit® S100-coated poly-ε-caprolactone microparticles: preparation, characterization and in vivo evaluation in rats.
Amin, MM; Ghorab, DM; Khowessah, OM; Tadros, MI, )		1.93
" When compared to celecoxib powder, F10 microparticles enhanced the bioavailability and extended the duration of drug-plasma concentration in rats."( Colon-targeted celecoxib-loaded Eudragit® S100-coated poly-ε-caprolactone microparticles: preparation, characterization and in vivo evaluation in rats.
Amin, MM; Ghorab, DM; Khowessah, OM; Tadros, MI, )		0.82
"Drug/polymer nanoparticles are well suited for providing rapid oral absorption and increased bioavailability of BCS Class II drugs."( Polymeric nanoparticles for increased oral bioavailability and rapid absorption using celecoxib as a model of a low-solubility, high-permeability drug.
Bello, A; Beyerinck, R; Bloom, C; Morgen, M; Shamblin, S; Song, W; Steenwyk, R; Wilkinson, K, 2012)		0.6
" PK and efficacy data from a randomized, double-blind, 12-week study of celecoxib dosed at 3 and 6 mg/kg twice a day (bid) as an investigational suspension formulation in 152 JRA patients aged 2 to 17 years, PK data from 36 adult RA patients, and relative bioavailability data in healthy adults comparing suspension or capsule sprinkles with the commercial capsule were analyzed."( Dosing celecoxib in pediatric patients with juvenile rheumatoid arthritis.
Bello, A; Bloom, BJ; Hutmacher, MM; Krishnaswami, S; Robbins, JL; West, C, 2012)		1.07
"Fibrous ordered mesoporous carbon (FOMC) was developed as a new drug delivery system for loading an insoluble drug, designed to be orally administered, and then to enhance the drug loading capacity, improve the dissolution rate, enhance the oral bioavailability and reduce the gastric damage."( Inclusion of celecoxib into fibrous ordered mesoporous carbon for enhanced oral bioavailability and reduced gastric irritancy.
Jiang, H; Jiang, T; Sun, C; Wang, S; Wu, C; Zhang, J; Zhao, P; Zhi, Z, 2012)		0.75
"This study is the first to demonstrate in canines the ability of silica-lipid hybrid (SLH) microparticles to enhance the bioavailability and efficacy of a poorly water-soluble drug after oral administration."( Silica-lipid hybrid (SLH) formulations enhance the oral bioavailability and efficacy of celecoxib: An in vivo evaluation.
Boyd, BJ; Edwards, GA; Ngo, D; Nguyen, TH; Porter, CJ; Prestidge, CA; Santos, L; Tan, A, 2013)		0.61
" The mean relative bioavailability of MC1 formulation to plain celecoxib was 157."( Influence of microcrystal formulation on in vivo absorption of celecoxib in rats.
Nasr, M, 2013)		0.87
"The bioavailability of crystalline pharmaceutical substances is often limited by their poor aqueous solubility but it can be improved by formulating the active substance in the amorphous state that is featured with a higher apparent solubility."( Mesoporous calcium carbonate as a phase stabilizer of amorphous celecoxib--an approach to increase the bioavailability of poorly soluble pharmaceutical substances.
Andersson, M; Forsgren, J; Mihranyan, A; Nilsson, P, 2013)		0.63
"In order to characterize the in situ intestinal permeability and in vivo oral bioavailability of celecoxib (CXB), a poorly water-soluble cyclooxygenase (COX)-2 inhibitor, various formulations including the self-emulsifying drug delivery system (SEDDS) and supersaturating SEDDS (S-SEDDS) were compared."( In situ intestinal permeability and in vivo oral bioavailability of celecoxib in supersaturating self-emulsifying drug delivery system.
Chae, BR; Choi, YW; Lee, DH; Lee, KM; Song, SH; Song, WH; Yeom, DW; Yoo, HJ, 2014)		0.86
"Poor aqueous solubility and bioavailability of drugs are one of the important factors affecting the absorption of drugs and consequently their therapeutic effectiveness."( Design and characterization of microcrystals for enhanced dissolution rate of celecoxib.
Kaza, R; Lakshmi, K; Reddy, MP, 2013)		0.62
"The present investigation is aimed at improving the ocular bioavailability of a poorly water soluble drug, celecoxib, to offer new options in the treatment of chronic eye diseases, such as age-related macular degeneration and diabetic retinopathy."( Synthesis, characterization and in vitro studies of celecoxib-loaded poly(ortho ester) nanoparticles targeted for intraocular drug delivery.
Jablonski, MM; Palamoor, M, 2013)		0.85
" Furthermore, the oral bioavailability of CEB-loaded MSU-FC in fasted rats was compared with that of the marketed product."( A novel three-dimensional large-pore mesoporous carbon matrix as a potential nanovehicle for the fast release of the poorly water-soluble drug, celecoxib.
Gao, C; Li, C; Sun, B; Wang, H; Wang, S; Wang, Y; Zhang, Y, 2014)		0.6
" The relative bioavailability of CEB for CEB-loaded MSU-FC was 172%."( A novel three-dimensional large-pore mesoporous carbon matrix as a potential nanovehicle for the fast release of the poorly water-soluble drug, celecoxib.
Gao, C; Li, C; Sun, B; Wang, H; Wang, S; Wang, Y; Zhang, Y, 2014)		0.6
"Sodium diclofenac (Na-DFC) and celecoxib (CLXB) are common nonsteroidal anti-inflammatory (NSAID) drugs which suffer from poor bioavailability and severe side effects when consumed orally, and their transdermal delivery might present important advantages."( HIV-TAT enhances the transdermal delivery of NSAID drugs from liquid crystalline mesophases.
Aserin, A; Cohen-Avrahami, M; Garti, N; Ottaviani, MF; Shames, AI, 2014)		0.69
"Celecoxib beneficially affects the outcome of renal IRI by lowering the expression of COX-2 and hence reducing oxidative stress and increasing the bioavailability of NO."( Celecoxib modulates nitric oxide and reactive oxygen species in kidney ischemia/reperfusion injury and rat aorta model of hypoxia/reoxygenation.
AbdelMoneim, L; Omar, AG; Senbel, AM, 2014)		3.29
"Uniform mesoporous carbon spheres (UMCS) were used as a carrier to improve the bioavailability of the model drug, celecoxib (CEL)."( The mechanism for increasing the oral bioavailability of poorly water-soluble drugs using uniform mesoporous carbon spheres as a carrier.
Wang, B; Wang, S; Wang, T; Zhao, P; Zhao, Q, 2016)		0.64
" Celecoxib (CLX) is a poorly water soluble drug with its bioavailability being limited by its poor dissolution."( Comparing various techniques to produce micro/nanoparticles for enhancing the dissolution of celecoxib containing PVP.
Garekani, HA; Homayouni, A; Nokhodchi, A; Sadeghi, F; Varshosaz, J, 2014)		1.53
" The lead compound demonstrated very good oral bioavailability in mice, slow metabolic degradation, modest distribution into the brain and a remarkable anti-inflammatory efficacy in carrageenan-induced mouse paw edema model."( Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core.
Gavalas, A; Geronikaki, A; Hammock, B; Hwang, SH; Iurchenko, V; Ivanenkov, Y; Krasavin, M; Morisseau, C; Mujumdar, P; Sarnpitak, P; Zozulya, S, 2014)		0.4
" The present study demonstrated that formulation of celecoxib-PVP-TPGS solid dispersion nanoparticles using the SAS process is a highly effective strategy for enhancing the bioavailability of poorly water-soluble celecoxib."( Formulation, characterization, and in vivo evaluation of celecoxib-PVP solid dispersion nanoparticles using supercritical antisolvent process.
Baek, IH; Choo, GH; Ha, ES; Kim, MS, 2014)		0.9
"Polymer based nanoparticle formulations have been shown to increase drug bioavailability and/or reduce drug adverse effects."( Effect of formulation variables on preparation of celecoxib loaded polylactide-co-glycolide nanoparticles.
Cooper, DL; Harirforoosh, S, 2014)		0.66
"Mesoporous materials are promising candidates for improving dissolution rate of poorly water-soluble drugs in vitro and their bioavailability in vivo."( Systematic in vitro and in vivo study on porous silicon to improve the oral bioavailability of celecoxib.
Araújo, F; Correia, A; Hirvonen, J; Järvinen, K; Kovalainen, M; Lehto, VP; Lehtonen, M; Leppänen, J; Näkki, S; Rantanen, J; Riikonen, J; Santos, HA; Xu, W, 2015)		0.64
"Self emulsifying drug delivery system (SEDDS) has been increasingly used for improving the oral bioavailability of poorly water soluble drugs."( Role of solid carriers in pharmaceutical performance of solid supersaturable SEDDS of celecoxib.
Bansal, AK; Chavan, RB; Modi, SR, 2015)		0.64
" The strong capability of the spray-dried SPLNs to attain 'true' supersaturation state makes them a promising approach for bioavailability enhancement of poorly soluble drugs."( Solubility enhancement of BCS Class II drug by solid phospholipid dispersions: Spray drying versus freeze-drying.
Bauer-Brandl, A; Fong, SY; Ibisogly, A, 2015)		0.42
" Based on computational values, LLW-3-6 has physiochemical characteristics that should allow for improved bioavailability in comparison to that of celecoxib."( Celecoxib and LLW-3-6 Reduce Survival of Human Glioma Cells Independently and Synergistically with Sulfasalazine.
Winfield, LL; Yerokun, T, 2015)		2.06
" Omission of a lipophilic portion of the compound led to 26, a readily orally bioavailable inhibitor with potency in HWB comparable to celecoxib."( Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
Antonysamy, S; Bhattachar, SN; Campanale, KM; Chandrasekhar, S; Condon, B; Desai, PV; Fisher, MJ; Groshong, C; Harvey, A; Hickey, MJ; Hughes, NE; Jones, SA; Kim, EJ; Kuklish, SL; Luz, JG; Norman, BH; Rathmell, RE; Rizzo, JR; Schiffler, MA; Seng, TW; Thibodeaux, SJ; Woods, TA; York, JS; Yu, XP, 2016)		0.64
"Celecoxib (CXB) is a Biopharmaceutical Classification System class II drug in which its oral bioavailability is limited by poor aqueous solubility."( Solid Phospholipid Dispersions for Oral Delivery of Poorly Soluble Drugs: Investigation Into Celecoxib Incorporation and Solubility-In Vitro Permeability Enhancement.
Bauer-Brandl, A; Brandl, M; Fong, SY; Martins, SM, 2016)		2.1
" Consistent with the findings from the non-sink in vitro dissolution tests, the amorphous solid dispersions with the highest molecular weight PVPs (K30 and K60) resulted in significantly higher in vivo bioavailability (AUC0-24h) compared with pure amorphous and crystalline CCX."( Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions.
Becker, C; Francke, NM; Holm, P; Holm, R; Jørgensen, EB; Knopp, MM; Langguth, P; Mu, H; Nguyen, JH; Rades, T, 2016)		0.65
"The unique physiological limitations of the eye have been assigned as reason of low bioavailability by conventional drug delivery systems."( Fabrication and evaluation of lipid nanoparticulates for ocular delivery of a COX-2 inhibitor.
Kumar, A; Majumdar, DK; Sahoo, PK; Sharma, AK; Sharma, N; Sharma, RK, 2016)		0.43
"Curcumin (CUR) and celecoxib (CLX) are two highly hydrophobic drugs which show bioavailability problems due to their poor aqueous solubility."( Inulin based micelles loaded with curcumin or celecoxib with effective anti-angiogenic activity.
Annese, T; Chlapanidas, T; Mandracchia, D; Ribatti, D; Ruggieri, S; Trapani, A; Trapani, G; Tripodo, G, 2016)		1.02
" In dog, 14 had oral bioavailability (74%), clearance (3."( Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors.
Antonysamy, S; Bhattachar, SN; Chandrasekhar, S; Fisher, MJ; Fretland, AJ; Gooding, K; Harvey, A; Hughes, NE; Kuklish, SL; Luz, JG; Manninen, PR; McGee, JE; Navarro, A; Norman, BH; Partridge, KM; Quimby, SJ; Schiffler, MA; Sloan, AV; Warshawsky, AM; York, JS; Yu, XP, 2016)		0.43
" Hence, MMC shows promise as a general drug delivery vehicle for increasing the bioavailability of compounds with dissolution rate- or solubility-limited absorption."( Supersaturation of poorly soluble drugs induced by mesoporous magnesium carbonate.
Bergström, C; Strømme, M; Welch, K; Zardán Gómez de la Torre, T; Zhang, P, 2016)		0.43
" Our formulations improved celecoxib bioavailability due to their bioadhesivness, thus preventing their rapid removal."( Stability and Ocular Pharmacokinetics of Celecoxib-Loaded Nanoparticles Topical Ophthalmic Formulations.
Abd-Elgawad, AH; Ibrahim, MM; Jablonski, MM; Soliman, OA, 2016)		1
" However, this approach is frequently limited by the bioavailability and toxicity of the combined agents and delivery at ratios to specific locations that synergistically kill cancer cells."( Nanoparticle-Based Celecoxib and Plumbagin for the Synergistic Treatment of Melanoma.
Gowda, R; Kardos, G; Robertson, GP; Sharma, A; Singh, S, 2017)		0.78
" In this study, PK parameters and absolute oral bioavailability expressed as percentage (F%) of celecoxib (10 mg/kg BW), mavacoxib (4 mg/kg BW) and meloxicam (1 mg/kg BW) were determined following single oral (PO) and intravenous (IV) administration to cockatiels (Nymphicus hollandicus)."( Comparative population pharmacokinetics and absolute oral bioavailability of COX-2 selective inhibitors celecoxib, mavacoxib and meloxicam in cockatiels (Nymphicus hollandicus).
Antonissen, G; Croubels, S; De Backer, P; De Baere, S; Devreese, M; Dhondt, L; Gehring, R; Goessens, T; Haesendonck, R, 2017)		0.89
" This randomised, open-label, crossover study compared the bioavailability of both components after CTC administration under fed and fasting conditions."( The Effect of Food on Tramadol and Celecoxib Bioavailability Following Oral Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label, Single-Dose, Crossover Study in Healthy Volunteers.
Encabo, M; Encina, G; Escriche, M; Gascon, N; Lahjou, M; Plata-Salamán, C; Sicard, E; Smith, K; Videla, S, 2018)		0.76
"As reported for standard-formulation celecoxib, food increased the bioavailability of celecoxib from single-dose CTC."( The Effect of Food on Tramadol and Celecoxib Bioavailability Following Oral Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label, Single-Dose, Crossover Study in Healthy Volunteers.
Encabo, M; Encina, G; Escriche, M; Gascon, N; Lahjou, M; Plata-Salamán, C; Sicard, E; Smith, K; Videla, S, 2018)		1.03
" The benzoyl chloride derivatives were selected to have different hydrophobic groups and this aims to increase the lipophilicity of the final compounds hoping to increase the bioavailability and thus improve the anti-inflammatory activity."( Synthesis, In-vivo and In-vitro Anti-inflammatory Evaluation of some Novel Coumarin Derivatives.
Al-Wabli, R; El-Haggar, R; Fouad, M, 2018)		0.48
" Therefore, CEL-ADI and CEL-SAC eutectics may offer a novel formulation strategy to enhance the solubility and oral bioavailability of CEL."( Preparation, characterization, and evaluation of celecoxib eutectic mixtures with adipic acid/saccharin for improvement of wettability and dissolution rate.
Abuzar, SM; Hong, SH; Hwang, SJ; Hyun, SM; Joo, Y; Kang, H; Kwon, KA; Lee, BJ; Lee, S; Velaga, S, 2019)		0.77
"7-fold increase in the bioavailability of CXB compared with the free CXB-treated group (p < 0."( Preparation and evaluation of celecoxib-loaded proliposomes with high lipid content.
Baek, MJ; Jeon, D; Kim, DD; Kim, DH; Kim, KT; Lee, JY, 2019)		0.8
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
" The bioavailability of the water insoluble drug was also significantly improved by the reduction of particle size into nano-size."( Continuous production of celecoxib nanoparticles using a three-dimensional-coaxial-flow microfluidic platform.
Di, D; Fang, L; Liu, C; Qu, X; Quan, P, 2019)		0.82
" Low solubility and bioavailability issues related with celecoxib lead to the development and advancement in the discovery and research of some possible formulation administered either orally, topically or via transdermal route."( A journey of celecoxib from pain to cancer.
Purohit, P; Saxena, P; Sharma, PK, 2020)		1.17
" Often, only one phospholipid type is used for the formulation development and only one formulation, optimized according to in vitro parameters, is included in oral bioavailability studies."( Do Phospholipids Boost or Attenuate Drug Absorption? In Vitro and In Vivo Evaluation of Mono- and Diacyl Phospholipid-Based Solid Dispersions of Celecoxib.
Bauer-Brandl, A; Brandl, M; Ejskjær, L; Holm, R; Jacobsen, AC, 2021)		0.82
" Celecoxib has low systemic bioavailability due to its low water solubility."( Tablet Formulation of a Synthesized Celecoxib Potassium Salt and Development of a Validated Method for Its Analysis.
Abualhasan, M; Shehab, KA; Shraim, N; Zatar, N, )		1.32
" The relative bioavailability (BA) of the M3 and SD6 formulations was also significantly improved as oral bioavailability (167."( Therapeutic effects of celecoxib polymeric systems in rat models of inflammation and adjuvant-induced rheumatoid arthritis.
Ahn, JB; Choi, JS; Heo, KS; Lee, DH; Myung, CS; Park, JS; Sim, S, 2020)		0.87
" Further, we have conducted BOILED-Egg plot and bioavailability radar analysis for the curcumin and celecoxib."( Curcumin-Celecoxib: a synergistic and rationale combination chemotherapy for breast cancer.
Alqahtani, AM; Chandrasekaran, B; Chidambaram, K; Dhanaraj, P; Pino-Figueroa, A; Venkatesan, K, 2021)		1.25
" However, its low bioavailability and long term exposure related cardiovascular side effects, limit its clinical application."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021)		0.99
"The effect of PIP on the oral bioavailability of CXB in mice was investigated using HPLC analysis."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021)		0.99
"PIP as a bioenhancer increased the oral bioavailability of CXB (129%)."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021)		0.99
" Therefore, newer formulation strategies are always warranted to address poor aqueous solubility and oral bioavailability with extended shelf life."( Amorphous Salts Solid Dispersions of Celecoxib: Enhanced Biopharmaceutical Performance and Physical Stability.
Bansal, AK; Joshi, P; Kashyap, MC; Mandal, SK; Mukesh, S; Sangamwar, AT; Sathe, V, 2021)		0.89
" Nanomedicine has played a crucial role in improving the efficacy of treatment by controlling the release of pharmacologically active ingredients to increase bioavailability and achieve uniform and targeted delivery of drug."( Characterization and in vivo evaluation of nanoformulations in FCA induced rheumatoid arthritis in rats.
Aslam, B; Faisal, MN; Muhammad, F; Siddique, R, 2021)		0.62
" However, the links between low NO bioavailability and COX-2 overexpression in LSECs are unknown."( Celecoxib reduces hepatic vascular resistance in portal hypertension by amelioration of endothelial oxidative stress.
Gao, J; Jia, X; Liu, R; Tai, Y; Tang, C; Tang, S; Tong, H; Zhang, L; Zhao, C, 2021)		2.06
" Our findings demonstrate the differential bioavailability of celecoxib between normal and polyp tissues and its potential effects on clinical response in patients with FAP."( Celecoxib Colorectal Bioavailability and Chemopreventive Response in Patients with Familial Adenomatous Polyposis.
Advani, S; Day, RS; Malek, J; Shureiqi, I; Wei, B; Yang, P; Zuo, X, 2022)		2.4
" Our findings demonstrated the differential bioavailability of celecoxib between normal and polyp tissues and its potential effects on clinical chemopreventive response in patients with FAP."( Celecoxib Colorectal Bioavailability and Chemopreventive Response in Patients with Familial Adenomatous Polyposis.
Advani, S; Day, RS; Malek, J; Shureiqi, I; Wei, B; Yang, P; Zuo, X, 2022)		2.4
" These results indicate that MMC may be helpful in increasing the bioavailability and obtaining a continuous release of CXB, and similar substances, in vivo."( Increasing the Transport of Celecoxib over a Simulated Intestine Cell Membrane Model Using Mesoporous Magnesium Carbonate.
Bergström, C; Gómez de la Torre, J; Zardán Gómez de la Torre, T, 2021)		0.92
" The latter enhance the solubility, bioavailability and drug delivery and hence can decrease the frequency of administration which is of great clinical value."( A single oral dose of celecoxib-loaded solid lipid nanoparticles for treatment of different developmental stages of experimental schistosomiasis mansoni.
Abou-El-Naga, IF; El-Temsahy, MM; Elsawy, ESA; Ibrahim, EI; Makled, S; Mogahed, NMFH, 2022)		1.04
" In examining the effect of celecoxib on 15-LOX-1 for reducing adenomatous polyps in patients with familial adenomatous polyposis (FAP), Yang and colleagues point out the potential importance of drug bioavailability in blood, normal, and neoplastic colorectal tissue in patient response."( The Importance of Drug Concentration at the Site of Action: Celecoxib and Colon Polyp Prevention as a Case Study.
Martinez, JA; Thompson, PA, 2022)		1.26
" Higher elimination half-life, AUC, MRT and lowered clearance rate denotes the extended bioavailability of the drug in blood."( Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation.
Alqahtani, A; Ather, H; Atiya, A; Begum, MY; Ghazwani, M; Hani, U; M Osmani, RA; Rahamathulla, M; Siddiqua, A, 2022)		0.98
"Celecoxib is generally used for the treatment of rheumatoid arthritis, however its poor bioavailability and cytotoxicity in pure form have reduced its therapeutic efficacy."( Rectal Administration of Celecoxib Liquid Suppositories with Enhanced Bioavailability and Safety in Rats.
Baseer, A; Jiao, Y; Ud-Din, F; Xie, S, 2023)		2.66
"Self-nanoemulsifying drug delivery systems (SNEDDS) represent an interesting platform for improving the oral bioavailability of poorly soluble lipophilic drugs."( Development and Characterization of Celecoxib Solid Self-nanoemulsifying Drug Delivery Systems (S-SNEDDS) Prepared Using Novel Cellulose-Based Microparticles as Adsorptive Carriers.
Baudron, V; Beine, B; Bernhardt, A; Klein, S; Schmied, FP, 2022)		1
"The present study investigated the oral bioavailability of celecoxib when incorporated into solid lipid nanoparticles either dissolved or suspended."( The influence on the oral bioavailability of solubilized and suspended drug in a lipid nanoparticle formulation: In vitro and in vivo evaluation.
Elbrink, K; Holm, R; Kiekens, F; Loomans, T; Roelant, D; Van Hees, S, 2022)		0.96
" The results showed that MMC may be a promising drug delivery excipient for increasing the bioavailability of compounds with solubility-limited absorption."( Bioavailability of Celecoxib Formulated with Mesoporous Magnesium Carbonate-An In Vivo Evaluation.
Bergström, C; Cheung, O; Lindmark, T; Strømme, M; Zardán Gómez de la Torre, T, 2022)		1.05
" In here we hypothesized that curcumin-loaded chitosan-coated solid lipid nanoparticles (CuCsSLN) are able to increase its overall bioavailability and hence its antioxidant and mitochondria;/lysosomal protective properties of curcumin."( Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and Mitochondria.
Ebrahimi, HA; Esmaeli, S; Khezri, S; Salimi, A, 2023)		1.14
" The 90% confidence interval for the bioavailability of the T compared to the R was calculated using maximum drug plasma concentration, area under the plasma concentration-time curve from time zero to the last quantifiable concentration point, and area under the plasma concentration-time curve from time zero to infinity for a single oral dose in volunteers, and the data obtained were all between 80% and 125%, indicating that the T and R have bioequivalence and good safety during fasting and fed administration."( Bioequivalence of Celecoxib Capsules in Chinese Healthy Volunteers.
Chen, J; Dong, L; Fan, Y; Feng, J; Guan, R; He, J; Huang, H; Li, R; Long, S; Zhang, J; Zhao, M; Zou, W, 2023)		1.24
" The obtained results indicate that CLX bioavailability has been considerably improved without being toxic to the heart with the aid of NE and advocate the use of PDL NE for developing oral formulations for poorly soluble drugs."( Attenuation of celecoxib cardiac toxicity using Poly(δ-decalactone) based nanoemulsion via oral route.
Bansal, KK; Maru, S; Rosenholm, JM; Verma, J; Wilen, CE, 2023)		1.26

Dosage Studied

Celecoxib plasma concentrations were determined at intervals over 12 hours after a 250-mg/m(2) dose and again 1 week later after twice-daily dosing (steady state) Study demonstrates the possibility of determining the appropriate dosage of celecoxib for each individual through the PBPK modeling with CYP2C9 genomic information.

ExcerptRelevanceReference
"The 2 arthritis trials identified SC-58635 dosage levels that were consistently effective in treating the signs and symptoms of arthritis and were distinguished from placebo on standard arthritis scales."( Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects.
Geis, GS; Hubbard, RC; Isakson, PC; Lanza, FL; Lipsky, PE; Schwartz, BD; Simon, LS; Talwalker, S, 1998)		0.3
" In clinical trials, celecoxib dosed at 100, 200, and 400 mg BID was found to significantly reduce the signs and symptoms of rheumatoid arthritis (RA) and osteoarthritis."( Celecoxib, a selective cyclooxygenase-2 inhibitor for the treatment of rheumatoid arthritis and osteoarthritis.
Goldenberg, MM, 1999)		2.07
" All celecoxib doses were efficacious compared with placebo, although the 50-mg twice-daily dosage regimen was minimally effective."( Treatment of osteoarthritis with celecoxib, a cyclooxygenase-2 inhibitor: a randomized controlled trial.
Bensen, WG; Fiechtner, JJ; Geis, GS; Hubbard, RC; Isakson, PC; McMillen, JI; Verburg, KM; Woods, EM; Yu, SS; Zhao, WW, 1999)		1.1
" This study examined the dose-response effect of celecoxib when administered during the initiation and postinitiation stages."( Chemoprevention of colon cancer by specific cyclooxygenase-2 inhibitor, celecoxib, administered during different stages of carcinogenesis.
Hirose, Y; Kelloff, G; Lubet, R; Paulson, S; Rao, CV; Reddy, BS; Seibert, K; Steele, V, 2000)		0.79
" Once and twice daily celecoxib dosage regimens provided comparable efficacy."( Celecoxib: a review of its use in osteoarthritis, rheumatoid arthritis and acute pain.
Clemett, D; Goa, KL, 2000)		2.06
" The active pharmaceutical ingredient was extracted from its finished dosage form (capsule) using methanol."( A validated LC method for the quantitative determination of celecoxib in pharmaceutical dosage forms and purity evaluation in bulk drugs.
Narayana, CL; Rao, DS; Reddy, GO; Srinivasu, MK, 2000)		0.55
" As a result, drugs that have little or no COX-1 activity across their therapeutic dosage range have been developed."( COX-2 selective nonsteroidal anti-Inflammatory drugs: do they really offer any advantages?
Hawkey, CJ; Jackson, LM, 2000)		0.31
" A dose-response relationship between celecoxib and upper GI symptoms was not apparent."( Upper gastrointestinal tolerability of celecoxib, a COX-2 specific inhibitor, compared to naproxen and placebo.
Agrawal, NM; Bensen, WG; Burke, TA; Geis, GS; Makuch, RW; Maurath, CJ; Zabinski, RA; Zhao, SZ, 2000)		0.85
" The usual recommended daily dosage of celecoxib is 200 mg (in one or two intakes per day), to be increased up to 400 mg (two intakes per day) if necessary."( [Pharma-clinics. The drug of the month. Celecoxib (Celebrex)].
Scheen, AJ, 2001)		0.85
" The active pharmaceutical ingredient was extracted from its finished dosage form (capsule) using ethanol."( LC separation of ortho and meta isomers of celecoxib in bulk and formulations using a chiral column.
Lakshmi Narayana, C; Om Reddy, G; Sreenivas Rao, D; Srinivasu, MK, 2001)		0.57
" The availability of 2 effective regimens provides patients and physicians with increased flexibility in the selection of an appropriate dosing regimen for celecoxib therapy."( Comparison of once-daily and twice-daily administration of celecoxib for the treatment of osteoarthritis of the knee.
Geis, GS; Hubbard, RC; Williams, GW; Yu, SS; Zhao, W, 2001)		0.75
"Celecoxib pharmacokinetics was evaluated after single and multiple oral dosing; after dosing in a solution and as a solid; with and without food; and after administration into different sites of the GI tract using dog."( Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption.
Cook, CS; Gresk, CJ; Jessen, SM; Karim, A; Lawal, Y; Maziasz, TJ; Paulson, SK; Vaughn, MB; Yan, B, 2001)		2.08
" They also summarize indications, contraindications and dosing recommendations."( Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice.
Hersh, EV; Moore, PA, 2001)		1.75
" Groups 2 and 3 also received experimental diet containing celecoxib (500 and 1500 ppm, respectively) for 8 weeks, starting a week before the first dosing of AOM."( Suppression of occurrence and advancement of beta-catenin-accumulated crypts, possible premalignant lesions of colon cancer, by selective cyclooxygenase-2 inhibitor, celecoxib.
Hara, A; Hirose, Y; Katayama, M; Kuno, T; Mori, H; Qiao, Z; Shimizu, M; Yamada, Y; Yoshimi, N, 2001)		0.75
" The observed increase in time to occlusion was abolished when celecoxib was administered to animals dosed with HDA-ER (80."( Effects of selective cyclooxygenase-2 inhibition on vascular responses and thrombosis in canine coronary arteries.
Barrett, TD; Crofford, LJ; Driscoll, EM; Hennan, JK; Huang, J; Lucchesi, BR; Park, AM; Willens, DE, 2001)		0.55
" Therefore, we examined the time dependence of toxicity (chronotoxicity) and of antitumor effects (chronotherapy) of celecoxib to determine optimal time of day for dosing with respect to light-dark cycles."( Chronotherapy and chronotoxicity of the cyclooxygenase-2 inhibitor, celecoxib, in athymic mice bearing human breast cancer xenografts.
Blumenthal, RD; Burton, J; Flefleh, C; Goldenberg, DM; Lew, W; Waskewich, C, 2001)		0.76
" The suggested methods were used to determine doxazosin mesylate and celecoxib in bulk powder, laboratory-prepared mixtures and pharmaceutical dosage forms (cardura tablet and celebrex capsule)."( Stability-indicating methods for the determination of doxazosin mezylate and celecoxib.
Abo-Talib, NF; Bebawy, LI; Moustafa, AA, 2002)		0.78
" During repeated dosage with the specific COX-2 inhibitors, the 24 hour urinary excretion of sodium is only inhibited for the first day of treatment while the excretion of sodium is still decreased over the first 3 hours after the individual doses."( Comparative analgesia, cardiovascular and renal effects of celecoxib, rofecoxib and acetaminophen (paracetamol).
Day, RO; Graham, GG; Graham, RI, 2002)		0.56
"A micellar electrokinetic chromatographic (MEKC) method was developed for the quantification of celecoxib, a COX-2 inhibitor in pharmaceutical dosage forms within the total analysis time of 7 min."( Determination of celecoxib, a COX-2 inhibitor, in pharmaceutical dosage forms by MEKC.
Reddy, GO; Sreenivas Rao, D; Srinivasu, MK, 2002)		0.87
"A new UV spectrophotometric method (UV method) and a reversed phase liquid chromatographic method (LC method) for the quantitative estimation of celecoxib, a selective COX-2 inhibitor, in pure form and in solid dosage form were developed in the present study."( Determination of celecoxib in pharmaceutical formulations using UV spectrophotometry and liquid chromatography.
Jadhav, PR; Patil, SP; Saha, RN; Sajeev, C; Srinivasan, N, 2002)		0.85
"Randomized dose-response study."( Celecoxib, a cyclooxygenase 2 inhibitor as a potential chemopreventive to UV-induced skin cancer: a study in the hairless mouse model.
Black, HS; Gerguis, J; Guevara, A; Lewis, AT; Orengo, IF; Phillips, R, 2002)		1.76
" This trial evaluated the maximum approved OTC dosing regimen (400 mg x 3, q4-6h) of ibuprofen liquigels compared to a single dose of celecoxib (200 mg) and placebo in 174 patients with moderate orsevere pain following surgical extraction of impacted third molars."( Efficacy and tolerability of nonprescription ibuprofen versus celecoxib for dental pain.
Ashraf, E; Cooper, SA; Doyle, G; Jayawardena, S, 2002)		0.76
" Patient's Assessment of Ankle Pain Visual Analog Scale on Weight Bearing responses, also given on days 4 and 8, showed that celecoxib was as efficacious in the treatment of ankle sprain as the maximum therapeutic dosage of ibuprofen and that, compared with placebo, it reduced pain significantly more (P < ."( Efficacy of celecoxib versus ibuprofen in the treatment of acute pain: a multicenter, double-blind, randomized controlled trial in acute ankle sprain.
Ekman, EF; Fiechtner, JJ; Fort, JG; Levy, S, 2002)		0.9
" The mean once-daily dosing rates and their 95% confidence intervals were determined by binomial data analysis."( COX-2-specific inhibitors: prescribing patterns in a large managed care health system and strategies to minimize costs.
Cryer, B; Kelley, CL; Kelly, KC; Weideman, RA, 2002)		0.31
" The percentage of once-daily or less than once-daily dosing was celecoxib 100 mg (17%), celecoxib 200 mg (67%), celecoxib overall (49%), rofecoxib 12."( COX-2-specific inhibitors: prescribing patterns in a large managed care health system and strategies to minimize costs.
Cryer, B; Kelley, CL; Kelly, KC; Weideman, RA, 2002)		0.55
"Celecoxib plasma concentrations were determined at intervals over 12 hours after a 250-mg/m(2) dose and again 1 week later after twice-daily dosing (steady state)."( Single-dose and steady-state pharmacokinetics of celecoxib in children.
Baruchel, S; Gammon, J; Klein, J; Koren, G; Stempak, D, 2002)		2.01
"This is the first report of celecoxib pharmacokinetics in children, and the results indicate that there are significant differences between children and adults with respect to celecoxib disposition; hence these data may have implications when dosing schedules are planned for this population."( Single-dose and steady-state pharmacokinetics of celecoxib in children.
Baruchel, S; Gammon, J; Klein, J; Koren, G; Stempak, D, 2002)		0.86
" The low dosage of the COX-2 inhibitor did not disrupt c-myc and cell viability."( Cyclooxygenase (COX)-2 and granulosa cell apoptosis in vitro.
Caffrey, AS; Chan, PJ; Corselli, JU; King, A; Patton, WC; Swensen, RE, 2002)		0.31
"In a 12-month, multicenter, prospective, open-label trial, patients with OA of the knee or hip or rheumatoid arthritis received celecoxib at doses ranging from that recommended for the treatment of OA (200 mg/d) to twice the recommended daily dosage (400 mg/d)."( A 12-month, multicenter, prospective, open-label trial of radiographic analysis of disease progression in osteoarthritis of the knee or hip in patients receiving celecoxib.
Burr, A; Katz, TK; Lefkowith, JB; Sharp, JT; Tindall, EA; Verburg, K; Wallemark, CB, 2002)		0.72
"For diclofenac, area under the concentration-time curve over the dosage interval (AUC(tau)) was larger in young subjects (3."( Influence of age and cytochrome P450 2C9 genotype on the steady-state disposition of diclofenac and celecoxib.
Brenner, SS; Dilger, K; Herrlinger, C; Hofmann, U; Klotz, U; Marx, C; Mürdter, TE, 2003)		0.54
" This would indicate that both drugs need no dosage reduction in the elderly (at least up to 75 years) and that, besides CYP2C9, additional CYP species contribute to the elimination of both agents."( Influence of age and cytochrome P450 2C9 genotype on the steady-state disposition of diclofenac and celecoxib.
Brenner, SS; Dilger, K; Herrlinger, C; Hofmann, U; Klotz, U; Marx, C; Mürdter, TE, 2003)		0.54
"2% at 1 and 2h after dosing (P<0."( The anti-inflammatory effects of the phosphodiesterase inhibitor pentoxifylline in the rat.
Abdel-Salam, OM; Arbid, MS; Baiuomy, AR; El-Shenawy, SM, 2003)		0.32
"Recently, the Food and Drug Administration increased the celecoxib dosage recommendation from 200 mg to 400 mg for acute pain management."( The efficacy of celecoxib premedication on postoperative pain and recovery times after ambulatory surgery: a dose-ranging study.
Issioui, T; Klein, K; Recart, A; Shah, M; Stool, L; Watcha, MF; White, PF, 2003)		0.91
" Swiss-Webster mice were dosed with celecoxib and rofecoxib and challenged with CT in ligated small intestinal loops, and intestinal segments from mice deficient in COX-1 and COX-2 were challenged with CT."( Role of cyclooxygenase enzymes in a murine model of experimental cholera.
Boldogh, I; Gessell-Lee, DL; Olano, JP; Peterson, JW; Popov, VL, 2003)		0.59
" The drug's effect as well as adverse effects should be actively sought, and dosage alterations made in order to enhance the drug's effect."( Introduction to monitoring. What is what you prescribed actually doing?
George, A; Shakib, S, 2003)		0.32
"To determine if changes in blood pressure and changes in class or dosing of antihypertensive drugs were significantly different in patients treated with celecoxib versus rofecoxib, two cyclooxygenase (COX)-2 inhibitors."( Comparison of changes in blood pressure measurements and antihypertensive therapy in older, hypertensive, ambulatory care patients prescribed celecoxib or rofecoxib.
Dickerson, LM; Nietert, PJ; Ornstein, SM; Rothenberg, RJ, 2003)		0.72
"60) to have had the dosage of their antihypertensive drug increased and also the dosage increased sooner (p<0."( Comparison of changes in blood pressure measurements and antihypertensive therapy in older, hypertensive, ambulatory care patients prescribed celecoxib or rofecoxib.
Dickerson, LM; Nietert, PJ; Ornstein, SM; Rothenberg, RJ, 2003)		0.52
" However, significantly more rofecoxib-treated patients had the dosage of their existing antihypertensive drug increased compared with those receiving celecoxib."( Comparison of changes in blood pressure measurements and antihypertensive therapy in older, hypertensive, ambulatory care patients prescribed celecoxib or rofecoxib.
Dickerson, LM; Nietert, PJ; Ornstein, SM; Rothenberg, RJ, 2003)		0.72
" Differences observed in blood pressure response between COX inhibitors may not be related in their sensitivity but rather their dosing frequency."( Effects of COX inhibition on blood pressure and kidney function in ACE inhibitor-treated blacks and hispanics.
Alausa, T; Bakris, GL; Folker, A; Hung, E; Izhar, M, 2004)		0.32
" This interaction has a significant clinical relevance and may warrant dosage adjustment when celecoxib is co-administered with rifampicin in chronic treatment conditions, such as tuberculosis, leprosy and other infections of joints, bones, etc."( Influence of rifampicin pretreatment on the pharmacokinetics of celecoxib in healthy male volunteers.
Chandrasekhar, K; Jayasagar, G; Krishna Kumar, M; Madhusudan Rao, Y, 2003)		0.78
" Eight-week-old TRAMP mice were randomly divided and fed either control diet (AIN 76A) or a custom prepared AIN 76A diet containing 1500-ppm celecoxib ad libitum for 24 weeks, a dosage that would compare with the normal recommended dose for the treatment of human disease."( Suppression of prostate carcinogenesis by dietary supplementation of celecoxib in transgenic adenocarcinoma of the mouse prostate model.
Adhami, VM; Fu, P; Gupta, S; Hafeli, UO; Lewin, JS; MacLennan, GT; Mukhtar, H; Subbarayan, M, 2004)		0.76
" The dosage of 200 mg twice a day is more efficacious than that of 200 mg daily."( [Clinical evaluation of celecoxib in treating type IIIA chronic prostatitis].
Liu, J; Yang, W; Ye, Z; Zeng, X; Zhang, X; Zhou, S; Zhou, X, 2004)		0.63
" There were no clear dosage or duration effects."( Relationship between COX-2 specific inhibitors and hypertension.
Avorn, J; Levin, R; Schneeweiss, S; Solomon, DH, 2004)		0.32
" Rofecoxib taken at supra-therapeutic dosage was recognised to increase the incidence of myocardial infarction."( [Safety of selective inhibitors of inducible cyclooxygenase-2 taken for a long period].
Lamarque, D, 2004)		0.32
" Timing of administration, inadequate dosing and possible altered pharmacokinetics in pregnancy may explain the lack of efficacy."( The effect of celecoxib on intrathecal morphine-induced pruritus in patients undergoing Caesarean section.
Irwin, MG; Lee, LH; Lim, J; Wong, CK, 2004)		0.68
" These results showed that celecoxib had an antiinflammatory effect in usual dosage in CPD patients."( Effects of celecoxib on high-sensitivity C-reactive protein in chronic peritoneal dialysis patients.
Chang, JW; Chi, HS; Kim, SB; Kim, SH; Lee, SK; Min, WK; Park, JS, 2004)		1.01
" The average concentration of celecoxib in milk during the 8-hour dosing interval was 66 microg/L (95% CI: 41-89)."( Transfer of celecoxib into human milk.
Boger, J; Hale, TW; McDonald, R, 2004)		0.99
" Cohesiveness, low bulk density and compressibility, and poor flow properties of celecoxib impart complications in it's processing into solid dosage forms."( Formulation design of self-microemulsifying drug delivery systems for improved oral bioavailability of celecoxib.
Bhadra, R; Ghosal, SK; Moulik, SP; Ray, S; Subramanian, N, 2004)		0.76
" The energy supplied by these processing steps tends to overcome the energy barriers between different solid-state forms, thus yielding undesirable changes in the physicochemical and material characteristics of drugs or their dosage forms."( Effect of processing on Celecoxib and its solvates.
Bansal, AK; Chawla, G, 2004)		0.63
" The method is suitable not only for the estimation of active ingredients in pharmaceutical dosage forms but also in vitro estimations in human plasma."( Development and validation of a reversed-phase liquid chromatographic method for separation and simultaneous determination of COX-2 inhibitors in pharmaceuticals and its application to biological fluids.
Meena, S; Nagaraju, D; Rao, AR; Rao, RN, 2005)		0.33
" These observations suggest a potential clinical use of combined dosing of COX-2 inhibitors and cytotoxic drugs at lower, nontoxic dose than currently used to treat advanced prostate cancer."( Cyclooxygenase-2 inhibitor celecoxib augments chemotherapeutic drug-induced apoptosis by enhancing activation of caspase-3 and -9 in prostate cancer cells.
Carey, RI; Dandekar, DS; Lokeshwar, BL; Lopez, M, 2005)		0.63
" After three days, a cumulative dosage of 200 mg of CE in refracted doses were given."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.
D'Amato, G; D'Amato, M; Liccardi, G; Piccolo, A; Piscitelli, E; Salzillo, A; Senna, G, 2005)		0.73
" All patients began treatment with celecoxib, at a starting dosage of 100 mg twice daily; patients could increase this dosage to 200 mg twice daily or could switch to another NSAID while maintaining the same treatment strategy."( Nonsteroidal antiinflammatory drugs reduce radiographic progression in patients with ankylosing spondylitis: a randomized clinical trial.
Béhier, JM; Calin, A; Dougados, M; Heijde, Dv; Landewé, R; Olivieri, I; Wanders, A; Zeidler, H, 2005)		0.61
" With celecoxib, studies have shown that a 50% lower dosage is effective and causes fewer adverse effects."( How celecoxib could be safer, how valdecoxib might have been.
Cohen, JS, 2005)		1.37
"Curcumin potentiates the growth inhibitory effect of celecoxib by shifting the dose-response curve to the left."( Celecoxib and curcumin synergistically inhibit the growth of colorectal cancer cells.
Arber, N; Dvory-Sobol, H; Kazanov, D; Lev-Ari, S; Lichtenberg, D; Madar-Shapiro, L; Marian, B; Pinchuk, I; Strier, L, 2005)		2.02
" The cardiovascular risks of COX-2 inhibitors appear heterogeneous, influenced not only by the drug class, but also individual drug, dosage and patient characteristics."( Celecoxib and cardiovascular risks.
Brophy, JM, 2005)		1.77
" The objective of this study was to improve in vivo tumor growth control of nasopharyngeal carcinoma (NPC), treated at a subcurative dosage by using a combination of Hypericin-PDT and COX-2 inhibitor, Celebrex (CX)."( Anti-angiogenic effects of Hypericin-photodynamic therapy in combination with Celebrex in the treatment of human nasopharyngeal carcinoma.
Olivo, M; Soo, KC; Yee, KK, 2005)		0.33
"The purpose of this research was to analyze the devitrification of amorphous celecoxib (CEL) in the presence of different stressors (temperature, pressure, and/or humidity) encountered during processing of solid dosage forms."( Devitrification of amorphous celecoxib.
Bansal, AK; Gupta, P, 2005)		0.85
"The relative 'dose' of celecoxib to which infants are exposed via milk is very low, suggesting that breastfeeding during routine dosing would pose minimal risk."( Quantification of infant exposure to celecoxib through breast milk.
Begg, EJ; Doogue, MP; Gardiner, SJ; Zhang, M, 2006)		0.92
" In the murine model study, we found that long-term dosing with 13-cRA or celecoxib alone or in combination did not increase survival in animals with U87MG tumors but modestly increased survival in animals with U251HF tumors."( Combination chemotherapy with 13-cis-retinoic acid and celecoxib in the treatment of glioblastoma multiforme.
Giglio, P; Groves, MD; Hess, K; Jochec, J; Levin, VA; Puduvalli, VK; Yung, WK, 2006)		0.81
" After three days, a cumulative dosage of 200 mg of CE in refracted doses was given."( Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and other non-steroidal anti-inflammatory drugs.
Cazzola, M; D'Amato, G; D'Amato, M; De Giglio, C; Liccardi, G; Manfredi, D; Piscitelli, E, 2005)		0.73
" Short term dosing studies in vitro were performed in the HT-29 colon carcinoma cell line that was incubated with Cx using the MTT test to assess IC50."( Luminal delivery and dosing considerations of local celecoxib administration to colorectal cancer.
Gati, I; Haupt, S; Kleinstern, J; Rubinstein, A; Zioni, T, 2006)		0.58
"At the dosage studied, celecoxib did not have a beneficial effect on research subjects with ALS, and it was safe."( Trial of celecoxib in amyotrophic lateral sclerosis.
Andreasson, KI; Cudkowicz, ME; Drachman, DB; Rothstein, JD; Schoenfeld, DA; Shefner, JM; Zhang, H, 2006)		1.06
" The available power was insufficient to reliably assess risks among patients with previous myocardial infarction treated with other NSAIDs, dose-response relationships or interaction with aspirin."( The coronary risk of cyclo-oxygenase-2 inhibitors in patients with a previous myocardial infarction.
Brophy, JM; Lévesque, LE; Zhang, B, 2007)		0.34
" This may be clinically important as this dose of celecoxib can be achieved in human serum following standard anti-inflammatory dosing of 100 mg."( Celecoxib and curcumin additively inhibit the growth of colorectal cancer in a rat model.
Arber, N; Giladi, N; Kazanov, D; Lev-Ari, S; Liberman, E; Sagiv, E; Shpitz, B, 2006)		2.03
" We demonstrate that a reduction of cyclooxygenase 2 gene dosage rescued the ovarian aging phenotype of the Wv mice, whereas homozygous deletion was accompanied by a compensatory increase in ovarian cyclooxygenase 1 expression and prostaglandin E(2) synthesis."( A reduction of cyclooxygenase 2 gene dosage counters the ovarian morphological aging and tumor phenotype in Wv mice.
Cai, KQ; Hamilton, TC; Klein-Szanto, A; Smedberg, JL; Smith, ER; Xu, XX; Yang, WL, 2007)		0.34
" The onset of analgesia (PID >or= 1) for all CS-706 doses occurred within 1 hour after dosing (P<0."( A randomized, double-blind, celecoxib- and placebo-controlled study of the effectiveness of CS-706 in acute postoperative dental pain.
Bandy, DP; Daniels, SE; Desjardins, PJ; Lawson, JE; Link, AJ; Moberly, JB; Truitt, KE; Xu, J, 2007)		0.63
" The cardiovascular risks of the different cyclooxygenase-2 inhibitors are not homogeneous, however, and are likely influenced not only by a class effect, but also by individual drug, dosage and patient characteristics."( Cardiovascular effects of cyclooxygenase-2 inhibitors.
Brophy, JM, 2007)		0.34
"This multicenter, double-blind, randomized, placebo-controlled, parallel-group study assessed renal function during dosing with etoricoxib 90 mg daily, celecoxib 200 mg twice daily, and naproxen 500 mg twice daily."( Effects of etoricoxib and comparator nonsteroidal anti-inflammatory drugs on urinary sodium excretion, blood pressure, and other renal function indicators in elderly subjects consuming a controlled sodium diet.
Gertz, BJ; Gottesdiener, KM; Hilliard, DA; Hreniuk, D; Lasseter, KC; Miller, J; Schwartz, JI; Snyder, KM; Thach, C, 2007)		0.54
" Pain intensity was measured using the categorical scale and the primary efficacy variable was the summed pain intensity difference over 8 hours after dosing (SPID-8)."( Lumiracoxib 400 mg compared with celecoxib 400 mg and placebo for treating pain following dental surgery: a randomized, controlled trial.
Davis, N; Fricke, J; Krammer, G; Yu, V, 2008)		0.63
" Recently, cardiotoxic effects associated with conventional modes of delivery of celecoxib have made it pertinent to develop alternate dosage forms capable of selectively delivering the drug topically to affected joints."( Niosomal gel for site-specific sustained delivery of anti-arthritic drug: in vitro-in vivo evaluation.
Jain, S; Kaur, K; Sapra, B; Tiwary, AK, 2007)		0.57
"The combination of bortezomib and celecoxib was well tolerated, without dose limiting toxicities observed throughout the dosing ranges tested, and will be studied further at the highest dose levels investigated."( Bortezomib in combination with celecoxib in patients with advanced solid tumors: a phase I trial.
Chaudhary, U; Dunder, S; Green, M; Hayslip, J; Kraft, A; Meyer, M; Montero, AJ; Salzer, S; Sherman, C, 2007)		0.9
"Continuous dosing of the combination of capecitabine and celecoxib was well tolerated, produced antiangiogenic effects, and has antitumor activity."( Metronomic antiangiogenic therapy with capecitabine and celecoxib in advanced tumor patients--results of a phase II study.
Arends, J; Drevs, J; Frost, A; Häring, B; Hennig, J; Medinger, M; Mross, K; Steinbild, S; Strecker, R; Unger, C, 2007)		0.83
" However, given the increased cardiovascular risks associated with the use of this drug, close patient supervision and strict adherence to dosage and administration guidelines established by the Unites States Food and Drug Administration are of paramount importance."( The effect of a selective cyclooxygenase-2 inhibitor (celecoxib) on chronic periodontitis.
Damoulis, PD; Hibberd, PL; Papas, AS; Singh, M; Stark, PC; Yen, CA, 2008)		0.59
" Finally, these compounds have shown efficacy when dosed orally in multiple acute and chronic prostaglandin and leukotriene dependent in vivo models."( Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
Abraham, WM; Albert, L; Behnke, ML; Chen, L; Clark, JD; Donahue, F; Foley, MA; Goodwin, DG; Hegen, M; Hu, B; Hu, Y; Ipek, M; Keith, J; Kirincich, SJ; Ku, MS; Lee, KL; McKew, JC; Michalak, R; Murphy, EA; Nickerson-Nutter, CL; Ramarao, MK; Shen, MW; Sum, FW; Tam, S; Thakker, P; Thomason, J; Williams, C; Wooder, L; Wu, K; Xu, X, 2008)		0.35
" On each of the next 3 days, rats which showed perfect learning (n=51) received true or sham suprathreshold electroconvulsive shocks (ECS; 60 mC) in a factorial design; daily dosing with drug or vehicle was continued."( Celecoxib as an in vivo probe of cyclooxygenase-2 mechanisms underlying retrograde amnesia in an animal model of ECT.
Andrade, C; Chandra, JS; Sanjay Kumar Rao, N; Singh, NM; Thyagarajan, S; Vinod, PS, 2008)		1.79
" For meloxicam, we found 100% tolerance at a dosage of 15 mg, including the patient who showed a reaction to the celecoxib."( [Tolerance to celecoxib and meloxicam in patients with intolerance to nonsteroidal anti-inflammatory drugs].
Martínez-Cócera, C; Reig Rincón de Arellano, I; Rodríguez-Alvarez, M; Vázquez-Cortés, S; Vázquez-Fuertes, L, 2008)		0.92
" Orally dosed in vivo studies in rats demonstrated superior pharmacokinetics for SLH microcapsules."( Silica-lipid hybrid (SLH) microcapsules: a novel oral delivery system for poorly soluble drugs.
Davey, AK; Prestidge, CA; Rades, T; Simovic, S; Tan, A, 2009)		0.35
" Standard GI parameters (gastric emptying rate and fluid volume) were varied according to the dosing conditions."( Prediction of food effects on the absorption of celecoxib based on biorelevant dissolution testing coupled with physiologically based pharmacokinetic modeling.
Dressman, JB; Janssen, N; Jantratid, E; Kesisoglou, F; Mao, Y; Reppas, C; Shono, Y; Vertzoni, M, 2009)		0.61
" Compared to the previous report, drug loading capacity was significantly improved, enabling the formulation of dosage forms which are of suitable size for peroral application."( Preparation and evaluation of celecoxib-loaded microcapsules with self-microemulsifying core.
Dreu, R; Gasperlin, M; Homar, M; Kerc, J, 2009)		0.64
" Patient compliance was very good; no patient had to reduce the celecoxib dosage nor interrupt treatment."( Phase II nonrandomized study of the efficacy and safety of COX-2 inhibitor celecoxib on patients with cancer cachexia.
Antoni, G; Dessì, M; Macciò, A; Madeddu, C; Mantovani, G; Massa, E; Panzone, F; Serpe, R, 2010)		0.83
" Starting chemotherapy dosage (dose level: 0) was capecitabine 550 mg/m bid, day 1 to 5 every week through out x-ray therapy, irinotecan 30 mg/ m IV on days 1, 8, 22, 29 (no treatment on day 15 and day 36), and celecoxib 400 mg PO bid from day 1 till the last day of radiation."( A phase I study of capecitabine, irinotecan, celecoxib, and radiation as neoadjuvant therapy of patients with locally advanced rectal cancer.
Alqaisi, M; Bernal, P; Bush, D; Byrd, J; Garberoglio, C; Hussein, F; Malik, I, 2010)		0.81
"Recommended dosage for future trials is capecitabine 625 mg/m bid, irinotecan 35 mg/m, and celecoxib 400 mg orally bid in combination with pelvic radiation."( A phase I study of capecitabine, irinotecan, celecoxib, and radiation as neoadjuvant therapy of patients with locally advanced rectal cancer.
Alqaisi, M; Bernal, P; Bush, D; Byrd, J; Garberoglio, C; Hussein, F; Malik, I, 2010)		0.84
" Aerosolization of Cxb-NLC improved the Cxb pulmonary bioavailability compared to solution formulation which will potentially lead to better patient compliance with minimal dosing intervals."( Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers.
Chougule, M; Jackson, T; Patel, AR; Patlolla, RR; Singh, M; Tata, PN, 2010)		0.6
" Agents such as celecoxib, which are highly COX-2 specific and have shown excellent efficacy in relieving inflammation and associated pain, unfortunately exhibit only modest aqueous solubility, thus restricting dosing options."( [Selective inhibitors of cyclooxygenase-2 (COX-2), celecoxib and parecoxib: a systematic review].
Mateos, JL, 2010)		0.96
"Eighteen subjects completed drug dosing and both colonoscopies."( The safety and efficacy of celecoxib in children with familial adenomatous polyposis.
Ayers, GD; Burke, CA; Church, J; Eagle, C; Half, E; Hasson, H; Hawk, E; Lynch, PM; Patterson, S; Richmond, E; Woloj, M, 2010)		0.66
" PGE(2) levels in mice dosed with R-2-phenylpropionic acid were elevated."( Role of COX-2 in nonsteroidal anti-inflammatory drug enteropathy in rodents.
Bjarnason, IT; Hotz-Behofsits, C; Simpson, RJ; Walley, M, 2010)		0.36
" Study drug was dosed daily until the onset of the next menses."( A nonhormonal model for emergency contraception: prostaglandin synthesis inhibitor effects on luteal function and lifespan, a pilot study.
Edelman, AB; Hennebold, JD; Jensen, JT, 2010)		0.36
" Celecoxib serum concentrations were increased by the increase in celecoxib dosage and the maximum drug concentration (Cmax) was 20."( Drug interaction between celecoxib and methotrexate in organic anion transporter 3-transfected renal cells and in rats in vivo.
Endou, H; Fujimura, A; Kanai, Y; Maeda, A; Miyamoto, E; Saito, K; Tsuruoka, S; Ushijima, K, 2010)		1.57
" Our findings suggest that the imbalance between AA and PGE2, characterized by increased AA at a low dosage and decreased PGE2 at a high dosage of celecoxib, was an important indicator of cytotoxicity of celecoxib on H22 cells."( The inhibitory effect of celecoxib on mouse hepatoma H22 cell line on the arachidonic acid metabolic pathway.
Chen, L; Lv, X; Xiang, D; Xu, Z; Zhang, M; Zhang, X, 2010)		0.86
" Therefore, the present study was designed to evaluate the effect of combined dosage of celecoxib and fish oil in experimental mammary carcinogenesis."( Evaluation of the role of oxidative stress in chemopreventive action of fish oil and celecoxib in the initiation phase of 7,12-dimethyl benz(α)anthracene-induced mammary carcinogenesis.
Aggarwal, R; Agnihotri, N; Kansal, S; Kaur, R; Negi, AK; Sarotra, P; Sharma, G, 2011)		0.82
"Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs)."( Investigation of atypical dissolution behavior of an encapsulated amorphous solid dispersion.
Bansal, AK; Dantuluri, AK; Puri, V, 2011)		0.37
" There were no differences between the dosage regimens, although a supplementary 50-mg dose of celecoxib 6 to 12 hours after the first dose appeared to provide additional efficacy over 24 hours."( Efficacy of low-dose celecoxib in patients with acute pain.
Berger, M; McCabe, D; Rizouk, J; Sanner, KM; Savino, L; Schachtel, BP; Schachtel, EP; Zhang, R, 2011)		0.91
"To investigate the dose linearity of celecoxib (CEL) pharmacokinetics from various non-lipid and lipid-based formulations; to probe the mechanisms of CEL absorption from a nano-structured silica-lipid hybrid (SLH) microparticle dosage form."( Silica-lipid hybrid (SLH) versus non-lipid formulations for optimising the dose-dependent oral absorption of celecoxib.
Davey, AK; Prestidge, CA; Tan, A, 2011)		0.85
" In HCT116 cells, celecoxib increased VEGF production with time-course and dose-response curves similar to those observed for the increase of the ER chaperone, GRP78."( Celecoxib induces cell apoptosis coupled with up-regulation of the expression of VEGF by a mechanism involving ER stress in human colorectal cancer cells.
Chen, S; Du, H; Li, W; Wang, Y; Zhang, Y, 2011)		2.15
" Neither association was observed when stratified by NSAID type (aspirin and other NSAIDs), nor did dose-response patterns emerge by frequency of use (average days per month)."( Use of nonsteroidal anti-inflammatory drugs and risk of basal cell carcinoma in the United States Radiologic Technologists study.
Alexander, BH; Cahoon, EK; Doody, MM; Freedman, DM; Linet, MS; Rajaraman, P, 2012)		0.38
"The objective was to derive dosing recommendations for the use of celecoxib in patients with juvenile rheumatoid arthritis (JRA) using pharmacokinetic (PK) and exposure-response data."( Dosing celecoxib in pediatric patients with juvenile rheumatoid arthritis.
Bello, A; Bloom, BJ; Hutmacher, MM; Krishnaswami, S; Robbins, JL; West, C, 2012)		1.07
"Amorphous solid dispersions (ASDs) may entail tailor-made dosage form design to exploit their solubility advantage."( Barrier coated drug layered particles for enhanced performance of amorphous solid dispersion dosage form.
Bansal, AK; Dantuluri, AK; Puri, V, 2012)		0.38
" The dry dosage form, in which >95% of the drug is encapsulated, meets the daily dose."( Development and characterization of a novel drug nanocarrier for oral delivery, based on self-assembled β-casein micelles.
Bachar, M; Barenholz, Y; Danino, D; Even-Chen, S; Mandelbaum, A; Perlstein, H; Portnaya, I, 2012)		0.38
"We investigated the safety and efficacy of the bilateral periarticular multimodal drug injection (PMDI) at a reduced dosage in patients undergoing simultaneous bilateral total knee arthroplasty (SBTKA)."( Use of reduced-dose periarticular injection for pain management in simultaneous bilateral total knee arthroplasty.
Chang, CB; Jeon, YT; Kang, YG; Kim, TK; Koh, IJ; Song, J, 2012)		0.38
"Although pulmonary dosing of large porous particles has been shown to sustain drug delivery for a few days, there are no reports on safety or long term delivery."( Supercritical fluid technology based large porous celecoxib-PLGA microparticles do not induce pulmonary fibrosis and sustain drug delivery and efficacy for several weeks following a single dose.
Dhanda, DS; Kompella, UB; Mirvish, SS; Tyagi, P, 2013)		0.64
"A gastric-retentive formulation amenable to dosing in rodents has the potential to enable sustained release in a preclinical setting."( Utility of gastric-retained alginate gels to modulate pharmacokinetic profiles in rats.
Cornelius, G; Dixon, G; Fancher, RM; Ford, K; Foster, KA; Gudmundsson, OS; Hageman, MJ; Proszynski, M; Sun, H, 2013)		0.39
" The type of interaction between components was determined by isobolographic analysis or by analysis of the log dose-response curves for drug combination and drugs alone."( Levetiracetam interacts synergistically with nonsteroidal analgesics and caffeine to produce antihyperalgesia in rats.
Micov, AM; Stepanović-Petrović, RM; Tomić, MA, 2013)		0.39
" Future clinical trials should investigate this association with maximum dosage of drugs, increased treatment duration, and monitoring of social and environmental changes."( NSAIDs are associated with lower depression scores in patients with osteoarthritis.
Aneja, A; Farkouh, ME; Gandhi, S; Greenberg, J; Iyengar, RL; Mosovich, S; Razzouk, L; Thorpe, K, 2013)		0.39
" Therefore, the present study was designed to investigate the effect of combined dosage of celecoxib and n-3 PUFA-rich fish oil in experimental mammary carcinogenesis."( Alteration in apoptosis and cell cycle by celecoxib and/or fish oil in 7,12-dimethyl benzene (α) anthracene-induced mammary carcinogenesis.
Agnihotri, N; Bhatnagar, A; Kansal, S; Negi, AK, 2013)		0.87
" Concerning the emotional pain responses revealed with USVs, we assumed that the antinociceptive effects were almost completely derived from duloxetine, since celecoxib was ineffective when administered alone or reduced the dosage of duloxetine when given in combination."( Synergistic analgesia of duloxetine and celecoxib in the mouse formalin test: a combination analysis.
Dong, YL; Gu, ZX; Lu, GJ; Sun, YH; Wang, W; Wang, YT; Wu, SX; Yang, J; Zhao, GL, 2013)		0.85
"Preclinical models show that an antiangiogenic regimen at low-dose daily (metronomic) dosing may be effective against chemotherapy-resistant tumors."( A phase II trial of a multi-agent oral antiangiogenic (metronomic) regimen in children with recurrent or progressive cancer.
Allen, JC; Bendel, AE; Campigotto, F; Chi, SN; Chordas, CA; Comito, MA; Goldman, S; Hubbs, SM; Isakoff, MS; Khatib, ZA; Kieran, MW; Kondrat, L; Manley, PE; Neuberg, DS; Pan, WJ; Pietrantonio, JB; Robison, NJ; Rubin, JB; Turner, CD; Werger, AM; Zimmerman, MA, 2014)		0.4
"Two methods, absorption correction and multivariate spectrophotometric methods were developed for simultaneous estimation of Celecoxib (CEL) and Diacerein (DIA) in combined dosage form."( Simultaneous spectrophotometric determination of celecoxib and diacerein in bulk and capsule by absorption correction method and chemometric methods.
Nandurbarkar, VP; Patel, AJ; Patel, NS; Patel, SG, 2014)		0.86
"A novel stability-indicating reverse phase high performance liquid chromatography method was developed and validated for the simultaneous determination of Celecoxib (CEL) and Diacerein (DIN) and its impurities in capsule dosage form."( Stability-indicating HPLC method for quantification of celecoxib and diacerein along with its impurities in capsule dosage form.
Bapatu, HR; Maram, RK; Murthy, RS, 2015)		0.86
" Cultures were treated with a therapeutic dosage of 5 commonly used statins: CEL, ATV + CEL, PGE2, and a selective antagonist of PGE2 receptor 4 (EP4)."( Statins enhance rotator cuff healing by stimulating the COX2/PGE2/EP4 pathway: an in vivo and in vitro study.
Brosh, T; Chechik, O; Dolkart, O; Gabet, Y; Liron, T; Maman, E; Somjen, D, 2014)		0.4
" We found that the surface modification of microparticles with HPMC and TPGS can be an effective formulation strategy for new dosage forms of poorly water-soluble active pharmaceutical ingredients (APIs) to provide higher solubility and dissolution."( Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant.
Baek, IH; Cho, W; Choo, GH; Ha, ES; Hwang, SJ; Jeong, HY; Jung, YS; Kim, JS; Kim, MS; Noh, J; Ok, J, 2015)		0.71
" Effects of orally dosed standard analgesics on CRANE were examined 48 h following bilateral CFA injection."( Complete Freund's adjuvant-induced reduction of exploratory activity in a novel environment as an objective nociceptive endpoint for sub-acute inflammatory pain model in rats.
Bannon, AW; Joshi, SK; Zhu, CZ, 2015)		0.42
" For the comparison in between the two dosage regimens, 100 mg BID oral celecoxib exhibited a greater probability to be the preferred one either in terms of pain intensity or function at the last follow-up time point."( Comparison between 200 mg QD and 100 mg BID oral celecoxib in the treatment of knee or hip osteoarthritis.
Gao, SG; Lei, GH; Li, H; Li, YS; Luo, W; Wei, J; Xiao, WF; Xiong, YL; Yang, T; Yang, TB; Zeng, C, 2015)		0.9
" In order to probe an alternative dosing design that would preclude this effect, we studied the efficacy of a low dose of the antidepressant imipramine (7 mg/kg/day) delivered via food pellets."( Animal Models of Depression and Drug Delivery with Food as an Effective Dosing Method: Evidences from Studies with Celecoxib and Dicholine Succinate.
Araújo-Correia, M; Cline, BH; Costa-Nunes, JP; Dolgov, O; Kubatiev, A; Markova, N; Steinbusch, HW; Strekalova, T; Valença, A; Yeritsyan, N, 2015)		0.63
"The primary purpose of this study was to process partially hydrolyzed PVOH grades (degree of hydroxylation (DH): 33-88%) via HME and to evaluate them as carrier for oral immediate release dosage forms in order to improve the release rate of poorly water soluble drugs (i."( Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications.
De Beer, T; De Jaeghere, W; Remon, JP; Van Bocxlaer, J; Vervaet, C, 2015)		0.42
" After the hydrogel was shown to be biocompatible and safe, an in vivo dose-response study was performed in order to determine safety and efficacy of the pNIPAAM MgFe-LDH hydrogel for intradiscal controlled delivery of CXB."( Biocompatibility and intradiscal application of a thermoreversible celecoxib-loaded poly-N-isopropylacrylamide MgFe-layered double hydroxide hydrogel in a canine model.
Craenmehr, EG; Creemers, LB; Dhert, WJ; Grinwis, GC; Kranenburg, HJ; Langelaan, ML; Meij, BP; Papen-Botterhuis, NE; Plomp, SG; Riemers, FM; Tellegen, AR; Tryfonidou, MA; Willems, N; Yang, HY, 2015)		0.65
"Rats were given either vehicle or rebamipide (30 mg/kg) orally twice daily for two days, then on the third day respective groups were dosed with either vehicle, celecoxib (40 mg/kg), or diclofenac (10 mg/kg) in addition to a respective dose of vehicle or rebamipide."( Celecoxib or diclofenac hepatic status in the presence or absence of rebamipide.
Denham, JW; Harirforoosh, S; Murrell, DE; Panus, PC; Rahmasari, Y, 2015)		2.06
"The poor aqueous solubility of BCS Class II drugs represents a major challenge for oral dosage form development."( Solubility enhancement of BCS Class II drug by solid phospholipid dispersions: Spray drying versus freeze-drying.
Bauer-Brandl, A; Fong, SY; Ibisogly, A, 2015)		0.42
" The drug co-loaded silica was then suspended in an aqueous vehicle facilitating the dosing to animals."( Enhanced oral delivery of celecoxib via the development of a supersaturable amorphous formulation utilising mesoporous silica and co-loaded HPMCAS.
Back, K; Bungay, P; Davis, J; Flanagan, N; Hudson, R; Lainé, AL; Price, D; Roberts, D, 2016)		0.73
" We used the WHO defined daily dose (DDD) as a tool to assess the dosage of sulfasalazine and celecoxib exposure."( Celecoxib and sulfasalazine had negative association with coronary artery diseases in patients with ankylosing spondylitis: A nation-wide, population-based case-control study.
Chiou, JY; Leong, PY; Li, TY; Wang, YH; Wei, JC; Wu, LC; Yeo, KJ, 2016)		2.1
"At the observed dosage and duration, CEL-NP may not affect CEL-associated electrolyte parameters in either plasma or urine; however, it does provide increased systemic exposure while potentially alleviating some gastrointestinal outcomes related to inflammation."( Assessment of celecoxib poly(lactic-co-glycolic) acid nanoformulation on drug pharmacodynamics and pharmacokinetics in rats.
Denham, JW; Hanley, GA; Harirforoosh, S; Murrell, DE; Panus, PC; West, KO, 2016)		0.79
"Standard dosing of the cyclooxygenase-2 inhibitor celecoxib slightly reduced perioperative cyclooxygenase activity during cancer surgery."( Impact of celecoxib on inflammation during cancer surgery: a randomized clinical trial.
Hiller, JG; Ho, KM; Kuruvilla, N; Millen, R; Ramsay, R; Riedel, B; Sampurno, S, 2017)		1.11
" Four additional DILI cases were identified after LY3031207 dosing had been stopped."( Dose-dependent acute liver injury with hypersensitivity features in humans due to a novel microsomal prostaglandin E synthase 1 inhibitor.
Campanale, K; Hall, DG; Henck, J; Hu, L; Jin, Y; Kam, J; Landschulz, W; McNearney, TA; Nakano, M; Phipps, K; Regev, A; Smith, C; Uetrecht, J; Yang, XY, 2018)		0.48
" Interventions included celecoxib at a dosage of 100-200 mg twice daily, ibuprofen at a dosage of 600-800 mg 3 times daily, or naproxen at a dosage of 375-500 mg twice daily."( Differences in Safety of Nonsteroidal Antiinflammatory Drugs in Patients With Osteoarthritis and Patients With Rheumatoid Arthritis: A Randomized Clinical Trial.
Bao, W; Berger, MF; Borer, JS; Graham, DY; Husni, ME; Libby, P; Lincoff, AM; Lüscher, TF; Menon, V; Nissen, SE; Solomon, DH; Wang, Q; Wisniewski, LM; Wolski, KE; Yeomans, ND, 2018)		0.79
" However, because of the complicated pharmacokinetics of combined drug formulations, the majority of combination strategies show severe adverse effects at high dosage and poor biodistribution in vivo."( Celecoxib-Induced Self-Assembly of Smart Albumin-Doxorubicin Conjugate for Enhanced Cancer Therapy.
Jin, X; Shi, L; Wu, C; Xu, L; Xue, B; Yang, J; Zhu, X, 2018)		1.92
"579), the rescue dosage rate (p=0."( A Comparison of Analgesic Effect between Loxoprofen and Celecoxib and the Frequency of the Hemorrhage Following Tonsillectomy.
Ariki, M; Fukushima, N; Hirai, T; Miyahara, N; Yoshiga, A, 2016)		0.68
"The amorphous solid dispersion (ASD) technique has been employed to formulate poorly-soluble drugs, however, development of solid dosage forms with ASD is challenging due to the high propensity of amorphous drug to precipitate upon dissolution."( Development of controlled release amorphous solid dispersions (CRASD) using polyvinyl acetate-based release retarding materials: Effect of dosage form design.
Chen, K; Ghaffari, A; Kane, A; Lugtu-Pe, JA; Wu, XY, 2018)		0.48
"Oral dosage form has limited control over the release of drug from dosage form, hence effective plasma level concentration do not achieve at site of action."( In vitro characterization of elementary osmotic tablet containing celecoxib.
Sheaikh, SS, 2018)		0.72
"Using patient-derived glioblastoma stem cell (GSC) cultures from 15 GBM patients, we described stem cell properties of individual cultures, determined the dose-response relationships of the drugs in the CUSP9, and assessed the efficacy the CUSP9 combination with TMZ in concentrations clinically achievable."( The efficacy of a coordinated pharmacological blockade in glioblastoma stem cells with nine repurposed drugs using the CUSP9 strategy.
Grieg, Z; Langmoen, IA; Sandberg, CJ; Skaga, E; Skaga, IØ; Vik-Mo, EO, 2019)		0.51
" Optimal standardized dosing and drug combination for preoperative multimodal analgesia remains to be elucidated."( Preoperative multimodal analgesia decreases 24-hour postoperative narcotic consumption in elective spinal fusion patients.
Haffner, M; Hwang, J; Klineberg, E; Migdal, C; Nathe, R; Roberto, R; Saiz, AM, 2019)		0.51
" Celecoxib is administered at 200 mg or 400 mg dosage before the surgery."( The efficacy of celecoxib for pain management of arthroscopy: A meta-analysis of randomized controlled trials.
Jiang, H; Li, P; Wan, R, 2019)		1.77
"Celecoxib administered at 200 mg or 400 mg dosage before the surgery decreases postoperative pain intensity of arthroscopy."( The efficacy of celecoxib for pain management of arthroscopy: A meta-analysis of randomized controlled trials.
Jiang, H; Li, P; Wan, R, 2019)		2.3
" Indeed, the lipophilic and poorly soluble celecoxib is orally dosed as an immediate release capsule without any colon-targeting delivery strategy."( Insight into the colonic disposition of celecoxib in humans.
Augustijns, P; Brouwers, J; Lemmens, G; Snoeys, J; Vanuytsel, T, 2020)		1.09
" Hence topical use of celecoxib may be preferred over oral dosing because of lower systemic absorption and to avoid the unwanted side effects."( Celecoxib reduces Deoxynivalenol induced proliferation, inflammation and protein kinase C translocation via modulating downstream targets in mouse skin.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mandal, P; Mishra, S; Rath, SK; Srivastava, S; Tripathi, A; Wahajuddin, M, 2020)		2.32
" A pharmacokinetic study on orally dosed CEL samples (5-mg CEL/kg) was carried out in normal and propantheline (PPT)-treated rats to mimic impaired gastric motility."( Self-Emulsifying Drug Delivery System of Celecoxib for Avoiding Delayed Oral Absorption in Rats with Impaired Gastric Motility.
Ogino, M; Onoue, S; Sato, H; Seto, Y; Suzuki, H; Yakushiji, K, 2020)		0.82
" The current work presents three newly developed UV spectrophotometric methods depending on minimal mathematical manipulations on the zero-order spectrum namely: absorption correction, induced dual-wavelength, and Fourier self deconvoluted method; for the simultaneous determination of celecoxib and ramipril in their pharmaceutical combined dosage forms with amlodipine."( Smart UV spectrophotometric methods based on simple mathematical filtration for the simultaneous determination of celecoxib and ramipril in their pharmaceutical mixtures with amlodipine: A comparative statistical study.
Attala, K; Elsonbaty, A, 2021)		1.01
" To reduce the onset time for a faster action and to lower the manufacturing cost, the tablet dosage form is more preferred."( Direct compression tablet formulation of celecoxib enabled with a pharmaceutical solvate.
Sun, CC; Wang, K, 2021)		0.89
", drug amorphization inside the final dosage form."( The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization.
Berthelsen, R; Hansen, AK; Hempel, NJ; Knopp, MM; Löbmann, K; Merkl, P; Sotiriou, GA; Teleki, A, 2021)		0.62
" This study demonstrates the possibility of determining the appropriate dosage of celecoxib for each individual through the PBPK modeling with CYP2C9 genomic information."( Physiologically based pharmacokinetic (PBPK) modeling for prediction of celecoxib pharmacokinetics according to CYP2C9 genetic polymorphism.
Bae, JW; Cho, CK; Jang, CG; Jung, EH; Kang, P; Kim, YH; Lee, SY; Lee, YJ; Park, HJ, 2021)		1.08
"Poor aqueous solubility is a major limiting factor during the development of BCS Class II drug candidates in a solid oral dosage form."( Tailoring Release Profiles of BCS Class II Drugs Using Controlled Release Amorphous Solid Dispersion Beads with Membrane-Reservoir Design: Effect of Pore Former and Coating Levels.
Chen, K; Ghaffari, A; Kane, A; Lin, BY; Lugtu-Pe, JA; Wu, XY, 2021)		0.62
" Studies investigating optimal dosing for celecoxib and urea cream are recommended."( Prophylactic strategies for hand-foot syndrome/skin reaction associated with systemic cancer treatment: a meta-analysis of randomized controlled trials.
Franco, PIG; Li, RK; Pandy, JGP, 2022)		0.99
" Solid-SNEDDS (S-SNEDDS) combine the advantages of L-SNEDDS with those of solid dosage forms, particularly stability."( Development and Characterization of Celecoxib Solid Self-nanoemulsifying Drug Delivery Systems (S-SNEDDS) Prepared Using Novel Cellulose-Based Microparticles as Adsorptive Carriers.
Baudron, V; Beine, B; Bernhardt, A; Klein, S; Schmied, FP, 2022)		1
" Finally, this investigation displayed promising outcomes that both solubilized and suspended celecoxib in the lipid core of the solid lipid nanoparticles offers the potential to improve the compound's oral bioavailability and thereby reduce the dosing frequency."( The influence on the oral bioavailability of solubilized and suspended drug in a lipid nanoparticle formulation: In vitro and in vivo evaluation.
Elbrink, K; Holm, R; Kiekens, F; Loomans, T; Roelant, D; Van Hees, S, 2022)		0.94
" amorphisation within the final dosage form by microwave irradiation."( Development of a multiparticulate drug delivery system for in situ amorphisation.
Berthelsen, R; Boyd, BJ; Holm, TP; Knopp, MM; Kokott, M; Löbmann, K; Quodbach, J, 2022)		0.72
"Antidepressant-induced jitteriness/anxiety syndrome is characterized as anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, and (hypo)mania, which appear immediately after initiation or increased dosage of an antidepressant."( Jitteriness/anxiety syndrome caused by coadministration of celecoxib, a selective COX-2 inhibitor, with escitalopram and trazodone in a patient with depression and spondylolisthesis.
Kanno, M; Noto, K; Shirata, T; Suzuki, A; Yano, S, 2023)		1.15
" Celecoxib capsules were continuously given orally to patients in the SC group at a dosage of 200 mg daily for 2 weeks."( Modulation effects of different treatments on periaqueductal gray resting state functional connectivity in knee osteoarthritis knee pain patients.
Chen, Y; Cheng, S; Dong, X; He, W; Hu, S; Jiang, N; Li, X; Li, Z; Liang, F; Sun, N; Sun, R; Tang, C; Wintermark, M; Yang, W; Zeng, F; Zhang, X; Zhou, J; Zhou, Y, 2023)		1.82
" In this survey, the prescribed dosage was reduced or discontinued in 150 and 56 patients, respectively, receiving celecoxib and diclofenac prescribed alone, as recorded in a Japanese database of adverse drug events."( Plasma and Hepatic Exposures of Celecoxib and Diclofenac Prescribed Alone in Patients with Cytochrome P450 2C9*3 Modeled after Virtual Oral Administrations and Likely Associated with Adverse Drug Events Reported in a Japanese Database.
Adachi, K; Murayama, N; Nakano, H; Ohyama, K; Saito, Y; Sato, T; Shimizu, M; Tanaka, Y; Yamazaki, H, 2023)		1.4
" The proposed spectrophotometric techniques could be applied for the routine analysis and quality control of the studied drugs in their dosage form."( Eco-friendly simultaneous multi-spectrophotometric estimation of the newly approved drug combination of celecoxib and tramadol hydrochloride tablets in its dosage form.
Belal, F; Hadad, GM; Ramadan, HS; Salam, RAA; Salim, MM, 2023)		1.12
" In the end, the perspective of a formulator, facing various challenges related to unfavorable physicochemical properties of celecoxib upon the development of new oral dosage forms, long-acting injectables, and topical formulations, including the latest trends in the pharmaceutical technology, such as the application of mesoporous carriers, biodegradable microparticles, lipid-based nanosystems, or spanlastics, was presented."( Challenges and Opportunities for Celecoxib Repurposing.
Bąk, U; Krupa, A, 2023)		1.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
cyclooxygenase 2 inhibitorA cyclooxygenase inhibitor that interferes with the action of cyclooxygenase 2.
geroprotectorAny compound that supports healthy aging, slows the biological aging process, or extends lifespan.
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
pyrazoles
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
toluenesAny member of the class of benzenes that is a substituted benzene in which the substituents include one (and only one) methyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

PathwayProteinsCompounds
Celecoxib Action Pathway3573
Celecoxib Metabolism Pathway811

Protein Targets (188)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
pregnane X receptorRattus norvegicus (Norway rat)Potency56.23410.025127.9203501.1870AID651751
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency47.80973.189029.884159.4836AID1224846; AID1224894
RAR-related orphan receptor gammaMus musculus (house mouse)Potency24.34190.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency15.67470.173734.304761.8120AID1346859; AID1346924
USP1 protein, partialHomo sapiens (human)Potency47.39350.031637.5844354.8130AID504865
PPM1D proteinHomo sapiens (human)Potency8.28910.00529.466132.9993AID1347411
SMAD family member 3Homo sapiens (human)Potency15.67470.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency22.55390.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency28.66850.000714.592883.7951AID1259368; AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency47.99640.000221.22318,912.5098AID1259243; AID1259247; AID588516; AID743035; AID743036; AID743042; AID743054; AID743063
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency52.11410.013326.981070.7614AID1346978
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.79430.001318.074339.8107AID926; AID938
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency69.39230.000657.913322,387.1992AID1259377; AID1259378; AID1259394
progesterone receptorHomo sapiens (human)Potency68.45010.000417.946075.1148AID1346784; AID1346795; AID1347036
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.21360.01237.983543.2770AID1346984; AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency12.52110.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency37.51670.000214.376460.0339AID588532; AID720691; AID720692; AID720719
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency34.71040.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.59400.000817.505159.3239AID1159527; AID1159531; AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency45.42180.001530.607315,848.9004AID1224819; AID1224820; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency32.19790.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency10.21610.005428.02631,258.9301AID1346982; AID1346985; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency35.78720.000229.305416,493.5996AID1259244; AID1259248; AID588514; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080
GVesicular stomatitis virusPotency12.30180.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency13.80290.00108.379861.1304AID1645840
67.9K proteinVaccinia virusPotency13.53450.00018.4406100.0000AID720579; AID720580
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency31.35330.001024.504861.6448AID588534; AID588535; AID743212; AID743215; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency42.28310.001019.414170.9645AID588537; AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency16.09530.023723.228263.5986AID743222; AID743223
caspase-3Homo sapiens (human)Potency52.11410.013326.981070.7614AID1346978
IDH1Homo sapiens (human)Potency23.10930.005210.865235.4813AID686970
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency42.98410.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency43.34130.001628.015177.1139AID1224843; AID1224895
activating transcription factor 6Homo sapiens (human)Potency29.54840.143427.612159.8106AID1159516
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency36.22270.154917.870243.6557AID1346877; AID1346891
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency44.781219.739145.978464.9432AID1159509; AID1159518
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency29.84880.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency113.00400.039147.5451146.8240AID1224845
Caspase-7Cricetulus griseus (Chinese hamster)Potency68.58960.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency10.00000.010039.53711,122.0200AID588545
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.92900.00419.984825.9290AID504444
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency40.87070.01789.637444.6684AID588834
caspase-3Cricetulus griseus (Chinese hamster)Potency68.58960.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency31.23220.000323.4451159.6830AID743065; AID743066; AID743067
heat shock protein beta-1Homo sapiens (human)Potency54.73270.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency35.35990.000627.21521,122.0200AID651741; AID743202; AID743219
gemininHomo sapiens (human)Potency23.10190.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency61.00630.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency9.29230.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency12.30180.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency55.17370.002319.595674.0614AID651631; AID720552
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency61.00630.001551.739315,848.9004AID1259244
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Nuclear receptor ROR-gammaHomo sapiens (human)Potency33.49150.026622.448266.8242AID651802
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency44.66843.981146.7448112.2020AID720708
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency12.30180.01238.964839.8107AID1645842
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency54.26110.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency54.26110.011912.222168.7989AID651632
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency12.30180.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Carbonic anhydrase IIHomo sapiens (human)IC50 (µMol)0.02100.02100.02100.0210AID977608
Carbonic anhydrase Astrosclera willeyanaKi0.73200.03201.51729.6000AID644379
Carbonic anhydrase Sulfurihydrogenibium sp. YO3AOP1Ki0.00690.00450.16240.8760AID1268964
Carbonic anhydrase Stylophora pistillataKi0.03420.00000.686710.0000AID436565; AID552130
Carbonic anhydraseStylophora pistillataKi0.69000.00000.50715.7100AID552131
Prostaglandin E synthaseHomo sapiens (human)IC50 (µMol)0.48250.00102.030810.0000AID1274610; AID1274611
Histone deacetylase 3Homo sapiens (human)IC50 (µMol)1.63700.00040.619610.0000AID1390009
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)IC50 (µMol)48.00000.00251.45139.0000AID645642; AID757858
Carbonic anhydrase 12Homo sapiens (human)Ki0.01800.00021.10439.9000AID1067227; AID1193929; AID258733; AID493892; AID620688; AID711038; AID770582
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC50 (µMol)11.37750.00051.41288.2000AID1268104; AID347221; AID393818; AID647091
Prostaglandin G/H synthase 2 Bos taurus (cattle)IC50 (µMol)0.05700.00050.57393.4000AID160731
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)68.50000.00001.18439.6140AID1750298; AID1750299
Cytochrome c oxidase subunit 1Ovis aries (sheep)IC50 (µMol)19.35006.50006.50006.5000AID1557947; AID1565302; AID514960
Cytochrome c oxidase subunit 2Ovis aries (sheep)IC50 (µMol)0.08810.04260.08810.1600AID1846819; AID1846849; AID1846856; AID514961
Catechol O-methyltransferaseMus musculus (house mouse)IC50 (µMol)4.52400.03600.03600.0360AID281535; AID281536
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Cytochrome c oxidase subunit 2Homo sapiens (human)IC50 (µMol)0.37100.02000.84933.0000AID1501860; AID1565303; AID1717039
Carbonic anhydrase 1Homo sapiens (human)IC50 (µMol)30.04440.00582.14107.9000AID1796989; AID254687; AID50344; AID50345
Carbonic anhydrase 1Homo sapiens (human)Ki46.41380.00001.372610.0000AID1067230; AID1142833; AID1188134; AID1190063; AID1193925; AID1194024; AID1195369; AID1262263; AID1268962; AID1275913; AID1287517; AID1434427; AID1439685; AID1453412; AID1628036; AID1798769; AID238536; AID238957; AID258729; AID349605; AID367820; AID369271; AID414955; AID427125; AID436563; AID493883; AID497127; AID552127; AID577526; AID612725; AID620685; AID644380; AID711046; AID711214; AID725955; AID743515; AID764719; AID770586
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)12.56940.00021.10608.3000AID1796989; AID254699; AID47748; AID47749; AID625236
Carbonic anhydrase 2Homo sapiens (human)Ki0.45150.00000.72369.9200AID1061069; AID1067229; AID1142834; AID1188135; AID1190064; AID1193926; AID1194025; AID1195370; AID1240217; AID1262264; AID1268963; AID1275912; AID1278409; AID1287518; AID1434428; AID1439687; AID1453413; AID1628037; AID1796771; AID1798769; AID1849543; AID238574; AID238986; AID254247; AID258730; AID349606; AID367821; AID369272; AID414956; AID427124; AID436564; AID437749; AID493884; AID497129; AID552128; AID577527; AID612726; AID620686; AID644381; AID648179; AID648180; AID669115; AID711045; AID711213; AID725956; AID743514; AID764718; AID770585
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)27.89370.00032.177410.0000AID1061773; AID1063669; AID1077241; AID1125015; AID1125533; AID1125684; AID1141098; AID1141756; AID1142444; AID1154878; AID1164201; AID1164203; AID1172862; AID1177822; AID1177984; AID1188777; AID1194587; AID1196112; AID1204712; AID1226814; AID1238183; AID1250473; AID1253839; AID1262448; AID1268956; AID1285031; AID1288451; AID1292030; AID1301936; AID1306897; AID1310720; AID1334716; AID1357039; AID1368421; AID1373660; AID1374329; AID1397088; AID1403471; AID1409073; AID1420987; AID1426399; AID1437453; AID1443233; AID1454306; AID1461593; AID1464059; AID1464290; AID1501859; AID1517245; AID1542241; AID1551016; AID1568917; AID1569917; AID1592992; AID1608176; AID162017; AID162018; AID162020; AID162022; AID162146; AID162176; AID162177; AID1630905; AID1632806; AID1650563; AID1659926; AID1667491; AID1694419; AID1709974; AID1711784; AID1712993; AID1713247; AID1717038; AID1739492; AID1752435; AID1763090; AID1783310; AID1798182; AID1800496; AID1800497; AID1801480; AID1801526; AID1802056; AID1802571; AID1802573; AID1802579; AID1802609; AID1802612; AID1802788; AID1803031; AID1810791; AID1902042; AID241083; AID241126; AID241382; AID241488; AID261404; AID270013; AID271286; AID289278; AID293936; AID301223; AID313335; AID314261; AID321895; AID323716; AID330496; AID344873; AID368225; AID410033; AID427144; AID432204; AID443489; AID447528; AID448077; AID457928; AID458547; AID479549; AID494634; AID501378; AID510444; AID512137; AID570436; AID578495; AID579473; AID594414; AID598520; AID600505; AID603428; AID622474; AID633796; AID648186; AID648561; AID649269; AID658647; AID665183; AID695143; AID724443; AID744753; AID755520; AID763516
Carbonic anhydrase 3Homo sapiens (human)Ki77.13330.00022.010210.0000AID301578; AID493885; AID711044
Procathepsin LHomo sapiens (human)IC50 (µMol)0.56000.00021.66619.5100AID1253840
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)7.30800.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki7.24700.00322.28879.3160AID625207
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC50 (µMol)16.58500.07002.12673.5000AID1798182
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)26.61000.00030.30952.3000AID271286
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC50 (µMol)4.29500.00011.68479.3200AID1689635; AID1802610
Quinolone resistance protein NorAStaphylococcus aureusIC50 (µMol)40.00007.00008.50009.7000AID669743
Adenosine receptor A3Homo sapiens (human)IC50 (µMol)24.62200.00001.89408.5470AID625196
Adenosine receptor A3Homo sapiens (human)Ki13.91700.00000.930610.0000AID625196
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)1.00000.00002.015110.0000AID625249
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)10.00000.00002.800510.0000AID302411
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)26.61000.00030.32092.3000AID271286
Beta-3 adrenergic receptorHomo sapiens (human)IC50 (µMol)16.12400.00233.24158.0600AID625206
Beta-3 adrenergic receptorHomo sapiens (human)Ki12.09300.00302.30986.0450AID625206
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)24.62200.00021.874210.0000AID625196
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki13.91700.00010.949010.0000AID625196
Calpain-2 catalytic subunitHomo sapiens (human)IC50 (µMol)0.00200.00200.24300.6000AID46698
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)1.51600.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.69200.00020.725710.0000AID625202
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.12000.00031.38338.4000AID629712
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)27.99400.00031.84739.2250AID625252
D(1A) dopamine receptorHomo sapiens (human)Ki13.99700.00010.836310.0000AID625252
Prostaglandin G/H synthase 1Mus musculus (house mouse)IC50 (µMol)3.64010.00072.08445.1000AID160561; AID1851455; AID241917; AID302412; AID363508; AID456475; AID641613; AID753960
Carbonic anhydrase 4Homo sapiens (human)Ki0.64400.00021.97209.9200AID1439688; AID1849544; AID238575; AID493886; AID711043
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)21.92560.00021.557410.0000AID1055838; AID1077204; AID1143529; AID1179976; AID1198998; AID1301936; AID1311611; AID1398036; AID1436691; AID1474823; AID1483246; AID1488610; AID1503671; AID1519089; AID1549680; AID1550470; AID1576160; AID1591462; AID1595291; AID161324; AID161331; AID161333; AID161337; AID161475; AID161480; AID161484; AID161487; AID161491; AID161494; AID161499; AID161503; AID161504; AID161654; AID161660; AID161669; AID161995; AID162312; AID1650563; AID1684449; AID1689632; AID1709977; AID1721658; AID1742031; AID1751818; AID1751820; AID1799729; AID1854722; AID1859070; AID1895998; AID241307; AID281535; AID309449; AID369088; AID382814; AID392041; AID403703; AID432546; AID432549; AID456477; AID54531; AID54536; AID54545; AID547629; AID568556; AID612057; AID625243; AID629713; AID675695; AID694223; AID734525; AID738676
Carbonic anhydrase 6Homo sapiens (human)Ki0.08420.00011.47109.9200AID1798769; AID369273; AID493889; AID711040
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)7.30800.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki7.24700.00031.465610.0000AID625207
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)13.50000.00020.552110.0000AID281535
CruzipainTrypanosoma cruziIC50 (µMol)263.00000.00022.04508.0000AID484274; AID484275
Sodium/hydrogen exchanger 1Rattus norvegicus (Norway rat)IC50 (µMol)33.10000.01000.64613.9000AID432204
Indoleamine 2,3-dioxygenase 1Mus musculus (house mouse)IC50 (µMol)0.00600.00601.625110.0000AID1783311
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)6.27600.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki3.33400.00000.70488.1930AID625222
Delta-type opioid receptorMus musculus (house mouse)Ki25.01050.00000.53939.4000AID1188134; AID1188135
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.02100.00000.60689.2330AID1188135
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki50.00000.00000.38458.6000AID1188134
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC50 (µMol)131.07000.00000.54509.1000AID1742034; AID592803
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.79400.00001.27259.9000AID493887; AID711042
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)4.12810.00010.995010.0000AID1055837; AID1060962; AID1061774; AID1077203; AID1077240; AID1125534; AID1125685; AID1125896; AID1140776; AID1142445; AID1143530; AID1154879; AID1164203; AID1177989; AID1179977; AID1194588; AID1198999; AID1204713; AID1226815; AID1238184; AID1250474; AID1262449; AID1268137; AID1268957; AID1285029; AID1285032; AID1301937; AID1311601; AID1334717; AID1357040; AID1368422; AID1373661; AID1398037; AID1403472; AID1409074; AID1426401; AID1436692; AID1437454; AID1443235; AID1461599; AID1464060; AID1464291; AID1474824; AID1483247; AID1488611; AID1498930; AID1501906; AID1503672; AID1506618; AID1506619; AID1506622; AID1517246; AID1519090; AID1532167; AID1549678; AID1550471; AID1559629; AID1559630; AID1568918; AID1569918; AID1576161; AID1591463; AID1592998; AID1595292; AID160434; AID160742; AID160743; AID1607870; AID1608177; AID1608416; AID162341; AID162344; AID162472; AID162482; AID162484; AID162489; AID162493; AID162494; AID162498; AID162503; AID162507; AID162635; AID162636; AID162644; AID162651; AID162652; AID162656; AID162659; AID1632807; AID1650564; AID1667492; AID1684450; AID1689633; AID1709975; AID1721659; AID1727721; AID1739493; AID1742032; AID1751817; AID1751819; AID1752430; AID1763091; AID1767344; AID1783311; AID1798182; AID1799729; AID1801480; AID1801526; AID1802573; AID1802612; AID1810792; AID1854723; AID1859071; AID1896014; AID1902043; AID241308; AID254798; AID254882; AID270014; AID280834; AID281536; AID289279; AID309450; AID347222; AID362870; AID363802; AID368226; AID369089; AID382813; AID392040; AID393819; AID403704; AID432545; AID432548; AID447529; AID456478; AID457929; AID46698; AID494635; AID501379; AID54555; AID54560; AID54712; AID547628; AID568555; AID579474; AID580343; AID592802; AID603429; AID612058; AID625244; AID629712; AID633795; AID639980; AID648187; AID648562; AID649270; AID660182; AID665184; AID675696; AID675704; AID694220; AID695144; AID724444; AID734522; AID738675; AID755521
Prostaglandin G/H synthase 2Homo sapiens (human)Ki0.00050.00050.41861.5000AID1751838
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)0.40280.00291.786810.0000AID1268102; AID1462012; AID1503672; AID160599
Carbonic anhydraseMethanosarcina thermophilaKi0.57500.06000.97148.5000AID239145; AID239146
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)24.62200.00001.819410.0000AID625196
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki13.91700.00000.965010.0000AID625196
Carbonic anhydrase 7Homo sapiens (human)Ki2.17000.00021.37379.9000AID1060765; AID1193927; AID493890; AID711039; AID764717; AID770584
Urotensin-2 receptorRattus norvegicus (Norway rat)IC50 (µMol)7.60000.03403.16687.6000AID1310720
Carbonic anhydraseSaccharomyces cerevisiae S288CKi0.10800.08200.56098.7000AID367822
Histone deacetylase 4Homo sapiens (human)IC50 (µMol)1.63700.00061.052610.0000AID1390009
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)10.21500.00010.54948.4000AID1143529; AID660182
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)33.10000.00010.506510.0000AID323716
Prostaglandin G/H synthase 2Ovis aries (sheep)IC50 (µMol)3.55100.00101.453910.0000AID1063670; AID1067406; AID1125016; AID1141097; AID1141757; AID1164051; AID1172863; AID1177823; AID1188778; AID1196113; AID1253840; AID1288452; AID1292031; AID1306900; AID1310721; AID1397089; AID1420988; AID1454307; AID1506626; AID1532672; AID1542242; AID1551017; AID160730; AID160732; AID1630906; AID1659927; AID1694420; AID1711785; AID1712994; AID1713248; AID1800496; AID1800497; AID1802056; AID1802571; AID1802579; AID1802609; AID1802788; AID1803031; AID241084; AID241127; AID241383; AID241489; AID242224; AID261405; AID271287; AID301224; AID313337; AID314262; AID321896; AID323717; AID330497; AID344874; AID410034; AID427145; AID432205; AID443490; AID448078; AID458548; AID479548; AID510445; AID512136; AID578496; AID594415; AID598521; AID600506; AID622556; AID647092; AID658648; AID744752; AID763515
Prostaglandin G/H synthase 2Ovis aries (sheep)Ki0.49000.49006.45009.8600AID1802057
Carbonic anhydrase Mycobacterium tuberculosis H37RvKi7.76000.01202.72389.1200AID711032
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)7.70000.00020.660310.0000AID603428
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.02100.00000.27869.0000AID1188135
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi10.35000.00483.38419.8400AID1798985; AID349607; AID711034
Carbonic anhydrase 2Mycobacterium tuberculosis H37RvKi0.71300.00902.20969.8400AID437750; AID711033
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)2.43100.00071.841946.0000AID625256
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.93100.00021.11158.0280AID625256
Prostaglandin G/H synthase 2Mus musculus (house mouse)IC50 (µMol)11.14870.00050.40086.2000AID1125683; AID160595; AID162005; AID1751871; AID1751872; AID1851456; AID241918; AID293935; AID302413; AID363509; AID379225; AID456476; AID456477; AID456478; AID570437; AID641618; AID734521; AID753959
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)1.41100.00010.55439.9000AID1390009; AID1390010
Mitogen-activated protein kinase 14Homo sapiens (human)IC50 (µMol)0.81000.00010.72667.8000AID241924
Carbonic anhydrase 9Homo sapiens (human)IC50 (µMol)0.01600.00030.63029.3900AID1796990; AID254700; AID48294
Carbonic anhydrase 9Homo sapiens (human)Ki1.02220.00010.78749.9000AID1067228; AID1193928; AID1439690; AID1796771; AID1798769; AID1849546; AID238987; AID254248; AID258732; AID369274; AID493891; AID620687; AID711037; AID770583
Carbonic anhydrase, alpha family Hydrogenovibrio crunogenus XCL-2Ki0.98100.00250.32341.1000AID1268965
Carbonic anhydrase Cryptococcus neoformans var. grubiiKi3.05600.01000.73648.3470AID669116
Carbonic anhydraseMethanothermobacter thermautotrophicus str. Delta HKi38.50005.35005.35005.3500AID239250
Carbonic anhydraseCandida albicans SC5314Ki1.52670.01051.44448.3470AID1799266; AID427122; AID669117
Carbonic anhydrase Anopheles gambiae (African malaria mosquito)Ki0.17300.00980.51174.3600AID1195371
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)0.05000.01431.37567.5000AID1403472
Delta carbonic anhydraseConticribra weissflogiiKi0.26500.04960.99789.2000AID1061066
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)14.90330.00291.823210.0000AID1462011; AID1503672; AID162011
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ki0.11600.00701.21749.1700AID744415
Prostaglandin G/H synthase 1Canis lupus familiaris (dog)IC50 (µMol)5.57005.57005.57005.5700AID161324
Carbonic anhydrase 13Homo sapiens (human)Ki0.09800.00031.23099.8000AID493893; AID711036
Cyclooxygenase-2 Canis lupus familiaris (dog)IC50 (µMol)0.90000.63001.77333.7900AID162335
Histone deacetylase 7Homo sapiens (human)IC50 (µMol)1.63700.00071.02609.9000AID1390009
Histone deacetylase 2Homo sapiens (human)IC50 (µMol)1.63700.00010.72219.9700AID1390009
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Carbonic anhydrase 4Bos taurus (cattle)IC50 (µMol)16.81520.02100.20600.6200AID1796989; AID48112; AID48114
Carbonic anhydrase 4Bos taurus (cattle)Ki0.29000.00300.59349.6500AID238597; AID258731
Polyamine deacetylase HDAC10Homo sapiens (human)IC50 (µMol)1.63700.00050.72459.9000AID1390009
Histone deacetylase 11 Homo sapiens (human)IC50 (µMol)1.63700.00030.92989.9000AID1390009
Carbonic anhydrase 15Mus musculus (house mouse)Ki0.05730.00091.884610.0000AID1798769; AID369275; AID493895
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)1.63700.00070.99479.9000AID1390009
P2Y purinoceptor 12Rattus norvegicus (Norway rat)IC50 (µMol)0.04000.02000.34000.9600AID1061774
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)1.14000.00000.53769.9000AID1390009; AID1390013
Histone deacetylase 9Homo sapiens (human)IC50 (µMol)1.63700.00050.94139.9000AID1390009
Carbonic anhydrase 14Homo sapiens (human)Ki0.68900.00021.50999.9000AID493894; AID711035
Histone deacetylase 5Homo sapiens (human)IC50 (µMol)1.63700.00070.961010.0000AID1390009
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.09300.00001.34129.9700AID493888; AID711041
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GTP-binding protein (rab7)Canis lupus familiaris (dog)EC50 (µMol)30.00000.02201.21466.4190AID2041
ras protein, partialHomo sapiens (human)EC50 (µMol)30.00000.02000.22371.9660AID2047; AID2050
Rac1 proteinHomo sapiens (human)EC50 (µMol)36.52650.02025.986029.5100AID2048; AID2055
cell division cycle 42 (GTP binding protein, 25kDa), partialHomo sapiens (human)EC50 (µMol)30.00000.05633.055413.5100AID2019; AID2020
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)EC50 (µMol)30.00000.00070.42361.7650AID2047
Prostaglandin G/H synthase 2Homo sapiens (human)Kd0.78910.00901.87258.4000AID1802596
Ras-related protein Rab-2ACanis lupus familiaris (dog)EC50 (µMol)30.00000.15800.37770.7042AID2045
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase Brucella suis 1330Kinact0.01800.01700.86285.8700AID459696
interferon gamma precursorHomo sapiens (human)AC5022.18000.128015.173038.6100AID1259418
prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Active Concentration20.000020.000020.000020.0000AID1421
Prostaglandin G/H synthase 2Homo sapiens (human)Inhibition0.02800.02800.02800.0280AID160249
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (764)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processProstaglandin E synthaseHomo sapiens (human)
prostaglandin metabolic processProstaglandin E synthaseHomo sapiens (human)
signal transductionProstaglandin E synthaseHomo sapiens (human)
cell population proliferationProstaglandin E synthaseHomo sapiens (human)
negative regulation of cell population proliferationProstaglandin E synthaseHomo sapiens (human)
sensory perception of painProstaglandin E synthaseHomo sapiens (human)
regulation of fever generationProstaglandin E synthaseHomo sapiens (human)
positive regulation of prostaglandin secretionProstaglandin E synthaseHomo sapiens (human)
regulation of inflammatory responseProstaglandin E synthaseHomo sapiens (human)
cellular oxidant detoxificationProstaglandin E synthaseHomo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
type B pancreatic cell development3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
hyperosmotic response3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phospholipase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
calcium-mediated signaling3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
actin cytoskeleton organization3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
T cell costimulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
activation of protein kinase B activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to insulin stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of mast cell degranulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein autophosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to epidermal growth factor stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
extrinsic apoptotic signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of protein localization to plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of sprouting angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1 Bos taurus (cattle)
cellular oxidant detoxificationProstaglandin G/H synthase 1 Bos taurus (cattle)
meiotic spindle organizationProstaglandin G/H synthase 2 Bos taurus (cattle)
prostaglandin biosynthetic processProstaglandin G/H synthase 2 Bos taurus (cattle)
ovarian cumulus expansionProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of protein phosphorylationProstaglandin G/H synthase 2 Bos taurus (cattle)
response to oxidative stressProstaglandin G/H synthase 2 Bos taurus (cattle)
cyclooxygenase pathwayProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of embryonic developmentProstaglandin G/H synthase 2 Bos taurus (cattle)
cellular response to interleukin-1Prostaglandin G/H synthase 2 Bos taurus (cattle)
cellular oxidant detoxificationProstaglandin G/H synthase 2 Bos taurus (cattle)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of oocyte maturationProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of meiotic cell cycle process involved in oocyte maturationProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
response to hypoxiaCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial electron transport, cytochrome c to oxygenCytochrome c oxidase subunit 2Homo sapiens (human)
lactationCytochrome c oxidase subunit 2Homo sapiens (human)
cellular respirationCytochrome c oxidase subunit 2Homo sapiens (human)
proton transmembrane transportCytochrome c oxidase subunit 2Homo sapiens (human)
ATP synthesis coupled electron transportCytochrome c oxidase subunit 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
response to bacteriumCarbonic anhydrase 3Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 3Homo sapiens (human)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
response to hypoxiaCalpain-2 catalytic subunitHomo sapiens (human)
blastocyst developmentCalpain-2 catalytic subunitHomo sapiens (human)
proteolysisCalpain-2 catalytic subunitHomo sapiens (human)
myoblast fusionCalpain-2 catalytic subunitHomo sapiens (human)
female pregnancyCalpain-2 catalytic subunitHomo sapiens (human)
response to mechanical stimulusCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCalpain-2 catalytic subunitHomo sapiens (human)
protein autoprocessingCalpain-2 catalytic subunitHomo sapiens (human)
regulation of interleukin-6 productionCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to interferon-betaCalpain-2 catalytic subunitHomo sapiens (human)
response to hydrogen peroxideCalpain-2 catalytic subunitHomo sapiens (human)
behavioral response to painCalpain-2 catalytic subunitHomo sapiens (human)
regulation of cytoskeleton organizationCalpain-2 catalytic subunitHomo sapiens (human)
proteolysis involved in protein catabolic processCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to lipopolysaccharideCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to amino acid stimulusCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of myoblast fusionCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of phosphatidylcholine biosynthetic processCalpain-2 catalytic subunitHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
bicarbonate transportCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 4Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 6Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceBifunctional epoxide hydrolase 2Homo sapiens (human)
positive regulation of gene expressionBifunctional epoxide hydrolase 2Homo sapiens (human)
dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
cholesterol homeostasisBifunctional epoxide hydrolase 2Homo sapiens (human)
stilbene catabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
phospholipid dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
regulation of cholesterol metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 7Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 7Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 7Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 7Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 7Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 4Homo sapiens (human)
Golgi organizationRas-related protein Rab-2ACanis lupus familiaris (dog)
protein transportRas-related protein Rab-2ACanis lupus familiaris (dog)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipopolysaccharideMitogen-activated protein kinase 14Homo sapiens (human)
DNA damage checkpoint signalingMitogen-activated protein kinase 14Homo sapiens (human)
cell morphogenesisMitogen-activated protein kinase 14Homo sapiens (human)
cartilage condensationMitogen-activated protein kinase 14Homo sapiens (human)
angiogenesisMitogen-activated protein kinase 14Homo sapiens (human)
osteoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
placenta developmentMitogen-activated protein kinase 14Homo sapiens (human)
response to dietary excessMitogen-activated protein kinase 14Homo sapiens (human)
chondrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusMitogen-activated protein kinase 14Homo sapiens (human)
glucose metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 14Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 14Homo sapiens (human)
signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
skeletal muscle tissue developmentMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of gene expressionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myotube differentiationMitogen-activated protein kinase 14Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 14Homo sapiens (human)
fatty acid oxidationMitogen-activated protein kinase 14Homo sapiens (human)
platelet activationMitogen-activated protein kinase 14Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 14Homo sapiens (human)
osteoclast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated protein kinase signaling cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 14Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
response to muramyl dipeptideMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of interleukin-12 productionMitogen-activated protein kinase 14Homo sapiens (human)
response to insulinMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of hippo signalingMitogen-activated protein kinase 14Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusMitogen-activated protein kinase 14Homo sapiens (human)
response to muscle stretchMitogen-activated protein kinase 14Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of protein import into nucleusMitogen-activated protein kinase 14Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of erythrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
glucose importMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of glucose importMitogen-activated protein kinase 14Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
stem cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
striated muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationMitogen-activated protein kinase 14Homo sapiens (human)
bone developmentMitogen-activated protein kinase 14Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipoteichoic acidMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to ionizing radiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to UV-BMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of brown fat cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular senescenceMitogen-activated protein kinase 14Homo sapiens (human)
stress-induced premature senescenceMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to virusMitogen-activated protein kinase 14Homo sapiens (human)
regulation of synaptic membrane adhesionMitogen-activated protein kinase 14Homo sapiens (human)
regulation of cytokine production involved in inflammatory responseMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast fusionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Canis lupus familiaris (dog)
cellular oxidant detoxificationProstaglandin G/H synthase 1Canis lupus familiaris (dog)
one-carbon metabolic processCarbonic anhydrase 13Homo sapiens (human)
response to oxidative stressCyclooxygenase-2 Canis lupus familiaris (dog)
embryo implantationCyclooxygenase-2 Canis lupus familiaris (dog)
regulation of blood pressureCyclooxygenase-2 Canis lupus familiaris (dog)
response to nematodeCyclooxygenase-2 Canis lupus familiaris (dog)
positive regulation of prostaglandin biosynthetic processCyclooxygenase-2 Canis lupus familiaris (dog)
positive regulation of fever generationCyclooxygenase-2 Canis lupus familiaris (dog)
prostaglandin secretionCyclooxygenase-2 Canis lupus familiaris (dog)
positive regulation of peptidyl-serine phosphorylationCyclooxygenase-2 Canis lupus familiaris (dog)
regulation of cell population proliferationCyclooxygenase-2 Canis lupus familiaris (dog)
negative regulation of apoptotic processCyclooxygenase-2 Canis lupus familiaris (dog)
decidualizationCyclooxygenase-2 Canis lupus familiaris (dog)
brown fat cell differentiationCyclooxygenase-2 Canis lupus familiaris (dog)
cellular response to hypoxiaCyclooxygenase-2 Canis lupus familiaris (dog)
cellular response to non-ionic osmotic stressCyclooxygenase-2 Canis lupus familiaris (dog)
cellular response to fluid shear stressCyclooxygenase-2 Canis lupus familiaris (dog)
positive regulation of brown fat cell differentiationCyclooxygenase-2 Canis lupus familiaris (dog)
cellular oxidant detoxificationCyclooxygenase-2 Canis lupus familiaris (dog)
regulation of neuroinflammatory responseCyclooxygenase-2 Canis lupus familiaris (dog)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressCyclooxygenase-2 Canis lupus familiaris (dog)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 14Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
response to bacteriumCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (229)

Processvia Protein(s)Taxonomy
glutathione transferase activityProstaglandin E synthaseHomo sapiens (human)
glutathione peroxidase activityProstaglandin E synthaseHomo sapiens (human)
prostaglandin-D synthase activityProstaglandin E synthaseHomo sapiens (human)
protein bindingProstaglandin E synthaseHomo sapiens (human)
glutathione bindingProstaglandin E synthaseHomo sapiens (human)
prostaglandin-E synthase activityProstaglandin E synthaseHomo sapiens (human)
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein serine/threonine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
ATP binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase activator activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein serine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1 Bos taurus (cattle)
heme bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
metal ion bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
peroxidase activityProstaglandin G/H synthase 2 Bos taurus (cattle)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2 Bos taurus (cattle)
heme bindingProstaglandin G/H synthase 2 Bos taurus (cattle)
metal ion bindingProstaglandin G/H synthase 2 Bos taurus (cattle)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytochrome-c oxidase activityCytochrome c oxidase subunit 2Homo sapiens (human)
cytochrome-c oxidase activityCytochrome c oxidase subunit 2Homo sapiens (human)
copper ion bindingCytochrome c oxidase subunit 2Homo sapiens (human)
protein bindingCytochrome c oxidase subunit 2Homo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 3Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 3Homo sapiens (human)
nickel cation bindingCarbonic anhydrase 3Homo sapiens (human)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
calcium-dependent cysteine-type endopeptidase activityCalpain-2 catalytic subunitHomo sapiens (human)
calcium ion bindingCalpain-2 catalytic subunitHomo sapiens (human)
protein bindingCalpain-2 catalytic subunitHomo sapiens (human)
cytoskeletal protein bindingCalpain-2 catalytic subunitHomo sapiens (human)
cysteine-type peptidase activityCalpain-2 catalytic subunitHomo sapiens (human)
enzyme bindingCalpain-2 catalytic subunitHomo sapiens (human)
protein-containing complex bindingCalpain-2 catalytic subunitHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 4Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 6Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
magnesium ion bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide hydrolase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
toxic substance bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
10-hydroxy-9-(phosphonooxy)octadecanoate phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lipid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
protein homodimerization activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lysophosphatidic acid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 7Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
GTPase activityRas-related protein Rab-2ACanis lupus familiaris (dog)
GTP bindingRas-related protein Rab-2ACanis lupus familiaris (dog)
GDP bindingRas-related protein Rab-2ACanis lupus familiaris (dog)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 14Homo sapiens (human)
enzyme bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein phosphatase bindingMitogen-activated protein kinase 14Homo sapiens (human)
mitogen-activated protein kinase p38 bindingMitogen-activated protein kinase 14Homo sapiens (human)
NFAT protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Canis lupus familiaris (dog)
heme bindingProstaglandin G/H synthase 1Canis lupus familiaris (dog)
metal ion bindingProstaglandin G/H synthase 1Canis lupus familiaris (dog)
protein bindingCarbonic anhydrase 13Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 13Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 13Homo sapiens (human)
peroxidase activityCyclooxygenase-2 Canis lupus familiaris (dog)
enzyme bindingCyclooxygenase-2 Canis lupus familiaris (dog)
heme bindingCyclooxygenase-2 Canis lupus familiaris (dog)
protein homodimerization activityCyclooxygenase-2 Canis lupus familiaris (dog)
metal ion bindingCyclooxygenase-2 Canis lupus familiaris (dog)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Bos taurus (cattle)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 14Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (140)

Processvia Protein(s)Taxonomy
nuclear envelope lumenProstaglandin E synthaseHomo sapiens (human)
endoplasmic reticulum membraneProstaglandin E synthaseHomo sapiens (human)
membraneProstaglandin E synthaseHomo sapiens (human)
perinuclear region of cytoplasmProstaglandin E synthaseHomo sapiens (human)
membraneProstaglandin E synthaseHomo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
nucleus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasm3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
focal adhesion3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
postsynaptic density3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasmic vesicle3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell projection3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1 Bos taurus (cattle)
nuclear inner membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
nuclear outer membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
endoplasmic reticulum membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrionCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial inner membraneCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial respiratory chain complex IVCytochrome c oxidase subunit 2Homo sapiens (human)
membraneCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial membraneCytochrome c oxidase subunit 2Homo sapiens (human)
respiratory chain complex IVCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial matrixCytochrome c oxidase subunit 2Homo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytoplasmCarbonic anhydrase 3Homo sapiens (human)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
membrane raftCalpain-2 catalytic subunitHomo sapiens (human)
nucleusCalpain-2 catalytic subunitHomo sapiens (human)
cytoplasmCalpain-2 catalytic subunitHomo sapiens (human)
lysosomeCalpain-2 catalytic subunitHomo sapiens (human)
endoplasmic reticulumCalpain-2 catalytic subunitHomo sapiens (human)
Golgi apparatusCalpain-2 catalytic subunitHomo sapiens (human)
cytosolCalpain-2 catalytic subunitHomo sapiens (human)
plasma membraneCalpain-2 catalytic subunitHomo sapiens (human)
focal adhesionCalpain-2 catalytic subunitHomo sapiens (human)
external side of plasma membraneCalpain-2 catalytic subunitHomo sapiens (human)
dendriteCalpain-2 catalytic subunitHomo sapiens (human)
cortical actin cytoskeletonCalpain-2 catalytic subunitHomo sapiens (human)
pseudopodiumCalpain-2 catalytic subunitHomo sapiens (human)
neuronal cell bodyCalpain-2 catalytic subunitHomo sapiens (human)
membrane raftCalpain-2 catalytic subunitHomo sapiens (human)
extracellular exosomeCalpain-2 catalytic subunitHomo sapiens (human)
perinuclear endoplasmic reticulumCalpain-2 catalytic subunitHomo sapiens (human)
calpain complexCalpain-2 catalytic subunitHomo sapiens (human)
chromatinCalpain-2 catalytic subunitHomo sapiens (human)
cytoplasmCalpain-2 catalytic subunitHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 4Homo sapiens (human)
rough endoplasmic reticulumCarbonic anhydrase 4Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentCarbonic anhydrase 4Homo sapiens (human)
Golgi apparatusCarbonic anhydrase 4Homo sapiens (human)
trans-Golgi networkCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
external side of plasma membraneCarbonic anhydrase 4Homo sapiens (human)
cell surfaceCarbonic anhydrase 4Homo sapiens (human)
membraneCarbonic anhydrase 4Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 4Homo sapiens (human)
transport vesicle membraneCarbonic anhydrase 4Homo sapiens (human)
secretory granule membraneCarbonic anhydrase 4Homo sapiens (human)
brush border membraneCarbonic anhydrase 4Homo sapiens (human)
perinuclear region of cytoplasmCarbonic anhydrase 4Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
extracellular regionCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
cytosolCarbonic anhydrase 6Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomal matrixBifunctional epoxide hydrolase 2Homo sapiens (human)
cytosolBifunctional epoxide hydrolase 2Homo sapiens (human)
extracellular exosomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
cytosolCarbonic anhydrase 7Homo sapiens (human)
cytoplasmCarbonic anhydrase 7Homo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
autophagosome membraneRas-related protein Rab-2ACanis lupus familiaris (dog)
acrosomal vesicleRas-related protein Rab-2ACanis lupus familiaris (dog)
endoplasmic reticulum membraneRas-related protein Rab-2ACanis lupus familiaris (dog)
endoplasmic reticulum-Golgi intermediate compartment membraneRas-related protein Rab-2ACanis lupus familiaris (dog)
melanosomeRas-related protein Rab-2ACanis lupus familiaris (dog)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
spindle poleMitogen-activated protein kinase 14Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 14Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
nuclear speckMitogen-activated protein kinase 14Homo sapiens (human)
secretory granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 14Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Canis lupus familiaris (dog)
cytosolCarbonic anhydrase 13Homo sapiens (human)
myelin sheathCarbonic anhydrase 13Homo sapiens (human)
intracellular membrane-bounded organelleCarbonic anhydrase 13Homo sapiens (human)
cytoplasmCarbonic anhydrase 13Homo sapiens (human)
cytosolCarbonic anhydrase 13Homo sapiens (human)
nuclear inner membraneCyclooxygenase-2 Canis lupus familiaris (dog)
nuclear outer membraneCyclooxygenase-2 Canis lupus familiaris (dog)
cytoplasmCyclooxygenase-2 Canis lupus familiaris (dog)
endoplasmic reticulum membraneCyclooxygenase-2 Canis lupus familiaris (dog)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
side of membraneCarbonic anhydrase 4Bos taurus (cattle)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
membraneCarbonic anhydrase 14Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 14Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 14Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2256)

Assay IDTitleYearJournalArticle
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID457929Inhibition of human recombinant COX2 by enzyme immunoassay2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID1064082Inhibition of COX-1 in human whole blood assessed as thromboxane B2 production by RIA2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID1272698Ratio of IC50 for human COX2 to IC50 for ovine COX1 by prostaglandin biosynthesis assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.
AID1718965Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in IL-1beta level at 3 mg/kg, ig measured after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID302413Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1550477Antiinflammatory activity against carrageenan-induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 2 hrs post-carrageenan injection (Rvb = 36.4%)2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID683133Inhibition of ovine COX2 assessed as PGE2 production using arachidonic acid as substrate2012European journal of medicinal chemistry, Nov, Volume: 57Sulfonilamidothiopyrimidone and thiopyrimidone derivatives as selective COX-2 inhibitors: synthesis, biological evaluation, and docking studies.
AID1733229Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 40 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 3 days by plethysmometeric method 2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID612059Membrane permeabilization activity assessed as release of calcein from liposomes after 10 mins by fluorescence assay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID349607Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID238987Inhibitory activity against human carbonic anhydrase IX at 0.09 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID1140776Inhibition of human recombinant COX-2 expressed in insect cell system using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs.
AID725956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID649269Inhibition of ovine COX-1 by enzyme immuno assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.
AID753952Analgesic activity in Swiss albino mouse inflammatory pain model assessed as inhibition of acetic acid-induced writhing at 20 mg/kg, po administered 30 mins prior to acetic acid challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID611754Selectivity ratio of inhibition for sheep COX-1 to inhibition for sheep COX-2 at 20 uM2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents.
AID1244901Antihyperalgesic effect in po dosed Swiss mouse assessed as inhibition of CFA-induced paw withdrawal threshold after 2 hrs2015European journal of medicinal chemistry, Sep-18, Volume: 102Regioselectively controlled synthesis of 3(5)-(trifluoromethyl)pyrazolylbenzenesulfonamides and their effects on a pathological pain model in mice.
AID23814Plasma half-life was determined after intravenous administration of 10 mg/kg of compound in male rat1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID1141757Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors.
AID1851476Anti-hyperalgesic activity in carrageenan-induced hyperalgesia male Sprague-Dawley rat model assessed as paw edema volume at 10 mg/kg, po measured 30 mins after compound administration by plethysmometer analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID1204712Inhibition of ovine COX1 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities.
AID241083Inhibition of ovine Prostaglandin G/H synthase 12004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1517246Inhibition of human recombinant COX-2 by EIA method2019European journal of medicinal chemistry, Dec-01, Volume: 183New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.
AID629717Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID1565317Analgesic activity in Wistar albino rat assessed as reaction time at 12.5 mg/kg, ip measured after 60 mins for 15 secs by hot plate method (Rvb = 4.67 +/- 0.52 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1742038Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as change in paw volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 5 hrs by Vernier caliper method (Rvb = 19.48 +/- 0.26 milli2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1767346Antiproliferative activity against rat C6 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID349605Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID321897Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Diazen-1-ium-1,2-diolated and nitrooxyethyl nitric oxide donor ester prodrugs of anti-inflammatory (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic acids: synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID1684442Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan stimulation and measured after 3 hrs by plethysmometric method relative to control2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID1752444Inhibition of LPS induced NO production in mouse RAW264.7 cells at 0.01 uM in the presence of 500 ng/mL LPS measured after 24 hrs by Griess reagent based assay relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1436691Inhibition of COX1 (unknown origin)2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID585030Inhibition of MDR1 in Staphylococcus aureus ATCC 29213 assessed as increase in accumulation of ampicillin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID598520Inhibition of ovine COX1 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Design, synthesis, and biological evaluation of substituted hydrazone and pyrazole derivatives as selective COX-2 inhibitors: Molecular docking study.
AID414955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1565315Analgesic activity in Wistar albino rat assessed as reaction time at 25 mg/kg, ip measured after 180 mins for 15 secs by hot plate method (Rvb = 3.87 +/- 0.38 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1275910Inhibition of Vibrio cholerae beta-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1069521Selectivity ratio of IC50 for COX-1 in human whole blood to IC50 for COX-2 in human whole blood2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID641615Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells at 0.1 uM after 24 hrs by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1125532Membrane permeabilizing activity of the compound in calcein-loaded egg phosphatidylcholine liposomes assessed as release of calcein from liposomes at pH 6.8 after 10 mins by fluorescence assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
AID1193929Inhibition of human recombinant CA-12 after 15 mins by stopped-flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.
AID1439692Selectivity ratio of Ki for human membrane-associated carbonic anhydrase 4 to Ki for recombinant human tumor-associated carbonic anhydrase 92017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID1751838Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1053263Antagonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as inhibition of agonist-induced cAMP accumulation at 8 uM preincubated for 10 mins prior to agonist addition measured after 30 mins by HTRF assay relative to 2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1711785Inhibition of Ovine COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID254248Inhibition of catalytic domain of human recombinant carbonic anhydrase IX2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
AID539312Analgesic activity against carrageenan-induced thermal hyperalgesia in Sprague-Dawley rat assessed as paw withdrawal latency administered 1 to 3 hrs after carrageenan challenge2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.
AID1549681Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID312225Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 6 hrs relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1292028Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced foot paw edema measured 2 hrs post carrageenan challenge by plethysmometry2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.
AID1377474Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID510444Inhibition of sheep COX1 by spectrophotometry2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID1711787Inhibition of soya bean 15-LOX by enzyme immunoassay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID1483265Antiarthritic activity in adjuvant-induced Lewis rat model of arthritis assessed as reduction in movement disorder administered via oral gavage once daily starting from day 15 to 25 post adjuvant injection measured post last dose
AID1179977Inhibition of COX2 (unknown origin) by solid phase ELISA method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.
AID501379Inhibition of human recombinant COX2 by EIA2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
AID363807Antioxidant activity assessed as hydroxyl radical scavenging activity at 100 uM2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
AID660180Inhibition of IL-1beta-induced PGE2 production in human HCA-7 cells at 1 uM after 72 hrs by EIA2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.
AID1324214Antioxidant activity in Kunming mouse CFA-induced arthritis model assessed as malondialdehyde level in serum at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction by ELISA (Rvb = 15.5 +/- 1.1 nmol/ml)2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID600504Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID183637Anti-inflammatory activity in vivo by carrageenan paw edema assay in rat at a dose of 30 mg/kg2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
AID1576160Inhibition of human recombinant COX1 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1712994Inhibition of ovine COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 2 mins by colorimetric analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID456488Antiinflammatory activity against carrageenan-induced paw edema rat inflammatory model assessed as paw pressure at 20 mg/kg, po after 120 mins2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1551023Antiinflammatory activity against carrageenan-induced paw oedema in albino rat assessed as hind paw thickness at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs by caliper method (Rvb = 1.24 +/- 0.02 millimeter)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID281546Cell cycle arrest in human LNCaP cells by accumulation at S phase at 10 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID160432Percentage of inhibition of Prostaglandin G/H synthase 2 activity in human whole blood(HWB) at 10 uM2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1077238Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 50 mg/kg, po administered 1 hr prior to formalin challenge measured after 30 mins relative to control2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID744751Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Molecular design, synthesis and biological evaluation of cyclic imides bearing benzenesulfonamide fragment as potential COX-2 inhibitors. Part 2.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1301938Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID664977Ulcerogenic activity in fasted albino rat assessed as ulcer index at 50 mg/kg po administered qd for 3 days measured on day 42012European journal of medicinal chemistry, Jul, Volume: 53New quinazolinone-pyrimidine hybrids: synthesis, anti-inflammatory, and ulcerogenicity studies.
AID1071437Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 2 hrs relative to vehicle-treated control2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID1763098Inhibition of LPS-induced 15(S)-HETE production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
AID1711791Ulcerogenic activity in rat assessed as incidence of ulcer at 50 mg/kg, po administered once daily for 3 consecutive days and measured after 1 hr post last dose (Rvb = 0%)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID1268958Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.
AID175864In vivo activity in rat air pouch.2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID1591462Inhibition of COX1 (unknown origin)2019Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15
Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities.
AID175863In vivo activity determined using minimum of four dose points, 8-10 animals/group in rat adjuvant arthritis.2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID1420989Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX2
AID1595290Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of microsomal PGE2 synthase expression in plasma at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge measured after 2 hrs by microplate read2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID252036Percent inhibition of 4% sodium chloride-induced abdominal constriction in rat after 30 min of 50 mg/kg oral dose of the compound2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID1501859Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA2017European journal of medicinal chemistry, Oct-20, Volume: 139Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
AID512138Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of new (E)- and (Z)-1,2,3-triaryl-2-propen-1-ones as selective COX-2 inhibitors.
AID1565319Analgesic activity in Wistar albino rat assessed as reaction time at 12.5 mg/kg, ip measured after 180 mins for 15 secs by hot plate method (Rvb = 3.87 +/- 0.38 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1689633Inhibition of human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID460655Inhibition of phagocyte respiratory burst in human HL60 cells after 6 to 7 days by luminol-induced chemiluminescence2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID162652Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.
AID427124Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID1569920Inhibition of soyabean 15-LOX preincubated for 5 mins followed by susbtrate addition measured after 10 mins by colorimetric method
AID162644Inhibitory activity against prostaglandin G/H synthase 22000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID9740Tmax (time to reach maximum concentration) was after oral administration at 5 mg/kg2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID676453Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX22012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low gastric ulcerogenic activity.
AID629716Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT colorimetric assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID1063670Inhibition of ovine COX2 using arachidonic acid as substrate by chemiluminescence assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors.
AID1204106Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Sulfonamide inhibition study of the β-class carbonic anhydrase from the caries producing pathogen Streptococcus mutans.
AID369090Selectivity index, ratio of IC50 for COX1 to IC50 COX22009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives.
AID671468Selectivity ratio of IC50 for human HT-29 cells to MIC for Staphylococcus aureus ATCC 292132012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus.
AID1550481Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 4 hrs post-carrageenan injection (Rvb = 41%)2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID314261Inhibition of ovine COX1 by chemiluminescent assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1268963Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID271288Selectivity index, IC50 for ovine COX1/IC50 for ovine COX22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID369272Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID753959Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1310731Ulcerogenicity in Wistar albino rat assessed as damage in gastric mucosa at 30.9 umol/kg, po qd for 3 days measured 1 hr post last dose2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID770586Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1278409Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID312245Inhibition of ethanol-induced gastric mucosal damage in Wistar rat at 60 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID183502Antiinflammatory activity in vivo by carrageenan paw edema assay in rat at a dose of 3 mg/kg2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
AID408273Antiinflammatory activity in sc dosed Albino rat assessed as protection against carrageenan-induced paw edema measured 4 hrs after carrageenan challenge2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity.
AID626163Permeability of the compound from basolateral to apical side of transepithelial human Caco2 model assessed as secretory transport by mass balance study2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors.
AID1262267Inhibition of Chionodraco hamatus alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID603428Inhibition of ovine COX1 by enzyme immuno assay2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.
AID243850Percent inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles at 100 uM2005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
AID494637Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema after 3 hrs2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID1576183Nephrotoxicity in rat assessed as effect on distal tubule at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID301578Inhibition of human recombinant CA 3 assessed as CO2 hydration by stopped flow kinetic assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides.
AID501698Antiinflammatory activity in rat assessed as inhibition of FCA-induced hypersensitivity at 20 and 50 mg/kg, po bid for 5 days2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
AID1143090Inhibition of ovine COX1 at 5 uM2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID363515Selectivity ratio of IC50 for human COX1 to IC50 for human COX2 by whole blood assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1750299Inhibition of recombinant 6His-tagged PDE5A1 catalytic domain (unknown origin) expressed in Escherichia coli using TAMRA-cGMP or FAM-cAMP as substrate incubated for 1.5 hrs by IMAP-FP assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID1453411Inhibition of Burkholderia pseudomallei beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1727723Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 10 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID241609In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
AID1849546Binding affinity to human recombinant CA9 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
AID1689622Ulcerogenic activity in albino rat assessed as average severity of gastric lesions at 0.028 mM/kg, po measured after 4 hrs by microscopic analysis (Rvb = 0 No_unit)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID347221Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1274610Inhibition of mPGES1 (unknown origin) by enzymatic assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID346085Inhibition of arachidonic acid-induced PGF2alpha release in rat MC9 cells at 0.30 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID309449Inhibition of COX12007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID753949Inhibition of platelet COX1 in human whole blood assessed as inhibition of serum TXB2 production after 1 hr by radioimmunoassay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID258732Inhibitory activity against cloned human CA92006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.
AID282432Inhibition of COX2 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
AID641770Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat assessed as paw weight at 10 mg/kg, po administered 4 hrs post challenge measured after 30 mins (Rvb = 61.5+/-3.4 g)2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID162006Ability to inhibit Prostaglandin G/H synthase 1 by using freshly harvested mouse peritoneal macrophages2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
AID647086Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents.
AID301225Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Novel (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic ester prodrugs possessing a diazen-1-ium-1,2-diolate moiety: design, synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID623150Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID1751829Drug concentration in C57BL/6J mouse plasma at 10 mg/kg, po administered as cassette dose measured at 4 hrs by LC/MS/MS analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1336927Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID598524Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Design, synthesis, and biological evaluation of substituted hydrazone and pyrazole derivatives as selective COX-2 inhibitors: Molecular docking study.
AID1190067Selectivity index, ratio of Ki for human recombinant carbonic anhydrase 1 to Ki for Plasmodium falciparum Eta-carbonic anhydrase2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID669529Inhibition of COX2 in LPS-stimulated human whole blood assessed as residual PGE2 level at 5 uM preincubated for 15 mins prior to LPS-stimulation measured after 24 hrs by LC-MS/MS analysis relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).
AID669752Inhibition of norA overexpressed in Staphylococcus aureus SA1199B coexpressing A116E GrlA mutation potentiation of EtBr MIC at >6.25 ug/mL by checkerboard assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID1067226Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 92014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1288448Analgesic activity in ip dosed albino Swiss mouse assessed as decrease in licking or blowing time administered as single dose measured after 1 hr by hot plate test2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID346084Inhibition of arachidonic acid-induced PGF2-alpha release in rat MC9 cells at 0.0005 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID50344Inhibitory activity of compound against human carbonic anhydrase I2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1377475Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID1374326Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced edema in hind paw administered ip measured after 4 to 6 hrs relative to control2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.
AID238597Inhibitory activity against bovine carbonic anhydrase IV (bCAIV)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
AID408272Toxicity in Albino rat assessed as gastric-ulcerogenic effect at 30 uM/kg, po twice daily for 3 days2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity.
AID488209Cytotoxicity against human PC3 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID1542242Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID412001Antiinflammatory activity in po dosed Wistar rat assessed as inhibition of carrageenan-induced paw edema measured 3 hrs post carrageenan challenge2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID1464066Ulcerogenic activity in Wistar albino rat assessed as relative ulcerogenicity at 50 mg/kg, po treated for 3 successive days measured at 2 hrs post last dose relative to celecoxib2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID1064094Antihyperalgesic activity in Swiss albino mouse assessed as reduction in carrageenan-induced inflammation at 10 mg/kg, po after 120 mins relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID323719Antiinflammatory activity against carrageenan-induced foot paw edema in orally dosed rat after 3 hrs2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
AID1240214Inhibition of Nostoc commune gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1739493Inhibition of human recombinant COX2 by colorimetric analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID54536In vitro inhibitory potency against U-937 microsomal COX-11999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
AID281557Cell cycle arrest in human PC3 cells by accumulation at subG1 phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID770581Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 92013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1217717Time dependent inhibition of CYP2C9 (unknown origin) at 30 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1503674Antiinflammatory activity in albino rat assessed as protection against carrageenan-induced paw edema at 10 umol/kg, sc pretreated for 1 hr followed by carrageenan challenge measured after 4 hrs by plethysmometer (Rvb = 0%)2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1713248Inhibition of ovine COX-2 assessed as appearance of oxidized TMPD level by EIA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study.
AID161333Inhibition of human Prostaglandin G/H synthase 11999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.
AID539313Antiinflammatory effect in complete Freund's adjuvant-induced Lewis rat arthritis model assessed as reduction in paw swelling by volume displacement plethysmometry2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.
AID560389Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID620686Inhibition of human carbonic anhydrase 2-catalyzed CO2 hydration activity by stopped flow assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID629718Antiproliferative activity against human HepG2 cells after 48 hrs by MTT colorimetric assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID1576176Ulcerogenic activity in rat assessed as effect on gastric submucosa at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID281550Cell cycle arrest in human LNCaP cells by accumulation at G1 phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID660183Inhibition of IL-1beta-induced PGE2 production in human HCA-7 cells after 72 hrs by EIA2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.
AID711039Inhibition of human recombinant full length CA7 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1268105Selectivity index, ratio of IC50 for rat COX2 to IC50 for calf COX12016European journal of medicinal chemistry, Jan-27, Volume: 108Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.
AID432205Inhibition of ovine COX2 by enzyme-immuno assay2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1498930Inhibition of human COX2 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by TLC2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery.
AID743515Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID393211Inhibition of COX2 in LPS-stimulated human whole blood assessed as inhibition of PGE2 production at 10 uM by radioimmunoassay2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives.
AID340786Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX2 by whole blood assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole-3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity.
AID547625Antiinflammatory activity in Sprague-Dawley rat assessed as reduction of cotton pellet-induced dry weight of granuloma measured after 7 days2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID243786In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood at 10 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
AID1462015In-vivo inhibition of COX2 in rat at 20 mg/kg measured after 20 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1288453Selectivity index, ratio of IC50 for ovine COX-1 to ovine COX-22016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID578496Inhibition of ovine COX2 assessed as PGF2alpha level by EIA2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase.
AID612732Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 2 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID161499Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID493884Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1689635Inhibition of 5-LOX (unknown origin) using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 10 mins2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID1576182Nephrotoxicity in rat assessed as effect on proximal tubule at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1278413Inhibition of recombinant Colwellia psychrerythraea gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1443232Inhibition of ovine COX1 at 60 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID671467Antiproliferative activity against human HT-29 cells after 24 hrs by MTT assay2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus.
AID1591463Inhibition of COX2 (unknown origin)2019Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15
Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities.
AID1398041Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID393822Antiinflammatory activity against carrageenan-induced foot paw edema in po dosed rat after 3 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Synthesis of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID1595294Toxicity in carrageenan-induced albino rat paw edema model assessed as Inhibition of cytosolic PGE2 synthase expression in plasma at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge measured after 2 hrs by microplate reader based monoclonal sand2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID1711790Ulcerogenic activity in rat assessed as average number of ulcers at 50 mg/kg, po administered once daily for 3 consecutive days and measured after 1 hr post last dose (Rvb = 0)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID1190064Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID1902043Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID432547Selectivity ratio of IC50 for human COX1 to IC50 for human COX2 expressed in african green monkey COS cells2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1268104Inhibition of COX1 in calf endotheliocyte assessed as 6keto-PGF1alpha production pretreated for 20 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by radioimmuno assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.
AID1474825Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations.
AID613462Inhibition of interferon gamma induced STAT3 phosphorylation in human PANC1 cells at 25 to 50 M pretreated 2 hrs prior to interferon-gamma challenge measured after 302011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID258729Inhibitory activity against cloned human CA12006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.
AID746194Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in COX-2 expression at 10 uM2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1608177Inhibition of recombinant human COX2 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID1727724Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 1 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID404499Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 16 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID493893Inhibition of human recombinant carbonic anhydrase 13 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID648187Inhibition of human recombinant COX2 by fluorescence assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Synthesis and evaluation of fluorobenzoylated di- and tripeptides as inhibitors of cyclooxygenase-2 (COX-2).
AID1902036Cell cycle arrest in human HepG2 cells assessed as increase in cell accumulation at G1/G0 phase at 100 uM measured after 24 to 48 hrs by propidium iodide staining based FACS analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID313338Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw edema volume at 10 mg/kg, po after 2 hrs2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID1689631Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 4 hr by plethysmometer analysis relative to control (Rvb = 0 %)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID369271Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID587236Inhibition of human COX2 assessed as PGE2 formation at 33 uM by LC-MS-MS analysis2011Journal of natural products, Feb-25, Volume: 74, Issue:2
Bioactive compounds from the fern Lepisorus contortus.
AID1751852Inhibition of COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production incubated for 1 hr by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID46697In vitro potency against human Prostaglandin G/H synthase 2 in the human whole blood assay.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
AID1717038Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID1576181Nephrotoxicity in rat assessed as effect on glomeruli at 50 mg/kg surrounded by Bowmann's capsule by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID160593Inhibitory constant against prostaglandin G/H synthase 2 (COX-2)2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
AID228024Inhibitory effect on production of cyclooxygenase-2 (COX-2) prostaglandin E2 (PGE2) in human IL1-beta stimulated synovial cells2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
AID1198996Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID1503672Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID183650Inhibition of carrageenan-induced rat foot oedema following 3 mg/kg administration.2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID1858293Inhibition of COX-2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production at 10 uM pretreated for 2 hrs followed by stimulation with LPS for 24 hrs by ELISA
AID693440Antiinflammatory activity in rat assessed as reduction of carrageenan-induced oedema in right hind paw at 10 mg/kg, po after 4 hrs post carrageenan-challenge2012European journal of medicinal chemistry, Dec, Volume: 58Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
AID1053265Agonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as stimulation of cAMP accumulation at 8 uM after 30 mins by HTRF assay relative to SKF812972013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID392039Inhibition of COX1 at 1 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1751821Half life in human liver microsomes2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID577527Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID501378Inhibition of ovine COX1 by EIA2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
AID1752445Inhibition of LPS induced NO production in mouse RAW264.7 cells at 0.1 uM in the presence of 500 ng/mL LPS measured after 24 hrs by Griess reagent based assay relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID270013Inhibition of COX12006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1721659Inhibition of COX2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.
AID693436Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw pressure at 10 mg/kg, po after 45 mins post carrageenan-challenge2012European journal of medicinal chemistry, Dec, Volume: 58Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
AID734527Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID1846856Inhibition of ovine COX-2 by colorimetric inhibitor screening assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID293132Toxicity in rat assessed as ulcerogenic potential2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines as potent analgesic and anti-inflammatory agents.
AID229532Ratio of IC50 values at Cyclooxygenase-1 and Cyclooxygenase-21999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID719859Antiinflammatory activity in rat assessed as inhibition of carageenaan-induced paw edema relative to control2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Recent developments and biological activities of thiazolidinone derivatives: a review.
AID1156829Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 4 hrs relative to control2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID160565In vitro inhibitory activity against prostaglandin G/H synthase 2 using mouse peritoneal macrophage method2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID763517Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha at 30 uM preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride relative to control2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
AID1483262Antiinociceptive activity in carrageenan induced Sprague-Dawley rat model of pain assessed as reversal of paw thermal hyperalgesia administered via po 0.5 hrs prior to carrageenan challenge measured 3 hrs post challenge
AID648181Inhibition of human wild type carbonic anhydrase 2 Leu204Ser mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors.
AID330498Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX22008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID1125125Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 2 hrs relative to control2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID488205Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID1391977Analgesic activity in rat model of chronic joint pain assessed as reversal of pain by measuring weight bearing level at 30 mg/kg, po dosed twice daily for 5 days relative to untreated control2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP
AID1262263Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID293935Inhibition of mouse COX22007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
AID160399In vitro percent Inhibition of recombinant human prostaglandin G/H synthase 2 (COX-2) at a concentration of 10 uM2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1576180Hepatotoxicity in rat assessed as effect on hepatocytes in periportal area at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1125015Inhibition of ovine COX1 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Synthesis and biological evaluation of new pyrazolone-pyridazine conjugates as anti-inflammatory and analgesic agents.
AID669117Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID1483260Antiinflammatory activity in carrageenan induced Sprague-Dawley rat model of inflammation assessed as reduction in PGE2 levels in air pouch administered via po 1 hr prior to carrageenan challenge measured 3 hrs post challenge by ELISA
AID162156In vitro inhibitory activity against prostaglandin G/H synthase 1 (COX-1) from the microsomal fraction of ram seminal vesicles at 10 uM concentration2004Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
AID1357041Selectivity index, ratio of IC50 for inhibition of ovine COX1 to IC50 for human COX22018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.
AID1196116Analgesic activity in ip dosed albino Swiss mouse assessed as licking or blowing latency time measured 60 mins post dose by hot plate method2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID458549Selectivity for ovine COX2 over ovine COX12010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors.
AID1397088Inhibition of ovine COX1 assessed as reduction in PGH2 production by enzyme immunoassay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Synthesis and biological properties of aryl methyl sulfones.
AID177223Inhibition of carrageenan paw edema in rats2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID1077204Inhibition of human COX1 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA2014European journal of medicinal chemistry, Apr-09, Volume: 76Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.
AID104515Evaluated in vivo for oral dose required to produce antiinflammatory activity in the rat paw edema assay (male Wistar rat)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1164201Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1565305Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 25 mg/kg, ip measured after 1 hr by plethysmometric method (Rvb = 1.43 +/- 0.19 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID412148Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as increase in paw volume at 20 mg/kg, po measured 3 hrs after carrageenan challenge relative to control2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide.
AID1530014Cytotoxicity against human 293T cells by MTT assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
AID1501868Selectivity index, ratio of IC50 for human COX2 to IC50 for AKR1C3 (unknown origin)2017European journal of medicinal chemistry, Oct-20, Volume: 139Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
AID392037Inhibition of COX2 at 1 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1551027Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs by caliper method relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID456475Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID162308Compound was tested for the inhibition of human Prostaglandin G/H synthase 1 (COX-1) in human whole blood2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID711214Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1549673Antiproliferative activity against mouse B16F10 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1689634Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1426403Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 3 hrs relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1632807Inhibition of recombinant human COX2 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Structure-activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies.
AID261413Inhibitory activity against 4% NaCl-induced abdominal constriction in Sprague-Dawley rat after 60 min of 5 mg/kg, po2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID302411Inhibition of recombinant CYP2C9 by fluorescence inhibition assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
CYP2C9 structure-metabolism relationships: substrates, inhibitors, and metabolites.
AID1141098Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID623148Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 10 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID420791Gastrointestinal toxicity in Albino mouse assessed ulcer index at 300 mg/kg, po2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
AID261405Inhibitory activity against ovine COX22006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID1357040Inhibition of human COX2 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1454308Selectivity index, ratio of IC50 ovine COX1 to IC50 for ovine COX22017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides.
AID665184Inhibition of human recombinant COX2 by enzymatic fluorescence assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Radiosynthesis of a ¹⁸F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo.
AID1712992Analgesic activity in Swiss albino mouse administered ip and measured after 60 mins by hot plate method2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID1262266Inhibition of weddell seal alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID406720Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced paw edema after 3 hrs2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids: synthesis, nitric oxide release studies and anti-inflammatory activities.
AID1718961Antiarthritic activity in CFA-induced rheumatoid arthritis Wistar rat model assessed as increase in weight at 3 mg/kg, ig measured after 14 to 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID1426400Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 1 hr relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1274611Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID254687Inhibitory concentration against carbonic anhydrase I2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID1902049Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID243653Percentage inhibition of Prostaglandin G/H synthase 2 in murine J774 cells at 1 uM2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
AID600505Inhibition of ovine COX1 by chemiluminescent assay2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID182758In vivo inhibitory activity against carrageenan induced paw edema in Sprague-Darley rats after oral administration of the compound2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
AID1194028Inhibition of recombinant Nostoc commune gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID1142446Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID510445Inhibition of sheep COX2 by spectrophotometry2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID183006Analgesic activity at 60 min post drug administration (50 mg/kg, ip)using the 4% NaCl-induced abdominal constriction assay in rat.2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID1576168Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 8 hrs relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID647091Inhibition of bovine COX1 assessed as PGE2 formation preincubated for 10 mins by ELISA2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents.
AID190377Percent ulceration was determined in rats at a dose of 200 mg/kg (10 animals)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID1781911Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated with compound for 2 hrs followed by LPS stimulation measured after 18 hrs by gGriess reagent based assay2021Journal of natural products, 11-26, Volume: 84, Issue:11
Total Syntheses and Anti-inflammatory Activities of Syringin and Its Natural Analogues.
AID744750Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema measured after 2 hrs plethysmometric analysis2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Molecular design, synthesis and biological evaluation of cyclic imides bearing benzenesulfonamide fragment as potential COX-2 inhibitors. Part 2.
AID1226816Selectivity index, ratio of IC50 for ovine COX-1 to human recombinant COX-22015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID280835Inhibition of COX1 in human whole blood assessed as TxB2 production after 1 hr2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.
AID239794Ratio of IC50 for prostaglandin G/H synthase 1 and prostaglandin G/H synthase 22004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID587695Antiinflammatory activity against xylene-induced ear edema in Kunming mouse assessed as reduction in ear swelling thickness at 100 mg, ip administered 2 hrs post challenge measured after 30 mins2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Investigations on cytotoxicity and anti-inflammatory potency of licofelone derivatives.
AID233868Selectivity expressed as IC50 COX-1/IC50 COX-22004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1188137Inhibition of Porphyromonas gingivalis Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID484278Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 0.6% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1287517Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID161484In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 11999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID744753Inhibition of ovine COX1-mediated prostaglandin alpha production by enzyme immuno assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Molecular design, synthesis and biological evaluation of cyclic imides bearing benzenesulfonamide fragment as potential COX-2 inhibitors. Part 2.
AID711036Inhibition of human recombinant CA13 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID612060Selectivity ratio of IC50 for human COX-1 to IC50 for human COX-22011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID29698Pharmacokinetic parameter Tmax was determined in male Wistar rat after 100 mg/kg oral dose of the compound2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1694420Inhibition of Ovine COX-2 by chemiluminescent enzyme method2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID1483264Antiarthritic activity in adjuvant-induced Lewis rat model of arthritis assessed as reduction in arthritis score administered via oral gavage once daily starting from day 15 to 25 post adjuvant injection measured post last dose
AID1064096Antihyperalgesic activity in Swiss albino mouse assessed as reduction in carrageenan-induced inflammation at 10 mg/kg, po after 60 mins relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID746193Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in 5-LOX expression at 10 uM2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID24142Gastric toxicity of the compound.2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID671465Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus.
AID701000Inhibition of 12-lipoxygenase in A23187-stimulated human PMNL assessed as reduction of 12(S)-H(P)ETE formation preincubated 15 mins by RP-HPLC analysis in presence of exogenous arachidonic acid2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
AID1608176Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID238536Inhibitory activity against human carbonic anhydrase I (hCAI)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
AID639980Inhibition of COX2 assessed as inhibition of PGE2 production using arachidonic acid as substrate after 10 mins by ELISA2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Enzymatic transformation of caffeic acid with enhanced cyclooxygenase-2 inhibitory activity.
AID1336925Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1057886Inhibition of mPGES-1 in human HeLa cells using PGH2 as substrate assessed as inhibition of IL-1beta/TNFalpha-stimulated PGE2 production at 100 uM after 24 hrs by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID382813Inhibition of human recombinant COX22008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.
AID547631Gastrointestinal toxicity in albino rat assessed as ulcerogenicity at 30 uM/kg, po bid for 3 days measured after 6 hrs of last post dose2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID762999Inhibition of ovine COX2 assessed as PGF2alpha production by reduction of PGH2 with stannous chloride at 40 uM by enzyme immunoassay relative to control2013Journal of natural products, Aug-23, Volume: 76, Issue:8
Rotenoids from Boerhaavia diffusa as potential anti-inflammatory agents.
AID1435838Anti-inflammatory activity in Swiss albino mouse assessed as inhibition of xylene-induced ear edema at 30 mg/kg, ip pretreated for 1 hr followed by xylene challenge measured after 30 mins relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Development of CXCR4 modulators by virtual HTS of a novel amide-sulfamide compound library.
AID673510Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 synthesis up to 24 hrs by radioimmunoassay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID244252Selectivity for Prostaglandin G/H synthase 2 (COX-2) and Prostaglandin G/H synthase 1 (COX-1) in human whole blood as ratio of IC502005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
AID183701Evaluated in vivo for antiinflammatory activity at 30 mg/kg oral dose in the carrageenan-induced rat paw edema (male Wistar rat)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1896014Inhibition of COX2 (unknown origin)2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
AID641611Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells at 1 uM incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1336956Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at greater G2 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 0.20%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1198995Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID161687Compound was evaluated for percent inhibition of prostaglandin G/H synthase 1 in human whole blood (HWB) at a concentration of 100 um; not determined2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID1559629Inhibition of human COX22020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.
AID1437454Inhibition of recombinant human COX2 using arachidonic acid as substrate assessed as decrease in PGF2 production preincubated for 15 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
AID578495Inhibition of ovine COX1 assessed as PGF2alpha level by EIA2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase.
AID453640Inhibition of COX2 in IL1-beta induced human A549 cells assessed as reduction of 6-keto-PGF1-alpha formation up to 5 uM preincubated for 15 mins by ELISA2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.
AID711044Inhibition of human recombinant full length CA3 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1179978Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.
AID161671Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
AID460906Gastrointestinal toxicity in Wistar albino rat assessed as ulceration at 100 mg/kg/day, po administered twice daily for 3 days2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID623147Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID1426404Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 5 hrs relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID448077Inhibition of ovine COX1 by chemiluminescent enzyme assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors.
AID700999Inhibition of 15-lipoxygenase in A23187-stimulated human PMNL assessed as reduction of 15(S)-H(P)ETE formation preincubated 15 mins by RP-HPLC analysis in presence of exogenous arachidonic acid2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
AID1311608Antiproliferative activity against human 293T cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID778725Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis.
AID1403480Ulcerogenicity in Wistar rat assessed as effect on gastro-esophageal junction at 60 mg/kg, po after 6 hrs by H and E staining based light microscopic method2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID647087Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents.
AID1519096Antiinflammatory activity against albino rats assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po measured after 4 hrs relative to control
AID193930% Inhibition (antiinflammatory) on carrageenan rat paw edema, 3 hours after oral administration of 50 mg/kg compound2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID1141099Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID460899Antiinflammatory activity in Wistar albino rat acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr before formalin challenge measured after 1 hr by plethysmometer relative to control2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1550480Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 4 hrs post-carrageenan injection (Rvb = 4.88 +/-2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID1542241Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID427145Inhibition of ovine COX2 by chemiluminescence assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID580343Inhibition of COX22011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.
AID1405926Antioxidant activity assessed as hydroxyl radical scavenging activity2018European journal of medicinal chemistry, Aug-05, Volume: 156Current progress on antioxidants incorporating the pyrazole core.
AID1506622Inhibition of human COX2 by fluorescence based assay2017MedChemComm, Mar-01, Volume: 8, Issue:3
Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).
AID1551030Ulcerogenicity in albino rat assessed as ulcer index at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose (Rvb = 0 No_unit)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID510446Selectivity index, ratio of IC50 for sheep COX1 to IC50 for sheep COX22010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID1125685Inhibition of human recombinant COX-2 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID258731Inhibitory activity against CA4 isolated from bovine lung microsomes2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.
AID641780Selectivity ratio of IC50 for platelet COX1 in human whole blood to IC50 for COX2 in human whole blood2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID28216Half life of compound was determined at 1 mg/kg intravenous administration in rat; Not tested2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID1268955Ulcerogenic activity in po dosed formalin-induced rat foot paw edema model assessed as ulcer index at antiinflammatory ED502016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.
AID560393Antibacterial activity against Escherichia coli ATCC 25922 infected in mouse RAW264.7 cells at 64 ug/ml after 24 to 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID1320389Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced COX2 expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID347225Antioxidant activity assessed as hydroxyl radical scavenging activity2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID261404Inhibitory activity against ovine COX12006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID1659927Inhibition of ovine COX2 by ELISA
AID346079Inhibition of IgE-specific antigen-induced PGF2-alpha release in rat MC9 cells at 0.0005 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID1336953Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G2 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.08%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID585027Inhibition of MDR1-mediated vincristine-resistance in Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ciprofloxacin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1069516Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in number of leukocytes in pleural space at 10 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative t2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID492302Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid-induced abdominal constrictions at 100 umol/kg, po administered 40 mins before acetic acid challenge measured for 25 mins relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID1067408Inhibition of ovine COX1 at 50 uM by peroxidase activity-based colorimetric assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.
AID243090Ratio of inhibition of carbonic anhydrase IV in human to that of carbonic anhydrase IV in bovine2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
AID160246Evaluation for percent inhibition of prostaglandin G/H synthase 2 in human whole blood (HWB) at a concentration of 1 um2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID497222Toxicity in Wistar albino rat assessed as ulcerogenic activity at 300 mg/kg, po qd for 3 days2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1390011Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID674721Gastrointestinal toxicity in Wistar albino rat assessed as incidence of stomach ulceration at 0.029 mmol/kg, po2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID492314Antiinflammatory activity against zymosan A-induced peritonitis in Swiss mouse assessed as inhibition of granulocyte infiltration in to peritoneal cavity at 100 mg/kg, po administered 40 mins before zymosan A challenge measured after 6 hrs relative to con2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID363520Analgesic activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure at 10 mg/kg, po after 60 mins2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID580340Inhibition of COX1 at 30 uM2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.
AID161475In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 12000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID1064080Inhibition of COX-2 in human whole blood assessed as prostaglandin E2 production by RIA2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID312241Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 120 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID160252In vitro average percent Inhibition of Prostaglandin G/H synthase 2 (COX-2) at a concentration of 1 uM in human whole blood by human whole blood assay2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1595293Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of PGE2 production in plasma at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge measured after 2 hrs by microplate reader based enzyme immu2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID1275911Inhibition of Vibrio cholerae alpha-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1565313Analgesic activity in Wistar albino rat assessed as reaction time at 25 mg/kg, ip measured after 60 mins for 15 secs by hot plate method (Rvb = 4.67 +/- 0.52 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID501380Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
AID1718969Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in spleen index at 3 mg/kg, ig measured after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID241382In vitro inhibition of ovine prostaglandin G/H synthase 12004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID1285032Inhibition of recombinant human COX-2 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.
AID161848Ratio of in vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 1 to that of recombinant human Prostaglandin G/H synthase 22003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
AID161494In vitro inhibitory concentration required to block recombinant human prostaglandin G/H synthase 1 (COX-1)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID234313Selectivity of IC50 COX-2/COX-1 was determined2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1311644Inhibition of PGE2 secretion in human HeLa cells at 0.1 uM after 24 hrs by EIA monoclonal assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID459696Inhibition of Brucella suis CA1 expressed in Escherichia coli BL21(DE3) by stopped-flow CO2-hydration assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis.
AID1810793Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-22021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID711033Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3588c pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1194587Inhibition of ovine COX1 using fluorometric substrate after 15 mins2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Five new phorbol esters with cytotoxic and selective anti-inflammatory activities from Croton tiglium.
AID1565328Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency time at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 5 hrs by planter test (Rvb = 7.5 2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID408486Inhibition of recombinant Curvularia lunata trihydroxynaphthalene reductase2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Towards the first inhibitors of trihydroxynaphthalene reductase from Curvularia lunata: synthesis of artificial substrate, homology modelling and initial screening.
AID755521Inhibition of human recombinant COX2 by fluorescence assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
1,4-Diaryl-substituted triazoles as cyclooxygenase-2 inhibitors: Synthesis, biological evaluation and molecular modeling studies.
AID1750298Inhibition of recombinant full length GST-tagged PDE5A1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using TAMRA-cGMP as substrate incubated for 1.5 hrs by IMAP-FP assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID349606Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID1630905Inhibition of ovine COX1 by enzyme immunoassay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1057877Inhibition of LPS-stimulated COX2 in human whole blood assessed as reduction in PGE2 production by measuring remaining activity at 5 uM preincubated for 15 mins followed by LPS addition measured after 24 hrs by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID585016Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 3359132011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID458547Inhibition of ovine COX1 by enzyme chemiluminescent enzyme assay2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors.
AID1188777Inhibition of ovine COX1 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and molecular docking study of novel quinoxalin-2(1H)-ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity.
AID1712993Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 2 mins by colorimetric analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID162011In vitro inhibitory concentration against rat prostaglandin G/H synthase 12001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
AID578498Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX22011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase.
AID585224Inhibition of MDR1 in Staphylococcus aureus ATCC 29213 assessed as increase in accumulation of ciprofloxacin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID664978Selectivity ratio of IC50 for ovine COX2 to ovine COX12012European journal of medicinal chemistry, Jul, Volume: 53New quinazolinone-pyrimidine hybrids: synthesis, anti-inflammatory, and ulcerogenicity studies.
AID1462017In-vivo inhibition of COX2 in rat at 20 mg/kg measured after 60 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID323717Inhibition of ovine COX2 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
AID161668Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in human whole blood2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID269466Anti-inflammatory activity in orally dosed Wistar rat assessed as reduction of carrageenan-induced paw edema2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
N-acylated sulfonamide sodium salt: a prodrug of choice for the bifunctional 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamide class of COX-2 inhibitors.
AID1251003Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.
AID560391Antibacterial activity against Francisella tularensis SchuS4 infected in mouse RAW264.7 cells after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID330497Inhibition of ovine COX2 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID1751871In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant plasma exposures2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1426406Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as leucocytic infiltration in sub mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID160731In vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2)2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID344874Inhibition of ovine COX2 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
AID293131Antiinflammatory activity in rat at 50 mg/kg, po2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines as potent analgesic and anti-inflammatory agents.
AID1503673Selectivity ratio of IC50 for human COX-1 to IC50 for human COX-22017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID657494Inhibition of LPS-induced COX2-mediated PGF1 production in mouse RAW264.7 cells at 100 nM after 24 hrs by EIA2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF₁ production.
AID1064115Analgesic activity in Swiss albino mouse assessed as reduction of acetic acid-induced writhing at 10 mg/kg, po measured every 10 mins after 5 mins of administration relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID1143089Toxicity in ip dosed mouse assessed as behavioral changes and death during observation up to 72 hrs2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID408271Antiinflammatory activity against carrageenan-induced paw edema in sc dosed Albino rat assessed as inhibition of paw edema volume measured 4 hrs after carrageenan challenge2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity.
AID1143092Selectivity index, ratio of ovine COX2 to ovine COX12014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID1462016In-vivo inhibition of COX2 in rat at 20 mg/kg measured after 40 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1320385Anti-inflammatory activity in Balb/c mouse assessed as reduction in TPA-induced dense dermal leukocyte infiltration at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by hematoxylin and eosin staining based microscop2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID293938Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 50 mg/kg, po after 5 hrs2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
AID160434Inhibition of human Prostaglandin G/H synthase 22001Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.
AID675704Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.
AID293936Inhibition of ovine COX12007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
AID641619Selectivity ratio of IC50 for COX1 in mouse J774 cells to IC50 for COX2 in mouse J774 cells2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID404474Inhibition of carrageenan-induced paw edema in Sprague-Dawley rat administered 2 hrs before carrageenan challenge at 25 mg/kg, po2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1739503Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell growth at 100 microM measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1409075Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for recombinant N-terminal His6-tagged human COX-22018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives.
AID641610Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells at 0.1 uM incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID437749Inhibition of human recombinant CA2 by stopped-flow hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID1069518Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in exudate volume at 20 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID603429Inhibition of human recombinant COX2 by enzyme immuno assay2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.
AID627514Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs by plethysmometer2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Synthesis of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide as anticancer and anti-inflammatory agents.
AID1464065Ulcerogenic activity in Wistar albino rat assessed as ulcer index at 50 mg/kg, po treated for 3 successive days measured at 2 hrs post last dose2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID1142837Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-2 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1742034Inhibition of human sEH using epoxy flour 7 as substrate measured after 30 mins by cell-based fluorescence assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID497215Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured after 1 hr relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID166902Variation of intraocular pressure in sixth day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1453410Inhibition of Francisella tularensis beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID162659Inhibitory concentration against human prostaglandin G/H synthase 2 at 25 degrees.2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Estimation of binding affinities for celecoxib analogues with COX-2 via Monte Carlo-extended linear response.
AID410034Inhibition of ovine COX2 by enzyme immuno assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID579474Inhibition of human recombinant COX-2 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors.
AID1529998Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
AID570438Inhibition of COX2 in mouse LPS-stimulated RAW264.7 cells after 30 mins2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
[I]-Celecoxib Analogues as SPECT Tracers of Cyclooxygenase-2 in Inflammation.
AID346080Inhibition of IgE-specific antigen-induced PGF2-alpha release in rat MC9 cells at 0.40 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID1503678Inhibition of rat kidney microsomal COX assessed as PGE2 level using arachidonic acid as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 40 mins by radio immunoassay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID456498Analgesic activity against zymosan-induced hyperalgesia in mouse assessed maximum effect measured up to 2 hrs2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID155356Compound was evaluated for its effective dose to inhibit gastric PGE-22000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID1464060Inhibition of recombinant human COX2 using arachidonic acid as substrate by colorimetric enzyme immune assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID404496Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 4 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1069522Inhibition of COX-2 in human whole blood assessed as PGE2 level in plasma after 5 mins by enzyme immunoassay2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID1659926Inhibition of ovine COX1 by ELISA
AID1742032Inhibition of recombinant human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's reagent based enzyme immunoassay2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1374327Inhibition of ovine COX1 at 5 uM using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.
AID403704Inhibition of human COX2 expressed in sf9 cells2005Journal of natural products, Oct, Volume: 68, Issue:10
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
AID1142445Inhibition of human recombinant COX2 after 2 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1125536Ratio of EC50 for membrane permeabilization to IC50 for human recombinant COX-22014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
AID1565332Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 2 hrs by Von-frey test (Rvb =2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1126478Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Anti-inflammatory components of Euphorbia humifusa Willd.
AID512137Inhibition of ovine COX1 by chemiluminescence assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of new (E)- and (Z)-1,2,3-triaryl-2-propen-1-ones as selective COX-2 inhibitors.
AID669530Inhibition of COX2 in LPS-stimulated human whole blood assessed as residual PGF2alpha level at 5 uM preincubated for 15 mins prior to LPS-stimulation measured after 24 hrs by LC-MS/MS analysis relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).
AID363513Inhibition of COX1 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1565304Selectivity index, ratio of IC50 for inhibition of ovine COX1 to IC50 for inhibition of recombinant human COX22019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1488618Antiproliferative activity against human 293T cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID243904Percentage inhibition activity at a concentration of 10 uM against cyclooxygenase 2 with the compound dissolved in DMSO2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.
AID1143094Analgesic activity in ip dosed albino Swiss mouse after 0.5 hrs by hot plate test2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID1060942Ratio of IC50 for COX-2 positive human HT-29 cells to IC50 for COX-2 positive human HT-29 cells transfected with CD44v6shRNA2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1730822Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 40 uM measured after 24 hrs by MTT assay relative to control2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice.
AID488201Inhibition of COX1 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID161480In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID1071435Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs relative to vehicle-treated control2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID1810812Tmax in Swiss albino mouse at 5 mg/kg, ip measured upto 24 hrs by LC-MS analysis2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1060954Cytotoxicity against COX-2 positive mouse APC10.1 cells transfected with CD44v6shRNA overexpressing HAS-2 assessed as growth inhibition after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID161846In vitro average percent Inhibition of Prostaglandin G/H synthase 1 (COX-1) at a concentration of 100 uM in human whole blood by human whole blood assay; Not tested2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID161660Inhibition of human Prostaglandin G/H synthase 12002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID1751860Chemo-protective activity in C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as 18F-FDG uptake in ileum at 300 mg/kg, po incorporated into chow diet administered daily for 2 weeks and measured after 14 days by ex vivo PET imaging analy2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1268962Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID1846833Anti-inflammatory activity against carrageenan-induced paw edema in PO dosed Wistar albino rat measured after 2 hrs2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID744415Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Carbonic anhydrase inhibitors: inhibition of the β-class enzyme from the pathogenic yeast Candida glabrata with sulfonamides, sulfamates and sulfamides.
AID577530Inhibition of Brucella suis carbonic anhydrase II by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID711045Inhibition of human recombinant full length CA2 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID323718Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
AID626160Absorptive transport of the compound from apical to basolateral side of transepithelial human Caco2 model2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors.
AID1443241Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as rise in paw volume at 150 ug/kg administered 1 hr followed by carrageenan challenge measured at 180 mins by plethysmometer (Rvb = 60.1%)2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1503676Inhibition of human kidney microsomal COX assessed as PGE2 level using arachidonic acid as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 40 mins by radio immunoassay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID369088Inhibition of COX1 by enzyme immunoassay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives.
AID427125Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID48114Inhibitory activity against bovine carbonic anhydrase IV was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1751826Volume of distribution at steady state in C57BL/6J mouse at 2 mg/kg, iv measured after 0.08 to 24 hrs2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID251921Percent inhibition of analgesic activity in a rat model 4% NaCl-induced abdominal constriction assay at 60 min2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1125683Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1709976Selectivity index, ratio of IC50 for recombinant ovine COX1 expressed in human OVCAR-3 cells to IC50 for recombinant human COX22021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID620689Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 9 catalytic domain2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1125126Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID1488614Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID603504Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced foot paw edema after 3 hrs2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.
AID622474Inhibition of ovine COX1 by enzyme immuno assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors.
AID644379Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID1139263Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production at 20 uM administered 1 hr prior to LPS challenge measured after 20 hrs by EIA relative to control2014Journal of natural products, Apr-25, Volume: 77, Issue:4
Suppression of inflammatory responses by handelin, a guaianolide dimer from Chrysanthemum boreale, via downregulation of NF-κB signaling and pro-inflammatory cytokine production.
AID1576169Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 12 hrs relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1061068Inhibition of Leishmania donovani chagasi recombinant beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID1853797Inhibition of COX2 (unknown origin) at 20 nM relative to control2022European journal of medicinal chemistry, Feb-15, Volume: 230Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID404464Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells in presence of arachidonic acid2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID669744Antibacterial activity against Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation by microdilution method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID746187Cytotoxicity against mouse APC10.1 cells assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID547626Antiinflammatory activity in albino rat assessed as reduction of carrageenan-induced paw edema at 10 umol/kg, sc administered 1 hr before carrageenan challenge measured after 4 hrs by plethysmometry2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID1568917Inhibition of ovine COX-1 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method
AID184044In vivo analgesic activity of compound was determined by inflammatory hyperalgesia model at 3 mg/kg perorally in rat2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID367820Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID560401Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells at 64 ug/ml after 24 hrs by broth microdilution method in presence of 80% human serum albumin2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID196175Effect on non perforated ulcers(NPU) at the dose of 100 mg/kg.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID539226Antiinflammatory activity against carrageenan-induced inflammation in Sprague-Dawley rat air pouch model assessed as reduction in PGE2 level administered 3 hrs after carrageenan challenge2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID166745Variation of intraocular pressure in day one at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1411784Anti-inflammatory activity in mouse assessed as inhibition of xylene induced ear edema at 30 mg/kg relative to control2018MedChemComm, Feb-01, Volume: 9, Issue:2
Recent development of lipoxygenase inhibitors as anti-inflammatory agents.
AID753950Inhibition of monocyte COX2 in human whole blood assessed as inhibition of LPS-induced plasma PGE2 production after 24 hrs by radioimmunoassay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1709975Inhibition of recombinant human COX22021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID1551020Antiinflammatory activity against carrageenan-induced paw oedema in albino rat assessed as hind paw thickness at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr by caliper method (Rvb = 0.73 +/- 0.03 millimeter)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID242224Inhibitory concentration against Prostaglandin G/H synthase 2 from sheep placenta at 100 uM2005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
AID1437453Inhibition of ovine COX1 using arachidonic acid as substrate assessed as decrease in PGF2 production preincubated for 15 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
AID282433Selectivity ratio of IC50 for human COX1 to IC50 for human COX22004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
AID1650563Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1464070Ulcerogenic activity in Wistar albino rat assessed as minimum vasocapillary dilation in stomach after 48 hrs by hematoxylin and eosin staining based microscopic analysis2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID282431Inhibition of COX1 in human whole blood assessed as inhibition of calcium ionophore A-23187-stimulated platelet aggregation by measuring TXB2 production2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
AID1164054Anti-inflammatory activity in Sprague-Dawley rat model of carrageenan-induced paw edema assessed as inhibition of paw edema volume at 150 umol/kg, po dosed 1 hr before carrageenan challenge and measured 3 hrs post carrageenan challenge2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID763000Inhibition of ovine COX1 assessed as PGF2alpha production by reduction of PGH2 with stannous chloride at 40 uM by enzyme immunoassay relative to control2013Journal of natural products, Aug-23, Volume: 76, Issue:8
Rotenoids from Boerhaavia diffusa as potential anti-inflammatory agents.
AID1550482Ulcerogenicity in albino rat assessed as gastric lesions at 10 mg/kg, po administered as single dose after 18 hrs of starvation challenge and measured after 4 hrs2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID471115Selectivity ratio of IC50 for COX1 to IC50 for COX2 in human whole blood2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID512136Inhibition of ovine COX2 by chemiluminescence assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of new (E)- and (Z)-1,2,3-triaryl-2-propen-1-ones as selective COX-2 inhibitors.
AID1751854Protein binding in human plasma assessed as unbound fraction2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1519091Selectivity index, ratio of IC50 for inhibition of human COX1 to IC50 for inhibition of human COX2
AID302417Inhibition of COX2 in LPS-induced monocyte assessed as PGE2 production in human whole blood2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1409073Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives.
AID411998Analgesic activity in Swiss mouse assessed as inhibition of acetic acid-induced abdominal constriction at 100 umol/kg, po administered 1 hr before acetic acid challenge2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID1752426Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 10 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1592992Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method2019European journal of medicinal chemistry, Apr-01, Volume: 167Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.
AID160248Evaluation for percent inhibition of recombinant prostaglandin G/H synthase 2 in human whole blood (HWB) at a concentration of 1 um2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID755520Inhibition of ovine COX1 by fluorescence assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
1,4-Diaryl-substituted triazoles as cyclooxygenase-2 inhibitors: Synthesis, biological evaluation and molecular modeling studies.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1077241Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1565311Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw volume at 12.5 mg/kg, ip measured after 3 hrs by plethysmometric method (Rvb = 1.75 +/- 0.33 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID753953Analgesic activity in Swiss albino mouse inflammatory pain model assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, po administered 30 mins prior to acetic acid challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1292029Analgesic activity in ip dosed albino Swiss mouse assessed as reduction in licking and blowing response at 58 deg C measured after 60 mins by hot plate test2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.
AID241308Inhibition of human cyclooxygenase-2 expressed in COS cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
AID1177989Inhibition of human recombinant COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay2014European journal of medicinal chemistry, Apr-22, Volume: 77Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.
AID1742033Selectivity index, ratio of IC50 for recombinant human COX1 to recombinant human COX22020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID281551Cell cycle arrest in human LNCaP cells by accumulation at S phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1240215Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID1717089Antiinflammatory activity in PGE2-induced paw edema in Balb/c mouse assessed as inhibition of paw edema at 50 mg/kg, ip administered 1 hr prior to PGE2 challenge and measured up to 5 hrs relative to control2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID733824Antinociceptive activity in po dosed Swiss albino mouse assessed as reduction in number of acetic acid-induced writhing counted 5 mins after acetic acid challenge counted for 10 mins2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID674724Gastrointestinal toxicity in Wistar albino rat assessed as incidence of stomach ulceration at 0.029 mmol/kg, po followed by another two compound doses in second and third days measured on fourth day post dose by acute ulcerogenicity study2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID733812Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 3 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 120 mins (Rvb = 31.4 +/- 3.7 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID234761Ratio of inhibitory activity against COX-1 and COX-22000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.
AID570436Inhibition of ovine purified COX1 after 20 mins2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
[I]-Celecoxib Analogues as SPECT Tracers of Cyclooxygenase-2 in Inflammation.
AID1357039Inhibition of ovine COX1 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.
AID560392Antibacterial activity against Salmonella enterica serovar Typhimurium ATCC 14028 infected in mouse RAW264.7 cells at 64 ug/ml after 24 to 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID724441Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.
AID579475Selectivity index ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors.
AID162646Inhibition of Prostaglandin G/H synthase 2 in human whole blood1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.
AID1334716Inhibition of ovine COX-1 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay
AID1060962Inhibition of COX-2 (unknown origin) by ELISA2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID289280Selectivity for ovine COX1 over human recombinant COX22007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1542243Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of ovine COX-22019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID1684451Selectivity index, ratio of IC50 for COX-1 (unknown origin) to IC50 for COX-2 (unknown origin)2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID193929% Inhibition (Analgesic) in rat 4% NaCl induced abdominal contriction assay, 60 min after intraperitoneal administration of 50 mg/kg of compound2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID234963Selectivity towards COX-2 versus COX-12001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
AID160599In vitro inhibitory concentration against rat Prostaglandin G/H synthase 22001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
AID1253841Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-22015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties.
AID1727725Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 0.1 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID1742031Inhibition of recombinant human COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's reagent based enzyme immunoassay2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID626162Secretory transport of the compound through transepithelial human Caco2 model2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors.
AID620687Inhibition of human carbonic anhydrase 9-catalyzed CO2 hydration activity by stopped flow assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1390010Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID162482In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 22000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID393214Inhibition of iNOS in LPS-stimulated mouse J774 cells assessed as inhibition of nitric oxide generation at 10 uM2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID457933Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced paw edema2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID460908Antiinflammatory activity in po dosed Wistar albino rat acute inflammatory model assessed as inhibition of formalin-induced paw edema administered 1 hr before formalin challenge measured after 3 hrs by plethysmometer2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID238986Inhibitory activity against human carbonic anhydrase II at 0.01 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID585025Inhibition of MDR1-mediated methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of chloramphenicol2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1398042Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1532673In vitro anti-inflammatory activity at 100 mg/ml incubated for 15 mins followed by heating for 10 mins and cooling by albumin denaturation assay relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Anti-inflammatory activity of triazine derivatives: A systematic review.
AID281552Cell cycle arrest in human LNCaP cells by accumulation at G2M phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1565344Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Randall-Selitto test2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1783311Inhibition of human recombinant COX-2 using arachidonic acid as substrate by fluorescence assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential.
AID743512Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1125895Inhibition of COX1 (unknown origin) at 100 uM by colorimetric method2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis of thio-heterocyclic analogues from Baylis-Hillman bromides as potent cyclooxygenase-2 inhibitors.
AID1301937Inhibition of human recombinant COX2 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID162146Inhibitory activity against prostaglandin G/H synthase 1 from ram seminal vesicles2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.
AID497271Cytotoxicity against human THP1 cells assessed as reduction in cell viability2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1443236Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID693435Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw pressure at 10 mg/kg, po after 30 mins post carrageenan-challenge2012European journal of medicinal chemistry, Dec, Volume: 58Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
AID1188779Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and molecular docking study of novel quinoxalin-2(1H)-ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity.
AID1153843Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as residual activity at 10 uM preincubated for 5 mins followed by substrate addition measured after 5 mins by HPLC analysis relative to control2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1.
AID477295Octanol-water partition coefficient, log P of the compound2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
AID1154875Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID1733230Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 40 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 4 days by plethysmometeric method 2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID641778Inhibition of platelet COX1-mediated TXB2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1751319Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Synthesis, docking, machine learning and antiproliferative activity of the 6-ferrocene/heterocycle-2-aminopyrimidine and 5-ferrocene-1H-Pyrazole derivatives obtained by microwave-assisted Atwal reaction as potential anticancer agents.
AID1064089Analgesic activity in po dosed Swiss albino mouse assessed as reduction of acetic acid-induced writhing measured every 10 mins after 5 mins of administration2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID585221Inhibition of MDR1 in Staphylococcus aureus ATCC 29213 assessed as increase in accumulation of chloramphenicol by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1403471Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1060946Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of 5-LOX protein expression at 5 uM after 24 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID160265In vitro inhibition of human Prostaglandin G/H synthase 2 (rexpressed in sf9 insect cells using baculo virus) enzyme at the concentration of 1 uM2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1565318Analgesic activity in Wistar albino rat assessed as reaction time at 12.5 mg/kg, ip measured after 120 mins for 15 secs by hot plate method (Rvb = 4.32 +/- 0.52 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID47748Inhibitory activity of compound against human carbonic anhydrase II2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1143536Antinociceptive activity in mouse assessed as inhibition of acetic acid-induced writhing at 0.05 mmol/kg, po administered 30 mins prior to acetic acid challenge measured for 20 mins after acetic acid injection2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1551019Antiinflammatory activity against carrageenan-induced paw oedema in albino rat assessed as hind paw thickness at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured immediately by caliper method (Rvb = 0.24 +/- 0.24 millimeter)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID753958Selectivity index, ratio of IC50 for COX1 in mouse J774 cells to IC50 for COX2 in mouse J774 cells2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1154879Inhibition of human recombinant COX2 using arachidonic acid as substrate2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID560403Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells after 24 hrs by broth microdilution method in presence of 10% fetal bovine serum2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID585220Inhibition of MDR1 in Mycobacterium smegmatis ATCC MC2155 assessed as increase in accumulation of kanamycin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1060940Ratio of IC50 for COX-2 positive mouse APC10.1 cells overexpressing HAS-2 to IC50 for COX-2 positive mouse APC10.1 cells transfected with CD44v6shRNA overexpressing HAS-22014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID695144Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.
AID1501856Anti-osteoarthritis activity in knee osteoarthritis patient assessed as cartilage volume in medial area dosed orally for 2 consecutive years by MRI method relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Recent advances in polysaccharides for osteoarthritis therapy.
AID1551025Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 2 hrs by caliper method relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID241383In vitro inhibition of ovine prostaglandin G/H synthase 22004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID48294Inhibitory activity against human carbonic anhydrase IX was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1142444Inhibition of ovine COX1 after 2 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1141756Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID160269In vitro percent Inhibition of recombinant human prostaglandin G/H synthase 2 (COX-2) at a concentration of 1 uM2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID161987Percentage of inhibition of Prostaglandin G/H synthase 1 activity in human whole blood (HWB) at 10 uM2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID312233Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 120 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1071438Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 1 hr relative to vehicle-treated control2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID54555In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood.2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.
AID1503670Ulcerogenicity in albino rat assessed as at 30 umol/kg, po administered daily for 3 successive days in two equal doses at 0 and 12 hrs measured at 6 hrs post last dose by magnifying lens based assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1168409Anti-inflammatory activity in carrageenan-induced rat foot paw edema model assessed as reduction in paw volume at 20 mg/kg dosed 30 mins before carrageenan injection and measured 5 hrs after carrageenan challenge2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Synthesis of new 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles: a search for novel nitric oxide donor anti-inflammatory agents.
AID234556Selectivity against COX-2 over COX-12004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID312243Inhibition of ethanol-induced gastric mucosal damage in Wistar rat at 30 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID183306Anti-inflammatory activity at 5 hr post drug administration using the carrageenan-induced rat paw edema assay2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID162335In vitro inhibitory activity against canine prostaglandin G/H synthase 2.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID1164050Inhibition of ovine COX1 assessed as reduction in PGF2alpha formation incubated for 18 hrs by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID1177822Inhibition of ovine COX1 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay2014European journal of medicinal chemistry, Nov-24, Volume: 87Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents.
AID1632808Selectivity ratio of IC50 for ovine COX-1 to IC50 for recombinant human COX-22016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Structure-activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies.
AID234657Tested for COX-2 selectivity over COX-1 using freshly harvested mouse peritoneal macrophages2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
AID406722Inhibition of COX2 at 100 uM2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids: synthesis, nitric oxide release studies and anti-inflammatory activities.
AID1718974Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in cell infiltration at 3 mg/kg, ig after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID54559In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
AID1858294Inhibition of COX-2 in LPS-treated mouse J774 cells assessed as inhibition of PGE2 production using arachidonic acid as substrate at 10 uM preincubated with LPS for 24 hrs followed by incubation with compound for 2 hrs and then later treated with arachido
AID577526Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID1292030Inhibition of ovine COX1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.
AID1320390Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced p65 expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID1718967Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in IL6 level at 3 mg/kg, ig measured after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID447532Selectivity ratio of IC50 for ovine COX1 to IC50 for human COX22009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.
AID733816Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 10 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 60 mins (Rvb = 33.9 +/- 3.7 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1783312Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential.
AID404466Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1576175Ulcerogenic activity in rat assessed as effect on parietal cells at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID367822Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID363514Inhibition of COX2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID363511Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production at 1 uM after 15 mins by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID368225Inhibition of ovine COX1 by enzyme immuno assay2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Synthesis of 1-(methanesulfonyl- and aminosulfonylphenyl)acetylenes that possess a 2-(N-difluoromethyl-1,2-dihydropyridin-2-one) pharmacophore: evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID1718975Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in cartilage damage at 3 mg/kg, ig after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID1576165Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 1 hr relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1193927Inhibition of human recombinant CA-7 after 15 mins by stopped-flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.
AID1751869Selectivity ratio of IC50 for COX1 in human whole blood assessed as reduction in calcium ionophore-stimulated TXB2 production to IC50 for COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1060960Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID414961Inhibition of Mycobacterium tuberculosis H37Rv recombinant beta-carbonic anhydrase 1 expressed in Escherichia coli BL21 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID585223Inhibition of MDR1 in Mycobacterium smegmatis ATCC MC2155 assessed as increase in accumulation of chloramphenicol by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID633795Inhibition of human recombinant COX-2 assessed as PGF2alpha production by enzyme immunoassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Fragment-based design, docking, synthesis, biological evaluation and structure-activity relationships of 2-benzo/benzisothiazolimino-5-aryliden-4-thiazolidinones as cycloxygenase/lipoxygenase inhibitors.
AID1568919Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for recombinant human COX-2
AID226197Inhibitory concentration was measured against Cyclooxygenase-2 in human whole blood2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID669743Inhibition of norA-mediated EtBr efflux in Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation by fluorometry2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID479548Inhibition of ovine COX2 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Mono-, di-, and triaryl substituted tetrahydropyrans as cyclooxygenase-2 and tumor growth inhibitors. Synthesis and biological evaluation.
AID1125894Inhibition of COX2 (unknown origin) at 100 uM by colorimetric method2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis of thio-heterocyclic analogues from Baylis-Hillman bromides as potent cyclooxygenase-2 inhibitors.
AID764719Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID648561Competitive inhibition of ovine COX1 by enzyme immunoassay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.
AID162494In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 21999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID1752447Inhibition of LPS induced NO production in mouse RAW264.7 cells at 10 uM in the presence of 500 ng/mL LPS measured after 24 hrs by Griess reagent based assay relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID711032Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID580341Inhibition of COX2 at 30 uM2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.
AID1739495Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1069512Plasma concentration in Wistar rat lambda carrageenan-induced pleurisy model at 20 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs by SPE-HPLC analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID1742040Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of paw edema at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Vernier caliper method relative to control2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1357049Anti-inflammatory activity in Swiss albino mouse model of carrageenan-induced-paw edema assessed as inhibition of paw edema at 5 mg/kg, ip after 3 hrs2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.
AID648562Competitive inhibition of human recombinant COX2 by enzyme immunoassay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.
AID427122Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID620692Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 12 catalytic domain2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1143087Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced foot paw edema after 2 hrs by plethysmometer analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID1183331Inhibition of ovine COX1 using fluorometric substrate at 100 uM by fluorescent inhibitor screening assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core.
AID175862In vivo activity determined using minimum of four dose points, 5 animals/group in rat carrageenan edema.2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID623146Inhibition of sodium arachidonate-induced PGE2 production in human SUM149 cells assessed as PGE2 level per 1000 cells at 0.1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 3.15 +/- 0.19 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID644380Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID379225Inhibition of LPS-induced COX2 activity in C57BL/6J mouse peritoneal macrophages by RIA2006Journal of natural products, Nov, Volume: 69, Issue:11
Triterpene saponins from clematis mandshurica.
AID183112Inhibitory activity against carrageenan induced rat paw edema after peroral administration2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID1439691Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for recombinant human tumor-associated carbonic anhydrase 92017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID382418Inhibition of COX1 at 3 uM2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
2-Amino-5-thiazolyl motif: a novel scaffold for designing anti-inflammatory agents of diverse structures.
AID497216Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured after 2 hrs relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1426402Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX22017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1443237Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 80 uM after 24 hrs by MTT assay relative to control2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID649270Inhibition of human recombinant COX-2 by enzyme immuno assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.
AID693847Toxicity in Wistar albino rat assessed as ulcer index at 75 mg/kg/day, po administered for 4 days measured after 12 hrs fasting post-last dose2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel 3-substituted-1-aryl-5-phenyl-6-anilinopyrazolo[3,4-d]pyrimidin-4-ones: docking, synthesis and pharmacological evaluation as a potential anti-inflammatory agents.
AID1077203Inhibition of human COX2 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA2014European journal of medicinal chemistry, Apr-09, Volume: 76Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.
AID1551021Antiinflammatory activity against carrageenan-induced paw oedema in albino rat assessed as hind paw thickness at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 2 hrs by caliper method (Rvb = 0.84 +/- 0.02 millimeter)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID1752446Inhibition of LPS induced NO production in mouse RAW264.7 cells at 1 uM in the presence of 500 ng/mL LPS measured after 24 hrs by Griess reagent based assay relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1357045Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhings at 5 mg/kg, ip measured 30 mins post acetic acid challenge2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.
AID1549677Antiproliferative activity against human 293T cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID457930Selectivity ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID1439687Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID1565312Analgesic activity in Wistar albino rat assessed as reaction time at 25 mg/kg, ip measured after 30 mins for 15 secs by hot plate method (Rvb = 4.21 +/- 0.41 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1057875Inhibition of LPS-stimulated COX2 in human whole blood assessed as reduction in PGF2alpha production by measuring remaining activity at 5 uM preincubated for 15 mins followed by LPS addition measured after 24 hrs by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID1569917Inhibition of ovine COX-1 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay
AID1689624Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 1 hr by plethysmometer analysis (Rvb = 2.08 +/- 0.16 mm)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID1810797Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 5 mg/kg, ip administered 30 mins prior to acetic acid challenge and measured after 30 mins relative to control2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1742047Cardiotoxicity in albino Wistar rat assessed as change in serum PGI2 level at 100 mg/kg, po administered for 2 weeks and measured on day 15 by ELISA2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1632806Inhibition of ovine COX1 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Structure-activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies.
AID634814Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in macrophage count in bronchoalveolar lavage fluid at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by 2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID232766Selectivity index of IC50 (COX-1) to that of IC50 (COX-2) was determined2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.
AID1125016Inhibition of ovine COX2 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Synthesis and biological evaluation of new pyrazolone-pyridazine conjugates as anti-inflammatory and analgesic agents.
AID443492Selectivity ratio of IC50 for ovine COX-1 to IC50 for ovine COX-22009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
AID600506Inhibition of ovine COX2 by chemiluminescent assay2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1262448Inhibition of ovine COX-1 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID1659928Selectivity index, ratio of IC50 for ovine COX1 to IC50 for COX2 by ELISA
AID404470Inhibition of PGE2 production in carrageenan-stimulated rat air pouch model at 2 mg/kg, ip after 6 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1334718Selectivity index, ratio of IC50 for human recombinant COX-2 to IC50 for ovine COX-1
AID1576167Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 4 hrs relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID54560In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
AID492312Analgesic activity in Swiss mouse assessed as increase in latency of paw licking at 100 umol/kg, po after 150 mins measured for 60 seconds by hot plate test (Rvb = 5.1 +/- 0.4 seconds)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID1739505Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1551018Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of ovine COX-22019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID363326Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
AID54531In vitro inhibition of cyclooxygenase-1 by inhibition of TXB2 generation with 1 uM arachidonic acid in human platelets2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.
AID161337In vitro potency against human Prostaglandin G/H synthase 1 in U937 microsomes. 1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
AID353527Antiinflammatory activity in rat assessed as inhibition of carrageenan induced paw edema at 10 mg/kg after 1 hr relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
AID1391943Analgesic activity in rat model of Freund's complete adjuvant-induced acute inflammatory pain assessed as reversal of FCA-induced hypersensitivity at 10 mg/kg, po relative to untreated control2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP
AID1532167Inhibition of recombinant human COX-2 expressed in Baculovirus infected sf9 cells using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by ELISA2019European journal of medicinal chemistry, Jan-15, Volume: 162Medicinal chemistry of vicinal diaryl scaffold: A mini review.
AID184173In vivo anti-inflammatory activity by air pouch model at 1 mg/kg perorally in rat.2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID1739502Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth at 100 microM measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1367390Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced iNOS expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Two new dammarane-type triterpene saponins from Korean red ginseng and their anti-inflammatory effects.
AID28332Pharmacokinetic parameter Cmax was determined in male Wistar rat after 100 mg/kg oral dose of the compound2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID471360Antiinflammatory activity against gamma carrageenan-induced pleurisy in Wistar rat assessed as inhibition of exudate production in pleural cavity at 20 mg/kg, ip administered 30 mins before gamma carrageenan challenge measured after 4 hrs2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID1077237Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 50 mg/kg, po administered 1 hr prior to formalin challenge measured after 1 hr relative to control2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1674494Activation of COX2 in LPS-induced mouse RAW264.7 cells at 10 uM preincubated for 90 mins followed by LPS administration measured after 3 hrs by fluorimetric analysis relative to control2020Journal of natural products, 08-28, Volume: 83, Issue:8
Cacalol Acetate, a Sesquiterpene from
AID674712Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 1 hr before carrageenan challenge measured 1 hr post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID456489Antiinflammatory activity against carrageenan-induced paw edema rat inflammatory model assessed as paw volume at 20 mg/kg, po after 60 mins2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID753948Selectivity ratio of IC50 for platelet COX1 in human whole blood to IC50 for monocyte COX2 in human whole blood2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1126479Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Anti-inflammatory components of Euphorbia humifusa Willd.
AID1464063Antiinflammatory activity in po dosed Wistar albino rat assessed as inhibition of carrageenan-induced left hind paw edema pretreated for 1 hr followed by carrageenan addition measured after 2 hrs2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID1751855Protein binding in human colon assessed as unbound fraction2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID456476Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1854725Inhibition of soybean 5-LOX2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID623149Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 0.1 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID241917In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
AID1565316Analgesic activity in Wistar albino rat assessed as reaction time at 12.5 mg/kg, ip measured after 30 mins for 15 secs by hot plate method (Rvb = 4.21 +/- 0.41 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID393819Inhibition of human recombinant COX2 by enzyme immunoassay2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Synthesis of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID1061170Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID241924Inhibitory concentration against p38 alpha MAP kinase calculated by CoMFA model; FlexX score=-12.4 kcal/mol2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
The molecular basis for coxib inhibition of p38alpha MAP kinase.
AID1143538Antiinflammatory activity against carrageenan-induced hind paw Albino Wistar rat model assessed as reduction in nitric oxide level in hind paw at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge by griess reagent based microplate reader analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1565338Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 5 hrs by Von-frey test (Rvb =2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1398040Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID1474823Inhibition of COX1 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations.
AID1712995Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-22016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID585026Inhibition of MDR1-mediated Mycobacterium smegmatis MC2 155 ATCC assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of chloramphenicol2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1196112Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID1143534Antioxidant activity in carrageenan-induced hind paw Albino Wistar rat model assessed as increase in GSH level in hind paw joint at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge measured per gm of tissue by plate reader analysis (Rvb = 0.58 +2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1177990Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22014European journal of medicinal chemistry, Apr-22, Volume: 77Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.
AID1373660Inhibition of ovine COX1 assessed as reduction in Prostaglandin production by enzyme immunoassay2018Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.
AID1721660Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.
AID1168908Inhibition of human recombinant COX-2 expressed in insect cell system using arachidonic acid as substrate assessed as rate of TMPD oxidation incubated for 1 min prior to substrate addition by spectrophotometry2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
AID1569919Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-2
AID1069520Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in exudate volume at 5 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID161669Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in the sensitive U937 microsome assay2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID363519Analgesic activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure at 10 mg/kg, po after 30 mins2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1851471Anti-hyperalgesic activity in carrageenan-induced hyperalgesia male Sprague-Dawley rat model assessed as paw withdrawal threshold at 10 mg/kg, po measured 15 mins after compound administration by paw pressure test2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID280834Activity of COX2 in human heparinized blood assessed as inhibition of LPS-induced PGE2 production after 24 hrs2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.
AID674713Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 2 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID622470Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced hind paw edema measured after 3 hrs post dose2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors.
AID1727720Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 100 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID547628Inhibition of human recombinant COX2 after 45 mins2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID1057593Inhibition of ovine COX1 using arachidonic acid as substrate at 10 uM incubated 5 mins prior to substrate addition measured after 5 mins by HPLC analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
AID1198997Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID1061773Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID1140775Inhibition of rat seminal vesicle COX-1 using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs.
AID1194027Inhibition of recombinant Porphyromonas gingivalis gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID241126In vitro inhibitory concentration against ovine Cyclooxygenase-12005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
AID734526Antitumor activity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID1742036Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as change in paw volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 1 hr by Vernier caliper method (Rvb = 0.24 +/- 16.36 millim2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1667493Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of human recombinant COX-22020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.
AID634813Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in neutrophil count in bronchoalveolar lavage fluid at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by 2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID1156832Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to celecoxib2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID453626Inhibition of ovine COX1 at 5 uM2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.
AID175865In vivo activity in rat air pouch.2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID281559Cell cycle arrest in human PC3 cells by accumulation at S phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1143526Antiinflammatory activity against carrageenan-induced hind paw Albino Wistar rat model assessed as reduction in serum IL-1 beta level at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge by ELISA2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1142833Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1569918Inhibition of human COX-2 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay
AID160745Relative free energy of binding of compound to wild-type Prostaglandin G/H synthase 2; (deltaG=RT ln IC50)2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Rationale for the observed COX-2/COX-1 selectivity of celecoxib from Monte Carlo simulations.
AID641614Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells at 0.01 uM after 24 hrs by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1324217Antioxidant activity in Kunming mouse CFA-induced arthritis model assessed as total antioxidant capacity in serum at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction by ELISA (Rvb = 2.9 +/- 0.5 U/ml)2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID1061774Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID1177996Binding affinity to COX-2 (unknown origin) by ESI mass spectrometry2014European journal of medicinal chemistry, Apr-22, Volume: 77Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.
AID1902040Inhibition of human COX-2 at 5 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID711042Inhibition of human recombinant full length CA5A pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID585019Inhibition of MDR1-mediated methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ampicillin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1896930Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID1367389Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced cox-2 expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Two new dammarane-type triterpene saponins from Korean red ginseng and their anti-inflammatory effects.
AID1125128Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs relative to control2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID1684449Inhibition of COX-1 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID1896928Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID734524Antitumor activity against mouse B16F10 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID1752448Inhibition of LPS induced NO production in mouse RAW264.7 cells at 100 uM in the presence of 500 ng/mL LPS measured after 24 hrs by Griess reagent based assay relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID711212Inhibition of recombinant Vibrio cholerae carbonic anhydrase expressed in Escherichia coli (DE3) preincubated for 15 mins by stopped-flow CO2 hydrase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1436688Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 3 hrs by plethysmometer relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID497218Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured after 4 hrs relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1453413Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1750318Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by incubation with substrate for 5 mins by colorimetric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID347228Inhibition of TNF-alpha-stimulated adhesion of human MM6 cells to BAEC at 40 uM by static assay relative to control2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID177221In vivo inhibition of carrageenan-induced air pouch in rats2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID669742Inhibition of norA-mediated EtBr efflux in Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation at 50 uM by fluorometry2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID1488611Inhibition of COX2 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID1902050Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1168907Antiinflammatory activity in albino Wistar rat paw edema model assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 to 5 hrs by plethysmometry relative to vehicle-treated2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
AID1694421Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of ovine COX-22021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID711043Inhibition of human recombinant full length CA4 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID587232Inhibition of human COX2 assessed as PGE2 formation at 46 nM by LC-MS-MS analysis2011Journal of natural products, Feb-25, Volume: 74, Issue:2
Bioactive compounds from the fern Lepisorus contortus.
AID1730824Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 22 hrs by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice.
AID281560Cell cycle arrest in human PC3 cells by accumulation at G2M phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1156826Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID753954Analgesic activity in Swiss albino mouse inflammatory pain model assessed as inhibition of acetic acid-induced writhing at 5 mg/kg, po administered 30 mins prior to acetic acid challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1310726Anti-inflammatory activity against Wistar albino rat model of carrageenan-induced paw edema assessed as reduction in paw thickness at 15 mg/kg, po measured after 2 hrs relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID1595298Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of carrageenan-induced right hind paw edema at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge and measured at 3 hrs after carrageenan trea2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID1377476Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 5 hrs relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID183004Analgesic activity at 30 min post drug administration (50 mg/kg, ip)using the 4% NaCl-induced abdominal constriction assay in rat.2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID1506626Inhibition of ovine COX2 using arachidonic acid substrate by TMPD dye based colorimetry2017MedChemComm, Mar-01, Volume: 8, Issue:3
Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).
AID700996Inhibition of human recombinant COX-2 mediated formation of 12-HHT from arachidonic acid assessed as remaining activity at 10 uM after 5 mins by HPLC analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
AID353530Antiinflammatory activity in rat assessed as inhibition of carrageenan induced paw edema at 10 mg/kg after 4 hrs relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
AID658650Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced foot paw edema at 100 mg/kg, ip measured after 2 hrs2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID1739506Antiproliferative activity against human MCF-7 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID697538Plasma concentration in rat2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Predicting new indications for approved drugs using a proteochemometric method.
AID1895998Inhibition of COX1 (unknown origin)2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
AID1483263Antiarthritic activity in adjuvant-induced Lewis rat model of arthritis assessed as reduction in paw edema administered via oral gavage once daily starting from day 15 to 25 post adjuvant injection measured post last dose
AID1169135Antiinflammatory activity in orally dosed Sprague-Dawley rat model of carrageenan-induced air pouch inflammation assessed as reduction in PGE2 level by ELISA method2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
AID162177In vitro inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID312232Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 60 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1751823Half life in human hepatocytes2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID560390Antibacterial activity against Francisella tularensis LVS infected in mouse RAW264.7 cells after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID711041Inhibition of human recombinant full length CA5B pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1689629Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 3 hr by plethysmometer analysis relative to control (Rvb = 0 %)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID587694Antiinflammatory activity against xylene-induced ear edema in Kunming mouse assessed as reduction in ear swelling weight at 100 mg, ip administered 2 hrs post challenge measured after 30 mins2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Investigations on cytotoxicity and anti-inflammatory potency of licofelone derivatives.
AID182047In vivo inhibition of contralateral paw swelling after oral treatment for 28 days (1 mg/kg od) was determined by adjuvabt arthritis in rat2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID598521Inhibition of ovine COX2 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Design, synthesis, and biological evaluation of substituted hydrazone and pyrazole derivatives as selective COX-2 inhibitors: Molecular docking study.
AID25975Pharmacokinetic parameter AUC(area under curve) was determined in male Wistar rat after 100 mg/kg oral dose of the compound2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1557947Inhibition of ovine COX1 preincubated for 5 mins followed by arachidonic acid addition and measured after 2 mins by colorimetric method2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.
AID162176Inhibitory activity against prostaglandin G/H synthase 1 (COX-1)2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
AID694223Inhibition of COX-1 by chemiluminescent assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID193931% Inhibition (antiinflammatory) on carrageenan rat paw edema, 5 hours after oral administration 50 mg/kg of compound2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID1143096Analgesic activity in ip dosed albino Swiss mouse after 2 hrs by hot plate test2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID347222Inhibition of COX2 in LPS-stimulated human blood2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1262452Ulcerogenic activity in rat assessed as ulcer index at 100 mg/kg2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID155354Compound was evaluated for its effective dose to inhibit exudate PGE-22000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID585217Inhibition of MDR1 in Mycobacterium smegmatis ATCC MC2155 assessed as increase in accumulation of ampicillin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID243659Percentage inhibition of Prostaglandin G/H synthase 2 in murine J774 cells at 10 uM2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
AID1426405Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as degenrative changes with necrotic changes in gastric mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1125533Inhibition of purified ovine COX-1 by enzyme immunoassay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
AID281538Inhibition of 5LOX in human whole blood assessed as inhibition of calcium ionophore A 23187-stimulated 5HETE production by HPLC analysis2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1188170Cytotoxicity against human MDA-MB-231 cells assessed as cell viability at 100 ug/ml after 24 to 48 hrs by trypan blue exclusion assay (Rvb = 86.21 +/- 1.80%)2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Design, synthesis, in silico and in vitro studies of novel 4-methylthiazole-5-carboxylic acid derivatives as potent anti-cancer agents.
AID1684448Ulcerogenic activity in Wistar rat assessed as incidence of gastric ulceration by measuring severity index at 60 mg/kg, po measured after 17 hrs by microscopic analysis2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID746181Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HCA-7 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1565300Inhibition of ovine COX1 assessed as reduction in PGF2alpha at 10 uM incubated for 2 mins using arachidonic acid as substrate by ELISA relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1194024Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID497201Antiinflammatory activity in human THP1 cells assessed as reduction in LPS and IFN-gamma-induced MCP level after 24 hrs2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1550475Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 1 hr post-carrageenan injection (Rvb = 30.3%)2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID246823Reduced Freund's complete adjuvant (FCA)-induced arthritis in rats2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
AID493887Inhibition of human recombinant carbonic anhydrase 5a after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID254699Inhibitory concentration against carbonic anhydrase II2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID667791Inhibition of recombinant human COX2 assessed as PGE2 formation at 10 uM by enzyme immunoassay2012European journal of medicinal chemistry, Aug, Volume: 54Indole based cyclooxygenase inhibitors: synthesis, biological evaluation, docking and NMR screening.
AID432561Ratio of drug level in brain to blood in rat2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID738674Selectivity index, ratio of IC50 for COX1 in human blood to IC50 for COX2 in human blood2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and -2-alkylsulfonyl-1H-imidazole derivatives.
AID1530015Cytotoxicity against human LO2 cells by MTT assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
AID629714Antiproliferative activity against human MCF7 cells after 48 hrs by MTT colorimetric assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID746183Cytotoxicity against human HCA-7 cells assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1464061Selectivity index, ratio of IC50 for ovine COX1 to IC50 for recombinant human COX22017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID620691Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human recombinant carbonic anhydrase 9 catalytic domain2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID232913Ratio of cox-1/cox-2 was determined2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID1854724Ratio IC50 for inhibition of COX-1 (unknown origin) over IC50 for inhibition of COX-2 (unknown origin)2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID1689636Ulcerogenic activity in albino rat assessed as average number of gastric ulcers at 0.028 mM/kg, po measured after 4 hrs by microscopic analysis (Rvb = 0 No_unit)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID1742041Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of paw edema at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 5 hrs by Vernier caliper method relative to control2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID456480Inhibition of COX1 in human whole blood assessed as thromboxane B2 production by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID657495Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF₁ production.
AID484381Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 120 uM by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID717365Inhibition of ovine COX1 peroxidase activity assessed as TMPD oxidation at 20 uM by colorimetric analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones.
AID404481Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1241380Selectivity index, ratio of inhibition of human recombinant COX2 to inhibition of ovine COX12015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID427146Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1730825Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL1beta production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 22 hrs by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice.
AID54545Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes.1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
AID162656Inhibitory concentration against Prostaglandin G/H synthase 22001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID414956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1324208Antiinflammatory activity in Kunming mouse CFA-induced arthritis model assessed as COX-2 level in serum at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction by ELISA (Rvb = 85.3 +/- 0.1 ng/L)2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID1902041Inhibition of human COX-2 at 50 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1751862Antitumor activity in C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as reduction in total ileum polyp area at 300 mg/kg, po administered as suspension for 10 to 12 weeks2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID249062Inhibitory dose against carrageenan-induced rat paw edema at 3 hr after oral dose2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID1694426Antiproliferative activity against human cells MCF-7 assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID641771Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat assessed as paw weight at 10 mg/kg, po administered 4 hrs post challenge measured after 60 mins (Rvb = 61.5+/-3.4 g)2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID353528Antiinflammatory activity in rat assessed as inhibition of carrageenan induced paw edema at 10 mg/kg after 2 hrs relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
AID412002Inhibition of PGHS2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID1244906Antihyperalgesic effect in Swiss mouse assessed as inhibition of CFA-induced paw withdrawal threshold at 300 mg/kg, po after 0.5 to 6 hrs2015European journal of medicinal chemistry, Sep-18, Volume: 102Regioselectively controlled synthesis of 3(5)-(trifluoromethyl)pyrazolylbenzenesulfonamides and their effects on a pathological pain model in mice.
AID1902063Induction of apoptosis in human HepG2 cells assessed as decrease in Bcl-2 expression at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID161833In vitro percent Inhibition of recombinant human prostaglandin G/H synthase 1 (COX-1) at a concentration of 100 uM2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1143905Inhibition of human recombinant COX2 assessed as residual activity preincubated at 5 uM for 5 mins by HPLC analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase.
AID1711784Inhibition of Ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID412003Inhibition of PGHS1 in human whole blood assessed as inhibition of TXB2 production at 100 uM by radioimmunoassay2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID1311602Selectivity ratio of IC50 for human COX1 to IC50 for human COX22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID1742037Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as change in paw volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Vernier caliper method (Rvb = 17.00 +/- 0.28 milli2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID369089Inhibition of COX2 by enzyme immunoassay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives.
AID1436689Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 5 hrs by plethysmometer relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID1751827Half life in C57BL/6J mouse at 2 mg/kg, iv measured after 0.08 to 24 hrs2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID194462In vivo inhibition of Carrageenan-induced rat paw edema was determined in male Sprague-Dawley rat at a dose of 10 mg/kg2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID1461597Gastrointestinal toxicity in adjuvant-induced Wistar rat arthritis model assessed as ulcer index treated for 7 days measured on day 21 post arthritis induction2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID241489In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 22004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1238184Inhibition of recombinant human COX-2 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors.
AID1426409Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as corrugations of muscular layer in stomach at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID484274Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID312235Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 30 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID241127In vitro inhibitory concentration against ovine Cyclooxygenase-22005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
AID162341Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 2 in human blood2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID1565306Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 25 mg/kg, ip measured after 2 hrs by plethysmometric method (Rvb = 1.58 +/- 0.21 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1319330Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated for 30 mins followed by LPS stimulation for 20 to 24 hrs by LC/MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors.
AID304224Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production2007Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID312227Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema after 4 hrs2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1549676Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID241488In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 12004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1549733Antitumor activity against mouse B16F10 cells implanted in nude mouse assessed as decrease in tumor weight at 20 mg/kg, ip administered once per 2 days for 14 days by caliper method relative to control2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1164209Selectivity index, ratio of IC50 for purified ovine COX1 in presence of porcine liver esterase to IC50 for human recombinant COX2 in presence of porcine liver esterase2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1192236Inhibition of human recombinant COX2 at 10 uM by TMPD oxidation based colorimetric assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Environmentally benign synthesis, molecular properties prediction and anti-inflammatory activity of novel isoxazolo[5,4-d]isoxazol-3-yl-aryl-methanones via vinylogous Henry nitroaldol adducts as synthons.
AID560405Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells at 64 ug/ml after 24 hrs by broth microdilution method in presence of 80% fetal bovine serum2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID1902051Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID229282Ratio of IC50 of COX-1 to that of COX-2.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID1763092Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2
AID711034Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID194620Inhibition of PGE 2 production in air-pouch model in male Lewis-rat at a dose of 0.3 mg/kg2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID594415Inhibition of ovine COX2 after 5 mins by enzyme immunoassay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID726232Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID161691Compound was tested in vitro for inhibition of human recombinant Prostaglandin G/H synthase 11998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.
AID1742035Analgesic activity in albino mouse assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, po administered 1 hr prior to acetic acid challenge and measured after 5 to 15 mins relative to control2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1446227Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production at 5 uM preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins relative to control2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure.
AID1193925Inhibition of human recombinant CA-1 after 15 mins by stopped-flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.
AID1071436Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs relative to vehicle-treated control2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID1390014Inhibition of full length recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Boc-Lys-(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1532671Anti-inflammatory activity in carrageenan-induced Swiss albino rat assessed as reduction in paw edema by measuring swelling thickness at 10 ml/kg, po pretreated for 1 hr followed by carrageenan addition and measured up to 6 hrs at 1 hr interval relative t2019European journal of medicinal chemistry, Jan-15, Volume: 162Anti-inflammatory activity of triazine derivatives: A systematic review.
AID297561Metabolic stability in presence of human recombinant CYP2C9 at 1 uM after 30 mins2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
CYP2C9 structure-metabolism relationships: optimizing the metabolic stability of COX-2 inhibitors.
AID160266In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 (COX-2) at 10 uM expressed in sf-9 cells infected with baculovirus2004Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
AID1060958Cytotoxicity against COX-2 positive human HCA-7 cells assessed as growth inhibition by CellTiter-96 AQueous assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1849543Binding affinity to human recombinant CA2 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
AID304223Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production2007Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1727727Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 0.001 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID1241379Inhibition of human recombinant COX2 using arachidonic acid as substrate at 1 uM preincubated for 5 mins measured after 2 mins by colorimetric analysis2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID460902Antiinflammatory activity in Wistar albino rat acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr before formalin challenge measured after 4 hrs by plethysmometer relative to control2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID408274Antiinflammatory activity in sc dosed Albino rat assessed as protection against carrageenan-induced paw edema measured 4 hrs after carrageenan challenge relative to indomethacin2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity.
AID1437459Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 umol/kg, ip administered 1 hr post carrageenan challenge measured at 5 hrs post compound dosing relative to control
AID241084Inhibition of ovine Prostaglandin G/H synthase 22004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1306900Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID1763094Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DAF-FM based fluorescence analysis
AID1628037Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID410036Antiinflammatory activity against carrageenan-induced orally dosed rat assessed paw edema after 3 hrs2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID1576173Ulcerogenic activity in rat assessed as average severity of ulcers formed at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID166749Variation of intraocular pressure in fifth day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID669745Antibacterial activity against wild type Staphylococcus aureus SA1199 expressing norA by microdilution method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID1810813Cmax in Swiss albino mouse at 5 mg/kg, ip measured upto 24 hrs by LC-MS analysis2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1902048Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID479869Growth inhibition of human NCI60 cells after 48 hrs by sulforhodamine B assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Mono-, di-, and triaryl substituted tetrahydropyrans as cyclooxygenase-2 and tumor growth inhibitors. Synthesis and biological evaluation.
AID1324220Antioxidant activity in Kunming mouse CFA-induced arthritis model assessed as superoxide dismutase activity in serum at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction by ELISA (Rvb = 66.7 +/- 0.9 U/ml)2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID489468Inhibition of COX-2-mediated PGE2 production in LPS-induced mouse RAW 264.7 cells at 10 uM after 24 hrs by EIA2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells.
AID1503671Inhibition of human COX-1 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by thin layer chromatographic method2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1752441Analgesic activity in mouse model of acetic-acid induced writhing assessed as inhibition of writhing at 30 mg/kg, po once daily administered for 3 days prior to acetic acid injection measured after 20 mins relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID281547Cell cycle arrest in human LNCaP cells by accumulation at G2M phase at 10 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID160257In vitro average percent Inhibition of Prostaglandin G/H synthase 2 (COX-2) at a concentration of 10 uM in human whole blood by human whole blood assay2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1143527Antiinflammatory activity against carrageenan-induced hind paw Albino Wistar rat model assessed as reduction in serum TNF-alpha level at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge by ELISA2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID242132In vitro inhibitory concentration against Prostaglandin G/H synthase 1 (COX-1) in human whole blood2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
AID1143524Antiinflammatory activity in Albino Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge measured 3 hrs post-carrageenan injection by plethysmometer analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID436564Inhibition of human recombinant CA2 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID1125535Selectivity ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
AID460900Antiinflammatory activity in Wistar albino rat acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr before formalin challenge measured after 2 hrs by plethysmometer relative to control2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1501860Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA2017European journal of medicinal chemistry, Oct-20, Volume: 139Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
AID503311Antiproliferative activity against human PC3 cells at 10 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID725955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1595297Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of carrageenan-induced right hind paw edema at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge and measured at 1 hr after carrageenan treat2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID1169138Antiarthritic activity in Lewis rat model of adjuvant-induced arthritis administrated by oral gavage once daily2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
AID669749Inhibition of norA overexpressed in Staphylococcus aureus SA1199B coexpressing A116E GrlA mutation assessed as potentiation of ciprofloxacin MIC by checkerboard assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID568555Inhibition of human COX22011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Structure-based parallel medicinal chemistry approach to improve metabolic stability of benzopyran COX-2 inhibitors.
AID1576166Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 3 hrs relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1752432Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 10 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID612057Inhibition of human whole blood COX-1 assessed as production of TXB2 after 24 hrs by EIA2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID160595Inhibitory activity against prostaglandin G/H synthase 2 (COX-2)2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
AID753960Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1733227Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 40 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 1 day by plethysmometeric method r2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID594414Inhibition of ovine COX1 after 5 mins by enzyme immunoassay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID1443239Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as rise in paw volume at 150 ug/kg administered 1 hr followed by carrageenan challenge measured at 30 mins by plethysmometer (Rvb = 49.5%)2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID393818Inhibition of bovine COX1 by enzyme immunoassay2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Synthesis of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID711533Half life in rat2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1426407Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as blood vessel dilation in sub-mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1501905Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately2017Journal of natural products, 09-22, Volume: 80, Issue:9
Lipid Peroxidation and Cyclooxygenase Enzyme Inhibitory Compounds from Prangos haussknechtii.
AID746189Cytotoxicity against human HT-29 cells assessed as growth inhibition after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1368421Inhibition of ovine COX1 assessed as reduction in PGF2alpha level using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition by ELISA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.
AID261409Anti-inflammatory activity against carrageenan-induced edema in Sprague-Dawley rat paw after 3 hrs of 30 mg/kg, po2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID660182Inhibition of COX2 by fluorescence assay2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.
AID239250Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID1238185Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for recombinant human COX-22015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors.
AID1565340Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 2 hrs by Randall-Selitto test2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID161654Inhibitory activity against prostaglandin G/H synthase 12000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID1194588Inhibition of human recombinant COX2 using fluorometric substrate after 15 mins2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Five new phorbol esters with cytotoxic and selective anti-inflammatory activities from Croton tiglium.
AID1851473Anti-hyperalgesic activity in carrageenan-induced hyperalgesia male Sprague-Dawley rat model assessed as paw withdrawal threshold at 10 mg/kg, po measured 45 mins after compound administration by paw pressure test2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID193928% Inhibition (Analgesic) in rat 4% NaCl induced abdominal contriction assay, 30 min after intraperitoneal administration of 50 mg/kg of compound2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID497128Inhibition of human recombinant carbonic anhydrase 1 Phe91Asn mutant expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors.
AID1739504Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1125534Inhibition of human recombinant COX-2 by enzyme immunoassay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
AID1752440Analgesic activity in mouse model of acetic-acid induced writhing assessed as number of writhes at 30 mg/kg, po once daily administered for 3 days prior to acetic acid injection measured after 20 mins (Rvb = 29.13+/-9.36)2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1694425Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID392038Inhibition of COX2 at 10 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1694419Inhibition of Ovine COX-1 by chemiluminescent enzyme method2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID492315Antiedematogenic activity in Swiss mouse assessed as decrease of capsaicin-induced paw edema weight at 100 umol/kg, po administered 40 mins before capsaicin challenge measured after 30 mins relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID1464069Ulcerogenic activity in Wistar albino rat assessed as lesion in stomach after 48 hrs by hematoxylin and eosin staining based microscopic analysis2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID1183335Inhibition of human recombinant COX2 using fluorometric substrate at 10 mM by fluorescent inhibitor screening assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core.
AID1143088Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced foot paw edema after 3 hrs by plethysmometer analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID1143530Inhibition of COX-2 (unknown origin)2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1156833Gastric toxicity in rat assessed as ulcer index at 0.28 mmol/kg, po2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID1896933Cytotoxicity against human HUVEC cells assessed as reduction in cell viability up to 50 uM by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID763516Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
AID1488617Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID552128Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID166761Variation of intraocular pressure in seventh day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1462018In-vivo inhibition of COX2 in rat at 20 mg/kg measured after 90 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1718959Antiarthritic activity in CFA-induced rheumatoid arthritis Wistar rat model assessed as reduction in foot swelling at 3 mg/kg, ig measured after 21 to 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID432552Inhibition of COX1 in human whole blood assessed as inhibition of lipopolysaccharide-induced TxB2 production after 30 min by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1365601Selectivity index, ratio of IC50 for rat seminal vesicles COX1 to IC50 for recombinant human COX22017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Recently reported biological activities of pyrazole compounds.
AID644721Selectivity ratio of IC50 for human recombinant COX2 to IC50 for ram seminal vesicle COX12012European journal of medicinal chemistry, Mar, Volume: 49Synthesis of novel 2-mercapto benzothiazole and 1,2,3-triazole based bis-heterocycles: their anti-inflammatory and anti-nociceptive activities.
AID312249Effect on acetic acid-induced chronic gastric ulcer Wistar rat assessed as area of ulcer at 30 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID302425Antiinflammatory activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure in rat at 10 mg/kg, po after 60 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID312236Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 60 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1576171Ulcerogenic activity in rat assessed as incidence of gastric ulceration at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days relative to control2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1320384Anti-inflammatory activity in Balb/c mouse assessed as reduction in TPA-induced epidermal hyperplasia at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by hematoxylin and eosin staining based microscopic analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID1164051Inhibition of ovine COX2 assessed as reduction in PGF2alpha formation incubated for 18 hrs by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID1055838Inhibition of COX1 (unknown origin)2013European journal of medicinal chemistry, , Volume: 70Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation.
AID229164Selectivity of IC50 COX-2/COX-1 was determined; Not determined2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1320381Anti-inflammatory activity in TPA-induced Balb/c mouse ear edema model assessed as reduction in TPA-induced ear edema at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs relative to control2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID1064091Antiinflammatory activity in Swiss albino mouse assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, po relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID1143523Antiinflammatory activity in Albino Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge measured 5 hrs post-carrageenan injection by plethysmometer analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID658653Antiinflammatory activity in ip dosed rat assessed as inhibition of carrageenan-induced foot paw edema measured after 2 hrs2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID738675Inhibition of COX2 in human blood assessed as TxB2 level after 1 hr by enzyme immunoassay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and -2-alkylsulfonyl-1H-imidazole derivatives.
AID471119Antiinflammatory activity against gamma carrageenan-induced pleurisy in Wistar rat assessed as inhibition of exudate production in pleural cavity at 10 mg/kg, ip administered 30 mins before gamma carrageenan challenge measured after 4 hrs2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID711046Inhibition of human recombinant full length CA1 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID330499Inhibition of LOX5 from human PBML cells at 10 uM by enzyme immuno assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID645642Inhibition of recombinant PDK1 using RPRAATF as substrate by scintillation counting2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
New inhibitor of 3-phosphoinositide dependent protein kinase-1 identified from virtual screening.
AID592808Antiallodynic activity in Sprague-Dawley rat von Frey hair mechanically-stimulated neuropathic pain model assessed as reversal of LPS-induced decrease in paw withdrawal latency at 10 mg/kg, sc administered 60 mins before LPS challenge2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID349608Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 3 expressed in Escherichia coli BL21 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID757858Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis2013European journal of medicinal chemistry, Jul, Volume: 65Stereoselective synthesis and anti-proliferative effects on prostate cancer evaluation of 5-substituted-3,4-diphenylfuran-2-ones.
AID1125129Ulcerogenic effect in albino rat assessed as ulcer index at 0.28 mmol/kg, po2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID1251008Cytotoxicity against HEK293T cells incubated for 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.
AID50345Inhibitory activity against human carbonic anhydrase I was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID312239Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 30 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID249060Inhibitory oral dose in carrageenan induced rat paw edema assay2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1436690Antiinflammatory activity in carrageenan-induced rat paw edema model assessed as inhibition of COX-2 level in paw at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 5 hrs relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID1172864Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1398039Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID162484In vitro inhibition against human Prostaglandin G/H synthase 22003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1684444Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 20 mg/kg, po administered 30 mins prior to acetic acid treatment and measured for 20 mins2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID1420986Antiproliferative activity against human Caco2 cells by MTT assay
AID1846818Anti-inflammatory activity against carrageenan-induced paw edema in rat relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID658649Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX22012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID1143091Inhibition of ovine COX2 at 5 uM2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID669515Inhibition of mPGES-1 in IL1beta and TNFalpha-stimulated human HeLa cells assessed as PGE2 level after 24 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).
AID497221Antiinflammatory activity in po dosed Wistar albino rat assessed as inhibition of formalin-induced paw edema after 3 hrs relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID493895Inhibition of mouse recombinant carbonic anhydrase 15 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1262450Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID560397Cytotoxicity against mouse RAW264.7 cells after 8 hrs by MTT assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID697539Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTS assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Predicting new indications for approved drugs using a proteochemometric method.
AID1287518Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID254247Inhibition of cloned human carbonic anhydrase II2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
AID671488Antibacterial activity against Staphylococcus aureus assessed as log decrease in bacterial CFU at 32 ug/ml after 24 hrs2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus.
AID1320391Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced phospho-Ser536 p65 expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID241918In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
AID160245Evaluation for percent inhibition of prostaglandin G/H synthase 2 in human whole blood (HWB) at a concentration of 10 um2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID1650564Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1168407Anti-inflammatory activity in carrageenan-induced rat foot paw edema model assessed as reduction in paw volume at 20 mg/kg dosed 30 mins before carrageenan injection and measured 1 hr after carrageenan challenge2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Synthesis of new 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles: a search for novel nitric oxide donor anti-inflammatory agents.
AID1291363Inhibition of recombinant Vibrio cholerae gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.
AID160740Compound was tested for the inhibition of human Prostaglandin G/H synthase 2 (COX-2) in human whole blood2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID406721Inhibition of COX1 at 100 uM2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids: synthesis, nitric oxide release studies and anti-inflammatory activities.
AID488203Inhibition of COX2 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID578497Inhibition of potato 5-LOX assessed as hydroperoxides production by EIA2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase.
AID1694423Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID1739492Inhibition of ovine COX1 by colorimetric analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1576174Ulcerogenic activity in rat assessed as effect on gastric mucosa at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID302416Selectivity ratio of IC50 for mouse COX1 to IC50 for mouse COX22007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID392046Anticancer activity against human PC3 cells2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID437750Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID363510Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production at 10 uM after 15 mins by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID612726Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID1902066Induction of apoptosis in human HepG2 cells assessed as increase in ratio of Bax/Bcl-2 expression at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID271284Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID160249Compound was tested in vitro for inhibition of human recombinant Prostaglandin G/H synthase 21998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.
AID224764Compound was evaluated for percent inhibition of recombinant prostaglandin G/H synthase 1 in human whole blood (HWB) at a concentration of 100 um2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID1390013Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1591464Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2019Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15
Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities.
AID413195Inhibition of human recombinant COX2 assessed as remaining activity at 5 uM relative to control2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.
AID270018Gastric toxicity in rat at 20 mg/kg, iv2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1851474Anti-hyperalgesic activity in carrageenan-induced hyperalgesia male Sprague-Dawley rat model assessed as paw withdrawal threshold at 10 mg/kg, po measured 60 mins after compound administration by paw pressure test2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID315991Inhibition of COX1 in human whole blood assessed as effect on A-23187-stimulated TxB2 production2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides.
AID162503In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 2 enzyme was determined2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.
AID241307Inhibition of human cyclooxygenase-1 expressed in COS cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
AID1902053Cytotoxicity against human LNCaP cells over expressing androgen receptor F876L mutant assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID634812Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in total cell count bronchoalveolar lavage fluid at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by Wri2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID665183Inhibition of ovine COX1 by enzymatic fluorescence assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Radiosynthesis of a ¹⁸F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo.
AID1667491Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.
AID1262453Gastrointestinal toxicity in rat assessed as ulcer incidence at 100 mg/kg2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID1565322Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency time at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 2 hrs by planter test (Rvb = 6.172019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1464059Inhibition of ovine COX1 using arachidonic acid as substrate by colorimetric enzyme immune assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID302419Selectivity ratio of IC50 for COX1 to IC50 for COX2 by human whole blood assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1474824Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations.
AID471116Inhibition of COX1 in human whole blood assessed as TXB2 production by enzyme immunoassay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID1488616Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID1810814AUC (0 to t) in Swiss albino mouse at 5 mg/kg, ip measured upto 24 hrs by LC-MS analysis2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID448078Inhibition of ovine COX2 by chemiluminescent enzyme assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors.
AID1268964Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID281558Cell cycle arrest in human PC3 cells by accumulation at G1 phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1192615Analgesic activity in Swiss albino mouse model assessed as reduction of acetic acid-induced writhes at 10 mg/kg, po administered 30 mins prior to acetic acid challenge measured after 5 mins for 10 mins relative to vehicle-treated control2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors.
AID552131Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1902035Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 level at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID497202Neuroprotective activity against LPS and IFN-gamma-stimulated neurotoxin production in human THP1 cell assessed as inhibition of THP1 cell secretion-induced toxicity to human SH-SY5Y cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID54712Inhibition of PGE-2 production in CHO cells expressing human COX-2.1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
AID1268965Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID1177984Inhibition of ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay2014European journal of medicinal chemistry, Apr-22, Volume: 77Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.
AID1434248Anti-inflammatory activity in para-xylene-induced Kunming mouse ear-swelling model assessed as inhibition of ear swelling at 5 mg/kg, ig measured after 1 hr relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Design, synthesis, biological evaluation, and molecular docking of chalcone derivatives as anti-inflammatory agents.
AID160566In vitro inhibitory concentration against prostaglandin G/H synthase 2 using freshly harvested mouse peritoneal macrophages2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.
AID1177823Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay2014European journal of medicinal chemistry, Nov-24, Volume: 87Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents.
AID161503Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay)2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
AID634816Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in inflammatory cells infiltration at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by hematoxylin and e2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID1426401Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID160264In vitro inhibition of human Prostaglandin G/H synthase 2 (expressed in sf9 insect cells using baculovirus) enzyme at a concentration of 10 M2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID312226Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 7 hrs relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1846847Anti-inflammatory activity against Carrageenan-induced paw edema in Swiss albino mouse assessed as change in paw volume at 10 mg/kg, PO measured for 3 to 6 hrs by plethysmometric analysis relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID577531Inhibition of Brucella suis carbonic anhydrase I by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID1689623Analgesic activity in albino mouse assessed as reduction in acetic acid-induced number of writhes at 0.028 mM/kg, po pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to cont2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID404507Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1142836Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-1 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1226815Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID436563Inhibition of human recombinant CA1 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID492310Analgesic activity in Swiss mouse assessed as increase in latency of paw licking at 100 umol/kg, po after 120 mins measured for 60 seconds by hot plate test (Rvb = 5.6 +/- 0.5 seconds)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID717363Selectivity ratio of ovine COX1 to ovine COX2 at 20 uM2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones.
AID456481Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 production by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1443233Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1324211Antiinflammatory activity in Kunming mouse CFA-induced arthritis model assessed as PGE2 level in serum at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction by ELISA (Rvb = 207 +/- 2.1 ng/L)2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID302418Inhibition of COX1 in human whole blood assessed as TXB2 production2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID162315Relative free energy of binding of compound to wild-type Prostaglandin G/H synthase 1;(deltaG=RT ln IC50)2001Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
Rationale for the observed COX-2/COX-1 selectivity of celecoxib from Monte Carlo simulations.
AID493890Inhibition of human recombinant carbonic anhydrase 7 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID484275Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1324223Antiinflammatory activity in Kunming mouse CFA-induced arthritis model assessed as inhibition of paw swelling at 30 mg/kg/day, po for 1 week administered on day 8 post CFA induction measured every 2 days during compound dosing2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID1061069Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID1730826Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL6 production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 22 hrs by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice.
AID1559631Antiinflammatory activity in rat model of carrageenan-induced paw edema model after 3 hrs2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.
AID1551024Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr by caliper method relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID176213Effective dose was determined in vivo in male Dawley rats by rat carrageenan-induced foot pad edema assay1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID177511In vivo inhibition of carrageenan-induced hyperalgesia in rats2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID648180Inhibition of human wild type carbonic anhydrase 2 Gln92Val mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors.
AID420790Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced paw edema at 300 umol/kg, po administered 1 hr before carrageenan challenge and measured 3 hrs after carrageenan challenge2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
AID1488610Inhibition of COX1 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID493889Inhibition of human recombinant carbonic anhydrase 6 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID585226Inhibition of MDR1 in Mycobacterium smegmatis ATCC MC2155 assessed as increase in accumulation of ciprofloxacin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1752438Antiinflammatory activity in mouse xylene induced ear edema model assessed as ear weight difference at 30 mg/kg, po once daily administered for 3 days prior to xylene stimulation and measured after 30 mins (Rvb = 13.64 =/- 2.55 mg)2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1285033Selectivity index,ratio of IC50 for ovine COX-1 to recombinant human COX-22016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.
AID177520In vivo inhibition of pyresis in rats2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID734521Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID1398038Selectivity index, ratio of IC50 for COX1 (unknown origin) to ratio of IC50 for COX2 (unknown origin)2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID510452Cytotoxicity against human HT-29 cells by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID1067406Inhibition of ovine COX2 by peroxidase activity-based colorimetric assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.
AID669746Antibacterial activity against norA-deficient Staphylococcus aureus SAK1902 by microdilution method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID281535Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1810792Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1060963Inhibition of ram seminal vesicle COX-1 assessed as conversion of arachidonic acid to PGH22014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID641612Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells at 10 uM incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1751851Protein occupancy at human recombinant COX-2 assessed as dissociation half life2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1464062Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced left hind paw edema at 50 mg/kg, po pretreated for 1 hr followed by carrageenan addition measured after 2 hrs relative to control2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
AID243778In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood at 1 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
AID479549Inhibition of ovine COX1 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Mono-, di-, and triaryl substituted tetrahydropyrans as cyclooxygenase-2 and tumor growth inhibitors. Synthesis and biological evaluation.
AID510449Cytotoxicity against human K562 cells assessed as inhibition of cell viability at 10 uM by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID1164055Anti-inflammatory activity in Sprague-Dawley rat model of carrageenan-induced paw edema assessed as inhibition of paw edema volume at 150 umol/kg, po dosed 1 hr before carrageenan challenge and measured 5 hrs post carrageenan challenge2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID1253840Inhibition of ovine COX-2 using arachidonic acid after 5 mins by colorimetric method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties.
AID733817Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 10 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 30 mins (Rvb = 34.8 +/- 3.0 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID194621Inhibition of PGE 2 production in air-pouch model in male Lewis-rat at a dose of 1 mg/kg2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID297562Inhibition of human recombinant COX1 by measuring PGE2 formation at 100 uM2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
CYP2C9 structure-metabolism relationships: optimizing the metabolic stability of COX-2 inhibitors.
AID1125124Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 1 hr relative to control2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID547627Antiinflammatory activity in albino rat assessed as reduction of carrageenan-induced paw edema at 10 umol/kg, sc administered 1 hr before carrageenan challenge measured after 4 hrs by plethysmometry relative to indomethacin2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID1550473Antiinflammatory activity against carrageenan-induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured immediately after carrageenan injection (Rvb = 3.462019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID770584Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1420982Antiproliferative activity against human MCF7 cells by MTT assay
AID314263Selectivity for ovine COX2 over ovine COX12008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1443235Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1403472Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1368423Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX22018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.
AID1689632Inhibition of human COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID1373661Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay2018Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.
AID363509Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1268137Inhibition of COX-2 (unknown origin)2016European journal of medicinal chemistry, Jan-27, Volume: 108Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.
AID1067230Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1057885Inhibition of mPGES-1 in human HeLa cells using PGH2 as substrate assessed as inhibition of IL-1beta/TNFalpha-stimulated PGE2 production at 1 to 10 uM after 24 hrs by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID258733Inhibitory activity against cloned human CA122006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.
AID622472Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors.
AID1188134Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID1241378Inhibition of ovine COX1 using arachidonic acid as substrate at 1 uM preincubated for 5 mins measured after 2 mins by colorimetric analysis2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID1168911Toxicity in rat assessed as ulceration at 60 mg/kg, po after 5 hrs2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
AID1403476Anti-inflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to control2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1060765Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay2014European journal of medicinal chemistry, Jan, Volume: 71Structure-based screening for the discovery of new carbonic anhydrase VII inhibitors.
AID1241384Toxicity in Wistar albino rat assessed as ulcer index at 20 mg/kg, po qd for 3 days measured after 6 hrs of last dose2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID1060955Cytotoxicity against COX-2 positive human HCA-7 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1319331Time at which plasma concentration remains above human whole blood IC50 level in human at 200 mg, po2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors.
AID309451Selectivity index, ratio of IC50 for COX2 to IC50 for COX12007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1713249Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-22016European journal of medicinal chemistry, Nov-10, Volume: 123Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study.
AID269462Inhibition of microsomal COX12006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
N-acylated sulfonamide sodium salt: a prodrug of choice for the bifunctional 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamide class of COX-2 inhibitors.
AID623151Inhibition of sodium arachidonate-induced PGE2 production in human SUM190 cells assessed as PGE2 level per 1000 cells at 10 uM preincubated for 2 hrs before sodium arachidonate challenge measured after 2 hrs by competitive EIA (Rvb = 6.43 +/- 1.87 pg/mL)2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells.
AID763514Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
AID363700Analgesic activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure at 10 mg/kg, po after 120 mins2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1595291Inhibition of human recombinant COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzyme2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID1783174Inhibition of human recombinant COX-1 at 10 uM using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition relative to control
AID568557Selectivity ratio of IC50 for human COX1 to IC50 for human COX22011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Structure-based parallel medicinal chemistry approach to improve metabolic stability of benzopyran COX-2 inhibitors.
AID252037Percent inhibition of 4% sodium chloride-induced abdominal constriction in rat after 60 min of 50 mg/kg oral dose of the compound2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
AID1751830Ratio of drug concentration in C57BL/6J mouse colon to plasma at 10 mg/kg, po measured after 4 hr by liquid chromatographic triple-quadrupole mass spectrometric method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1851472Anti-hyperalgesic activity in carrageenan-induced hyperalgesia male Sprague-Dawley rat model assessed as paw withdrawal threshold at 10 mg/kg, po measured 30 mins after compound administration by paw pressure test2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID1190065Inhibition of Plasmodium falciparum Eta-carbonic anhydrase pre-incubated for 15 mins before CO2 substrate addition by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID367821Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID1198999Inhibition of human recombinant COX2 by ELISA2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID312230Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 120 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1143533Antiinflammatory activity against carrageenan-induced hind paw Albino Wistar rat model assessed as reduction in nitric oxide level in hind paw at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge measured per mg of wet tissue by griess reagent ba2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1390009Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID585024Inhibition of MDR1-mediated vincristine-resistance in Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of chloramphenicol2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID281544Cell cycle arrest in human LNCaP cells by accumulation at subG1 phase at 10 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID363702Antiinflammatory activity against carrageenan-induced paw edema in rat assessed as paw volume at 10 mg/kg, po administered 4 hrs post carrageenan challenge measured after 60 mins2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1454306Inhibition of ovine COX12017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides.
AID746180Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in mouse APC10.1 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1398036Inhibition of COX1 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition and measured after 2 mins by ELISA2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID648186Inhibition of ovine COX1 by fluorescence assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Synthesis and evaluation of fluorobenzoylated di- and tripeptides as inhibitors of cyclooxygenase-2 (COX-2).
AID225286Effective dose for inhibition of edema after oral administration (95% confidence limits)2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID321896Inhibition of ovine COX2 by enzyme immunoassay2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Diazen-1-ium-1,2-diolated and nitrooxyethyl nitric oxide donor ester prodrugs of anti-inflammatory (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic acids: synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID1153845Inhibition of human recombinant COX-2 using arachidonic acid as substrate assessed as residual activity at 5 uM preincubated for 5 mins followed by substrate addition measured after 5 mins by HPLC analysis relative to control2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1.
AID1420984Antiproliferative activity against human HeLa cells by MTT assay
AID1902042Inhibition of full-length ovine COX-1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID647092Inhibition of ovine COX2 assessed as PGE2 formation preincubated for 10 mins by ELISA2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents.
AID1595296Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of carrageenan-induced right hind paw edema at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge and measured immediately after carrageenan t2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID456482Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX22010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID613463Anticancer activity against human HCT116 cells after 72 hrs by MTT assay2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).
AID1565321Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency time at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 1 hr by planter test (Rvb = 8.88 2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1241382Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced hind paw edema at 20 mg/kg, po after 3 hrs by plethysmometer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID479550Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Mono-, di-, and triaryl substituted tetrahydropyrans as cyclooxygenase-2 and tumor growth inhibitors. Synthesis and biological evaluation.
AID1060948Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-1 protein expression at 5 uM after 24 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1256042Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess assay2015Journal of natural products, Oct-23, Volume: 78, Issue:10
Anti-inflammatory Inositol Derivatives from the Whole Plant of Inula cappa.
AID130717In vivo inhibitory activity by mouse air-pouch assay at dose 2 MPK was determined.1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.
AID162651Inhibition of human Prostaglandin G/H synthase 22002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID1550484Ulcerogenicity in albino rat assessed as severity of gastric lesions at 10 mg/kg, po administered as single dose after 18 hrs of starvation challenge and measured after 4 hrs2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID269464Inhibition of human recombinant COX2 expressed in sf9 cells infected with baculovirus2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
N-acylated sulfonamide sodium salt: a prodrug of choice for the bifunctional 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamide class of COX-2 inhibitors.
AID281545Cell cycle arrest in human LNCaP cells by accumulation at G1 phase at 10 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID755519Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
1,4-Diaryl-substituted triazoles as cyclooxygenase-2 inhibitors: Synthesis, biological evaluation and molecular modeling studies.
AID1565346Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 5 hrs by Randall-Selitto test2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1684443Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan stimulation and measured after 4 hrs by plethysmometric method relative to control2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID162662Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
AID1437455Selectivity ratio of IC50 for ovine COX1 to IC50 for recombinant human COX2
AID1628038Inhibition of recombinant Plasmodium falciparum eta-carbonic anhydrase (181 to 538 residues) expressed in Escherichia coli artic express (DE3) preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID497208Inhibition of ovine COX1 at 10 uM2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID297563Inhibition of human recombinant COX2 by measuring PGE2 formation at 100 uM2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
CYP2C9 structure-metabolism relationships: optimizing the metabolic stability of COX-2 inhibitors.
AID1398037Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition and measured after 2 mins by ELISA2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID560406Antibacterial activity against Francisella tularensis SchuS4 infected in human THP1 cells at 4 ug/ml after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID585020Inhibition of MDR1-mediated Mycobacterium smegmatis MC2 155 ATCC assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ampicillin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1483261Antiinflammatory activity in carrageenan induced Sprague-Dawley rat model of inflammation assessed as reduction in paw edema administered via po 0.5 hrs prior to carrageenan challenge measured 1 to 4 hrs post challenge by plethysmometer
AID1287520Inhibition of recombinant Enterobacter sp. B13 beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID1060957Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID626161Permeability of the compound from apical to basolateral side of transepithelial human Caco2 model assessed as absorptive transport by mass balance study2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors.
AID183305Anti-inflammatory activity at 3h post drug administration using the carrageenan-induced rat paw edema assay2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID368228Antiinflammatory activity in orally dosed rat assessed as inhibition of carrageenan-induced paw edema after 3 hrs2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Synthesis of 1-(methanesulfonyl- and aminosulfonylphenyl)acetylenes that possess a 2-(N-difluoromethyl-1,2-dihydropyridin-2-one) pharmacophore: evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID160431Percentage of inhibition of Prostaglandin G/H synthase 2 activity in human whole blood(HWB) at 1 uM2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID1896927Antiproliferative activity against human NALM-6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID1711786Selectivity index, ratio of IC50 for Ovine COX-1 to IC50 for Ovine COX-22016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID162507In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID432545Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1071432Inhibition of ovine COX1 using TMPD as substrate at 20 uM incubated for 5 mins prior to substrate addition measured after 5 mins by colorimetry2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID1532672Inhibition of ovine COX2 by colorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Anti-inflammatory activity of triazine derivatives: A systematic review.
AID443491Inhibition of potato LOX-5 assessed as inhibition of hydroperoxide production after 5 mins by EIA2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
AID1439690Inhibition of recombinant human tumor-associated carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID629712Inhibition of COX2 by chemiluminescent enzyme assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID1420983Antiproliferative activity against human MDA231 cells by MTT assay
AID1320386Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced IL-1beta expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID1565334Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Von-frey test (Rvb =2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID724444Inhibition of human recombinant COX22013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.
AID1154873Inhibition of ovine COX1 using arachidonic acid as substrate at 10 uM2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID697540Binding affinity to mouse recombinant CDH11 extracellular domain 1-2 by surface plasmon resonance2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Predicting new indications for approved drugs using a proteochemometric method.
AID104510Evaluated in vivo for oral dose required to produce antiinflammatory activity in the rat paw edema assay (male Wistar rat)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID302427Antiinflammatory activity against carrageenan-induced paw edema in rat at 10 mg/kg, po2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID585028Inhibition of MDR1-mediated methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ciprofloxacin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1503677Inhibition of dog kidney microsomal COX assessed as PGE2 level using arachidonic acid as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 40 mins by radio immunoassay2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID746184Cytotoxicity against human HT-29 cells assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1750319Inhibition of ovine COX-2 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by incubation with substrate for 5 mins by colorimetric analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID243903Percentage inhibition activity at a concentration of 10 uM against cyclooxygenase 1 with the compound dissolved in DMSO2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.
AID1565301Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha at 10 uM incubated for 2 mins using arachidonic acid as substrate by ELISA relative to control2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID634817Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as increase in alveolar wall thickening at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by hematoxylin and eosin sta2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID695143Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.
AID456478Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 1 uM by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID460901Antiinflammatory activity in Wistar albino rat acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr before formalin challenge measured after 3 hrs by plethysmometer relative to control2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1462011Inhibition of COX-1 in rat peritoneal macrophages assessed as reduction in [125I]-6-Keto-PGF1alpha production using arachidonic acid as substrate pretreated for 30 mins followed by substrate addition measured after 30 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID393213Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production by radioimmunoassay2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives.
AID611753Inhibition of sheep COX-2 at 20 uM by cayman colorimetric assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents.
AID1164049Inhibition of ovine COX2 assessed as reduction in PGF2alpha formation at 10 uM incubated for 18 hrs by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID1077200Selectivity ratio of IC50 for human COX1 to IC50 for human COX22014European journal of medicinal chemistry, Apr-09, Volume: 76Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.
AID648179Inhibition of human wild type carbonic anhydrase 2 Asn67Ile mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors.
AID382419Inhibition of COX2 at 3 uM2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
2-Amino-5-thiazolyl motif: a novel scaffold for designing anti-inflammatory agents of diverse structures.
AID560398Selectivity index, ratio of IC50 for mouse RAW264.7 cells to MIC for Francisella novicida2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID488204Selectivity ratio of IC50 for COX2-mediated 12-hydroxyheptadecatrienoic acid production in human whole blood to IC50 for COX1-mediated 12-hydroxyheptadecatrienoic acid production in human whole blood2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID1206369Reversal of complete freund's adjuvant-induced thermal hypersensitivity in Sprague-Dawley rat at 30 mg/kg, po measured after 30 to 180 mins2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).
AID162003In vitro percentage inhibitory activity against prostaglandin G/H synthase 1 from freshly harvested mouse peritoneal macrophages at 10 ug/mL2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
AID1783173Inhibition of human recombinant COX-2 at 1 uM using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition
AID443490Inhibition of ovine COX-2 assessed as inhibition of transformation of AA to PGH2 by EIA2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
AID514962Selectivity index, ratio of IC50 for sheep COX1 to IC50 for COX22010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Design, synthesis, and biological evaluation of ketoprofen analogs as potent cyclooxygenase-2 inhibitors.
AID234974Selectivity as log (IC50[COX-1]/IC50[COX-2]).2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
AID1434428Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID746188Cytotoxicity against human HCA-7 cells assessed as growth inhibition after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID312228Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema after 4 hrs2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID461096Inhibition of potato tuber 5LOX by polarographic method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Pharmacophore modeling and virtual screening for designing potential 5-lipoxygenase inhibitors.
AID1420988Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA
AID1306898Antiinflammatory activity in ip dosed rat carrageenan-induced foot paw edema model measured after 2 hrs by plethysmometric analysis2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID161327Biochemical index for Prostaglandin G/H synthase 1 measured as, thromboxane 2 (TXB2) levels following blood coagulation2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.
AID588998Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MRP42010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1902044Selectivity index, ratio of IC50 for human COX-2 to IC50 for full-length ovine COX-12022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1902064Induction of apoptosis in human HepG2 cells assessed as down regulation of Bcl-xl expression at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1434429Inhibition of Burkholderia pseudomallei Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID497220Antiinflammatory activity in Wistar albino rat sub-acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured on day 8 relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID160732In vitro inhibitory activity against prostaglandin G/H synthase 2 from ovine2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1565307Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 25 mg/kg, ip measured after 3 hrs by plethysmometric method (Rvb = 1.75 +/- 0.33 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1751856Apparent permeability across apical to basolateral side in MDCK-MDR1 cells in presence of P-gp inhibitor2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID178934Effective dose required for the inhibition of adjuvant arthritis in Sprague-Darley rats2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
AID641779Inhibition of COX2-mediated PGE2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID323716Inhibition of ovine COX1 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
AID312238Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 180 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID363801Inhibition of bovine COX1 at 10 uM2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
AID443489Inhibition of ovine COX-1 assessed as inhibition of transformation of AA to PGH2 by EIA2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
AID258730Inhibitory activity against cloned human CA22006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II "selective" inhibitor celecoxib.
AID681931TP_TRANSPORTER: inhibition of E217betaG in the presence of Celecoxib at a concentration of 50uM in membrane vesicles from MRP4-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID1711792Ulcerogenic activity in rat assessed as ulcer index at 50 mg/kg, po administered once daily for 3 consecutive days and measured after 1 hr post last dose2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID1846819Inhibition of ovine COX-2 colorimetric enzyme immunoassay2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID1288446Antiinflammatory activity in ip dosed carrageenan induced Sprague-Dawley rat paw oedema model assessed as reduction of paw volume measured after 2 hrs by plethysmometer method2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID1751828Drug concentration in C57BL/6J mouse colon at 10 mg/kg, po administered as cassette dose measured at 4 hrs by LC/MS/MS analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1195369Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID1608416Inhibition of COX2 (unknown origin) by EIA2019European journal of medicinal chemistry, Oct-15, Volume: 180Role of sulphur-heterocycles in medicinal chemistry: An update.
AID1902077Down regulation of AR expression in human HepG2 cells at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1278412Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1311601Inhibition of human COX2 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID746190Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in mouse APC10.1 cells assessed as cell growth inhibition after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1067405Inhibition of ovine COX2 at 50 uM by peroxidase activity-based colorimetric assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.
AID1873515Antinociceptive activity in carrageenan-induced inflammatory pain Sprague-Dawley rat model assessed as increase in mechanical withdrawal threshold at 50 mg/kg, ip by von-frey filament assay2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Synthesis and biological evaluation of new series of benzamide derivatives containing urea moiety as sEH inhibitors.
AID1143535Antioxidant activity in carrageenan-induced hind paw Albino Wistar rat model assessed as inhibition of lipid peroxidation by measuring TBARS level in hind paw at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge by microplate reader analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1306901Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID510450Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell viability at 10 uM by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID1060956Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1550472Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX22019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID1336952Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at S phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 27.1%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1549678Inhibition of COX2 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1251005Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.
AID1217724Time dependent inhibition of CYP2D6 (unknown origin) at 30 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID734522Inhibition of COX-2 (unknown origin) by chemiluminescence assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID8128AUC (Area Under Plasma concentration-time curve) was after oral administration at 5 mg/kg2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID432203Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX22009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1733231Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 40 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 5 days by plethysmometeric method 2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID1462013Selectivity index, ratio of IC50 for COX1 in rat peritoneal macrophages to IC50 for COX2 in rat peritoneal macrophages2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1517245Inhibition of ovine COX-1 by EIA method2019European journal of medicinal chemistry, Dec-01, Volume: 183New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID161504Inhibition of human Prostaglandin G/H synthase 12001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID166906Variation of intraocular pressure in third day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1336951Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G1 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 69.5%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1767347Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
AID1810811Half life in Swiss albino mouse at 5 mg/kg, ip measured upto 24 hrs by LC-MS analysis2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID160742Inhibitory concentration against Prostaglandin G/H synthase 22001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID1443240Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as rise in paw volume at 150 ug/kg administered 1 hr followed by carrageenan challenge measured at 60 mins by plethysmometer (Rvb = 52.8%)2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1069519Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in exudate volume at 10 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID669747Antibacterial activity against Staphylococcus aureus SAK2378 overexpressing norA by microdilution method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID1630907Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID347226Antioxidant activity assessed as hydroxyl radical scavenging activity at 100 uM2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID289278Inhibition of ovine COX1 by measuring PGE22007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
AID251780Percent inhibition of anti-inflammatory activity in carrageenan induced rat paw edema at 3 hr2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1244900Antihyperalgesic effect in Swiss mouse assessed as inhibition of CFA-induced paw withdrawal threshold at 300 mg/kg, po after 2 hrs2015European journal of medicinal chemistry, Sep-18, Volume: 102Regioselectively controlled synthesis of 3(5)-(trifluoromethyl)pyrazolylbenzenesulfonamides and their effects on a pathological pain model in mice.
AID183015Analgesic activity was determined in rat using 4% sodium chloride-induced abdominal constriction assay at a duration of 30 min following a 1 mg/kg intraperitoneal dose2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID166757Variation of intraocular pressure in second day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1398043Cytotoxicity against human 293T cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.
AID1188138Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID627513Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs by plethysmometer2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Synthesis of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide as anticancer and anti-inflammatory agents.
AID1262451Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, po measured after 3hrs post carrageenan challenge2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID281549Cell cycle arrest in human LNCaP cells by accumulation at subG1 phase at 50 uM after 72 hrs by FACS flow cytometry2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID552129Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1193926Inhibition of human recombinant CA-2 after 15 mins by stopped-flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.
AID239146Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID1169137Antinociceptive activity in orally dosed Sprague-Dawley rat model of carrageenan-induced foot paw hyperalgesia assessed as paw withdrawal latency2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
AID471118Antiinflammatory activity against gamma carrageenan-induced pleurisy in Wistar rat assessed as inhibition of exudate production in pleural cavity at 5 mg/kg, ip administered 30 mins before gamma carrageenan challenge measured after 4 hrs2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID1549675Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1721658Inhibition of COX1 (unknown origin)2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.
AID1240217Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID1172863Inhibition of ovine COX22014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID644381Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID1551022Antiinflammatory activity against carrageenan-induced paw oedema in albino rat assessed as hind paw thickness at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hrs by caliper method (Rvb = 0.94 +/- 0.02 millimeter)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID1896929Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID312250Inhibition of ethanol-induced gastric mucosal damage in Wistar rat assessed as ulcer index at 30 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1551016Inhibition of ovine COX1 assessed as reduction in oxidized TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetric assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID1751831Tmax in C57BL/6J mouse at 10 mg/kg, po administered as cassette dose measured at 4 hrs by liquid chromatographic triple-quadrupole mass spectrometric method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID494635Inhibition of human COX2 by enzyme immunoassay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID1501857Anti-osteoarthritis activity in knee osteoarthritis patient assessed as cartilage volume in medial condylar area dosed orally for 2 consecutive years by MRI method relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Recent advances in polysaccharides for osteoarthritis therapy.
AID347224Ratio of IC50 for COX1 in bovine platelets to IC50 for COX2 in human blood2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1752428Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 0.1 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1196115Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema measured 2 hrs post dose by displacement plethysmometer analysis2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID1275912Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID488197Inhibition of 5-lipoxygenase in human whole blood assessed as inhibition of LTB4 production by HPLC method2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID456487Antiinflammatory activity against carrageenan-induced paw edema rat inflammatory model assessed as paw pressure at 20 mg/kg, po after 60 mins2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1368428Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.
AID1188778Inhibition of ovine COX2 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and molecular docking study of novel quinoxalin-2(1H)-ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity.
AID1426399Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1125686Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1501867Selectivity index, ratio of IC50 for ovine COX1 to IC50 for AKR1C3 (unknown origin)2017European journal of medicinal chemistry, Oct-20, Volume: 139Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
AID1154878Inhibition of ovine COX1 using arachidonic acid as substrate2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID183016Analgesic activity was determined in rat using 4% sodium chloride-induced abdominal constriction assay at a duration of 60 min following a 1 mg/kg intraperitoneal dose2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID1217729Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1287519Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID1810791Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID178667Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using therapeutic method; dose administered daily twice2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID1551028Ulcerogenicity in albino rat assessed as average severity score at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose (Rvb = 0 No_unit)2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID162017In vitro inhibition against ovine Prostaglandin G/H synthase 12003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID1751822Half life in mouse liver microsomes2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID404480Inhibition of PGF2alpha production in mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID161995Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 1 (COX-1)2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID1712991Antiinflammatory activity against Sprague-Dawley rat assessed as reduction in carragenan-induced paw edema administered ip and measured after 2 hrs by plethysmometry2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID1718973Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in synovial hyperplasia at 3 mg/kg, ig after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID1196113Inhibition of ovine COX2 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID552127Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1506618Inhibition of human recombinant COX2 by enzyme immuno assay2017MedChemComm, Mar-01, Volume: 8, Issue:3
Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).
AID493891Inhibition of human recombinant carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1373662Selectivity index, ratio of IC50 for ovine COX1 to recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells2018Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.
AID162339Biochemical index for Prostaglandin G/H synthase 2 measured as, PGE-2 levels in lipopolysaccharide (LPS)-challenged human whole blood2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.
AID1061067Inhibition of Porphyromonas gingivalis recombinant gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID1565358Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 1 hr by Randall-Selitto test 2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID592805Inhibition of human 5-lipoxygenase at 10 uM2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID1164052Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID1751872In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant ileum exposures2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID161324In vitro inhibitory activity against canine prostaglandin G/H synthase 1.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID447528Inhibition of ovine COX1 by enzyme immunoassay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.
AID1140777Selectivity index, ratio of IC50 for human recombinant COX-2 to IC50 for rat seminal vesicle COX-12014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs.
AID547629Inhibition of human platelets COX1 after 2 mins2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID1143529Inhibition of COX-1 (unknown origin)2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1238183Inhibition of ovine COX-1 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors.
AID674715Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 4 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID1718966Antiinflammatory activity against CFA-induced rheumatoid arthritis Wistar rat model assessed as decrease in TNFalpha level at 3 mg/kg, ig measured after 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID1576177Hepatotoxicity in rat assessed as effect on central veins in liver at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1154874Inhibition of human recombinant COX2 using arachidonic acid as substrate at 10 uM2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID392040Inhibition of COX22008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1199000Cytotoxicity against human 293T cells after 24 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID1217730Time dependent inhibition of CYP2B6 (unknown origin) at 30 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID733815Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 10 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 120 mins (Rvb = 31.4 +/- 3.7 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1334717Inhibition of human recombinant COX-2 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay
AID1576162Selectivity index, ratio of IC50 for human recombinant COX1 to IC50 for human recombinant COX2 using arachidonic acid as substrate2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1061169Inhibition of recombinant Methanosarcina thermophila gamma-CA CAM by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID1217713Time dependent inhibition of CYP3A4 (unknown origin) at 10 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1053259Antagonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin assessed as inhibition of agonist-induced effect at 8 uM after 15 mins by luminometric analysis relative to haloperidol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1188171Cytotoxicity against human MDA-MB-231 cells assessed as optical density after 24 hrs by MTT assay (Rvb =2.43 +/- 0.05 nm)2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Design, synthesis, in silico and in vitro studies of novel 4-methylthiazole-5-carboxylic acid derivatives as potent anti-cancer agents.
AID162001In vitro percentage inhibition against prostaglandin G/H synthase 1 using freshly harvested mouse peritoneal macrophages at 10 ug/mL concentration2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.
AID1595300Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of carrageenan-induced right hind paw edema at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge and measured at 6 hrs after carrageenan trea2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID494636Selectivity index, ratio of IC50 for sheep COX1 to IC50 for human COX22010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID579473Inhibition of ovine COX-1 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors.
AID1763096Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
AID1565309Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw volume at 12.5 mg/kg, ip measured after 1 hr by plethysmometric method (Rvb = 1.43 +/- 0.19 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1565342Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Randall-Selitto test2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID456486Antiinflammatory activity against carrageenan-induced paw edema rat inflammatory model assessed as paw pressure at 20 mg/kg, po after 30 mins2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1241381Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced hind paw edema at 20 mg/kg, po after 1 hr by plethysmometer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID1689628Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 3 hr by plethysmometer analysis (Rvb = 3.94 +/- 0.65 mm)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID47749Inhibitory activity against human carbonic anhydrase II was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1751857Equilibrium solubility of compound in in FASSIF at pH 6.52021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID160247Evaluation for percent inhibition of recombinant prostaglandin G/H synthase 2 in human whole blood (HWB) at a concentration of 10 um2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID363508Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1727719Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 1000 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID1709977Inhibition of COX1 in human OVCAR-3 cells assessed as reduction in PGE2 level incubated for 30 mins by ELISA2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID232500Selectivity ratio of COX-1/COX-22000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID1154876Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 12.5 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID177173In vivo efficacy was evaluated using a carrageenan-induced rat paw edema model as ED50.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
AID382814Inhibition of human platelet COX12008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.
AID613459Inhibition of STAT3 SH2 domain phosphorylation at Tyr705 in COX2-negative human HCT116 cells after 1 hr by Western blot analysis2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).
AID1268959Antiinflammatory activity in po dosed formalin-induced rat foot paw edema model assessed as paw thickness after 3 hrs2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.
AID1752427Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 1 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1143528Antiinflammatory activity against carrageenan-induced hind paw Albino Wistar rat model assessed as reduction in serum COX2 level at 0.05 mmol/kg, po treated 1 hr before carrageenan challenge by ELISA2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID432549Inhibition of human COX1 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1310721Inhibition of ovine COX-2 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID770582Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1397090Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX22018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Synthesis and biological properties of aryl methyl sulfones.
AID404510Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID161336In vitro potency against human Prostaglandin G/H synthase 1 (hCOX-1) in the human whole blood assay.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
AID1063669Inhibition of ovine COX1 using arachidonic acid as substrate by chemiluminescence assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors.
AID1156830Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 5 hrs relative to control2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID497129Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors.
AID1268957Inhibition of human recombinant COX2 by enzyme immuno assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.
AID1576161Inhibition of human recombinant COX2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID270014Inhibition of COX22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1851455Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate preincubated for 15 mins followed substrate addition and assessed as inhibition of PGE2 production after 30 mins by enzyme immuno-assay (EIA)2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID1374329Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by ELISA2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.
AID1464292Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX2
AID1336926Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID271283Inhibition of COX1 assessed as TBX2 production in human whole blood2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID694220Inhibition of COX-2 by chemiluminescent assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1069523Inhibition of COX-1 in human whole blood assessed as thromboxane B2 level in serum after 5 mins by enzyme immunoassay2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID312231Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 180 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID321895Inhibition of ovine COX1 by enzyme immunoassay2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Diazen-1-ium-1,2-diolated and nitrooxyethyl nitric oxide donor ester prodrugs of anti-inflammatory (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic acids: synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID1751863Antitumor activity in C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as mouse survival at 100 mg/kg, po administered daily as suspension and measured at day 82 by Kaplan-Meier method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID412000Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 100 umol/kg, po measured 3 hrs post carrageenan challenge2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID669115Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID711037Inhibition of human recombinant CA9 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1517247Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22019European journal of medicinal chemistry, Dec-01, Volume: 183New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.
AID161656Inhibitory activity against Prostaglandin G/H synthase 1 in human whole blood1999Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.
AID1397089Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Synthesis and biological properties of aryl methyl sulfones.
AID1057882Cytotoxicity against IL-1beta/TNFalpha-stimulated human HeLa cells assessed as cell viability at 100 uM after 24 hrs by WST-1 assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID746182Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT-29 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
AID1141096Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID239789Ratio of IC50 of Prostaglandin G/H synthase 1 and Prostaglandin G/H synthase 22005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
AID1288451Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID427123Inhibition of Cryptococcus neoformans recombinant Can2 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1576179Hepatotoxicity in rat assessed as effect on bile ducts at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1278410Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1565303Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1810799Antiinflammatory activity in Swiss albino mouse model of carrageenan-induced paw edema assessed as reduction in paw thickness at 5 mg/kg, administered 30 mins prior to carrageenan challenge and measured upto 360 mins relative to control2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1154877Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 25 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID1628036Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID622556Inhibition of ovine COX2 by enzyme immuno assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors.
AID1549727Inhibition of LPS-induced PGE2 production in mouse B16F10 cells at 6.25 uM incubated for 24 hrs by enzyme immunoassay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1767348Antiproliferative activity against human U-251 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
AID669748Inhibition of norA in wild type Staphylococcus aureus SA1199 expressing assessed as potentiation of ciprofloxacin MIC by checkerboard assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
AID1854722Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID494634Inhibition of sheep COX1 by enzyme immunoassay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID271285Selectivity index, IC50 for COX1/IC50 for COX2 in human whole blood2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID1156828Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to control2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID1751819Inhibition of human recombinant COX-2 assessed as reduction in peroxidase activity using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1409074Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives.
AID54538In vitro inhibitory potency against human COX-1 (HWB COX-2) by whole blood assay1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
AID1320387Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced IL-6 expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID620685Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration activity by stopped flow assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1071433Inhibition of ovine COX2 using TMPD as substrate at 20 uM incubated for 5 mins prior to substrate addition measured after 5 mins by colorimetry2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID1125684Inhibition of ovine COX-1 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID460904Antiinflammatory activity in Wistar albino rat sub-acute inflammatory model assessed as inhibition of turpentine oil-induced granuloma pouch exudate volume at 20 mg/kg, po 1 hr before turpentine oil challenge for 7 days assessed measured on day 82010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1689627Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 2 hr by plethysmometer analysis relative to control (Rvb = 0 %)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID196178Effect on perforated ulcers(PU) at the dose of 100 mg/kg.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID302424Antiinflammatory activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure in rat at 10 mg/kg, po after 120 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1854723Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.
AID497105Antiinflammatory activity in Wistar albino rat assessed as inhibition of turpentine oil-induced granuloma at 20 mg/kg, po qd for 7 days post turpentine oil challenge measured on day 82010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID162312Inhibitory concentration against Prostaglandin G/H synthase 12001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
AID1060959Cytotoxicity against COX-2 positive mouse APC10.1 cells overexpressing HAS-2 assessed as growth inhibition by CellTiter-96 AQueous assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1439688Inhibition of recombinant human membrane-associated carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID312240Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 60 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID493894Inhibition of human recombinant carbonic anhydrase 14 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1717040Selectivity index, ratio of IC50 for sheep COX1 to IC50 for recombinant human COX2 expressed in baculovirus infected Sf21 cells2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID448079Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors.
AID239145Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID641617Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells at 10 uM after 24 hrs by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1193928Inhibition of human recombinant CA-9 after 15 mins by stopped-flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.
AID1501906Inhibition of human COX2 expressed in insect cells using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately2017Journal of natural products, 09-22, Volume: 80, Issue:9
Lipid Peroxidation and Cyclooxygenase Enzyme Inhibitory Compounds from Prangos haussknechtii.
AID649271Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-22012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.
AID471363Antiinflammatory activity against gamma carrageenan-induced pleurisy in Wistar rat assessed as decrease in exudate volume in pleural cavity at 20 mg/kg, ip administered 30 mins before gamma carrageenan challenge measured after 4 hrs2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID239795Ratio of IC50 for Cyclooxygenase-1 and Cyclooxygenase-22005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
AID1763097Inhibition of LPS-induced IL-6 production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
AID1055834Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for human recombinant COX22013European journal of medicinal chemistry, , Volume: 70Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation.
AID492305Analgesic activity against formalin-induced acute pain in Swiss mouse assessed inhibition of nociception at 100 umol/kg, po administered 40 mins before formalin challenge measured for 15 to 30 mins relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID471117Inhibition of COX2 in LPS-stimulated human whole blood assessed as PGE2 production by enzyme immunoassay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID1751859Ratio of drug concentration in C57BL/6J mouse colon to portal vein plasma at 10 mg/kg, po measured after 4 hr by liquid chromatographic triple-quadrupole mass spectrometric method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID488207Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID1063671Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID570437Inhibition of mouse purified COX2 after 20 mins2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
[I]-Celecoxib Analogues as SPECT Tracers of Cyclooxygenase-2 in Inflammation.
AID1739501Antiproliferative activity against human A549 cells assessed as inhibition of cell growth at 100 microM measured after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID9724T1/2 (Half-life) was after oral administration at 5 mg/kg2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID1436693Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID160563Inhibitory activity against Prostaglandin G/H synthase 2 from freshly harvested mouse peritoneal macrophages2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
AID1752435Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID330496Inhibition of ovine COX1 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID1551029Ulcerogenicity in albino rat assessed as incidence of gastric ulceration at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID585023Inhibition of MDR1-mediated Mycobacterium smegmatis MC2 155 ATCC assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of kanamycin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID162165Inhibitory constant against prostaglandin G/H synthase 1 (COX-1)2002Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
AID1593008Antiinflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.
AID432551Inhibition of COX2 in human whole blood assessed as inhibition of lipopolysaccharide-stimulated PGE2 production after 24 hrs by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1565324Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency time at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by planter test (Rvb = 4.132019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID671466Antibacterial activity against Staphylococcus epidermidis ATCC 35984 after 24 hrs by broth microdilution method2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus.
AID460897Inhibition of ovine COX1 at 10 uM2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1751817Inhibition of COX2 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 1 hr in presence of 10% FBS by RapidFire High-Throu2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID344873Inhibition of ovine COX1 by enzyme immuno assay2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
AID1529997Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
AID413193Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 5 uM by cell-intact assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.
AID447529Inhibition of human recombinant COX2 by enzyme immunoassay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.
AID592801Inhibition of ovine COX-1 at 100 uM after 2 mins by fluorescence assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID1141097Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID1142838Inhibition of Helicobacter pylori carbonic anhydrase by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID223071Analysis of TXB2 as a function of COX-1 activity in heparinized human whole blood.2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID641618Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1595295Selectivity index, ratio of IC50 for human recombinant COX1 to IC50 for human recombinant COX-2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 sec2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID313335Inhibition of ovine COX12008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID353529Antiinflammatory activity in rat assessed as inhibition of carrageenan induced paw edema at 10 mg/kg after 3 hrs relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
AID733813Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 3 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 60 mins (Rvb = 33.9 +/- 3.7 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1529996Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
AID711213Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1439685Inhibition of recombinant human cytosolic carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects.
AID453634Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production at 5 uM preincubated for 10 mins2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.
AID585219Inhibition of MDR1 in methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as increase in accumulation of kanamycin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1069513Plasma concentration in Wistar rat lambda carrageenan-induced pleurisy model at 10 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs by SPE-HPLC analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID303267Inhibition of human recombinant COX2 expressed in insect sf9 cells assessed as arachidonic acid-stimulated reactive oxygen species at 10 uM after 30 mins2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A.
AID270015Selectivity index, IC50 for COX1 over IC50 for COX22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID161487In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 12003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
AID1436692Inhibition of COX2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.
AID1241383Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced hind paw edema at 20 mg/kg, po after 5 hrs by plethysmometer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis, biological evaluation and docking study of maleimide derivatives bearing benzenesulfonamide as selective COX-2 inhibitors and anti-inflammatory agents.
AID1751318Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Synthesis, docking, machine learning and antiproliferative activity of the 6-ferrocene/heterocycle-2-aminopyrimidine and 5-ferrocene-1H-Pyrazole derivatives obtained by microwave-assisted Atwal reaction as potential anticancer agents.
AID1859071Inhibition of COX-2 (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
AID1064097Antihyperalgesic activity in Swiss albino mouse assessed as reduction in carrageenan-induced inflammation at 10 mg/kg, po after 30 mins relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID457537Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha release at 10 uM by ELISA2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production.
AID492306Analgesic activity in Swiss mouse assessed as increase in latency of paw licking at 100 umol/kg, po after 60 mins measured for 60 seconds by hot plate test (Rvb = 4.9 +/- 0.5 seconds)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID497217Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured after 3 hrs relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID1310727Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema 15 mg/kg, po measured after 4 hrs relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID1503675In vivo inhibition of rat COX-2 assessed as decrease in plasma PGE2 level by EIA relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID585018Inhibition of MDR1-mediated vincristine-resistance in Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ampicillin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID161996In vitro inhibitory activity against prostaglandin G/H synthase 1 using mouse peritoneal macrophage method2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID763518Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha at 30 uM preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride relative to control2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
AID1262264Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID1462019In-vivo inhibition of COX2 in rat at 20 mg/kg measured after 120 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1179976Inhibition of COX1 (unknown origin) by solid phase ELISA method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.
AID493888Inhibition of human recombinant carbonic anhydrase 5b after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1164048Inhibition of ovine COX1 assessed as reduction in PGF2alpha formation at 10 uM incubated for 18 hrs by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID281539Antiproliferative activity against androgen-sensitive human LNCaP cells after 72 hrs by MTT test2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1851457Ratio IC50 for inhibition of COX1 in mouse J774 cells over inhibition of COX2 in mouse J774 cells2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID1368422Inhibition of human COX2 assessed as reduction in PGF2alpha level using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition by ELISA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.
AID1713247Inhibition of ovine COX-1 assessed as appearance of oxidized TMPD level by EIA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study.
AID161331Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 1 in human blood2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID162005Tested for inhibition against Prostaglandin G/H synthase 1 from mouse resident macrophages2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID657493Inhibition of recombinant human COX2 using arachidonic acid as substrate at 100 nM preincubated for 10 mins prior substrate addition measured after 2 mins by EIA2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF₁ production.
AID1055837Inhibition of human recombinant COX2 expressed in insect cell expression system using TMPD and arachidonic acid as substrate incubated for 1 min prior to substrate addition by spectrophotometry2013European journal of medicinal chemistry, , Volume: 70Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation.
AID620688Inhibition of human carbonic anhydrase 12-catalyzed CO2 hydration activity by stopped flow assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1462012Inhibition of COX-2 in rat peritoneal macrophages assessed as reduction in PGE2 production using radiolabelled-arachidonic acid as substrate pretreated for 30 mins followed by substrate addition measured after 30 mins2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.
AID1067227Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1752429Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 0.01 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1172862Inhibition of ovine COX12014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID1752439Antiinflammatory activity in mouse xylene induced ear edema model assessed as inhibition of auricular edemas at 30 mg/kg, po once daily administered for 3 days prior to xylene stimulation and measured after 30 mins relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1608178Selectivity index, ratio of IC50 for ovine COX1 to IC50 for recombinant human COX22019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID641774Antiinflammatory activity against carrageenan-induced edema in Sprague-Dawley rat assessed as right hind paw volume at 10 mg/kg, po administered 4 hrs post challenge measured after 60 mins2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1902054Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID180547The compound was tested in vivo for activity against adjuvant-induced arthritis in rat after peroral administration after peroral administration2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID302415Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels at 1 uM by radioimmunoassay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1310720Inhibition of ovine COX-1 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID176212Effective dose was determined in vivo in male lewis rats by rat adjuvant-induced arthritis assay1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID1565314Analgesic activity in Wistar albino rat assessed as reaction time at 25 mg/kg, ip measured after 120 mins for 15 secs by hot plate method (Rvb = 4.32 +/- 0.52 sec)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1739500Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.
AID1549728Antitumor activity against mouse B16F10 cells implanted in nude mouse assessed as reduction in tumor size at 20 mg/kg, ip administered once per 2 days for 14 days by caliper method2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1576178Hepatotoxicity in rat assessed as effect on portal veins at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID160561Tested for inhibition against Prostaglandin G/H synthase 2 from mouse resident macrophages2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID404479Inhibition of LTB4 production in mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID312234Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 180 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID281536Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID658648Inhibition of ovine COX2 by enzyme immuno assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID369273Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID753955Analgesic activity in Swiss albino mouse inflammatory pain model assessed as inhibition of acetic acid-induced writhing at 1 mg/kg, po administered 30 mins prior to acetic acid challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1057592Inhibition of human recombinant COX2 using arachidonic acid as substrate at 10 uM incubated 5 mins prior to substrate addition measured after 5 mins by HPLC analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
AID552130Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID456477Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 10 uM by RIA2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID176214Effective dose was determined in vivo in male Dawley rats by rat carrageenan-induced hyperalgesia assay1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
AID411999Analgesic activity in po dosed Swiss mouse assessed as inhibition of acetic acid-induced abdominal constriction administered 1 hr before acetic acid challenge2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes.
AID369274Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1461600Inhibition of soybean lipoxygenase preincubated for 5 mins followed by linoleic acid substrate addition measured after 20 mins by spectrophotometric method2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID497127Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors.
AID1453412Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1565326Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency time at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 4 hrs by planter test (Rvb = 5.472019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1226814Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID162167In vitro selectivity ratio of Prostaglandin G/H synthase 1 to Prostaglandin G/H synthase 22003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID1751820Inhibition of COX1 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 1 hr in presence of 10% FBS by RapidFire High-Throu2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID342462Half life in rat plasma2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID1684450Inhibition of COX-2 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.
AID271286Inhibition of ovine COX12006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID1164203Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID363325Inhibition of COX1 at 13.1 uM2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
AID1168909Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 20 uM after 24 hrs by ELISA2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
AID1077239Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID458548Inhibition of ovine COX2 by enzyme chemiluminescent enzyme assay2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors.
AID1437457Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 umol/kg, ip administered 1 hr post carrageenan challenge measured at 1 hr post compound dosing relative to control
AID641616Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells at 1 uM after 24 hrs by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID410033Inhibition of ovine COX1 by enzyme immuno assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID427144Inhibition of ovine COX1 by chemiluminescence assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1061772Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID162489In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID1064077Selectivity index, ratio of IC50 for COX-1 to IC50 for COX-2 in human whole blood2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID1763090Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition by colorimetric analysis
AID1551026Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 18 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hrs by caliper method relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID1390012Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID436565Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID1763095Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced intracellular ROS production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DCFH-DA staining based fluorescence analysis
AID232419Ratio of inhibition of COX-1 to COX-22000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
AID1434427Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1763091Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition by colorimetric analysis
AID612058Inhibition of human whole blood COX-2 assessed as production of PGE2 after 24 hrs by EIA2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID633796Inhibition of ovine COX1 assessed as PGF2alpha production by enzyme immunoassay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Fragment-based design, docking, synthesis, biological evaluation and structure-activity relationships of 2-benzo/benzisothiazolimino-5-aryliden-4-thiazolidinones as cycloxygenase/lipoxygenase inhibitors.
AID1595292Inhibition of human recombinant COX-2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzym2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID717364Inhibition of ovine COX2 peroxidase activity assessed as TMPD oxidation at 20 uM by colorimetric analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones.
AID1190063Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID313339Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw edema volume at 10 mg/kg, po after 4 hrs2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID1067229Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID242133In vitro inhibitory concentration against Prostaglandin G/H synthase 2 (COX-2) in human whole blood2005Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
AID1188136Inhibition of Helicobacter pylori Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID244091Ratio of IC50 for human COX-1 and COX-22004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
AID1336924Cytotoxicity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID683132Inhibition of COX2 assessed as PGE2 production using arachidonic acid as substrate at 5 nM by EIA2012European journal of medicinal chemistry, Nov, Volume: 57Sulfonilamidothiopyrimidone and thiopyrimidone derivatives as selective COX-2 inhibitors: synthesis, biological evaluation, and docking studies.
AID1694427Antiproliferative activity against human cells MCF-7 assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID8752Cmax (Maximum (Peak) plasma drug concentration) was after oral administration at 5 mg/kg2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID330501Inhibition of LOX15 from rabbit reticulocytes at 10 uM by enzyme immuno assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID289279Inhibition of human recombinant COX2 by measuring PGE22007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
AID744752Inhibition of ovine COX2-mediated prostaglandin alpha production by enzyme immuno assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Molecular design, synthesis and biological evaluation of cyclic imides bearing benzenesulfonamide fragment as potential COX-2 inhibitors. Part 2.
AID1292031Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID770585Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1251004Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.
AID1275913Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1443242Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as rise in paw volume at 150 ug/kg administered 1 hr followed by carrageenan challenge measured at 360 mins by plethysmometer (Rvb = 49.3%)2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1902039Inhibition of full-length ovine COX-1 at 50 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1630906Inhibition of ovine COX2 by enzyme immunoassay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1288450Ulcerogenicity in ip dosed fasted Sprague-Dawley rat after 24 hrs by hand lens2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID160061Inhibitory effect on production of cyclooxygenase-1 (COX-1) thromboxane B2 (TXB2) in human platelet cells2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
AID251920Percent inhibition of analgesic activity in a rat model 4% NaCl-induced abdominal constriction assay at 30 min2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID514960Inhibition of sheep COX12010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Design, synthesis, and biological evaluation of ketoprofen analogs as potent cyclooxygenase-2 inhibitors.
AID1071434Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 24 hrs relative to vehicle-treated control2014European journal of medicinal chemistry, Feb-12, Volume: 733D QSAR studies based in silico screening of 4,5,6-triphenyl-1,2,3,4-tetrahydropyrimidine analogs for anti-inflammatory activity.
AID243602Anti-inflammatory activity in rat paw edema assay at 50 mg/kg2005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
AID1306897Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID1650565Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX22020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1752434Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 0.1 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1767344Inhibition of human COX2 assessed as fluorescence by microplate reader
AID312224Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 4 hrs relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1742039Antiinflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of paw edema at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 1 hr by Vernier caliper method relative to control2020European journal of medicinal chemistry, Nov-01, Volume: 205Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.
AID1550470Inhibition of human COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID594416Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID184174In vivo anti-inflammatory activity determined by rat carrageenan paw edema method at 10 mg/kg perorally2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID674725Gastrointestinal toxicity in Wistar albino rat assessed as stomach ulcer index at 0.029 mmol/kg, po followed by another two compound doses in second and third days measured on fourth day post dose by acute ulcerogenicity study2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID162498In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 22003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
AID1607870Inhibition of COX2 (unknown origin)2019European journal of medicinal chemistry, Oct-01, Volume: 179Human disorders associated with inflammation and the evolving role of natural products to overcome.
AID1057883Cytotoxicity against IL-1beta/TNFalpha-stimulated human HeLa cells assessed as cell viability up to 10 uM after 24 hrs by WST-1 assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1.
AID743513Inhibition of Helicobacter pylori recombinant alpha carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1143086Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced foot paw edema after 1 hr by plethysmometer analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID492316Antiedematogenic activity in Swiss mouse assessed as inhibition of capsaicin-induced paw edema at 100 umol/kg, po administered 40 mins before capsaicin challenge measured after 30 mins relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID683292Analgesic activity against carrageenan-induced thermal hyperalgesia in Sprague-Dawley rat assessed as paw withdrawal latency at 100 umol/kg, po after 30 mins after 3 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.
AID1244904Antiedematogenic effect in Swiss mouse assessed as inhibition of CFA-induced paw edema at 300 mg/kg, po after 2 hrs2015European journal of medicinal chemistry, Sep-18, Volume: 102Regioselectively controlled synthesis of 3(5)-(trifluoromethyl)pyrazolylbenzenesulfonamides and their effects on a pathological pain model in mice.
AID1256041Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess assay relative to control2015Journal of natural products, Oct-23, Volume: 78, Issue:10
Anti-inflammatory Inositol Derivatives from the Whole Plant of Inula cappa.
AID711038Inhibition of human recombinant CA12 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID493885Inhibition of human recombinant carbonic anhydrase 3 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID493892Inhibition of human recombinant carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID178739Effective dose was evaluated by rat adjuvant arthritis model.1998Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.
AID1142834Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1143095Analgesic activity in ip dosed albino Swiss mouse after 1 hr by hot plate test2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID315993Selectivity for human COX2 over human COX1 by human whole blood assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides.
AID223079In vitro assay for PGE-2 production as a function of COX-2 inhibition in whole human blood cultured with lipopolysaccharide (LPS)2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
AID585031Inhibition of MDR1 in methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as increase in accumulation of ampicillin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID162306In vitro inhibition of Prostaglandin G/H synthase 1 (from ram seminal vesicles) at a concentration of 10 M2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID1565336Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 3 hrs by Von-frey test (Rvb =2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1565302Inhibition of ovine COX1 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID693437Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw pressure at 10 mg/kg, po after 60 mins post carrageenan-challenge2012European journal of medicinal chemistry, Dec, Volume: 58Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
AID612725Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID1849544Binding affinity to human recombinant CA4 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
AID1143531Selectivity index, ratio of IC50 for COX-1 (unknown origin) to IC50 for COX-2 (unknown origin)2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.
AID1503683Antiinflammatory activity in sc dosed Sprague-Dawley rat assessed as inhibition of cotton pellet-induced granuloma after 7 days2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID254700Inhibitory concentration against carbonic anhydrase IX2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID493883Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID1896939Inhibition of COX-2 in human NALM-6 cells assessed as downregulation of COX-2 expression by measuring COX-2 expression at 10 to 30 uM incubated for 48 hrs by DAPI staining based immunofluorescence based analysis relative to control2022Bioorganic & medicinal chemistry, Nov-05, Volume: 75Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
AID270017Anti-inflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 3 mg/kg, iv after 5 hrs2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1483247Inhibition of recombinant human COX-2 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis
AID180548The compound was tested in vivo for activity against carrageenan induced paw edema in rat after peroral administration2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID412149Antiinflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as increase in paw volume at 20 mg/kg, po measured 5 hrs after carrageenan challenge relative to control2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide.
AID514961Inhibition of sheep COX22010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Design, synthesis, and biological evaluation of ketoprofen analogs as potent cyclooxygenase-2 inhibitors.
AID346087Inhibition of IgE-specific antigen-induced LBT4 release in rat MC9 cells2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID436656Antiinflammatory activity against carrageenan-induced foot paw edema in rat assessed as reduction in paw size at 20 mg/kg, sc administered 30 mins before carrageenan challenge measured after 3 hrs relative to control2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Synthesis, biological evaluation and docking studies of novel benzopyranone congeners for their expected activity as anti-inflammatory, analgesic and antipyretic agents.
AID1565310Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw volume at 12.5 mg/kg, ip measured after 2 hrs by plethysmometric method (Rvb = 1.58 +/- 0.21 ml)2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID1902047Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID312252Inhibition of ethanol-induced gastric mucosal damage in Wistar rat assessed as ulcer index at 60 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID753951Analgesic activity in Swiss albino mouse inflammatory pain model assessed as inhibition of acetic acid-induced writhing at 40 mg/kg, po administered 30 mins prior to acetic acid challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.
AID1390015Selectivity ratio of IC50 for full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif.
AID1310722Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-22016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID1902038Inhibition of full-length ovine COX-1 at 5 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1709974Inhibition of recombinant ovine COX12021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID453627Inhibition of human recombinant COX2 at 5 uM2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.
AID1188135Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID1464290Inhibition of ovine COX1 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay
AID160743Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID313334Inhibition of ovine COX1 at 10 uM2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID1177824Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014European journal of medicinal chemistry, Nov-24, Volume: 87Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents.
AID281537Selectivity for COX2 over COX12004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1550479Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 3 hrs post-carrageenan injection (Rvb = 38.4%)2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID585029Inhibition of MDR1-mediated Mycobacterium smegmatis MC2 155 ATCC assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of ciprofloxacin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1592998Inhibition of human recombinant COX2 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method2019European journal of medicinal chemistry, Apr-01, Volume: 167Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.
AID432553Selectivity ratio of IC50 for COX1 to IC50 for COX2 in human whole blood2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID770583Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID675695Inhibition of COX12012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.
AID270016Anti-inflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 3 mg/kg, iv after 3 hrs2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
AID447533Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced paw edema after 3 hrs2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.
AID1461593Inhibition of ovine COX-1 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1288452Inhibition of ovine COX-2 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibition activities and molecular docking study of pyrazoline derivatives.
AID471362Antiinflammatory activity against gamma carrageenan-induced pleurisy in Wistar rat assessed as decrease in exudate volume in pleural cavity at 10 mg/kg, ip administered 30 mins before gamma carrageenan challenge measured after 4 hrs2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID635998Antiinflammatory activity in Wistar rat neutrophils assessed as decrease in LPS-induced PGE2 secretion at 10 nM after 18 hrs by EIA2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis, anti-inflammatory activity and molecular docking studies of 2,5-diarylfuran amino acid derivatives.
AID641772Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat assessed as paw weight at 10 mg/kg, po administered 4 hrs post challenge measured after 120 mins (Rvb = 61.5+/-3.4 g)2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1195370Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID48112Inhibitory activity of compound against bovine carbonic anhydrase IV2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride.
AID1483246Inhibition of human COX-1 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis
AID460652Cytotoxicity against LPS and IFN-gamma-stimulated human THP1 cells after 24 hrs2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1751824Half life in mouse hepatocytes2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1752437Solubility of the compound in water2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID312242Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 30 mg/kg, po after 180 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1403473Selectivity index, ratio of IC50 for ovine COX1 to IC50 for recombinant human COX22018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID313337Inhibition of ovine COX22008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID1169136Antiinflammatory activity in orally dosed Sprague-Dawley rat model of carrageenan-induced foot paw edema assessed as reduction in edema by plethysmometry2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
AID1846849Inhibition of ovine COX-2 using arachidonic acid as substrate measured after 2 mins by colorimetric enzyme immune assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID1550471Inhibition of human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID510451Cytotoxicity against human HDF cells assessed as inhibition of cell viability at 100 uM by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
AID724443Inhibition of ovine COX12013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.
AID1711789Ulcerogenic activity in rat assessed as average severity of ulcers at 50 mg/kg, po administered once daily for 3 consecutive days and measured after 1 hr post last dose (Rvb = 0)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID1306899Analgesic activity in ip dosed albino Swiss mouse assessed as nociceptive response measured after 60 mins by hot plate method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID693844Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po after 1 hr (Rvb = 0.85 +/- 0.01%)2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel 3-substituted-1-aryl-5-phenyl-6-anilinopyrazolo[3,4-d]pyrimidin-4-ones: docking, synthesis and pharmacological evaluation as a potential anti-inflammatory agents.
AID162636Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
AID460653Inhibition of MCP1 release in human THP1 cells after 24 hrs by ELISA2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1251002Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.
AID1718957Antiarthritic activity in CFA-induced rheumatoid arthritis Wistar rat model assessed as reduction in arthritis index at 3 mg/kg, ig for 28 days2021Bioorganic & medicinal chemistry letters, 02-15, Volume: 34Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
AID1437458Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 umol/kg, ip administered 1 hr post carrageenan challenge measured at 3 hrs post compound dosing relative to control
AID1519089Inhibition of human COX1 using arachidonic acid as substrate incubated for 2 mins by ELISA method
AID1717039Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID1751818Inhibition of human recombinant COX-1 assessed as reduction in peroxidase activity using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1285031Inhibition of ovine COX-1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.
AID1752431Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 100 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1405925Antioxidant activity assessed as inhibition of lipid peroxidation2018European journal of medicinal chemistry, Aug-05, Volume: 156Current progress on antioxidants incorporating the pyrazole core.
AID457535Inhibition of COX2 in human THP1 cells at 10 uM by enzyme immunoassay2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production.
AID560400Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells at 64 ug/ml after 24 hrs by broth microdilution method in presence of 50% human serum albumin2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID46698In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
AID1164053Anti-inflammatory activity in Sprague-Dawley rat model of carrageenan-induced paw edema assessed as inhibition of paw edema volume at 150 umol/kg, po dosed 1 hr before carrageenan challenge and measured 1 hr post carrageenan challenge2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.
AID184179In vivo antiinflammatory activity against rat carrageenan-induced foot paw edema model at 5 hr following a 1 mg/kg oral dose2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID693845Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po after 2 hrs (Rvb = 1.11 +/- 0.02%)2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel 3-substituted-1-aryl-5-phenyl-6-anilinopyrazolo[3,4-d]pyrimidin-4-ones: docking, synthesis and pharmacological evaluation as a potential anti-inflammatory agents.
AID275265Inhibition of Freund's complete adjuvant-induced arthritis in Lewis rat at 5 mg/kg, po2007Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.
AID1154880Selectivity for human recombinant COX2 to ovine COX12014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID1374330Selectivity ratio of compound effect for inhibition of ovine COX2 to compound effect for inhibition of ovine COX12018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.
AID177675Inhibition of carrageenan induced rat paw oedema.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID674714Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 3 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies.
AID238575Inhibitory activity against human carbonic anhydrase IV (hCAIV)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
AID241608In vitro inhibition of Prostaglandin G/H synthase 1 in human whole blood2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
AID547630Selectivity ratio of IC50 for human recombinant COX2 to IC50 for human platelets COX12010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
AID1549674Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID1069517Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in number of leukocytes in pleural space at 5 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative to2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID629713Inhibition of COX1 by chemiluminescent enzyme assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1902065Induction of apoptosis in human HepG2 cells assessed as up regulation of Bax expression at 75 uM measured after 20 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID244381Ratio of IC50 for Prostaglandin G/H synthase 1 and Prostaglandin G/H synthase 22004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.
AID1596636Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Novel resveratrol-based flavonol derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo.
AID460654Antineurotoxicity in human SH-SY5Y cells assessed as inhibition human THP1 cell supernatant-induced cytotoxicity compound pretreated 24 to 48 hrs to THP1 cells measured after 72 hrs of supernatant addition2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1420987Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA
AID492308Analgesic activity in Swiss mouse assessed as increase in latency of paw licking at 100 umol/kg, po after 90 mins measured for 60 seconds by hot plate test (Rvb = 5.9 +/- 0.8 seconds)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates.
AID420789Analgesic activity in Albino mouse assessed as inhibition of acetic acid-induced writhing at 300 umol/kg, po administered 1 hr before acetic acid challenge and measured 10 mins after acetic acid challenge2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
AID432548Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1311606Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID1727726Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate at 0.01 uM measured after 10 mins by fluorometric based multimode microplate reader relative to control
AID183113Inhibitory activity against carrageenan induced rat paw edema after peroral administration after 5 hours2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
AID734525Inhibition of COX-1 (unknown origin) by chemiluminescence assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID261408In vitro COX2 selectivity index (IC50 COX1/IC50 COX2)2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID613460Inhibition of STAT3 protein expression in COX2-negative human HCT116 cells at 10 to 50 uM after 1 hr by Western blot analysis2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).
AID1519090Inhibition of human COX2 using arachidonic acid as substrate incubated for 2 mins by ELISA method
AID1067225Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 122014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID225287Effective dose for inhibition of edema of the non injected paw in rat2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite.
AID658652Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced foot paw edema at 50 mg/kg, ip measured after 2 hrs2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID1550476Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 2 hrs post-carrageenan injection (Rvb = 4.72 +/-2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID1689630Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 4 hr by plethysmometer analysis (Rvb = 3.98 +/- 0.34 mm)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID733809Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced paw edema at 10 mg/kg, po administered 3 hrs 30 mins after carrageenan-challenge measured after 60 mins (Rvb = 2.48 +/- 0.06 mL)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1156827Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs relative to control2014European journal of medicinal chemistry, Aug-18, Volume: 83Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.
AID190164The compound was tested in vivo for gastric ulcerogenic activity in rat after peroral administration2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID1253839Inhibition of ovine COX-1 using arachidonic acid after 5 mins by colorimetric method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties.
AID239790In vitro selectivity for Prostaglandin G/H synthase 1 and Prostaglandin G/H synthase 22004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
AID1077235Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 50 mg/kg, po administered 1 hr prior to formalin challenge measured after 3 hrs relative to control2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1192235Inhibition of ovine COX1 at 10 uM by TMPD oxidation based colorimetric assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Environmentally benign synthesis, molecular properties prediction and anti-inflammatory activity of novel isoxazolo[5,4-d]isoxazol-3-yl-aryl-methanones via vinylogous Henry nitroaldol adducts as synthons.
AID281540Antiproliferative activity against androgen-independent human PC3 cells after 72 hrs by MTT test2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
AID1143093Gastrointestinal toxicity in albino rat assessed as ulcer index at 100 mg/kg, po qd for 3 days measured 6 hrs after last dose2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: novel celecoxib analogs as potent anti-inflammatory agents.
AID1488615Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID1292032Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.
AID28940Partition coefficient (logP)2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID693846Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po after 3 hrs (Rvb = 1.08 +/- 0.41%)2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel 3-substituted-1-aryl-5-phenyl-6-anilinopyrazolo[3,4-d]pyrimidin-4-ones: docking, synthesis and pharmacological evaluation as a potential anti-inflammatory agents.
AID1694424Antiproliferative activity against human MCF10A cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-15, Volume: 32Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.
AID1301936Inhibition of ovine COX1 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID1194026Inhibition of recombinant Methanosarcina thermophila gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID456499Analgesic activity against zymosan-induced hyperalgesia in mouse assessed maximum effect measured up to 6 hrs2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID641609Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells at 0.01 uM incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1752433Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins at 1 uM followed by substrate addition and measured after 2 mins by ELISA analysis relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID235863In vitro selectivity against COX-1 to that of COX-2 was determined2003Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.
AID162635Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay)2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
AID1196114Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID1488613Ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin)2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.
AID184177In vivo antiinflammatory activity against rat carrageenan-induced foot paw edema model at 3 hr following a 1 mg/kg oral dose2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID585022Inhibition of MDR1-mediated methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of kanamycin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1250473Inhibition of ovine COX-1 using arachidonic acid after 15 mins by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.
AID733373Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced paw edema at 3 mg/kg, po administered 3 hrs 30 mins after carrageenan-challenge measured after 60 mins (Rvb = 2.48 +/- 0.06 mL)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID1374328Inhibition of ovine COX2 at 5 uM using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5
Design, synthesis, anti-inflammatory activity and molecular docking of potential novel antipyrine and pyrazolone analogs as cyclooxygenase enzyme (COX) inhibitors.
AID1060947Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-2 protein expression at 5 uM after 24 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID162344In vitro inhibitory activity against human Prostaglandin G/H synthase 21999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.
AID261412Inhibitory activity against 4% NaCl-induced abdominal constriction in Sprague-Dawley rat after 30 min of 5 mg/kg, po2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID673511Inhibition of bovine 5-LOX assessed as inhibition of calcium ionophore A23187-induced leukotriene B4 formation by reversed phase HPLC analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.
AID658647Inhibition of ovine COX1 by enzyme immuno assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation and molecular modeling study of pyrazole and pyrazoline derivatives as selective COX-2 inhibitors and anti-inflammatory agents. Part 2.
AID1125896Inhibition of COX2 (unknown origin) by colorimetric method2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis of thio-heterocyclic analogues from Baylis-Hillman bromides as potent cyclooxygenase-2 inhibitors.
AID460903Antiinflammatory activity in Wistar albino rat sub-acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered daily for 7 days by plethysmometer relative to control2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID1506619Inhibition of human COX2 assessed as reduction in PGE2 production incubated for 2 mins using arachidonic acid substrate by enzyme immuno assay2017MedChemComm, Mar-01, Volume: 8, Issue:3
Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).
AID309450Inhibition of COX22007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID254882Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.
AID1519093Antiinflammatory activity against albino rats assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po measured after 2 hrs relative to control
AID460898Inhibition of human COX2 at 10 uM2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.
AID585021Inhibition of MDR1-mediated vincristine-resistance in Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration index after 24 to 48 hrs in presence of kanamycin2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID177358In vivo inhibition of adjuvant arthritis in rats2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID592803Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID271287Inhibition of ovine COX22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
AID243785In vitro inhibition of Prostaglandin G/H synthase 1 in human whole blood at 30 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
AID1168408Anti-inflammatory activity in carrageenan-induced rat foot paw edema model assessed as reduction in paw volume at 20 mg/kg dosed 30 mins before carrageenan injection and measured 3 hrs after carrageenan challenge2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Synthesis of new 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles: a search for novel nitric oxide donor anti-inflammatory agents.
AID166753Variation of intraocular pressure in fourth day at a dose of 150 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1549680Inhibition of COX1 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay2019European journal of medicinal chemistry, May-01, Volume: 169Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.
AID302414Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels at 10 uM by radioimmunoassay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1240216Inhibition of Methanosarcina thermophila recombinant gamma carbonic anhydrase by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID1320388Invivo inhibition of IKK-mediated NF-kB activation in Balb/c mouse assessed as decrease in TPA-induced TNFalpha expression at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by immunohistochemical analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID330500Inhibition of LOX12 from human platelets at 10 uM by enzyme immuno assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
AID432546Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID585218Inhibition of MDR1 in Staphylococcus aureus ATCC 29213 assessed as increase in accumulation of kanamycin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID162493In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus2004Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
AID1168912Toxicity in rat assessed as damage to epithelial layer of stomach at 60 mg/kg, po after 5 hrs2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.
AID1751825Clearance in C57BL/6J mouse at 2 mg/kg, iv measured after 0.08 to 24 hrs2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID497219Antiinflammatory activity in Wistar albino rat sub-acute inflammatory model assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po administered 1 hr prior to formalin challenge measured on day 1 relative to control2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID613461Inhibition of IL-6-induced STAT3 phosphorylation in human PANC1 cells at 25 to 50 M pretreated 2 hrs prior to IL-6 challenge measured after 30 mins2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).
AID738676Inhibition of COX1 in human blood assessed as PGE2 level incubated for 15 mins prior to LPS-challenge measured after 24 hrs by enzyme immunoassay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and -2-alkylsulfonyl-1H-imidazole derivatives.
AID634815Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in protein level in bronchoalveolar lavage fluid at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs by Bra2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID1188169Cytotoxicity against human MDA-MB-231 cells assessed as cell viability at 10 ug/ml after 24 to 48 hrs by trypan blue exclusion assay (Rvb = 87.54 +/- 2.11%)2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Design, synthesis, in silico and in vitro studies of novel 4-methylthiazole-5-carboxylic acid derivatives as potent anti-cancer agents.
AID162472Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 2 (COX-2)2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.
AID302412Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID1311611Inhibition of human COX1 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID301223Inhibition of ovine COX1 by enzyme immuno assay2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Novel (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic ester prodrugs possessing a diazen-1-ium-1,2-diolate moiety: design, synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID178666Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using therapeutic method; dose administered daily once2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives.
AID1689621Analgesic activity in albino mouse assessed as protection against acetic acid-induced writhing at 0.028 mM/kg, po pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID185800Inhibitory effect of compound on carrageenan-induced rat paw edema administered p.o. at 3 mg/kg2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
AID1902052Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2022Bioorganic & medicinal chemistry, 03-01, Volume: 57Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.
AID1125017Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Synthesis and biological evaluation of new pyrazolone-pyridazine conjugates as anti-inflammatory and analgesic agents.
AID1310723Inhibition of soybean 15-LOX using arachidonic acid as substrate by enzyme immunoassay2016European journal of medicinal chemistry, Aug-08, Volume: 118Synthesis of new thiazolo-celecoxib analogues as dual cyclooxygenase-2/15-lipoxygenase inhibitors: Determination of regio-specific different pyrazole cyclization by 2D NMR.
AID1311609Antiproliferative activity against human LO2 cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID1064095Antihyperalgesic activity in Swiss albino mouse assessed as reduction in carrageenan-induced inflammation at 10 mg/kg, po after 90 mins relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
AID1285029Inhibition of COX-2 (unknown origin)2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.
AID392042Selectivity ratio of IC50 for COX1 to IC50 for COX22008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1420985Antiproliferative activity against human HCT116 cells by MTT assay
AID174679Percentage of [51Cr]- secreted in feces was determined by fecal drug-induced bleeding method in rat at 100 mg/kg, bid for 5 days2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID694221Selectivity index, ratio of IC50 for COX-1 to IC50 for COX-22012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors.
AID1268956Inhibition of ovine COX1 by enzyme immuno assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.
AID764718Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID181152Hemoglobin levels in the different assays ranged from 11.5-14.7 g/dl.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.
AID1752430Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID403703Inhibition of human COX1 expressed in sf9 cells2005Journal of natural products, Oct, Volume: 68, Issue:10
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
AID1783310Inhibition of ovine COX-1 using arachidonic acid as substrate by fluorescence assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential.
AID641613Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay2011Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties.
AID1592996Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22019European journal of medicinal chemistry, Apr-01, Volume: 167Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.
AID368226Inhibition of human recombinant COX2 by enzyme immuno assay2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Synthesis of 1-(methanesulfonyl- and aminosulfonylphenyl)acetylenes that possess a 2-(N-difluoromethyl-1,2-dihydropyridin-2-one) pharmacophore: evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID560399Antibacterial activity against Francisella novicida infected in mouse RAW264.7 cells at 64 ug/ml after 24 hrs by broth microdilution method in presence of 10% human serum albumin2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Pharmacological exploitation of an off-target antibacterial effect of the cyclooxygenase-2 inhibitor celecoxib against Francisella tularensis.
AID238957Inhibitory activity against human carbonic anhydrase I at 0.09 uM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
AID660181Inhibition of COX2 at 5 uM by fluorescence assay2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.
AID313336Inhibition of ovine COX2 at 10 uM2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: a novel class of cyclooxygenase-2 inhibitors.
AID54711Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay1999Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
AID456479Selectivity index, ratio of IC50 for mouse COX1 to IC50 for mouse COX22010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID312251Inhibition of ethanol-induced gastric mucosal damage in Wistar rat assessed as ulcer index at 15 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID764717Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID160596Ability to inhibit Prostaglandin G/H synthase 2 by using freshly harvested mouse peritoneal macrophages2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors.
AID1605054Inhibition of SERCA in human PC3 cell microsomes by enzyme-coupled method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective.
AID1060941Ratio of IC50 for COX-2 positive human HCA-7 cells to IC50 for COX-2 positive human HCA-7 cells transfected with CD44v6shRNA2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
AID1711788Antiinflammatory activity against po dosed Wistar albino rat model of carrageenan-induced foot paw edema after 3 hrs2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
AID160730In vitro inhibition against ovine Prostaglandin G/H synthase 22003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID763515Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride2013Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors.
AID695145Selectivity ratio of IC50 for human recombinant COX2 to IC50 for ovine COX12012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.
AID1443234Inhibition of human recombinant COX2 at 60 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID1195371Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID675696Inhibition of COX22012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.
AID1077234Ulcerogenic effect in fasted Wistar albino rat at 50 mg/kg, po measured 2 hrs post last dose2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1751853Inhibition of COX1 in human whole blood assessed as reduction in calcium ionophore-stimulated TXB2 production incubated for 1 hr by ELISA2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID456491Antiinflammatory activity against carrageenan-induced paw edema rat inflammatory model assessed as suppression of paw edema at 20 mg/kg, po after 60 mins2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.
AID1125127Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 4 hrs relative to control2014European journal of medicinal chemistry, Apr-22, Volume: 771-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.
AID634818Antiinflammatory activity against LPS-induced inflammation in BALB/c mouse acute lung injury model assessed as reduction in wet/dry ratio of lung at 50 mg/kg, ip administered 1 hr prior to LPS challenge measured after 12 hrs2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
AID232767Selectivity index of IC50 against COX-1 to the IC50 against COX-22003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID1278411Inhibition of Nostoc commune gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1496188Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-stimulated COX2 protein expression at 20 uM preincubated for 2 hrs followed by LPS addition measured after 18 hrs by Western blot analysis2018Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12
Anti-allergic inflammatory components from Sanguisorba officinalis L.
AID1851456Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production and measured after 24 hrs by enzyme immuno-assay (EIA)2022European journal of medicinal chemistry, Nov-05, Volume: 241Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties.
AID673509Inhibition of bovine COX1 assessed as inhibition of calcium ionophore A23187-induced 12-hydroxyheptadecatrienoic acid formation by reverse-phase HPLC analysis2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.
AID697537Plasma concentration in human2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Predicting new indications for approved drugs using a proteochemometric method.
AID1311605Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID1576159Ulcerogenic activity in rat assessed as effect on mucosal blood vessel at 50 mg/kg by hematoxylin and eosin staining based assay2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1268102Inhibition of COX2 in rat abdominal macrophages assessed as PGE2 production pretreated for 30 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by EIA2016European journal of medicinal chemistry, Jan-27, Volume: 108Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.
AID312247Increase in body weight in acetic acid-induced chronic gastric ulcer Wistar rat at 30 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1061066Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID488198Inhibition of 5-lipoxygenase in human whole blood assessed as inhibition of 5-hydroxyeicosatetraenoic acid production by HPLC method2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
AID635997Antiinflammatory activity in Wistar rat neutrophils assessed as decrease in PGE2 level at 10 nM after 18 hrs by EIA2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis, anti-inflammatory activity and molecular docking studies of 2,5-diarylfuran amino acid derivatives.
AID1454307Inhibition of ovine COX22017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides.
AID1320383Anti-inflammatory activity in Balb/c mouse assessed as reduction in TPA-induced hyperkeratosis at 0.75 uM administered topically 6 mins prior to TPA administration measured after 6 hrs by hematoxylin and eosin staining based microscopic analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Anti-inflammatory activity effect of 2-substituted-1,4,5,6-tetrahydrocyclopenta[b]pyrrole on TPA-induced skin inflammation in mice.
AID1067228Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1595188Antiarthritic activity in adjuvant-induced Sprague-Dawley rat2019European journal of medicinal chemistry, Jun-01, Volume: 171Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.
AID1550474Antiinflammatory activity against carrageenan-induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 1 hr post-carrageenan injection (Rvb = 4.51 +/- 2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID312244Inhibition of ethanol-induced gastric mucosal damage in Wistar rat at 15 mg/kg, po2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID392041Inhibition of COX12008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
AID1336955Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at lesser G1 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.59%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID238574Inhibitory activity against human carbonic anhydrase II (hCAII)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
AID1859072Ratio IC50 for inhibition of COX-2 (unknown origin) over COX-1 (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
AID693434Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw pressure at 10 mg/kg, po after 15 mins post carrageenan-challenge2012European journal of medicinal chemistry, Dec, Volume: 58Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.
AID585225Inhibition of MDR1 in methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as increase in accumulation of ciprofloxacin by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID8516C24 after oral administration at 5 mg/kg2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
AID612731Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 1 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID1568918Inhibition of recombinant human COX-2 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method
AID743514Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1077240Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1198998Inhibition of human recombinant COX1 by ELISA2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.
AID363802Inhibition of human COX22008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
AID1053261Agonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin at 8 uM by luminometric analysis relative to quinpirol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1461599Inhibition of human COX-2 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID185799Inhibitory effect of compound on carrageenan-induced rat paw edema administered p.o. at 10 mg/kg2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
AID410035Inhibition of potato LOX5 by enzyme immuno assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
AID1689625Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 1 hr by plethysmometer analysis relative to control (Rvb = 0 %)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID620690Selectivity ratio of Ki for human carbonic anhydrase 1 to Ki for human recombinant carbonic anhydrase 12 catalytic domain2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Phenylethynylbenzenesulfonamide regioisomers strongly and selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic isoforms I and II.
AID1532668Inhibition of COX2 in LPS-induced human whole blood at 10 uM after 24 hrs by EIA relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Anti-inflammatory activity of triazine derivatives: A systematic review.
AID585017Antibacterial activity against Mycobacterium smegmatis MC2 155 ATCC2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID611752Inhibition of sheep COX-1 at 20 uM by cayman colorimetric assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1141758Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors.
AID1550478Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 3 hrs post-carrageenan injection (Rvb = 4.79 +/-2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.
AID314262Inhibition of ovine COX2 by chemiluminescent assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
AID1250474Inhibition of human recombinant COX-2 using arachidonic acid after 15 mins by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.
AID254798Inhibitory concentration against COX-2; (valus obtained by Kato et al.)2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.
AID1752442Cytotoxicity against mouse RAW 264.7 cells assessed as decreased cell viability at 0.01 to 10 uM measured after 18 hrs by MTT assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID344875Antiinflammatory activity against po dosed carrageenan-induced rat foot paw edema after 3 hrs2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
AID1689626Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 2 hr by plethysmometer analysis (Rvb = 3.28 +/- 0.41 mm)2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.
AID293937Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 50 mg/kg, po after 3 hrs2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
AID1551017Inhibition of ovine COX2 assessed as reduction in oxidized TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetric assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.
AID1336922Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID711035Inhibition of human recombinant CA14 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1434430Inhibition of Vibrio cholerae Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1752436Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.
AID1559630Inhibition of COX2 human HCA7 cells2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.
AID312237Analgesic activity in chronic model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 120 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1194025Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1713250Inhibition of potato 5-LOX assessed as reduction in hydroperoxide level by EIA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study.
AID657496Cytotoxicity against mouse RAW264.7 cells assessed as cell viability by propidium iodide staining based FACS-flow cytometry2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF₁ production.
AID1662955Inhibition of COX2 (unknown origin) up to 10 uM by ELISA2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents.
AID1846811Anti-inflammatory activity against carrageenan-induced paw edema in rat2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID497209Inhibition of human COX2 at 10 uM2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of novel pyrazole compounds.
AID162022In vitro inhibitory activity against prostaglandin G/H synthase 1 from ovine2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors.
AID342463Half life in human plasma2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID1311640Inhibition of cell adhesion in human HeLa cells assessed as reduction in cell attachment up to 8 uM after 1 hr by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID711040Inhibition of human recombinant full length CA6 pre-incubated for 15 mins by stopped-flow CO2 hydration method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
AID1069515Antiinflammatory activity in Wistar rat lambda carrageenan-induced pleurisy model assessed as decrease in number of leukocytes in pleural space at 20 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs relative t2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID161491In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 1 enzyme was determined2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.
AID369275Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID432204Inhibition of ovine COX1 by enzyme-immuno assay2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1262449Inhibition of human recombinant COX-2 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.
AID387743Antiinflammatory activity against po dosed carrageenan-induced rat foot paw edema model2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis of new 4-[2-(4-methyl(amino)sulfonylphenyl)-5-trifluoromethyl-2H-pyrazol-3-yl]-1,2,3,6-tetrahydropyridines: a search for novel nitric oxide donor anti-inflammatory agents.
AID1727721Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate measured after 10 mins by fluorometric based multimode microplate reader
AID635999Inhibition of COX-2 in LPS-stimulated rat leukocytes assessed as reduction in PGE2 production from arachidonic acid at 10 nM preincubated for 10 mins by EIA2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis, anti-inflammatory activity and molecular docking studies of 2,5-diarylfuran amino acid derivatives.
AID669119Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID1077236Antiinflammatory activity in Wistar albino rat assessed as inhibition of formalin-induced paw edema at 50 mg/kg, po administered 1 hr prior to formalin challenge measured after 2 hrs relative to control2014European journal of medicinal chemistry, Apr-09, Volume: 76Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.
AID1443238Inhibition of COX2 in mouse RAW264.7 cells assessed as LPS-induced PGE2 production at 50 uM after 24 hrs by enzyme immunoassay relative to control2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.
AID382815Selectivity for human recombinant COX2 over human platelet COX12008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.
AID160262Inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood at 10 uM2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID362870Inhibition of COX22008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Exploration of physicochemical properties and molecular modelling studies of 2-sulfonyl-phenyl-3-phenyl-indole analogs as cyclooxygenase-2 inhibitors.
AID1859070Inhibition of COX-1 (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
AID568556Inhibition of human COX12011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Structure-based parallel medicinal chemistry approach to improve metabolic stability of benzopyran COX-2 inhibitors.
AID1733228Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 40 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 2 days by plethysmometeric method 2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID312229Analgesic activity in acute model Wistar rat assessed as reversal of carrageenan-induced hind paw edema at 10 mg/kg, po after 60 mins by mechanical hyperalgesia test relative to celecoxib2008Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
New celecoxib derivatives as anti-inflammatory agents.
AID1311604Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID669116Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID162630In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID457928Inhibition of ovine COX1 by enzyme immunoassay2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
AID162018In vitro inhibitory activity against Prostaglandin G/H synthase 1 (COX-1)2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors.
AID493886Inhibition of human recombinant carbonic anhydrase 4 after 15 mins by stopped-flow CO2 hydration assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
AID304225Selectivity for human COX2 over human COX12007Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors.
AID585222Inhibition of MDR1 in methicillin-resistant Staphylococcus aureus ATCC 335913 assessed as increase in accumulation of chloramphenicol by EtBr efflux using flow cytometer2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID160400In vitro percent inhibition of prostaglandin G/H synthase 2 (COX-2) in human whole blood at 1 uM2003Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
AID229414Selectivity ratio for COX-1 over COX-22002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)
AID1667492Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.
AID302423Antiinflammatory activity against carrageenan-induced hyperalgesia in rat assessed as paw pressure in rat at 10 mg/kg, po after 30 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
AID585015Antibacterial activity against Staphylococcus aureus ATCC 292132011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
AID1204713Inhibition of human recombinant COX2 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay2015Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities.
AID1336923Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.
AID1751858Drug concentration in C57BL/6J mouse portal vein plasma at 10 mg/kg, po administered as cassette dose measured at 4 hrs by LC/MS/MS analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID1595299Anti-inflammatory activity against carrageenan-induced albino rat paw edema model assessed as inhibition of carrageenan-induced right hind paw edema at 10 umol/kg, sc treated 1 hr prior to carrageenan challenge and measured at 2 hrs after carrageenan trea2019European journal of medicinal chemistry, Jun-01, Volume: 171New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.
AID733814Antiinflammatory activity in Sprague-Dawley/Wistar rat assessed as decrease in carrageenan-induced hyperalgesia at 3 mg/kg, po administered 4 hrs after carrageenan-challenge measured after 30 mins (Rvb = 34.8 +/- 3.0 g)2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.
AID315992Inhibition of COX2 in human whole blood assessed as effect on LPS-stimulated PGE2 production2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides.
AID301224Inhibition of ovine COX2 by enzyme immuno assay2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Novel (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic ester prodrugs possessing a diazen-1-ium-1,2-diolate moiety: design, synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
AID229415Selectivity ratio (COX-1/COX-2)2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.
AID1576170Ulcerogenic activity in rat assessed as ulcer index at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID432550Selectivity ratio of IC50 for human COX1 to IC50 for human COX2 expressed in baculovirus-infected SF9 cells2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
AID1311607Antiproliferative activity against human A549 cells after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.
AID1434440Inhibition of human COX2 at 100 uM using arachidonic acid as substrate after 2 mins by fluorometric substrate-based fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Chemical synthesis and biological evaluation of ω-hydroxy polyunsaturated fatty acids.
AID1464291Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay
AID1142447Antiinflammatory activity in po dosed albino rat assessed as inhibition of carrageenan-induced paw edema administered 1 hr prior challenge measured 2 hrs post challenge2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID363512Selectivity ratio of IC50 for COX1 in arachidonic acid-stimulated mouse J774 cells to IC50 for COX2 in LPS-stimulated mouse J774 cells2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1576172Ulcerogenic activity in rat assessed as average number of ulcers formed at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days2019MedChemComm, Oct-01, Volume: 10, Issue:10
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.
AID1565330Antiinflammatory activity in Sprague-Dawley rat model of carrageenan-induced thermal hyperalgesia assessed as paw withdrawal latency pressure at 50 mg/kg, po administered 1 hr prior to carrageenan challenge and measured after 1 hr by Von-frey test (Rvb = 2019European journal of medicinal chemistry, Nov-15, Volume: 182Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.
AID592802Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1751849Selectivity ratio of IC50 for COX1 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production to IC50 for COX2 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
AID162020In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles2004Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
AID1069514Plasma concentration in Wistar rat lambda carrageenan-induced pleurisy model at 5 mg/kg, ip pretreated for 30 mins followed by lambda carrageenan-challenge measured after 4 hrs by SPE-HPLC analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1796989Carbonic Anhydrase Enzyme Inhibition Assay from Article 10.1021/jm030912m: \\Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.\\2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1801480In vitro Cyclooxygenase (COX) Inhibition Assay from Article 10.1016/j.bioorg.2015.09.002: \\1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.\\2015Bioorganic chemistry, Dec, Volume: 631-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.
AID1800496Cyclooxygenase (COX) Inhibition Assay from Article 10.1111/cbdd.12324: \\Synthesis and biologic evaluation of substituted 5-methyl-2-phenyl-1H-pyrazol-3(2H)-one derivatives as selective COX-2 inhibitors: molecular docking study.\\2014Chemical biology & drug design, Oct, Volume: 84, Issue:4
Synthesis and biologic evaluation of substituted 5-methyl-2-phenyl-1H-pyrazol-3(2H)-one derivatives as selective COX-2 inhibitors: molecular docking study.
AID1802571COX-1/COX-2 Inhibition Colorimetric Assay from Article 10.1016/j.bioorg.2016.11.008: \\Design, synthesis, cyclooxygenase inhibition and biological evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing amino/methanesulfonyl pharmaco
AID1802056In vitro COX Inhibition Assay from Article 10.1016/j.bioorg.2016.10.003: \\Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibi2016Bioorganic chemistry, 12, Volume: 69Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibitors: A hybrid pharmacophore approach.
AID1802573COX Inhibition Assay from Article 10.1016/j.bioorg.2016.11.014: \\In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings.\\2017Bioorganic chemistry, 02, Volume: 70In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings.
AID1802609In Vitro COX-1 and COX-2 Inhibitory Assay from Article 10.1016/j.bioorg.2017.03.012: \\New hybrid molecules combining benzothiophene or benzofuran with rhodanine as dual COX-1/2 and 5-LOX inhibitors: Synthesis, biological evaluation and docking study.\\2017Bioorganic chemistry, 06, Volume: 72New hybrid molecules combining benzothiophene or benzofuran with rhodanine as dual COX-1/2 and 5-LOX inhibitors: Synthesis, biological evaluation and docking study.
AID1798769CA Inhibition Assay from Article 10.1021/jm801267c: \\Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.\\2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1802788COX Inhibitor Screening Assay from Article 10.1016/j.bioorg.2017.04.012: \\Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors.\\2017Bioorganic chemistry, 06, Volume: 72Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors.
AID1799729Enzyme Inhibition Assay from Article 10.1080/14756360802188404: \\Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.\\2009Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 24, Issue:1
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.
AID1798182COX Inhibitor Screening Assay from Article 10.1021/jm0510474: \\Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.\\2006Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
AID1796771CA Inhibition Assay from Article 10.1021/jm050333c: \\Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide compl2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
AID1803031COX Inhibition Assay from Article 10.3109/14756366.2010.550890: \\Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity.\\2011Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 26, Issue:6
Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity.
AID1798985CA Inhibition Assay from Article 10.1021/jm9000488: \\Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.\\2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1800497In vitro COX-1 and COX-2 inhibition assay from Article 10.1111/cbdd.12336: \\Synthesis, molecular docking, and biological evaluation of some novel hydrazones and pyrazole derivatives as anti-inflammatory agents.\\2014Chemical biology & drug design, Oct, Volume: 84, Issue:4
Synthesis, molecular docking, and biological evaluation of some novel hydrazones and pyrazole derivatives as anti-inflammatory agents.
AID1799266CA Inhibition Assay from Article 10.1016/j.bmc.2009.05.002: \\Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.\\2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID1801526In vitro Cyclooxygenase Inhibition Assay from Article 10.1016/j.bioorg.2015.11.001: \\Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.\\2016Bioorganic chemistry, Feb, Volume: 64Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.
AID1802579In Vitro Cyclooxygenase (COX) Inhibition Assay from Article 10.1016/j.bioorg.2016.12.008: \\Design, synthesis and biological screening of some novel celecoxib and etoricoxib analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric s
AID1802610In Vitro Lipoxygenase (LOX) Inhibitory Assay from Article 10.1016/j.bioorg.2017.03.012: \\New hybrid molecules combining benzothiophene or benzofuran with rhodanine as dual COX-1/2 and 5-LOX inhibitors: Synthesis, biological evaluation and docking study.\\2017Bioorganic chemistry, 06, Volume: 72New hybrid molecules combining benzothiophene or benzofuran with rhodanine as dual COX-1/2 and 5-LOX inhibitors: Synthesis, biological evaluation and docking study.
AID1798982CA Inhibition Assay from Article 10.1021/jm9003126: \\Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.\\2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID1802057Enzyme Kinetics Assay from Article 10.1016/j.bioorg.2016.10.003: \\Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibitors: A 2016Bioorganic chemistry, 12, Volume: 69Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibitors: A hybrid pharmacophore approach.
AID1802596In Vitro COX Inhibition Assay from Article 10.1016/j.bioorg.2017.02.006: \\Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analg2017Bioorganic chemistry, 04, Volume: 71Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents.
AID1796990hCA IX Enzyme Inhibition Assay from Article 10.1021/jm030912m: \\Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.\\2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1802612Cyclooxygenase Inhibition Assay from Article 10.1016/j.bioorg.2017.04.002: \\New 1,2-diaryl-4-substituted-benzylidene-5-4H-imidazolone derivatives: Design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents.\\
AID1345206Human COX-2 (Cyclooxygenase)2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
AID1345206Human COX-2 (Cyclooxygenase)2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1345284Human COX-1 (Cyclooxygenase)2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
AID1346210Human carbonic anhydrase 12 (4.2.1.1 Carbonate dehydratases)2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1811Experimentally measured binding affinity data derived from PDB2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID493017Wombat Data for BeliefDocking2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5,052)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's77 (1.52)18.2507
2000's2296 (45.45)29.6817
2010's2146 (42.48)24.3611
2020's533 (10.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 144.94

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index144.94 (24.57)
Research Supply Index8.72 (2.92)
Research Growth Index5.65 (4.65)
Search Engine Demand Index275.30 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (144.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials843 (15.99%)5.53%
Reviews455 (8.63%)6.00%
Case Studies247 (4.68%)4.05%
Observational10 (0.19%)0.25%
Other3,718 (70.51%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (526)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Anti-Angiogenic Chemotherapy: A Phase II Trial of the Oral 5-Drug Regimen (Thalidomide, Celecoxib, Fenofibrate, Etoposide and Cyclophosphamide) in Patients With Relapsed or Progressive Cancer [NCT00357500]Phase 2101 participants (Actual)Interventional2005-01-31Completed
A Study to Evaluate Efficacy and Safety of Postoperative Intravenous Parecoxib Sodium Followed by Oral Celecoxib Post Total Knee Arthroplasty in Osteoarthritis Patients [NCT02198924]Phase 4246 participants (Actual)Interventional2014-12-31Completed
99Tc-MDP Versus Celecoxib Treatment in Patients With Knee Osteoarthritis [NCT02993029]40 participants (Anticipated)Interventional2017-09-01Recruiting
Tramadol Versus Celecoxib for Reducing Pain Associated With Outpatient Hysteroscopy: A Randomized Double Blind Placebo-Controlled Trial [NCT02071303]Phase 2210 participants (Actual)Interventional2014-05-31Completed
Epigenetically-Modified Autologous Tumor Cell Vaccines With ISCOMATRIX(TM) Adjuvant and Oral Celecoxib in Patients Undergoing Resection of Lung and Esophageal Cancers, Thymic Neoplasms, Thoracic Sarcomas, and Malignant Pleural Mesotheliomas [NCT01258868]Phase 144 participants (Actual)Interventional2010-12-01Terminated
Effect of Selective and Nonselective Cyclooxygenase Enzyme Inhibition on Arterial Blood Pressure and Cerebral Blood Flow With Exposure to Intermittent Hypoxia in Humans [NCT01280006]Phase 1/Phase 212 participants (Actual)Interventional2011-01-31Completed
Epigenetically-Modified Autologous Tumor Cell Vaccs and ISCOMATRIX(TM) Adjuvant With Metronomic Oral Cyclophosphamide and Celecoxib in Pts Undergoing Resection of Sarcomas, Melanomas, Germ Cell Tumors, or Epithelial Malignancies Metastatic to Lungs, Pleur [NCT01341496]Phase 141 participants (Actual)Interventional2011-04-18Terminated
A Phase II Trial Using a Combination of Oxaliplatin, Capecitabine, and Celecoxib With Concurrent Radiation for Patients With Newly Diagnosed Resectable Rectal Cancer [NCT00250835]Phase 238 participants (Actual)Interventional2005-04-30Terminated(stopped due to Low accrual)
Airway Intervention Registry (AIR) Extension: Recurrent Respiratory Papillomatosis [NCT03465280]400 participants (Anticipated)Observational [Patient Registry]2018-04-01Recruiting
Efficacy and Safety of Ningmitai Capsule Alone or Combined With Celecoxib in the Treatment of Chronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS): A Prospective, Randomized, Double-blind, Multicenter Clinical Study [NCT06159114]Phase 4240 participants (Anticipated)Interventional2023-12-01Not yet recruiting
Maintenance Treatment for Ovarian Carcinoma in Remission by an Antiangiogenic Treatment Strategy With Metronomic/Oral Chemotherapy (Cytophosphan Combined With Low-dose Methotrexate)and COX-2 Inhibition (Celecoxib) [NCT01175772]Phase 26 participants (Actual)Interventional2010-08-31Terminated(stopped due to Due to change in the national policy of medications)
Adjuvant Tumor Lysate Vaccine and Iscomatrix With or Without Metronomic Oral Cyclophosphamide and Celecoxib in Patients With Malignancies Involving Lungs, Esophagus, Pleura, or Mediastinum [NCT02054104]Phase 1/Phase 221 participants (Actual)Interventional2014-09-03Terminated(stopped due to Vaccine production halted in 2015, thus study is terminated.)
Open Label, Off Label Study to Evaluate the Safety, Tolerability and Preliminary Efficacy of Ciprofloxacin/Celecoxib Combination in Patients With ALS [NCT04090684]Phase 110 participants (Actual)Interventional2019-12-09Completed
A Pilot Study Assessing the Treatment Responsiveness of a Novel Osteoarthritis Stiffness Scale [NCT03570554]Phase 241 participants (Actual)Interventional2018-06-29Completed
Open-Label, Multicentre, Controlled Study Of Exemestane (Aromasin®) With Or Without Celecoxib (Celebrex®) In Postmenopausal Women With Advanced Breast Cancer (ABC) Having Progressed On Tamoxifen [NCT00038103]Phase 2111 participants (Actual)Interventional2002-01-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Efficacy, Tolerability, Safety and Pharmacokinetic Study of Single Doses of DFN-15 in Post-Surgical Dental Pain [NCT03554772]Phase 2120 participants (Actual)Interventional2018-06-19Completed
Opioid-Free Shoulder Arthroplasty [NCT03540030]Phase 486 participants (Actual)Interventional2016-09-30Completed
A Phase I/II Trial of a COX-2 Inhibitor, Celebrex (Celecoxib), [National Screening Committee# 719627] With Limited Field Radiation for Intermediate Prognosis Patients With Locally Advanced Non-Small Cell Lung Cancer, With Analysis of Prognostic Factors [NCT00046839]Phase 1/Phase 221 participants (Actual)Interventional2002-07-31Completed
Pre vs. Postoperative Adductor Canal Block for Total Knee Arthroplasty: Prospective Randomized Trial [NCT05974501]Phase 484 participants (Anticipated)Interventional2023-09-29Recruiting
Phase 2a Study Evaluating a Chemokine-Modulatory Regimen in Patients With Colorectal Cancer Metastatic to the Liver [NCT03403634]Phase 219 participants (Actual)Interventional2018-04-19Completed
An Open Label Trial of Celecoxib in the Treatment of Mild Thyroid Eye Disease [NCT02845336]Phase 27 participants (Actual)Interventional2017-03-05Terminated(stopped due to Poor enrollment)
A Trial Assessing the Outcome of Celecoxib Administration Versus Placebo Following Anterior Cruciate Ligament Reconstruction [NCT01186887]40 participants (Actual)Interventional2009-02-28Completed
A Multi-center, Double-blinded, Randomized, Active-controlled, Parallel Design, phaseII Study to Investigate the Efficacy and Safety of YYC301 in Subject With Knee Osteoarthritis. [NCT03850587]Phase 2261 participants (Actual)Interventional2018-08-30Completed
Traditional vs. Nonopioid Analgesia After Rotator Cuff Repair [NCT03818919]Phase 2100 participants (Anticipated)Interventional2019-01-22Recruiting
Open-Label, Three Way, Randomized, Single Dose Crossover Study Comparing Bioavailability of DFN-15 Oral Solution Under Fasting Conditions vs Comparator Under Fed Conditions and to Determine Food Effect of DFN-15 in Healthy Adult Subjects [NCT03282838]Phase 124 participants (Actual)Interventional2017-06-09Completed
Comparison of Analgesic Efficacy Among Pregabalin, Celecoxib, Pregabalin With Celecoxib and Placebo After Total Knee Arthroplasty Under Intrathecal Morphine [NCT01344213]Phase 4100 participants (Actual)Interventional2008-07-31Completed
Window of Opportunity Study Targeting the Inflammatory Milieu of Pregnancy Associated Breast Cancer [NCT01881048]Early Phase 142 participants (Actual)Interventional2009-12-08Active, not recruiting
[NCT02408146]80 participants (Anticipated)Interventional2014-01-31Recruiting
A Phase Ib Study of Chidamide in Combination With Celecoxib in Patients With Metastatic Colorectal Cancer Who Had Progression or Were Intolerant of at Least Two Lines of Systemic Therapies (CCmCC) [NCT05281276]Phase 112 participants (Anticipated)Interventional2022-09-20Recruiting
A Randomized Control Trial Study of the Efficacy of Celecoxib Versus Ketorolac for Perioperative Pain Control [NCT03331315]Phase 2170 participants (Actual)Interventional2013-09-01Completed
RESILIENCE: Effect of Comprehensive Celecoxib Through Treatment for Advanced-Stage Head and Neck Cancer: A Randomized, Double-Blinded, Placebo-Controlled Trial [NCT04162873]Phase 260 participants (Anticipated)Interventional2019-11-27Recruiting
Arginine Supplementation to Improve Cardiovascular and Endothelial Function After NSAID Treatment (ASCENT) [NCT04765644]Phase 444 participants (Actual)Interventional2021-06-10Completed
N2012-01: Phase 1 Study of Difluoromethylornithine (DFMO) and Celecoxib With Cyclophosphamide/Topotecan for Patients With Relapsed or Refractory Neuroblastoma [NCT02030964]Phase 130 participants (Anticipated)Interventional2013-12-31Active, not recruiting
A Phase 1, Multi-center, Open-label, 3-arm, Fixed Sequence Study to Assess the Effect of Co-administration of AZD9833 on the Pharmacokinetics of Midazolam (CYP3A4/5 Substrate), of Omeprazole (CYP2C19 Substrate), of Celecoxib (CYP2C9 Substrate) and of Dabi [NCT05438303]Phase 159 participants (Actual)Interventional2022-06-13Completed
Efficacy and Safety of Chuna Manual Treatment as an Adjunctive Therapy After Total Knee Arthroplasty: A Study Protocol for a Single-Center, Randomized, Assessor Blind, Parallel-Group Clinical Trial [NCT03625050]Phase 222 participants (Actual)Interventional2018-11-01Completed
A Multicenter Observational Study on the Use of Delivra-Celecoxib 8% Cream on Pain Experienced by Patients With Osteoarthritis of the Knees. [NCT03698916]6 participants (Actual)Observational2018-07-23Terminated(stopped due to Unable to recruit)
Multimodal Anesthesia and Analgesia for Total Shoulder and Reverse Total Shoulder Arthroplasty: A Randomized Controlled Trial [NCT03586934]Phase 30 participants (Actual)Interventional2018-06-01Withdrawn(stopped due to Difficult to enroll patients for the study)
[NCT02260336]80 participants (Anticipated)Interventional2014-10-31Enrolling by invitation
Intravitreal Celecoxib for Chronic Uveitis: A Phase I Investigational Safety Study [NCT02131012]Phase 14 participants (Actual)Interventional2015-06-30Terminated(stopped due to Difficulty recruiting)
A Randomized Controlled Trial on the Treatment of Severe Influenza A Infection [NCT02108366]Phase 3107 participants (Actual)Interventional2014-03-31Completed
RACIN, A Phase I Study of the Combination of Nivolumab Associated With Low-dose Radiation, Aspirin/ Celecoxib, and Either Ipilimumab or Low-dose Cyclophosphamide, Followed by Nivolumab Maintenance, in Patients With Advanced, TIL-negative Solid Tumors [NCT03728179]Phase 150 participants (Anticipated)Interventional2019-01-16Active, not recruiting
Effect of Acupuncture to Endothelial Dysfunction Induced by Ischemia-reperfusion Injury Via Adenosine Triphosphate-sensitive Potassium Channels or Prostaglandin Pathway [NCT02255006]36 participants (Anticipated)Interventional2014-05-31Recruiting
A Double-Blind, Placebo-Controlled, Randomized Comparison Study of the Efficacy of Celebrex 400 mg Single Dose Pre and Celebrex 200 mg Post Ambulatory Arthroscopic Knee Surgery for Total Analgesic Use After Surgery [NCT00633438]Phase 4204 participants (Actual)Interventional2004-01-31Completed
A Registry-Based Observational Study Assessing Clinical Outcomes In Familial Adenomatous Polyposis In Patients Receiving Celecoxib (Celebrex(Registered), Onsenal(Registered)) Compared With Control Patients [NCT00151476]68 participants (Actual)Observational2004-11-30Terminated(stopped due to See Detailed Description)
Traditional vs. Nonopioid Analgesia After Anterior Cruciate Ligament Reconstruction [NCT03818932]Phase 2/Phase 362 participants (Actual)Interventional2019-01-22Completed
Double-Blind, Triple Dummy, Parallel-Group, Randomized, Six-Month Study To Compare Celecoxib (200 Mg BID) With Diclofenac Sr (75 Mg BID) Plus Omeprazole (20 Mg QD) For Gastrointestinal Events In Subjects With Osteoarthritis And Rheumatoid Arthritis At Hig [NCT00141102]Phase 44,484 participants (Actual)Interventional2005-10-31Completed
"Double-Blind Parallel-Group Randomized Study Of Efficacy And Safety Of Continuous Use Of Celecoxib Vs. The Usual Use Of Celecoxib In The Treatment Of Subjects With Chronic Osteoarthritis Of The Hip Or Knee Who Require an Anti-inflammatory Medication for [NCT00139776]Phase 4875 participants (Actual)Interventional2005-07-31Completed
Factors Affecting the Speed of Recovery After Anterior Cruciate Ligament Reconstruction [NCT03770806]48 participants (Actual)Interventional2017-03-24Completed
Single Dose Oral Celecoxib (With or Without Acetaminophen) for Acute Post-operative Pain Following Impacted Third Molar Surgery. [NCT04790812]Phase 4100 participants (Anticipated)Interventional2021-04-22Recruiting
A Randomized, Factorial-Design, Phase II Trial of Temozolomide Alone and in Combination With Possible Permutations of Thalidomide, Isotretinoin and/or Celecoxib as Post-Radiation Adjuvant Therapy of Glioblastoma Multiforme [NCT00112502]Phase 2178 participants (Actual)Interventional2005-09-30Completed
Gastrointestinal (GI) Randomized Event And Safety Open-Label NSAID Study (GI-Reasons): A Randomized, Open-Label, Blinded-Endpoint, Parallel-Group Trial Of GI Safety Of Celecoxib Compared With Non-Selective Nonsteroidal Antiinflammatory Drugs (NSAIDS) In O [NCT00373685]Phase 48,067 participants (Actual)Interventional2006-10-31Completed
Multi-center, Randomized, Double Blinded, Active-controlled Phase III Clinical Trial to Assess the Efficacy and Safety of SKCPT in Patients With Knee Osteoarthritis [NCT05930080]Phase 3278 participants (Actual)Interventional2021-01-28Completed
Clinical Research of the Prognostic Influence of NSAIDS's Anti-inflammatory Effect on Senior Patients With Hip Fracture [NCT01583660]800 participants (Anticipated)Observational2012-01-31Recruiting
An Open-label Study in Healthy Subjects to Assess the Effect of Once-daily Multiple Dosing of AKB-6548 on the Pharmacokinetics of the CYP2C9 Substrate Celecoxib [NCT02502500]Phase 112 participants (Actual)Interventional2015-07-31Completed
Chinese Spondyloarthritis Inception Cohort [NCT05960864]1,000 participants (Anticipated)Observational2024-02-29Not yet recruiting
Multimodal Nonopioid Pain Protocol Following Shoulder Arthroplasty Surgery [NCT05488847]Phase 480 participants (Anticipated)Interventional2022-06-25Recruiting
The Effect of Celecoxib on Neuroinflammation in MDD: PET Imaging of a Novel Treatment Target With [18F]FEPPA [NCT04814355]Phase 442 participants (Anticipated)Interventional2018-08-01Recruiting
Neoadjuvant Immune Checkpoint Inhibition and Novel IO Combinations in Early-stage Colon Cancer (Amended Protocol of: Nivolumab, Ipilimumab and COX2-inhibition in Early Stage Colon Cancer: an Unbiased Approach for Signals of Sensitivity: The NICHE TRIAL) [NCT03026140]Phase 2268 participants (Anticipated)Interventional2017-03-29Recruiting
Celecoxib Versus Hyoscine Butyl-bromide in Reducing Pain Perception During Copper T380A Intrauterine Device Insertion: a Randomized Double-blind Controlled Trial [NCT03499743]105 participants (Actual)Interventional2018-04-20Completed
NSAIDs vs. Coxibs in the Presence of Aspirin: Effects on Platelet Function, Endothelial Function, and Biomarkers of Inflammation in Subjects With Rheumatoid Arthritis and Increased Cardiovascular Risk or Cardiovascular Disease [NCT03699293]Phase 430 participants (Anticipated)Interventional2018-09-22Recruiting
A Phase IV Open Label Randomized Multicenter Comparative Study Of Celecoxib Efficacy And Safety Versus Standard Doses Of Oral Diclofenac In Acute Pain Due To Cervical Sprain Related To Motor Vehicle Accident [NCT00894790]Phase 48 participants (Actual)Interventional2009-11-30Terminated(stopped due to See termination reason in detailed description.)
Evaluation of Anticancer Effect of Celecoxib as Adjuvant Therapy to Chemotherapy in Patients With Metastatic Colorectal Cancer [NCT03645187]Phase 450 participants (Anticipated)Interventional2018-08-01Recruiting
A Prospective Randomized Placebo Controlled Study to Evaluate the Effect of Celecoxib on the Efficacy and Safety of Amlodipine on Renal and Vascular Function in Subjects With Existing Hypertension Requiring Antihypertensive Therapy [NCT02979197]Phase 3105 participants (Actual)Interventional2016-11-03Completed
A Prospective, Randomized, Double-blinded, Double-dummy, Active-controlled, Multi-center, Interventional Study to Compare Gastro-protective Effect and Pain Relief Effect of Naxozol Compared to Celecoxib in Patients With Osteoarthritis [NCT02355236]Phase 4106 participants (Anticipated)Interventional2015-02-28Recruiting
Celecoxib for the Treatment of Non-muscle Invasive Bladder Cancer [NCT02343614]Phase 258 participants (Actual)Interventional2003-03-31Completed
Comparison of Postoperative Pain Management in Patients Undergoing Laparoscopic Colorectal Surgery Under Enhanced Recovery After Surgery (ERAS) Program, Laparoscopic Colorectal Surgery Without ERAS and Open Colorectal Surgery [NCT04997174]162 participants (Anticipated)Observational2021-10-31Recruiting
Adjunctive Use of Celecoxib in the Treatment of Bipolar Postpartum Depression: a Randomized, Double-blind, Placebo-controlled Trial [NCT02726659]Phase 31 participants (Actual)Interventional2016-05-31Terminated(stopped due to Difficulty recruiting participants because principal investigator noticed that the participants in the population were responding well to low doses of mood stabilizers and therefor would not be recruited into the study.)
I-SPY COVID TRIAL: An Adaptive Platform Trial to Reduce Mortality and Ventilator Requirements for Critically Ill Patients [NCT04488081]Phase 21,500 participants (Anticipated)Interventional2020-07-31Recruiting
Clinical Protocol for a Double-Blind, Placebo-Controlled, Randomized Dose-Ranging Study of Celecoxib (SC-58635) on the Acute Effect of Human UV-Irradiation [NCT02099136]Phase 245 participants (Actual)Interventional1999-09-30Completed
Phase I/II Study of Epirubicin and Celecoxib for Hepatocellular Carcinoma [NCT00057980]Phase 1/Phase 28 participants (Actual)Interventional2002-10-31Completed
Preemptive Analgesia in Total Knee Arthroplasty: Comparing the Effects of Single Dose Combined Celecoxib With Pregabaline and Repetition Dose Combined Celecoxib With Pregabaline (Double Blind Controlled Clinical Trial) [NCT03523832]Phase 230 participants (Actual)Interventional2015-07-01Completed
Gemcitabine and Celecoxib Combination Therapy in Treating Patients With R0 Resection Pancreatic Cancer [NCT03498326]Phase 2480 participants (Anticipated)Interventional2018-04-02Recruiting
Disitamab Vedotin Combined With Tislelizumab, Low-dose Capecitabine and Celecoxib as Salvage Therapy for HER2-positive Metastatic Colorectal Cancer: a Phase II Trial (DETECT) [NCT05578287]Phase 229 participants (Anticipated)Interventional2023-07-18Recruiting
A Randomized, Double-Blind, Multicenter, Placebo- and Active Comparator-Controlled Study to Evaluate Efficacy and Safety of MR308 in the Treatment of Acute Pain After Abdominal Hysterectomy Surgery Under General Anaesthesia (STARDOM2). [NCT03062644]Phase 31,138 participants (Actual)Interventional2017-04-05Completed
Oral Tramadol Versus Oral Celecoxib for Post-perineal Repair Analgesia After Spontaneous Vaginal Birth in Obese Women: A Randomised Controlled Trial [NCT03694873]Phase 4200 participants (Anticipated)Interventional2018-10-10Not yet recruiting
The Effects of Non-steroidal Anti-inflammatory Drugs on Circulating Markers of Bone Metabolism Following Plyometric Exercise in Humans [NCT05512013]Phase 112 participants (Actual)Interventional2022-02-15Completed
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524]Phase 12 participants (Actual)Interventional2020-04-01Active, not recruiting
Role of Oral Celecoxib 200 mg in Reducing Pain Associated With Colposcopic Directed Biopsy: A Randomized Triple-blind Placebo-controlled Trial [NCT03464552]Phase 4170 participants (Actual)Interventional2018-04-15Completed
STAMPEDE: Systemic Therapy in Advancing or Metastatic Prostate Cancer: Evaluation of Drug Efficacy: A Multi-Stage Multi-Arm Randomised Controlled Trial [NCT00268476]Phase 2/Phase 311,992 participants (Actual)Interventional2005-07-08Active, not recruiting
Decreasing Narcotics in Advanced Pelvic Surgery: A Randomized Study [NCT02110719]Phase 4138 participants (Actual)Interventional2014-03-31Completed
Phase I/II Trial Of Weekly Irinotecan And Docetaxel With The Addition Of Celecoxib In Advanced Non-Small Cell Lung Cancer [NCT00073866]Phase 1/Phase 20 participants Interventional2003-06-30Completed
A Phase III Study of YM177 (Postoperative Pain) -- An Etodolac- and Placebo-controlled, Multicenter, Double-blind, Group Comparison Study to Verify the Efficacy of YM177 (Celecoxib) in Postoperative Pain Patients -- [NCT01118572]Phase 3616 participants (Actual)Interventional2010-02-28Completed
A Two-Arm Phase II Chemoprevention Trial in Adenomatous Polyposis Coli Patients [NCT00033371]Phase 2205 participants (Actual)Interventional2001-12-13Completed
Metronomic Poly-chemotherapy for Metastatic Colorectal Cancer at Progression Following Established Treatments: Clinical and Laboratory Research [NCT02280694]Phase 245 participants (Actual)Interventional2015-01-31Completed
Prospective, Randomized, Open-label, Controlled Trial of Cyclooxygenase-2 Inhibitor (Celecoxib; Celebrex®) for Adjuvant Anticancer Effect in Patients With Biliary-pancreas Cancer. [NCT01111591]Phase 4220 participants (Anticipated)Interventional2008-11-30Enrolling by invitation
Manipulation Under Anesthesia (MUA) to Treat Postoperative Stiffness After Total Knee Arthroplasty: A Multicenter Randomized Clinical Trial [NCT02739035]Phase 4130 participants (Actual)Interventional2016-04-30Completed
Influence of the Celecoxib Administration Before Surgery for Endometrial Cancer on Indoleamine 2,3-dioxygenase 1 (IDO1) Tumor Expression and Immune Cells Tumor's Infiltration [NCT03896113]Phase 248 participants (Anticipated)Interventional2019-11-13Recruiting
Phase II Study of the Combination Carboplatin Plus Celecoxib in Heavily Pre-treated Recurrent Ovarian Cancer Patients [NCT01124435]Phase 245 participants (Actual)Interventional2003-10-31Completed
Effects of DFN-15 on Migraine With Allodynia [NCT03472378]Phase 251 participants (Actual)Interventional2018-05-09Completed
Allogeneic Tumor Cell Vaccine With Metronomic Oral Cyclophosphamide and Celecoxib as Adjuvant Therapy for Lung and Esophageal Cancers, Thymic Neoplasms, Thoracic Sarcomas, and Malignant Pleural Mesotheliomas [NCT01143545]Phase 110 participants (Actual)Interventional2010-12-07Terminated(stopped due to Closed accrual due to unpromising results and the opening of study 14C0053 targeting the same population.)
A Twelve Week, Randomized, Double Blind Parallel Group Study Of Two Doses Of Celecoxib Compared To Diclofenac In Patients With Ankylosing Spondylitis [NCT02528201]Phase 4330 participants (Actual)Interventional2002-09-30Completed
PECS Block vs. Multimodal Analgesia for Prevention of Persistent Postoperative Pain in Breast Surgery [NCT03084536]Phase 2134 participants (Actual)Interventional2017-06-07Completed
"NICE-COMBO: An Open Label Phase II Study Combining Nivolumab and Celecoxib in Patients With Advanced Cold Solid Tumors" [NCT03864575]Phase 268 participants (Anticipated)Interventional2019-08-15Not yet recruiting
Effect of Celebrex Pre-medication on the Intra and Post-treatment Endodontic Pain in Teeth With Symptomatic Irreversible Pulpitis: Double Blind Randomized Clinical Trial [NCT03339544]46 participants (Anticipated)Interventional2017-12-01Not yet recruiting
A Randomized, Placebo-Controlled, Parallel-Group, Double -Blind Study to Evaluate the Safety and Efficacy of Rofecoxib 12.5 mg and Celecoxib 200 mg in Patients With Osteoarthritis of the Knee [NCT00092365]Phase 3413 participants (Actual)Interventional2003-04-01Completed
Adjuvant Allogeneic Tumor Cell Vaccine With Metronomic Oral Cyclophosphamide and Celecoxib in Patients Undergoing Resection of Sarcomas, Melanomas, Germ Cell Tumors, or Epithelial Malignancies Metastatic to Lungs, Pleura, or Mediastinum [NCT01313429]Phase 119 participants (Actual)Interventional2011-03-04Terminated(stopped due to Per stopping rule if 12 patients underwent immune response analysis after 6 vaccinations and none developed a response, the protocol would stop accrual.)
Evaluation of Post-Procedure Administration of Celecoxib Following Shoulder Surgery: A Randomized Controlled Study [NCT03305068]Phase 4150 participants (Anticipated)Interventional2014-02-28Active, not recruiting
A Randomized, Open-label, Multiple-dose Clinical Trial to Evaluate the Safety/Tolerability and Pharmacokinetic Drug-drug Interaction Between DWP14012 and Three Different Kinds of NSAIDs in Healthy Male Volunteers [NCT04490434]Phase 1110 participants (Anticipated)Interventional2020-06-19Recruiting
Molecular Effects of Short-Term Celecoxib Treatment on Head and Neck Squamous Cell Carcinoma [NCT00596219]12 participants (Actual)Interventional2003-12-31Completed
INflammation-based Stratification for Immune-Targeted Augmentation in Major Depressive [NCT05644301]Phase 3240 participants (Anticipated)Interventional2023-01-31Not yet recruiting
Stress and Inflammation in the Pathophysiology of Late Life Depression [NCT02389465]Phase 4119 participants (Actual)Interventional2014-08-31Completed
The Effect of Celecoxib on Concurrent Chemoradiation With Weekly Nedaplatin in Nasopharyngeal Carcinoma [NCT02537925]Phase 3120 participants (Anticipated)Interventional2014-01-31Recruiting
A Double-Blind, Placebo-Controlled, Randomized Study of the Efficacy of Celecoxib as Add-on Therapy to Risperidone Versus Risperidone Alone in Patients With Schizophrenia [NCT00639483]Phase 2270 participants (Actual)Interventional2003-03-31Completed
Double-Blind, Placebo-Controlled, Randomized Two-Week Study, Comparing Small Bowel Lesions Associated With Celecoxib (200 mg BID) vs. Ibuprofen (800 mg TID) Plus Omeprazole (20 mg QD) [NCT00640809]Phase 4408 participants (Actual)Interventional2003-10-31Completed
Phase I/II Dose Escalation Trial of Induction and Concomitant Erlotinib and Celecoxib With Radiation Therapy for Treatment of Poor Prognosis Head and Neck Cancer, Including Reirradiation [NCT00970502]Phase 1/Phase 215 participants (Actual)Interventional2007-02-28Completed
A Single Center, Double-blind, Placebo-controlled Phase I Single-dose Cross-over Study in Healthy Subjects to Investigate the Inhibitory Effect of CG100649, Celecoxib, Naproxen, and Acetazolamide on the Activity of Cyclooxygenases (COX-1, COX-2) and Carbo [NCT00780325]Phase 126 participants (Actual)Interventional2008-10-31Terminated(stopped due to A total of three parts were planned for this study. The sponsor funded only Part 1, so that neither Part 2 nor Part 3 of this study has been conducted.)
Randomized, Double-Blind, Parallel Group, Placebo-Controlled Multi-Center Study Evaluating the Efficacy of PN400 (VIMOVO) Twice Daily (Bid) and Celecoxib Once Daily (qd) in Patients With Osteoarthritis of the Knee [NCT00665431]Phase 3610 participants (Actual)Interventional2008-04-30Completed
A Phase II/III Randomized, Double-Blind, Placebo-Controlled Clinical Trial Of Celecoxib In Subjects With Actinic Keratoses [NCT00027976]Phase 2/Phase 30 participants (Actual)Interventional2001-12-31Withdrawn
A Pilot, Open-Label, Randomized, Crossover, Pharmacokinetic Study Of Enhanced Bioavailability Formulations Of Celecoxib In Healthy Volunteers [NCT00813241]Phase 116 participants (Actual)Interventional2009-01-31Completed
The Clinical Efficacy of Non-steroidal Anti-inflammation Drugs in Patients With Benign Prostatic Hyperplasia: A Prospective Randomized Multicenter Trial [NCT00687388]Phase 40 participants (Actual)Interventional2008-05-31Withdrawn(stopped due to in order to prepare a new clinical trial to evaluate with pathological change)
A 26-Week, Randomized, Placebo- and Active-Comparator-Controlled, Parallel-Group, Double-Blind, 2-Part Study to Assess the Safety and Efficacy of Etoricoxib 30 mg Versus Celecoxib 200 mg in Patients With Osteoarthritis (Study 1) [NCT00092768]Phase 3500 participants (Actual)Interventional2004-03-01Completed
Randomized Study of Pre-Prostatectomy Celecoxib or Placebo [NCT02840162]Phase 234 participants (Actual)Interventional2001-05-31Terminated(stopped due to Drug safety concerns)
Phase I Evaluation of Adjuvant Oral Decitabine and Tetrahydrouridine With or Without Celecoxib in Patients Undergoing Pulmonary Metastasectomy [NCT02839694]Phase 10 participants (Actual)Interventional2016-07-07Withdrawn
A Phase 3, Open-Label, Randomized, Parallel Group Study to Evaluate the Efficacy and Safety of Intrapleural Administration of Adenovirus-Delivered Interferon Alpha-2b (rAd-IFN) in Combination With Celecoxib and Gemcitabine in Patients With Malignant Pleur [NCT03710876]Phase 353 participants (Actual)Interventional2019-01-21Active, not recruiting
A Multicentre, Comparative, Randomised, Double-blind, Double-dummy Clinical Trial on the Efficacy and Safety of Condrosulf Versus Celebrex and Versus a Placebo in the Treatment of Knee Osteoarthritis [NCT02079727]Phase 3604 participants (Actual)Interventional2014-06-12Completed
Clinical Protocol for an Open Label Study of Celecoxib (SC-58635) on the Acute Effect of Human UV-Irradiation [NCT02090933]Phase 225 participants (Actual)Interventional2004-03-31Completed
A Maintenance Protocol of Sirolimus in Combination With Metronomic Chemotherapy in Children With High-Risk Solid Tumors [NCT04469530]Phase 250 participants (Anticipated)Interventional2020-09-16Recruiting
Celecoxib Window of Opportunity Trial to Assess Tumor and Stroma Responses [NCT03185871]Phase 20 participants (Actual)Interventional2017-09-20Withdrawn(stopped due to Slow accrual)
Randomized Comparison of Two Pre-induction Analgesia Regimens: Multimodal vs Acetaminophen in the Reduction of Post-operative Pain Following Ureteroscopy With Lithotripsy for Kidney Stones Evaluated With Text Messaging [NCT03549611]Phase 40 participants (Actual)Interventional2018-08-01Withdrawn(stopped due to elected not to proceed with the study)
Effect of a Multimodal Pain Regimen on Pain Control, Patient Satisfaction and Narcotic Use in Orthopaedic Trauma Patients [NCT02160301]Phase 40 participants (Actual)Interventional2017-11-30Withdrawn(stopped due to Insufficient infrastructure/funding for enrollment)
Phase I/IIa Clinical Trial Evaluating the Safety and Efficacy of Rintatolimod Combined With IFNα2b (Bioferon®) to Enhance the Effectiveness of Pembrolizumab in Patients With Metastatic Triple Negative Breast Cancer [NCT05756166]Phase 1/Phase 212 participants (Anticipated)Interventional2023-12-30Not yet recruiting
Safety and Efficacy of Low-intensity Laser Therapy in the Treatment of Chronic Musculoskeletal Pain: a Multicenter Randomized Controlled Trail [NCT06009900]860 participants (Anticipated)Interventional2023-09-01Not yet recruiting
A Three-Part, Phase I Study Of Orally Administered GRC 27864, A Novel, Microsomal Prostaglandin E Synthase-1 Enzyme (mPGES-1) Inhibitor, To Evaluate The Safety, Tolerability And PK Of Single Ascending Doses In Healthy, Adult Subjects (Part 1a), And Of A S [NCT02179645]Phase 176 participants (Actual)Interventional2014-05-31Completed
Preemptive Analgesia Combination of Celecoxib and Pregabalin in Total Hip Arthroplasty: Comparison of the Effects of Single Dose and Repeated Doses (Double-Blind Randomized Clinical Trial) [NCT05509946]Phase 2/Phase 330 participants (Anticipated)Interventional2022-10-01Not yet recruiting
Phase II Clinical Trial of Tumour Vaccination By Intradermal Delivery of Autologous Dendritic Cells Transduced With Adenoviral Vector (AD5F35) Expressing Latent Membrane Protein-1 (LMP-1) and Latent Membrane Protein-2 (LMP-2) Genes in Combination With Cel [NCT00589186]Phase 235 participants (Anticipated)Interventional2007-11-30Active, not recruiting
"A Phase II Trial of Celecoxib Plus Chemotherapy [Docetaxel or Pemetrexed] in Patients With Previously Treated, COX Dependent Recurrent Non-Small Cell Lung Cancer" [NCT00520845]Phase 223 participants (Actual)Interventional2007-10-31Terminated(stopped due to slow accrual)
A Pilot, Open-Label, Randomized, Crossover, Pharmacokinetic Study Of Enhanced Bioavailability Celecoxib Formulations D1, D2 And D3 In Healthy Volunteers [NCT00925106]Phase 116 participants (Actual)Interventional2009-07-31Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study Of CP-195543 And Celecoxib Dual Therapy In The Treatment Of The Signs And Symptoms Of Rheumatoid Arthritis In Subjects Who Are Inadequately Controlled On Methotrexate [NCT00424294]Phase 270 participants (Actual)Interventional2006-06-30Terminated(stopped due to See Detailed Description field)
A Randomized, Blinded, Placebo-Controlled Study of the Effect of Naproxen, Aspirin, Celecoxib, or Clopidogrel on Gastroduodenal Healing [NCT00778193]Phase 4125 participants (Actual)Interventional2007-10-31Completed
Multiple-dose, Randomized, Subject and Observer Blinded, Placebo-controlled, Double-dummy Study of Epicutaneously Applied Ketoprofen Transfersome® Gel With or Without Combination With Oral Celecoxib for the Treatment of Muscle Pain Induced by Eccentric Ex [NCT01020279]Phase 182 participants (Actual)Interventional2009-10-31Completed
A Study of the Efficacy and Tolerability of Once Daily Celebrex (Celecoxib) and Three Times Daily Ibuprofen vs. Placebo in the Treatment of Subjects With Osteoarthritis of the Knee [NCT00630929]Phase 4388 participants (Actual)Interventional2003-01-31Completed
A Double-blind, Placebo-Controlled, Randomized, Comparison Study of the Efficacy of Celebrex 400 mg Single Dose Pre and Celebrex 200 mg Post Ambulatory Arthroscopic Knee Surgery for Total Analgesic Use After Surgery [NCT00633386]Phase 4200 participants (Actual)Interventional2003-02-28Completed
Modulating Celecoxib Induced Blood Pressure Changes by Timed Administration of Aspirin and the Human Chronobiome [NCT03590821]Early Phase 160 participants (Anticipated)Interventional2023-12-31Not yet recruiting
A Phase II Trial of Combination Therapy With Celecoxib and Taxotere for the Treatment of Stage D3 Prostate Cancer [NCT00215345]Phase 266 participants Interventional2002-08-31Recruiting
COmparison of the Effect of Treatment With NSAIDs Added to Anti-TNF Therapy Versus Anti-TNF Therapy Alone on Progression of StrUctural Damage in the Spine Over Two Years in Patients With ankyLosing Spondylitis: a Randomized Controlled Multicentre Trial [NCT02758782]Phase 4156 participants (Actual)Interventional2016-09-30Completed
Evaluating Celecoxib Activity in Mycobacterium Tuberculosis: A Whole Blood Bactericidal Activity Study in Healthy Volunteers [NCT02602509]Phase 118 participants (Actual)Interventional2015-11-30Completed
Development of Novel Diagnostic Tools and Therapeutic Strategies for Oral Cancer [NCT02739204]Phase 2270 participants (Anticipated)Interventional2013-11-30Recruiting
Celecoxib vs. Acetaminophen-codeine-caffeine for Postoperative Pain in Primary Elective Open Septorhinoplasty With Osteotomies: a Randomized Controlled Trial. [NCT04259333]Phase 460 participants (Anticipated)Interventional2020-03-01Recruiting
An Open-Label, Phase 1 Study in Healthy Volunteers to Evaluate the Drug-Drug Interaction Potential of CCX168 With Concomitant Medications [NCT06004947]Phase 132 participants (Actual)Interventional2016-01-14Completed
Effects of Duloxetine on Pain Relief After Total Knee Arthroplasty in Central Sensitization Patient : A Randomized, Controlled, Double-Blind Trial [NCT02600247]100 participants (Anticipated)Interventional2015-11-30Not yet recruiting
Rectal Abberant Crypt Foci And Other Intermediate Biomarkers For Sporadic Colorectal Neoplasia: Cross-Sectional Prevelance And Modulation By Celecoxib [NCT00043043]Phase 20 participants Interventional2003-05-31Completed
A 12-Week Symptomatic Effect Evaluation to Compare Celecoxib 200 mg QD, Celecoxib 200 mg BID and Diclofenac 75 mg SR BID in Patients With Ankylosing Spondylitis [NCT00648141]Phase 3458 participants (Actual)Interventional2003-01-31Completed
A Randomized, Double-blind, Placebo- and Active-Controlled, Multicenter, Phase 2 Trial to Evaluate the Efficacy and Safety of YH23537 in Patients With Osteoarthritis of the Knee [NCT02759198]Phase 2456 participants (Actual)Interventional2016-05-02Completed
AflacST1502: A Phase II Study of Sirolimus in Combination With Metronomic Chemotherapy in Children With Recurrent and/or Refractory Solid and CNS Tumors [NCT02574728]Phase 260 participants (Anticipated)Interventional2015-06-30Recruiting
Tramadol Versus Celecoxib in Reducing Pain Associated With IUD Insertion: A Double Blind Placebo Controlled Trial [NCT02827487]Phase 4210 participants (Anticipated)Interventional2016-07-01Recruiting
COX-2 Activity in Early and Advanced NSCLC and The Effect of Short-Term Administration of Specific COX-2 Inhibitors (Celecoxib) [NCT00653250]22 participants (Actual)Interventional2000-12-31Completed
Efficacy and Safety of Etanercept Dose Reduction in Patients With Ankylosing Spondylitis [NCT02638896]Phase 4100 participants (Anticipated)Interventional2016-01-31Not yet recruiting
Chemoprevention for Barrett's Esophagus Trial (CBET) [NCT00005878]Phase 20 participants Interventional2000-07-31Completed
[NCT02790203]100 participants (Anticipated)Interventional2016-06-30Not yet recruiting
Randomized, Double Blind, Positive- Controlled, Three-way Cross-over Human Experimental Biomarker Study of V116517 in Healthy Male Subjects [NCT02695745]Phase 137 participants (Actual)Interventional2011-09-30Completed
Open Label Study to Evaluate the Safety, Tolerability and Preliminary Efficacy of Ciprofloxacin/Celecoxib Combination in Patients With ALS [NCT04165850]Phase 216 participants (Actual)Interventional2019-11-25Completed
Tramadol Versus Celecoxib for Reducing Pain During Operative Office Hysteroscopy: A Double Blind Placebo Controlled Trial. [NCT02736071]Phase 3210 participants (Anticipated)Interventional2016-06-30Recruiting
Celecoxib as Adjuvant Biologic Therapy in Patients With Early Stage Head and Neck and Lung Cancer [NCT00527982]Phase 21 participants (Actual)Interventional2005-09-30Terminated(stopped due to Termination due to poor accrual.)
An Open-Label Study of Intraoperative CA-008 Administration in Subjects Undergoing Bunionectomy [NCT03885596]Phase 236 participants (Actual)Interventional2019-03-25Completed
Evaluation of a Novel PET Radioligand as an Inflammatory Biomarker in Musculoskeletal Conditions [NCT03912428]Phase 1111 participants (Anticipated)Interventional2019-06-14Recruiting
A Randomized, Double Blind, Parallel-group Study Of Cardiovascular Safety In Osteoarthritis Or Rheumatoid Arthritis Patients With Or At High Risk For Cardiovascular Disease Comparing Celecoxib With Naproxen And Ibuprofen [NCT00346216]Phase 424,081 participants (Actual)Interventional2006-10-04Completed
A Randomized, Open-Label Study Comparing the Efficacy and Safety of Lidocaine Patch 5% With Celecoxib 200 mg in Patients With Chronic Axial Low Back Pain [NCT00904397]Phase 498 participants (Actual)Interventional2004-07-31Terminated(stopped due to Rofecoxib was withdrawn from the market due to safety concerns.)
Multicentre，A Phase II/III Randomized Study of Adjuvant Anti-Angiogenesis Therapy for Patients of High-Risk Oral Cavity Cancer [NCT00934739]Phase 2/Phase 3150 participants (Actual)Interventional2007-06-30Terminated
A DOUBLE BLIND, RANDOMIZED, PLACEBO-CONTROLLED COMPARISON OF THE EFFICACY, SAFETY, AND TOLERABILITY OF CELECOXIB 100-150 MG, INCLUDING INITIAL DOSES OF 50 AND 100 MG, AND PLACEBO IN THE SYMPTOMATIC TREATMENT OF PATIENTS WITH PAINFUL PHARYNGITIS [NCT00402987]Phase 3269 participants (Actual)Interventional2006-12-04Completed
Effect of COX-2 (Cyclooxygenase-2) and EGFR (Epidermal Growth Factor Receptor) Suppression on Molecular Markers of Angiogenesis and Proliferation in Squamous Cell Carcinoma of Oral Cavity - Prospective Randomized Study. [NCT02748707]Phase 264 participants (Actual)Interventional2015-08-18Active, not recruiting
Comparing Etoricoxib and Celecoxib for Preemptive Analgesia for Acute Postoperative Pain in Patients Undergoing Arthroscopic Anterior Cruciate Ligament Reconstruction: A Randomized Controlled Trial [NCT01017380]Phase 330 participants (Actual)Interventional2008-01-31Completed
Traditional vs. Nonopioid Analgesia After Arthroscopic Meniscus Surgery [NCT03820193]Early Phase 161 participants (Actual)Interventional2019-01-22Completed
Phase I Pilot Toxicity/Methods Validation Study of Celecoxib in Genotype-Positive Children With Familial Adenomatous Polyposis [NCT00685568]Phase 122 participants (Actual)Interventional2002-11-21Completed
A Study of the Efficacy and Tolerability of Once Daily Celebrex (Celecoxib) and Three Times Daily Ibuprofen vs. Placebo in the Treatment of Subjects With Osteoarthritis of the Knee [NCT00620867]Phase 4393 participants (Actual)Interventional2002-10-31Completed
Voice-preserving Treatment of Laryngeal Papilloma [NCT00592319]Phase 210 participants (Actual)Interventional2005-05-31Terminated(stopped due to 03/01/2009,due to date close to termination of this funding/study period)
A Double-Blind, Placebo Controlled Study of the Efficacy and Tolerability of Once Daily Celebrex (Celecoxib) vs. Placebo in the Treatment of Subjects With Osteoarthritis of the Knee Non-Responsive to Naproxen and Ibuprofen [NCT00638807]Phase 4388 participants (Actual)Interventional2003-12-31Completed
A Randomized, Multicenter, Double-Blind, Double-Dummy Study Comparing the Efficacy and Tolerability of Once Daily Celebrex (Celecoxib) and Naproxen 500 mg Twice Daily in the 6-month Treatment of Subjects With Osteoarthritis of the Knee [NCT00643799]Phase 4586 participants (Actual)Interventional2004-03-31Completed
Randomized, Double-Blind, Multicenter, Active Controlled Parallel Group Study to Evaluate the Efficacy and Safety of Celecoxib Suspension Compared to Naproxen Suspension in Patients With JRA [NCT00652925]Phase 3225 participants (Actual)Interventional2002-10-31Completed
A Phase 3, Multicenter, Double-blind and Placebo and Active Control Study to Evaluate the Efficacy and Safety of X0002 Spray in Treatment of Subjects With Osteoarthritis of the Knee [NCT05324163]Phase 3180 participants (Actual)Interventional2021-09-29Completed
Transition From Acute to Chronic Back Pain : Effect of L-dopa,Gender,and Associated Brain Plasticity [NCT04082715]Phase 20 participants (Actual)Interventional2019-10-31Withdrawn(stopped due to we don't have enough research funding.)
A Multimodal Analgesia Protocol Adapted for Ambulatory Surgery [NCT04015908]Phase 4100 participants (Actual)Interventional2019-08-01Completed
A Phase 4, 6-week, Randomized Double Blind, Multicenter, Active-controlled Trial To Evaluate The Effects Of Celecoxib (Celebrex) Or Naproxen On Blood Pressure In Pediatric Subjects With Juvenile Idiopathic Arthritis. [NCT00807846]Phase 4201 participants (Actual)Interventional2009-09-30Completed
A Phase III Placebo-Controlled Trial Of Celecoxib In Genotype Positive Subjects With Familial Adenomatous Polyposis [NCT00585312]Phase 3106 participants (Actual)Interventional2006-09-30Terminated(stopped due to See termination reason in detailed description.)
Multicenter, Randomized, Double-blind, Placebo- and Active-controlled Study of Safety and Efficacy of Two Dosages of Epicutaneously Applied Diractin® (Ketoprofen in Transfersome® Gel) for the Treatment of Osteoarthritis of the Knee [NCT00716547]Phase 31,399 participants (Actual)Interventional2008-05-31Completed
Phase I, Randomized, Open-Label, 2-Way Crossover Study to Evaluate Relative Bioavailability of Single Oral Dose of Celecoxib Administered as Marketed Product, or Overencapsulated Capsule in Healthy Volunteers [NCT00729495]Phase 180 participants (Anticipated)Interventional2008-07-31Completed
An Open Label Randomized Multicenter Comparative Study On Celecoxib Efficacy And Safety Versus Non-Selective NSAID In Acute Pain Due To Ankle Sprain [NCT00446797]Phase 4278 participants (Actual)Interventional2007-05-31Completed
A Multicentered Randomized Study of Celebrex (Celecoxib) in Patients With Recurrent Respiratory Papillomatosis [NCT00571701]Phase 250 participants (Actual)Interventional2008-02-29Completed
Modulation of Arachidonic Acid Metabolism by Chemopreventive Agents in Smokers [NCT01021215]Phase 1/Phase 284 participants (Actual)Interventional2010-05-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Phase 4 Study To Compare The Effect Of Celecoxib 100 Mg BID, Loxoprofen 60 Mg TID And Placebo On The Gastroduodenal Mucosa In Healthy Subjects [NCT00994461]Phase 4190 participants (Actual)Interventional2009-11-30Completed
A Phase II Trial of Celecoxib Plus Interferon Alpha in Metastatic Renal Cell Carcinoma Patients With 3+ COX-2 Tumor Immunostaining [NCT01158534]Phase 217 participants (Actual)Interventional2006-03-31Completed
A Double-blind, Randomized, Multicenter, Noninferiority, Phase II Repeat Dose Study of CG100649 Versus Celecoxib in Osteoarthritis Patients [NCT01341405]Phase 2125 participants (Actual)Interventional2011-04-30Completed
A Randomized Double Blinded Placebo-controlled Trial to Compare the Effect of Hyoscine-N-butyl Bromide (HBB) or Celecoxib Administered Alone Versus in Combination to Reduce Pain in Patients Undergoing Office Hysteroscopy. [NCT05911126]180 participants (Anticipated)Interventional2023-06-13Not yet recruiting
Prevention of Progression of Duodenal Adenomas to Cancer in Patients With Familial Adenomatous Polyposis (FAP) [NCT00808743]Phase 2/Phase 337 participants (Actual)Interventional2009-05-31Completed
A Randomized, Multicenter, Active And Placebo Controlled Parallel Group Study To Evaluate The Efficacy And Safety Of Celecoxib (Ym177) 200 Bid Compared To Loxoprofen 60 Mg Tid In Patients With Low Back Pain [NCT00141154]Phase 31,234 participants (Actual)Interventional2004-10-31Completed
Phase 4 Study of the Effect of Celecoxib on the Antiplatelet Effect of Aspirin and Clopidogrel [NCT00882388]Phase 440 participants (Actual)Interventional2005-03-31Completed
the Role of COX-2 Inhibitor(CELECOXIB) in Combination With Chemoradiation in Locally Advanced Head & Neck Carcinoma, Phase III Randomized Clinical Trial [NCT00603759]Phase 3122 participants (Actual)Interventional2006-04-30Active, not recruiting
A Multicenter, Randomized, Double-Blind, Double-Dummy Study Of The Safety, Tolerability And Efficacy Of Celecoxib 200 Mg Twice A Day (With A 400 Mg Attack Dose) Versus Sodium Diclofenac 75 Mg Twice A Day In Subjects With Acute Low Back Pain [NCT00640432]Phase 4244 participants (Actual)Interventional2003-10-31Completed
A Phase II Study of Metronomic and Targeted Anti-angiogenesis Therapy for Children With Recurrent/Progressive Medulloblastoma, Ependymoma and ATRT [NCT01356290]Phase 2100 participants (Anticipated)Interventional2014-04-30Recruiting
Cyclooxygenase-2 Inhibition in Radiation-Induced Oral Mucositis [NCT00698204]Phase 243 participants (Actual)Interventional2003-07-31Completed
A Placebo-Controlled, Double-Blind, Randomized Study of the Potential Interaction Between Aspirin and Ibuprofen or Celecoxib. [NCT00565500]Phase 424 participants (Actual)Interventional2003-04-30Completed
Randomized Phase 1/2 Evaluation of Neoadjuvant Administration of a Chemokine-Modulatory Regimen in Patients With Recurrent Resectable Colorectal Cancer [NCT01545141]Phase 1/Phase 215 participants (Actual)Interventional2012-10-31Terminated
A Phase II Trial Of Celecoxib (Celebrex) And Capecitabine (Xeloda) Combined With Pelvic Irradiation As Neoadjuvant Treatment Of Stage II or III Adenocarcinoma Of The Rectum [NCT00081224]Phase 23 participants (Actual)Interventional2004-12-31Terminated
Preemptive Anti-Inflammatory Use of Celecoxib in Knee Arthroplasty Surgery: a Double Blinded, Placebo-Controlled Study. [NCT00533247]200 participants (Anticipated)InterventionalNot yet recruiting
Breast Cancer Prevention Using Synergistic Prostaglandin Inhibitors (The Vitamin D/Celecoxib Study) [NCT01425476]Phase 1/Phase 245 participants (Actual)Interventional2008-07-31Completed
Observational Study of Effectiveness and Safety of Add-on Milgamma® and Milgamma® Compositum Step-Therapy in Routine Practice of Management of Adult Patients With Acute Non-Specific Low Back Pain Receiving Modern NSAIDs [NCT03892707]500 participants (Actual)Observational2018-12-15Completed
A Randomized, Open-Label Study Comparing the Efficacy and Safety of Lidocaine Patch 5% With Celecoxib 200 mg in Patients With Pain From Osteoarthritis of the Knee [NCT00904605]Phase 40 participants Interventional2004-06-30Terminated(stopped due to Safety concerns with the COX-2 specific inhibitor class of drug.)
A Prospective, Randomized, Double-Blind, Double-Dummy, Multi-Center Study Comparing Celecoxib and Ibuprofen Sr In The Management Of Acute Pain Post Orthopedic Or Gynecological Surgery [NCT00150280]Phase 3132 participants Interventional2004-10-31Completed
A 26-Week, Randomized, Placebo- and Active-Comparator-Controlled, Parallel-Group, Double-Blind, 2-Part Study to Assess the Safety and Efficacy of Etoricoxib 30 mg Versus Celecoxib 200 mg in Patients With Osteoarthritis (Study 2) [NCT00092781]Phase 3500 participants (Actual)Interventional2004-03-01Completed
Randomized, Double-Blind, Parallel Group, Placebo-Controlled Multi-Center Study Evaluating the Efficacy of PN400 (VIMOVO) Twice Daily (Bid) and Celecoxib Once Daily (qd) in Patients With Osteoarthritis of the Knee [NCT00664560]Phase 3614 participants (Actual)Interventional2008-04-30Completed
A Phase II Trial of Celecoxib With Preoperative Chemo- Radiation for Locally Advanced Rectal Cancer [NCT00931203]Phase 255 participants (Actual)Interventional2008-07-31Completed
A Multicenter, Randomized, Active-Controlled Comparison Study of the Incidence of Gastroduodenal Ulcers Associated With Celecoxib and Low Dose ASA Versus Naproxen and Low Dose ASA in Healthy Subjects (50-75 Years of Age) [NCT00137033]Phase 4605 participants Interventional2004-09-30Completed
Antiangiogenic Treatment Strategy With Metronomic Chemotherapy Regimen Combined With a Cox-2 Inhibitor and a Bisphosphonate for Patients With Metastatic Breast Cancer [NCT01067989]Phase 222 participants (Actual)Interventional2010-03-31Terminated(stopped due to No satisfactory acrual)
Minocycline and Celecoxib as Adjunctive Treatments of Bipolar Depression: A Factorial Design Randomised Controlled Trial [NCT02703363]Phase 3265 participants (Actual)Interventional2016-08-31Completed
Perioperative Use of Celecoxib to Improve Pain Control in Patients Undergoing Tonsillectomy: a Randomized, Double Blind, Placebo-controlled Trial [NCT00583453]Phase 218 participants (Actual)Interventional2007-10-31Completed
A Phase 3, Randomized, Double-Blind, Multicenter, Active-Controlled Trial To Evaluate The Efficacy And Safety Of Celecoxib (Celebrex®) And Indomethacin In The Treatment Of Moderate To Severe Acute Gouty Arthritis [NCT00549549]Phase 3402 participants (Actual)Interventional2008-02-29Completed
Randomized Pilot Trial of Oral Cyclophosphamide Versus Oral Cyclophosphamide With Celecoxib for Recurrent or Persistent Epithelial Ovarian, Fallopian Tube or Primary Peritoneal Cancer [NCT00538031]Phase 252 participants (Actual)Interventional2003-12-22Completed
Celecoxib for Pediatric Adenotonsillectomy: A Randomized Controlled Double Blinded Study [NCT00849966]Phase 2282 participants (Actual)Interventional2009-08-31Completed
Alzheimer's Disease Anti-Inflammatory Prevention Trial (ADAPT) [NCT00007189]Phase 32,625 participants Interventional2001-01-31Completed
Phase I-II Multiple-Dose Safety and Efficacy Study of a Selective Inhibitor of Cyclooxygenase - 2 (SC-58635) in Hereditary Non-Polyposis Colorectal Cancer (HNPCC) Patients and Carriers [NCT00001693]Phase 120 participants Interventional1998-03-31Completed
Phase II Double-Blind, Placebo Controlled, Randomized Study Of Celecoxib, A Selective COX-2 Inhibitor, In Oral Premalignant Lesions [NCT00014404]Phase 20 participants Interventional2000-10-31Completed
A Randomized, Double-Blind Study of the Biological Effects and Tolerability of Celecoxib as a Chemopreventive Agent in Current and Former Smokers [NCT00981201]Phase 3219 participants (Actual)Interventional2001-11-30Completed
A Phase I/II Trial of Celecoxib With Preoperative Chemoradiation for Resectable Rectal Cancer With In Vivo Analysis of Celecoxib Effector Pathways [NCT00188565]Phase 1/Phase 239 participants (Anticipated)Interventional2004-03-31Completed
A Phase II Study of Irinotecan (Camptosar), Cisplatin and Celebrex in Patients With Metastatic or Unresectable Esophageal Cancer [NCT00183807]Phase 26 participants (Actual)Interventional2003-10-31Terminated(stopped due to Insufficient Accrual)
The Efficacy and Safety of TDS-943 in the Treatment of Osteoarthritis of the Knee: Pivotal Study II [NCT00546832]Phase 3650 participants (Actual)Interventional2007-10-31Completed
Effect of Celecoxib on Postoperative Narcotic Use and Disease Severity in Patients With Aspirin-exacerbated Respiratory Disease and Chronic Rhinosinusitis: a Randomised Controlled Trial [NCT04147013]Phase 444 participants (Anticipated)Interventional2020-02-18Recruiting
A Double-blind, Placebo-controlled Investigation of Inter-individual Variability in Pharmacologic Response to Non-steroidal Anti-inflammatory Drugs [NCT02502006]Phase 116 participants (Actual)Interventional2015-11-30Terminated(stopped due to Funding was not available to complete enrollment)
Phase I/II Study of Chemoprevention With Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor Erlotinib (OSI-774, Tarceva) and Cyclooxygenase-2 (COX-2) Inhibitor (Celecoxib) in Premalignant Lesions of Head and Neck of Former Smokers [NCT00314262]Phase 1/Phase 217 participants (Actual)Interventional2006-10-31Completed
A Phase 2 Study of Cetuximab in Combination With Celecoxib in Colorectal Cancer [NCT00466505]Phase 217 participants (Actual)Interventional2005-05-31Completed
Celecoxib Japan Observational Study for the Patients With Acute Pain [NCT01876121]784 participants (Actual)Observational2012-07-31Completed
A Phase 2, Randomized, Double-Blind, Placebo and Active-Controlled Trial of LY2951742 in Patients With Mild to Moderate Osteoarthritis Pain of the Knee [NCT02192190]Phase 2268 participants (Actual)Interventional2014-07-31Terminated(stopped due to Interim assessment: Lack of efficacy)
A Multi-center, Open Label, Random Clinical Trial of Etanercept and Celecoxib Alone/Combined Treatment in Effectiveness and Safety of Active Ankylosing Spondylitis [NCT01934933]Phase 4150 participants (Actual)Interventional2014-09-24Completed
The Comparison of Multimodal Analgesic Protocols for Laparoscopic Cholecystectomy: Pharmacologic Interventions and Combination of Pharmacologic and Operative Interventions [NCT04788654]Phase 360 participants (Actual)Interventional2021-03-17Completed
Investigating the Effect of a Perioperative Analgesia Protocol on Postoperative Opioid Usage and Pain Control in Patients Undergoing Major Head and Neck Cancer Surgery Requiring Microvascular Free Flap Reconstruction [NCT04176419]Phase 330 participants (Anticipated)Interventional2020-01-17Active, not recruiting
Phase I Study of Erlotinib and Celecoxib in Former Smokers With Advanced Non-Small Cell Lung Cancer [NCT00088959]Phase 145 participants (Actual)Interventional2003-12-31Completed
A Randomized, Double Blind, Placebo Controlled Phase III Trial Evaluating the Role of Adjuvant Celecoxib in Completely Resected, High-Risk (pN1-2) Non-Small Cell Lung Cancer (NSCLC) Patients [NCT00211952]Phase 3542 participants Interventional2004-03-31Suspended
A Study Of Nasopharyngeal Carcinoma (NPC) Treated With Celecoxib And ZD1839 [NCT00212108]Phase 1/Phase 222 participants (Actual)Interventional2003-11-30Completed
Phase II Study on the Neoadjuvant Use of Chemotherapy and Celecoxib Therapy in Patients With Invasive Breast Cancer [NCT00135018]Phase 20 participants Interventional2006-02-28Completed
Evaluation and Treatment of Autonomic Failure. [NCT00223691]Phase 1389 participants (Actual)Interventional2002-03-31Completed
A Phase I Dose Escalation Study of Ascending Single and Multiple Doses of the MEK Inhibitor Zapnometinib in Healthy Subjects to Evaluate the Safety & Tolerability Compared to Placebo, Additionally Evaluating Pharmacokinetics and Pharmacodynamics of Target [NCT05555823]Phase 196 participants (Actual)Interventional2022-06-23Completed
Multimodal Pain Management After Robotic-Assisted Total Laparoscopic Hysterectomy [NCT04429022]Phase 368 participants (Actual)Interventional2020-11-24Completed
Efficacy of Opioid-limiting Pain Management Protocol in Men Undergoing Urethroplasty [NCT03859024]Phase 460 participants (Actual)Interventional2019-03-22Completed
Phase II Study of Celecoxib in HER-2/Neu Overexpressing Metastatic Breast Cancer Patients Who Have Failed Recombinant Humanized Anti-p 185HER Monoclonal Antibody Trastuzumab (HERCEPTIN) [NCT00006381]Phase 20 participants Interventional2000-06-30Completed
Phase IIb/III Chemoprevention Trial of Celecoxib to Prevent Recurrence of Superficial Bladder Cancer [NCT00006124]Phase 2/Phase 3152 participants (Anticipated)Interventional2000-06-30Completed
Does Optimal Pain Control With Pregabalin and Celecoxib Predict Improved Function After Total Hip Arthroplasty? [NCT00581685]Phase 331 participants (Actual)Interventional2008-01-31Completed
The Effects of Celecoxib on Bone Ingrowth in Porous Coated Titanium Ceramic Implants in Humans [NCT00585156]Early Phase 19 participants (Actual)Interventional2008-06-30Terminated(stopped due to New clinical finding with Celebrex and cardiac concerns.)
Phase I Clinical Trial Assessing the Combination of Chemokine Modulation With Neoadjuvant Chemotherapy in Triple Negative Breast Cancer [NCT04081389]Phase 19 participants (Actual)Interventional2019-12-06Completed
Glucosamine/Chondroitin Arthritis Intervention Trial (GAIT) [NCT00032890]Phase 31,588 participants Interventional2000-04-30Completed
SINCERE™: Safety in Idiopathic Arthritis: NSAIDs and Celebrex Evaluation Registry A Prospective Observational Registry Of Patients With Juvenile Idiopathic Arthritis (JIA) Treated With NSAIDs [NCT00688545]275 participants (Actual)Observational2009-04-30Terminated(stopped due to See termination reason in detailed description.)
Celecoxib In Biomarker Modulation Of Oral Precancerous Lesions: A Pilot Study [NCT00052611]Phase 223 participants (Actual)Interventional2002-06-30Completed
Phase I Study of Sequestered Transscleral, Controlled-Release Celecoxib Delivered Via Episcleral Reservoir for Treatment of Macular Edema & Inflammatory Disorders of the Eye Posterior Pole Including Sclera, Choroid, Retina or Vitreous [NCT04120636]Phase 13 participants (Anticipated)Interventional2021-03-05Active, not recruiting
Efficacy of Docetaxel (J 15) and Celecoxib in Metastatic Prostate Cancer [NCT00213694]52 participants Observational2003-11-30Completed
A Six Week Double-Blind, Randomized, Multicenter Comparison Study Of The Analgesic Effectiveness Of Celecoxib 200 Mg BID Compared To Tramadol Hydrochloride 50 Mg QID In Subjects With Chronic Low Back Pain [NCT00662558]Phase 3802 participants (Actual)Interventional2008-01-31Completed
Impact of Selective Cyclooxygenase-2 Inhibitor, Celecoxib on Cortical Excitability and Electrophysiological Property in Brain of Healthy Volunteer: Randomized, Double-blind, Placebo-controlled Study [NCT02711579]Phase 140 participants (Actual)Interventional2016-05-31Completed
A Phase 2 Study of Type-1 Polarized Dendritic Cell (αDC1) Vaccine in Combination With Tumor-Selective Chemokine Modulation (Interferon-α2b, Rintatolimod, and Celecoxib) in Subjects With Chemo-Refractory Metastatic Colorectal Cancer [NCT02615574]Phase 20 participants (Actual)Interventional2016-03-31Withdrawn(stopped due to Due to inadequate supply of drug)
Tramadol Versus Celecoxib for Reducing Pain During Office Hysteroscopy in Post Menopausal Women: A Double Blind Randomized Controlled Trial [NCT02736019]Phase 3210 participants (Anticipated)Interventional2016-06-30Recruiting
A Double-Blind, Placebo-Controlled Study of the Efficacy and Tolerability of Once Daily Celebrex® (Celecoxib) vs. Placebo in the Treatment of Subjects With Osteoarthritis of the Knee Non-Responsive to Naproxen and Ibuprofen [NCT00640627]Phase 4380 participants (Actual)Interventional2003-12-31Completed
Phase II, Randomized, Double-Blind, Multicenter Trial Of Celecoxib Vs Placebo For The Prevention Of Diarrhea Associated With CPT-11/5fu/LV Chemotherapy In Patients With Previously Untreated Metastatic Colorectal Cancer [NCT00037180]Phase 2212 participants Interventional2002-04-30Terminated
A Proof-of-concept Clinical Trial Assessing the Safety of the Coordinated Undermining of Survival Paths by 9 Repurposed Drugs Combined With Metronomic Temozolomide (CUSP9v3 Treatment Protocol) for Recurrent Glioblastoma [NCT02770378]Phase 1/Phase 210 participants (Actual)Interventional2016-11-30Completed
A Pilot, Open-Label, Dose Response Study Investigating the Effect of Low-Dose Celecoxib on SMN2 in Patients With Spinal Muscular Atrophy (SMA) [NCT02876094]Phase 21 participants (Actual)Interventional2019-01-29Terminated(stopped due to Terminated: Study halted prematurely and will not resume; participants are no longer being examined or receiving intervention)
Pilot COX-2 Activity in Early Stage Rectal Cancer -Short Term Administration of Celecoxib (SPORE) [NCT00608595]10 participants (Actual)Interventional2002-07-31Terminated(stopped due to low accrual)
Correlation Between Acute Analgesia and Long-Term Function Following Ankle [NCT02667730]Phase 4160 participants (Anticipated)Interventional2015-06-30Recruiting
Study Evaluating the Effect on Gastroduodenal Mucosa of PA32540, PA32540 and Celecoxib, and Aspirin With Celecoxib [NCT00700687]Phase 190 participants (Anticipated)Interventional2008-06-30Completed
Phase I Study of Gene Induction Mediated by Sequential Decitabine/Depsipeptide Infusion With or Without Concurrent Celecoxib in Subjects With Pulmonary and Pleural Malignancies [NCT00037817]Phase 134 participants (Actual)Interventional2002-05-17Completed
An Open-Label, Multicenter Study To Evaluate The Efficacy, Safety And Tolerability Of Celecoxib (YM177) In Patients With Posttraumatic Pain [NCT00976716]Phase 380 participants (Actual)Interventional2009-09-30Completed
A Selective COX-2 Inhibitor Provides Pain Control But Hinders Healing Following Arthroscopic Rotator Cuff Repair: A Prospective Randomized Comparison [NCT02850211]Phase 4180 participants (Actual)Interventional2011-09-30Completed
Effect of Celecoxib on Transitional Pain After Outpatient Surgery [NCT00664690]Phase 40 participants (Actual)InterventionalWithdrawn
Randomized, 16-Week, Multi-Phase, Double-Blind, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Efficacy of Fulranumab as Adjunctive Therapy in Subjects With Signs and Symptoms of Osteoarthritis of the Hip or Knee [NCT02301234]Phase 3111 participants (Actual)Interventional2015-03-25Completed
A Multi-center, Double-blind, Active-controlled, Randomized, Parallel-group Clinical Trial to Compare the Efficacy and Safety of CELBESTA® and CELEBREX® in Patients With Rheumatoid Arthritis [NCT02780323]Phase 4119 participants (Actual)Interventional2015-11-02Completed
Phase I Trial of Oral Etoposide in Combination With Celecoxib in Patients With Advanced Malignancies [NCT00551005]Phase 158 participants (Actual)Interventional2001-12-31Completed
A Double-Blind, Placebo-Controlled, Randomized 24-Month Study, Assessing The Effect Of Celecoxib (Celebrex) Long Term Treatment On Hip Osteoarthritis (OA) Progression OSCARE [NCT00163241]Phase 3666 participants Interventional2004-06-30Terminated(stopped due to Please see detailed description for termination reason.)
The Effects of a Prostaglandin Inhibitor on Ovulation and the Menstrual Cycle. [NCT00614406]11 participants (Actual)Interventional2008-01-31Completed
A Virtual Phase 2 Randomized, Placebo-controlled, Double-blind Study to Evaluate the Safety and Efficacy of the Combination of Famotidine and Celecoxib as a Post-exposure Prophylaxis (PEP) for Newly-infected COVID-19 Patients [NCT05077969]Phase 29 participants (Actual)Interventional2021-12-29Terminated(stopped due to Low recruitment)
Molecular Alterations in Human Ovarian Epithelium Induced by Chemopreventive Agents in Patients at Elevated Inherited Risk of Ovarian Cancer: A Controlled Pilot Study in Ovarian Cancer Chemoprevention [NCT00084370]0 participants (Actual)Interventional2002-06-30Withdrawn
A Phase II Evaluation of Weekly Paclitaxel (NSC #673089) and Celecoxib (Celebrex®, NSC #719627) in the Treatment of Recurrent or Persistent Platinum-Resistant Epithelial Ovarian or Primary Peritoneal Cancer [NCT00084448]Phase 20 participants Interventional2004-04-30Terminated
A Phase I Study of Irinotecan in Combination With Fixed Dose Celecoxib in Patients With Advanced Colorectal Cancer [NCT00084721]Phase 12 participants (Actual)Interventional2005-03-31Completed
Celecoxib Polyp Prevention Trial in Participants With Resected Stage I Colon Cancer [NCT00087256]Phase 318 participants (Actual)Interventional2004-07-31Terminated(stopped due to For scientific, logistic, and administrative reasons.)
In Vivo Selectivity of Cyclooxygenase Inhibitors in the Oral Surgery Model [NCT00006299]Phase 2120 participants Interventional1999-12-31Completed
Celecoxib as Add-on Therapy to Risperidone Versus Risperidone Alone in First-Episode and Drug-naive Patients With Schizophrenia [NCT00686140]200 participants (Actual)Interventional2006-06-30Completed
A 6-Week, Randomized, Double-Blind, Parallel-Group Study To Evaluate The Symptomatic Effects And Safety Of Celecoxib 200mg QD Compared To Diclofenac 75mg SR QD In Chinese Patients With Ankylosing Spondylitis, With 6-Week Extension Phase Treatment On Celec [NCT00762463]Phase 3240 participants (Actual)Interventional2009-07-31Completed
A Study to Identify Biomarker Modulation by a Cyclooxygenase-2 (COX-2) Inhibitor in Breast Tissue of Premenopausal Women at High Risk for Estrogen Receptor Negative (ERN) Breast Cancer [NCT00056082]Phase 2110 participants (Actual)Interventional2003-01-31Completed
Phase II Study of Gemcitabine, Cisplatin, and Celecoxib in the Treatment of Metastatic Pancreatic Cancer [NCT00176813]Phase 25 participants (Actual)Interventional2003-03-31Completed
A Randomized, Double-Blind, Multicenter, Comparative Study To Evaluate Efficacy And Safety Of An Additional Dose Of Celecoxib (YM177) In The Treatment Of Acute Pain After Oral Surgery Lateral Mandibular Impacted Third Molar Tooth Extraction [NCT01062113]Phase 2255 participants (Actual)Interventional2010-04-30Completed
Phase 2 Trial of Metronomic Treatment in Children and Adolescents With Recurrent or Progressive Neuroblastoma (NB) [NCT02641314]Phase 226 participants (Anticipated)Interventional2016-12-22Recruiting
A Multicentre Randomised Double Blind Placebo-Controlled Phase II Study of Celecoxib and Concurrent Radiotherapy in Stage II-III NSCLC. An Evaluation of Both Tumor Radiosensitization and Normal Tissue Protection [NCT00181532]Phase 2102 participants Interventional2003-05-31Completed
A Phase II Trial of Epirubicin With Estramustine Phosphate and Celecoxib for the Treatment of Hormone Resistant Prostate Cancer (HRPC) [NCT00218205]Phase 228 participants Interventional2002-07-31Recruiting
Low Dose Chemotherapy (Metronomic Therapy) Versus Best Supportive Care in Progressive and/or Refractory Pediatric Malignancies: a Double Blind Placebo Controlled Randomized Study [NCT01858571]Phase 3108 participants (Actual)Interventional2013-10-31Completed
EFFECTS OF NSAIDs ON CLINICAL OUTCOMES, SYNOVIAL FLUID CYTOKINE CONCENTRATION AND SIGNAL TRANSDUCTION PATHWAYS IN KNEE OSTEOARTHRITIS [NCT01860833]Phase 490 participants (Actual)Interventional2010-04-30Completed
A Phase 1 Open-Label Study Evaluating the Safety and Tolerability, and Pharmacokinetics of Navitoclax Monotherapy and in Combination With Ruxolitinib in Myeloproliferative Neoplasm Subjects [NCT04041050]Phase 185 participants (Actual)Interventional2019-11-08Active, not recruiting
A Double-Blind, Placebo-Controlled, Randomized, Crossover Pilot Study of the Efficacy of Celecoxib 200 mg QD in Relieving Pain and Walking Dysfunction in Osteoarthritis of the Knee. [NCT00597415]Phase 230 participants (Anticipated)Interventional2004-12-31Recruiting
Perioperative Pain Control With Celecoxib (Celebrex) in Total Knee Arthroplasty [NCT00598234]Phase 4120 participants (Anticipated)Interventional2006-09-30Completed
The Efficacy and Safety of TDS-943 in the Treatment of Osteoarthritis of the Knee: Pivotal Study I [NCT00546507]Phase 3650 participants (Actual)Interventional2007-10-31Completed
A Drug-drug Interaction Study of Capecitabine and Celecoxib in Patients With Advanced Solid Malignancies [NCT01705106]Phase 121 participants (Actual)Interventional2012-08-29Terminated(stopped due to The study was terminated early due to slow accrual.)
COX-2 Regulation of Renal Sodium Handling in Blood Pressure Maintenance [NCT00624559]Phase 412 participants (Actual)Interventional2008-02-29Completed
Effect of Pineapple Juice on the Pharmacokinetics of Celecoxib and Montelukast in Humans [NCT04374981]Phase 224 participants (Actual)Interventional2019-07-01Completed
A Phase 2, Randomized, Double-Blind, Single-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Indomethacin Test Capsules for the Treatment of Pain After Surgical Removal of Impacted Third Molars [NCT00964431]Phase 2203 participants (Actual)Interventional2009-08-31Completed
A Double-blind, Randomized, Multicenter, Active- and Placebo-Controlled Phase III Study to Evaluate the Efficacy and Safety of CG100649 in Osteoarthritis Patients [NCT01765296]Phase 3362 participants (Actual)Interventional2013-03-31Completed
Clinical Study on the Effect of Tizanidine on the Function and Pain of Patients After Shoulder Arthroscopy [NCT05852093]Early Phase 1100 participants (Anticipated)Interventional2023-06-01Not yet recruiting
A Randomized Phase II Trial of Cisplatin/Etoposide and Concurrent Radiotherapy With or Without Celecoxib in Patients With Unresectable Locally Advanced Non-small Cell Lung Cancer [NCT01503385]Phase 2100 participants (Anticipated)Interventional2011-12-31Recruiting
Phase 4 Study A Large Streamline Safety Study Designed to Compare the Cardiovascular Safety od Celecoxib Versus Traditional Non-selective NSAID's [NCT00447759]Phase 47,297 participants (Actual)Interventional2007-06-30Completed
Double-blind, Randomized, Dose-ranging, Parallel-group Comparison of the Efficacy and Safety of Extended Release Tramadol Hydrochloride (Tramadol HCl ER) 100 mg, 200 mg, 300 mg, Celecoxib 200 mg and Placebo in the Treatment of Osteoarthritis of the Knee a [NCT00348452]Phase 31,000 participants Interventional2002-09-30Completed
Clinical Trial of a COX-2 Inhibitor for the Treatment of Women With Preeclampsia [NCT00442676]Phase 20 participants (Actual)Interventional2009-06-30Withdrawn(stopped due to No patients were recruited. Treatment drug expired.)
A Pilot Study to Determine the Effect of Celecoxib on Markers of Inflammation in Patients With Hypertension and Coronary Artery Disease [NCT00471341]Phase 475 participants Interventional2002-07-31Completed
[NCT00500279]Phase 4900 participants (Anticipated)Interventional2006-11-30Recruiting
A Multicenter Randomized Phase III, Double-blind Study Comparing Efficacy of the Association of Exemestane and Celecoxib Versus Exemestane and Placebo in Menopausal Patients With Metastatic Breast Cancer. [NCT00525096]Phase 3157 participants (Actual)Interventional2003-07-31Completed
A Pilot Study of the Biologic Efficacy and Safety of the Addition of Celecoxib to a Program of Induction Chemotherapy and Neo-Adjuvant Chemo-Radiotherapy for the Treatment of Esophageal Cancer [NCT00520091]Phase 214 participants (Actual)Interventional2005-03-31Completed
Multi-center, Prospective Randomized, Comparative Open With Blinded Endpoints (PROBE) Trial to Assess the Safety and Effectiveness of Administration of Celecoxib in Patients With Intracerebral Hemorrhage [NCT00526214]44 participants (Actual)Interventional2007-10-31Completed
Celecoxib for Treatment of Postoperative Pain After Osteosynthesis of Distal Radius Fracture [NCT05288374]Phase 450 participants (Anticipated)Interventional2022-02-10Recruiting
Celecoxib-Mediated Inhibition of T Regulatory Cells in Human Lung Cancer [NCT00108186]Phase 10 participants (Actual)Interventional2004-10-31Withdrawn(stopped due to Couldn't accrue patients)
Celecoxib Versus Placebo as an Adjunct to Treatment-as-usual in Children and Youth With Obsessive-compulsive Disorder: A Single-site Randomized Quadruple-blind Phase II Study [NCT04673578]Phase 280 participants (Anticipated)Interventional2021-06-01Recruiting
Phase I Trial of Oral Cyclophosphamide in Combination With Celecoxib in Patients With Advanced Malignancies [NCT00551889]Phase 157 participants (Actual)Interventional2001-09-30Completed
Study to Evaluate Arthroplasty Specimens in the Phase 3 Fasinumab Program for Osteoarthritis of the Knee and Hip [NCT03949673]Phase 223 participants (Actual)Interventional2019-04-08Terminated(stopped due to Lack of enrollment)
Open-label, Multicenter, Randomized Study to Assess the Efficacy and Safety of Celecoxib 200mg Capsule QD and Celecoxib 100mg BID in Hand Osteoarthritis Patients [NCT03067194]Phase 4117 participants (Actual)Interventional2016-12-27Completed
The Effect Of Celecoxib On The Perioperative Inflammatory Response In Colon Cancer Patients - A Double-Blind Placebo-Controlled Trial [NCT01284504]1 participants (Actual)Interventional2011-01-31Terminated(stopped due to low accrual rate; the only participant withdrew after signing consent)
Prevention of Sporadic Colorectal Adenomas With Celecoxib [NCT00005094]Phase 31,170 participants (Anticipated)Interventional2000-03-31Completed
A Phase 3 Double Blinded, Randomized, Placebo Controlled Trial of Proton Pump Inhibitor for the Prevention of Recurrent Ulcer Bleeding in Patients Receiving a COX-2 Inhibitor [NCT00365313]Phase 3273 participants Interventional2002-08-31Completed
A Multiple-Dose, Dose-Escalation Study to Evaluate the Safety and Tolerability of LY3023703 in Healthy Subjects [NCT01849055]Phase 148 participants (Actual)Interventional2013-05-31Completed
A Pilot Phase II Trial of Celecoxib in Patients With Grade 2 or 3 Endometrioid-type, Clear Cell, and Papillary Serous Uterine Cancers [NCT00231829]Phase 223 participants Interventional2003-04-30Terminated(stopped due to Due to reported toxicity of Celecoxib at high doses)
Irinotecan Combined With Infusional 5-FU/Folinic Acid or Capecitabine and the Role of Celecoxib in Patients With Metastatic Colorectal Cancer [NCT00064181]Phase 386 participants (Actual)Interventional2003-05-31Completed
A Phase II Study Of Preoperative Celecoxib/Paclitaxel/Carboplatin For Squamous Cell And Adenocarcinoma Of The Esophagus [NCT00066716]Phase 239 participants (Actual)Interventional2003-06-30Completed
Prophylaxis of Heterotopic Ossification (HO) in Wartime Extremity Injuries, a Randomized Clinical Trial [NCT01631669]100 participants (Anticipated)Interventional2012-05-31Recruiting
A Phase II Trial of Gemcitabine and Celecoxib as First-Line Treatment for Patients With Advanced Metastatic Pancreatic Cancer [NCT00068432]Phase 228 participants (Actual)Interventional2003-12-31Completed
A Phase II Study of Celecoxib/Oxaliplatin/Capecitabine Combination Chemotherapy for Unresectable,Recurrent, or Metastatic Gastric/Gastroesophageal Junction Carcinoma [NCT00256321]Phase 24 participants (Actual)Interventional2004-10-31Terminated(stopped due to Closed due to poor accrual)
Phase II Study of Celecoxib, Capecitabine, and Irinotecan in Patients With Metastatic Colorectal Cancer [NCT00258232]Phase 20 participants Interventional2002-01-31Completed
Effect of Analgesics on the Irreversible Inactivation of Cyclooxygenase-1 Activity by Low Dose Aspirin and Endoscopic Evaluation of the Gastric Mucosal Effect [NCT00261586]Phase 492 participants (Actual)InterventionalCompleted
A Trial Of COX-2 Inhibitors In PSA Recurrence After Definitive Radiation Or Radical Prostatectomy For Prostate Cancer [NCT00073970]Phase 237 participants (Actual)Interventional2003-04-30Terminated(stopped due to Study stopped due to increased cardiovascular risks associated with Celebrex)
Phase I Trial of Bortezomib (VELCADE™) and Celecoxib in Patients With Advanced Solid Tumors [NCT00290680]Phase 136 participants (Anticipated)Interventional2005-03-31Completed
A Pilot Trial of a CEA-TRICOM Based Vaccine and Radiation to Liver Metastasis in Adults With CEA Positive Solid Tumors [NCT00081848]Phase 112 participants (Actual)Interventional2004-04-20Completed
A Phase 1, Randomized, 2-Period, 2-Sequence, Cross-over Study to Determine the Effect of ALXN1840 on the Metabolism of a CYP2C9 Substrate in Healthy Participants. [NCT04526197]Phase 136 participants (Actual)Interventional2020-07-07Completed
A Randomized, Placebo-Controlled, Parallel-Group, Double -Blind Study to Evaluate the Safety and Efficacy of Rofecoxib 12.5 mg and Celecoxib 200 mg in Patients With Osteoarthritis of the Knee [NCT00092352]Phase 3395 participants (Actual)Interventional2003-04-29Completed
Phase IB Study of Biomarker Modulation by Celecoxib vs. Placebo in Women With Newly-Diagnosed Breast Cancer [NCT00328432]Phase 1100 participants Interventional2003-06-30Completed
A Randomized Trial of Celecoxib and Rosiglitazone, Alone and in Combination, in Patients With Early Stage Non-Invasive Bladder Carcinoma Undergoing Cystoscopic Surveillance and in Patients With Muscle-Invasive Bladder Cancer Undergoing Radical Cystectomy [NCT00084578]0 participants (Actual)Interventional2004-03-31Withdrawn(stopped due to Withdrawn due to drug toxicity)
Multicenter, Double-Blind, Placebo-Controlled Randomized Phase III Study of Adjuvant Therapy With Celecoxib in Combination With Chemotherapy in Patients With Curatively Resected Stage III Colon Cancer [NCT00085163]Phase 30 participants Interventional2004-03-31Completed
A Randomized, Double Blind, Placebo-Controlled Trial of Celecoxib in Patients With Advanced Cancer [NCT00093678]0 participants (Actual)InterventionalWithdrawn
A Phase I Study of Concurrent CPT-11/Cisplatin and Celecoxib With Radiation Therapy for Patients With Unresectable Non-Small Cell Lung Cancer (NSCLC) [NCT00346801]Phase 120 participants (Actual)Interventional2003-09-30Completed
A Phase I Trial of Postoperative Radiation With Dose-Escalation of A Cox-2 Inhibitor, Celebrex™ (CELECOXIB) in Patients With Soft Tissue Sarcoma of the Extremity [NCT00450736]Phase 13 participants (Actual)Interventional2004-03-31Completed
Preoperative Treatment With NSAID in Colorectal Cancer Patients in Relationship to Tumor Host Reactions [NCT00473980]Phase 428 participants (Actual)Interventional1998-12-31Completed
[NCT00486460]Phase 30 participants Interventional2005-06-30Recruiting
Etude de la Reserve Vasomotrice Microcirculatoire cutanée [NCT00152724]85 participants (Actual)Observational1996-01-31Completed
A Randomized, Double Blind, Placebo-Controlled Trial of Celecoxib Versus Placebo in Men With Prostate Cancer With Rising PSA Following Prostatectomy or Radiation Therapy [NCT00136487]Phase 2/Phase 385 participants Interventional2002-10-31Completed
A Double-blind Randomized Comparison of Celecoxib Plus Esomeprazole Versus Naproxen Plus Esomeprazole for Prevention of Recurrent Ulcer Bleeding in Patients With Arthritis and Cardiothrombotic Diseases (NSAID#8 Study) [NCT00153660]Phase 3514 participants (Actual)Interventional2005-06-30Completed
Phase II Trial of Cisplatin, CPT-11, Celecoxib (PCC), Concurrent Radiation Therapy, and Surgery for Resectable Esophageal Cancer [NCT00137852]Phase 235 participants (Actual)Interventional2002-01-31Completed
Combination of 6-Thioguanine, Capecitabine, Celecoxib and Temozolomide or CCNU for Recurrent Anaplastic Glioma and Glioblastoma Multiforme [NCT00504660]Phase 275 participants (Actual)Interventional2003-09-30Completed
A Randomized Controlled Clinical Trial of Effectiveness of Yunnan Baiyao in Improving Fracture Pain [NCT05765747]58 participants (Anticipated)Interventional2023-04-01Not yet recruiting
A Phase II Study to Explore the Neoadjuvant Treatment of Serplulimab Combined With CAPEOX + Celecoxib in the Treatment of Locally Advanced Rectal Cancer [NCT05731726]Phase 250 participants (Anticipated)Interventional2023-02-22Recruiting
A Phase II Clinical Trial Using Metronomic Oral Low-dose Cyclophosphamide Alternating With Low-dose Oral Methotrexate With Continuous Celecoxib and Weekly Vinblastine in Children and Adolescents With Relapsed or Progressing Solid Tumours. [NCT01285817]Phase 279 participants (Actual)Interventional2011-01-12Completed
Randomized, Placebo-Controlled, Phase 2B Evaluation of Cyclooxygenase-2 Activity in Surgically Resected Primary Colorectal Adenomas and Carcinomas After 7 Days Pretreatment With Celecoxib [NCT00582660]Phase 240 participants (Actual)Interventional2001-12-31Completed
A Randomized, Placebo-Controlled Phase II Clinical Trial of Combination Erlotinib (Tarceva) and Celecoxib (Celebrex) Versus Erlotinib (Tarceva)/Placebo in Advanced Non-Small Cell Lung Cancer Patients [NCT00499655]Phase 2107 participants (Actual)Interventional2007-11-30Completed
Radiosensitization With a COX-2 Inhibitor (Celecoxib), With Chemoradiation for Cancer of the Head and Neck [NCT00581971]Phase 1/Phase 230 participants (Actual)Interventional2002-09-30Completed
A Randomized, Double-Blind, Phase 3 Study to Compare the Efficacy and Safety of Lansoprazole 30 mg QD and Naproxen 500 mg BID Versus Celecoxib 200 mg QD in Risk Reduction of Non Steroidal Anti-Inflammatory-Associated Ulcers in Osteoarthritis Subjects Taki [NCT00175032]Phase 31,045 participants (Actual)Interventional2003-07-31Completed
A Phase I/II Trial of the Cyclooxygenase-2 Inhibitor Celecoxib in the Treatment of Patients With Locally Advanced Carcinoma of the Cervix [NCT00152828]Phase 1/Phase 231 participants (Actual)Interventional2001-02-28Completed
Clinical Protocol For A Multicentre, Double-Blind, Randomised, Parallel Group Study To Compare The Efficacy and Tolerability Of Celecoxib Vs. Diclofenac In The Treatment Of Subjects With Osteoarthritis Of The Hip Requiring Joint Replacement Therapy [NCT00174317]Phase 4250 participants Interventional2003-08-31Completed
Vaccination With Autologous Dendritic Cells Pulsed With Tumor Antigens for Treatment of Patients With Malignant Melanoma. Phase I/II Study [NCT00197912]Phase 1/Phase 225 participants (Actual)Interventional2004-09-30Completed
An Open-label, Randomized, Crossover Study to Evaluate the Pharmacokinetic Interaction Between Tegoprazan and Non-steroidal Anti-inflammatory Drugs (NSAIDs) After Multiple Oral Dosing in Healthy Male Volunteers [NCT04639804]Phase 160 participants (Actual)Interventional2020-06-06Completed
Evaluation of Post Hospital Administration of Celecoxib Following Minimally Invasive Knee Replacement Surgery: A Randomized Controlled Study [NCT00474773]107 participants (Actual)Observational2007-06-30Completed
Celecoxib for Reducing Morphine Requirement After Thyroid Surgery: A Randomized Controlled Trial [NCT00520338]Phase 480 participants (Anticipated)Interventional2007-08-31Completed
Precision Psychiatry: Anti-inflammatory Medication in Immuno-metabolic Depression [NCT05415397]Phase 3140 participants (Anticipated)Interventional2022-09-28Recruiting
A 12 Weeks, Randomized, Double-blind, Multi-centers, Phase III Study to Evaluate the Efficacy and Safety of Shinbaro Capsule Compared With Celebrex Capsule in Patients With Osteoarthritis of Knee [NCT01535417]Phase 3198 participants (Actual)Interventional2009-05-31Completed
Phase II Trial of Atorvastatin and Celecoxib in Patients With Hormone-Dependent Prostate-Specific Antigen Progression After Local Therapy for Prostate Cancer. [NCT01220973]Phase 227 participants (Actual)Interventional2009-02-28Completed
Clinical Trial to Assess the Pharmacokinetic Interaction Between Celecoxib and Rebamipide in Healthy Male Volunteers [NCT01549743]Phase 130 participants (Actual)Interventional2012-05-09Completed
Phase II Study of Letrozole (Femara) and Celecoxib (Celebrex) in Postmenopausal Women With Hormone Receptor-Positive Locally Advanced or Metastatic Breast Cancer [NCT00101062]Phase 20 participants Interventional2004-01-31Terminated(stopped due to study drug unavailable)
A Phase IIb Cancer Prevention Trial of Celecoxib, a Selective COX-2 Inhibitor, in Oral Leukoplakia [NCT00101335]Phase 20 participants Interventional2003-11-30Completed
A Phase I Trial to Evaluate Cyclooxygenase 2 Inhibitor-Mediated Modulation of T Regulatory Cells in Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00104767]Phase 17 participants (Actual)Interventional2009-01-31Completed
Celecoxib for Chemoprevention of Primary Lung Cancer [NCT00020878]Phase 221 participants (Actual)Interventional2001-03-31Completed
A Randomized, Placebo-Controlled Trial Of Celecoxib In Men Pre-Prostatectomy For Clinically Localized Adenocarcinoma Of The Prostate: Evaluation Of Drug-Specific Biomarker Modulation [NCT00022399]Phase 273 participants (Actual)Interventional2002-04-25Completed
A Phase II, Double-Blind, Placebo-Controlled Clinical Trial To Assess Celecoxib As A Chemopreventive Agent Inhibiting UV-Induced Erythema And Cutaneous Carcinogenesis As Assessed Through Surrogate Biological Markers In Biopsied Skin After Exposure Of Skin [NCT00025051]Phase 20 participants (Actual)InterventionalWithdrawn
Clinical Protocol For A Phase II Double-Blind, Placebo-Controlled, Randomized Study Of Celecoxib (Sc-58635) In Oral Premalignant Lesions, Investigator IND [NCT00036283]Phase 242 participants Interventional2000-11-30Completed
Trial Of Oral Thalidomide, Celecoxib, Etoposide And Cyclophosphamide In Adult Patients With Relapsed Or Progressive Malignant Gliomas [NCT00047281]Phase 20 participants Interventional2004-03-31Completed
Preliminary Multi-Center Assessment of Laser and Medical Treatment of Diabetic Macular Edema [NCT00050479]Phase 3100 participants Interventional2002-12-31Completed
Lung Cancer Chemoprevention With Celecoxib In Ex-Smokers [NCT00055978]Phase 2112 participants (Actual)Interventional2002-10-31Completed
Pilot Randomized Trial Of Adjuvant Celecoxib In Patients With Early Stage Head And Neck And Non-Small Cell Lung Cancers [NCT00058006]Phase 20 participants Interventional2002-09-30Completed
Phase II Study Of Celecoxib In Metastatic Differentiated Thyroid Carcinoma [NCT00061906]Phase 225 participants (Actual)Interventional2003-01-31Completed
A Phase II Study of OSI 774 (IND Number 63383) in Combination With Celecoxib (Celebrex, Pharmacia) as Second-Line Therapy in Advanced Non-Small Cell Lung Cancer [NCT00062101]Phase 280 participants (Actual)Interventional2004-01-31Completed
A Randomized Double Blind Phase II Study of Preoperative Celecoxib/Paclitaxel/Carboplatin for Stage IIIA Non-Small Cell Lung Cancer [NCT00062179]Phase 27 participants (Actual)Interventional2003-03-31Completed
Phase II Study of the Combination of ZD1839 (Iressa) and Celecoxib in Patients With Platinum Refractory Non-Small Cell Lung Cance [NCT00068653]Phase 227 participants (Actual)Interventional2003-06-30Completed
An Exploratory, Open-Label Phase I Pharmacodynamic Study of COX-2 Inhibition With Celecoxib (Celebrex) and Aromatase Activity in Breast Cancer [NCT00070057]Phase 175 participants (Actual)Interventional2003-04-30Completed
Randomized Phase II Study of Eicosanoid Pathway Modulators and Cytotoxic Chemotherapy in Advanced Non-Small Cell Lung Cancer [NCT00070486]Phase 2140 participants (Actual)Interventional2003-12-31Completed
A Phase II Of An Optimized LV-5FU-Oxaliplatin Strategy With Celebrex In Metastatic Colorectal Cancer, Optimox2-Celecoxib Study [NCT00072553]Phase 20 participants Interventional2003-09-30Active, not recruiting
A Phase I Study of Weekly Administration of Oral Navelbine in Combination With the COX-2 Inhibitor Celebrex in Relapsed and/or Metastatic Breast Cancer [NCT00075673]Phase 16 participants (Actual)Interventional2003-11-30Terminated
A Randomized Phase II Trial of Bone-Targeted Therapy Consisting of Strontium-89 and Doxorubicin With or Without Celecoxib in Androgen-Independent Prostate Cancer [NCT00080782]Phase 214 participants (Actual)Interventional2002-02-28Terminated(stopped due to Low accrual due to competing trial.)
Protocol For A Multicentre, Double Blind, Parallel Group Pilot Study To Compare Celecoxib Long Term Vs Celecoxib Short Term Therapy In Treatment And Prevention Of New Flare In Patients With Osteoarthritis Of The Knee [NCT00137410]Phase 3200 participants Interventional2002-11-30Completed
Clinical Protocol For a Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Celecoxib (SC-58635) In The Prevention of Colorectal Sporadic Adenomatous Polyps (PRESAP) [NCT00141193]Phase 31,561 participants (Actual)Interventional2001-02-28Completed
[NCT00009230]Phase 30 participants Interventional2000-06-30Completed
Evaluation Of Celecoxib In Combination With Docetaxel In The Treatment Of Advanced Non-Small Cell Lung Cancer Patients Previously Treated With Platinum Based Chemotherapy [NCT00030420]Phase 224 participants (Actual)Interventional2001-10-31Completed
A Phase II Randomized, Double-Blind, Placebo-Controlled Clinical Trial of Celecoxib in Subjects With Basal Cell Nevus Syndrome [NCT00023621]Phase 260 participants (Anticipated)Interventional2001-02-28Completed
A Phase I/II Study Of COX-2 Inhibitor, CELEBREX (CELECOXIB), And Chemoradiation In Patients With Locally Advanced Cervical Cancer [NCT00023660]Phase 1/Phase 284 participants (Actual)Interventional2001-08-31Completed
Evaluation Of Celecoxib In Combination With Weekly Docetaxel In Elderly (70 Years) Or Poor Performance Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00030407]Phase 234 participants (Actual)Interventional2001-10-31Completed
Anti-Inflammation in AD: PET Imaging Supplement [NCT00065169]138 participants Interventional2000-11-30Completed
[NCT00065559]30 participants Interventional2003-04-30Terminated
A Phase I Trial Of A COX-2 Inhibitor (Celecoxib) In Combination With An EGFR Inhibitor (OSI-774) In Metastatic Non-Small Cell Lung Cancer [NCT00072072]Phase 10 participants Interventional2003-08-31Completed
S0212: Phase IIb Randomized Study of Celecoxib in Patients With High-Grade Squamous Intraepithelial Lesions of the Cervix [NCT00072540]Phase 20 participants (Actual)InterventionalWithdrawn(stopped due to drug issues)
A Phase 3, Randomized, Double-Blind, Multiple-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Diclofenac [Test] Capsules for the Treatment of Acute Postoperative Pain After Bunionectomy [NCT01462435]Phase 3428 participants (Actual)Interventional2011-10-31Completed
Phase II Study Of Temozolomide, Thalidomide And Celecoxib In Patients With Newly Diagnosed Glioblastoma Multiforme In The Post-Radiation Setting [NCT00047294]Phase 20 participants Interventional2001-04-30Completed
Multi-Center Randomized Phase I/II Trial to Study the Effects of Cyclooxygenase-2 Inhibition on the Response to Photodynamic Therapy in Patients With Age-Related Macular Degeneration [NCT00043680]Phase 260 participants Interventional2002-08-31Completed
Metronomic Chemotherapy With Anti-angiogenic Effect as Maintenance Treatment for Metastatic Colorectal Carcinoma Following Response to FOLFIRI+Bevacizumab: Clinical and Laboratory Studies [NCT01668680]Phase 280 participants (Anticipated)Interventional2012-09-30Terminated(stopped due to No satisfactory acrual)
Phase III Study of a Double-Blind Randomized Comparison of Famotidine Plus Celecoxib Versus Dologesics for Gastric Ulcer Healing in Arthritis Patients (NSAID#5A Study) [NCT00153673]Phase 3200 participants (Actual)Interventional2001-02-28Completed
Phase I/II Study of Celebrex and EPO906 in Patients With Metastatic Colorectal Cancer (CEPO906AUS10) [NCT00159484]Phase 1/Phase 275 participants (Actual)Interventional2004-10-31Active, not recruiting
A Randomized Double-Blind Phase II Trial of Celecoxib, A COX-2 Inhibitor, in the Treatment of Patients With Cervical Intraepithelial Neoplasia 2/3 or 3 (CIN 2/3 or 3) [NCT00081263]Phase 2130 participants (Actual)Interventional2005-06-30Completed
Phase 3 Randomized, Double-Blind, Multi-Dose, Placebo And NSAID Controlled Study To Evaluate The Efficacy And Safety Of Fasinumab In Patients With Pain Due To Osteoarthritis Of The Knee Or Hip [NCT03304379]Phase 31,650 participants (Actual)Interventional2017-10-26Completed
Anti-Angiogenic Chemotherapy: A Phase II Trial of Thalidomide, Celecoxib, Etoposide and Cyclophosphamide in Patients With Relapsed or Progressive Cancer [NCT00165451]Phase 220 participants (Actual)Interventional2001-06-30Completed
Evaluation Of Novel Therapeutic Agents (Celecoxib: NSC # 719627) Against Breast Cancer: An Innovative Randomized Phase II Trial Design [NCT00045591]Phase 239 participants (Actual)Interventional2003-02-28Terminated
A Phase I Study of Celecoxib, Irinotecan and Concurrent Radiotherapy in the Preoperative Treatment of Pancreatic Cancer [NCT00177853]Phase 123 participants (Anticipated)Interventional2006-12-31Terminated(stopped due to terminated)
Phase I Study of Secondary Primary Tumor Prevention With Epidermal Growth Factor Receptor (EGFR), Tyrosine Kinase Inhibitor Erlotinib (OSI-774, Tarceva™), and Cyclooxygenase-2 (COX-2) Inhibitor (Celecoxib) in Early Stage (Stage I/II) Squamous Cell Carcino [NCT00400374]Phase 110 participants (Actual)Interventional2007-08-31Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Efficacy, Tolerability, and Safety Study of DFN-15 in Episodic Migraine With or Without Aura [NCT03006276]Phase 3622 participants (Actual)Interventional2016-12-31Completed
Low Dose Aspirin Inhibition of COX-2 Derived PGE2 in Male Smokers [NCT01796951]Early Phase 16 participants (Actual)Interventional2013-02-28Completed
Phase I Study of Fluvastatin-Celebrex Association for Optico-chiasmatic Low Grade Gliomas and High Grade Gliomas Localized Outside the Brainstem, Relapsed or Refactory, in Children or Young Adults [NCT02115074]Phase 120 participants (Actual)Interventional2014-06-30Completed
A Randomized, Double-blinded, Placebo-controlled Study Investigating the Pharmacological Response to Celecoxib Using ex Vivo Human Whole-blood Assay (hWBA) and Broad-spectrum Lipidomics Analysis [NCT02413203]20 participants (Actual)Interventional2015-03-31Completed
A Phase 3b, Open-Label Study of HTX-011 as Part of a Scheduled Non-Opioid Multimodal Analgesic Regimen in Subjects Undergoing Total Knee Arthroplasty [NCT03974932]Phase 3116 participants (Actual)Interventional2019-06-05Completed
An Open Label, Randomized, Multiple-Dose, Two-Treatment, Two-Period, Two-Sequence, Crossover Study to Evaluate the Comparative Bioavailability of PrimeC (Ciprofloxacin and Celecoxib) Tablets to Ciprofloxacin Tablets Co-administered With Celecoxib Capsules [NCT05436678]Phase 119 participants (Actual)Interventional2022-07-26Completed
COLA: A Pilot Clinical Trial of COX-2 Inhibition in LAM and TSC [NCT02484664]Phase 212 participants (Actual)Interventional2016-06-15Completed
Preventive Effect of Celecoxib on Sorafenib-related Hand Foot Syndrome [NCT02961998]Phase 4116 participants (Actual)Interventional2015-07-31Completed
A Six Week Double-Blind, Randomized, Multicenter Comparison Study of the Analgesic Effectiveness of Celecoxib 200 mg BID Compared to Tramadol Hydrochloride 50 mg QID in Subjects With Chronic Low Back Pain [NCT00290901]Phase 4754 participants Interventional2006-03-31Completed
A Phase I/II Study of Celecoxib and Erlotinib Hydrochloride as Adjuvant Therapy for High Risk Patients With a History of Hepatocellular Carcinoma [NCT00293436]Phase 1/Phase 20 participants (Actual)Interventional2005-01-31Withdrawn
Cox-2-Inhibitor and Chemotherapy in Non-Small Cell Lung Cancer. A Prospective Randomized Double-Blind Study [NCT00300729]Phase 3319 participants (Actual)Interventional2006-05-31Active, not recruiting
Phase III Trial of Gemcitabine, Curcumin and Celebrex in Patients With Metastatic Colon Cancer [NCT00295035]Phase 3100 participants Interventional2006-03-31Not yet recruiting
Effectiveness and Safety of Celecoxib (Celebrex 200 mg) Combined With Joins in the Treatment of Degenerative Knee Osteoarthritis: a Randomized Controlled Trial [NCT04718649]216 participants (Anticipated)Interventional2021-01-31Not yet recruiting
A Relative Bioavailability Study Of Celecoxib Administered As Capsule Contents Sprinkled On Applesauce In Healthy Adult Volunteers [NCT00296127]Phase 124 participants Interventional2006-02-28Completed
Phase II Randomized Study Evaluting the Effect of Celecoxib as Maintenance Treatment of Stage IIIb Non-Small Cell Lung Cancer That Reponded or is Stable After Radiochemotherapy [NCT00274898]Phase 280 participants (Anticipated)Interventional2004-05-31Active, not recruiting
A Randomized Phase III Double Blind Trial Evaluating Selective COX-2 Inhibition in COX-2 Expressing Advanced Non-Small Cell Lung Cancer [NCT01041781]Phase 3313 participants (Actual)Interventional2010-02-28Terminated(stopped due to DSMB recommendation)
Quantitative Real Time PCR in Formalin Fixed Breast Tissue From Biopsy and Re-Excision Specimens: An Ancillary Protocol to a Chemoprevention Trial of Celecoxib [NCT00291122]100 participants Observational2003-01-31Completed
Celecoxib in the Management of Acute Renal Colic [NCT00304317]Phase 40 participants (Actual)Interventional2006-03-31Withdrawn(stopped due to PI is no longer at the University of Minnesota)
Effects of Celecoxib on Restenosis After Percutaneous Coronary Intervention and Evolution of Atherosclerosis (COREA) Trial [NCT00292721]Phase 4260 participants (Anticipated)Interventional2004-08-31Completed
C-2424: Phase II Study of Celecoxib, Capecitabine, and Irinotecan in Patients With Metastatic Colorectal Cancer [NCT00230399]Phase 215 participants Interventional2003-06-30Completed
Phase II Pilot Study of Pre-Operative Celecoxib (Celebrex) in Combination With Prolonged Venous Infusion 5FU and Radiation Therapy for Patients With Stage II/III Resectable Rectal Cancer [NCT00336960]Phase 224 participants (Actual)Interventional2002-07-31Completed
A Prospective, Randomized, Double-blinded, Multi-center, Trial to Evaluate Efficacy and Safety of Combination of Diacerein and Celecoxib Administered Orally in Patients With Knee Osteoarthritis [NCT03404479]Phase 490 participants (Anticipated)Interventional2018-01-25Recruiting
[NCT01623921]100 participants (Anticipated)Interventional2012-08-31Not yet recruiting
The Effect on Knee Joint Loads of Instruction in Analgesic Use Compared With NEUROMUSCULAR Exercise in Patients With Knee Osteoarthritis - A Single Blind RCT [NCT01638962]93 participants (Actual)Interventional2012-08-31Completed
A Phase III Trial of 6 Versus 12 Treatments of Adjuvant FOLFOX Plus Celecoxib or Placebo for Patients With Resected Stage III Colon Cancer [NCT01150045]Phase 32,527 participants (Actual)Interventional2010-06-30Active, not recruiting
Randomized Controlled Phase II Trial of Pre-operative Celecoxib Treatment in Breast Cancer [NCT01695226]Phase 20 participants Interventional2004-02-29Completed
Effect of Anti-inflammatory Treatments on the Symptoms, Cognition, and Functioning of Adolescents With Schizophrenia [NCT04020588]Phase 490 participants (Anticipated)Interventional2019-02-25Recruiting
A Molecule Basic Study of Early Warning for New Pathogenic Risk of Ankylosing Spondylitis [NCT01709656]120 participants (Actual)Interventional2012-03-31Completed
A Precision Medicine Approach to OCD Treatment: Targeting Neuroinflammation [NCT04786548]Phase 221 participants (Anticipated)Interventional2021-04-01Recruiting
Photodynamic Therapy-Induced Immune Modulation: Part III [NCT03643744]Phase 148 participants (Anticipated)Interventional2019-04-01Recruiting
ANGIOCOMB Antiangiogenic Therapy for Pediatric Patients With Diffuse Brain Stem and Thalamic Tumors [NCT01756989]Phase 250 participants (Anticipated)Interventional2005-01-31Completed
CI(R)CA : Coumadin Interaction With Rofecoxib, Celecoxib and Acetaminophen. A Prospective Double-blind, Placebo Controlled Study. [NCT01762891]22 participants (Actual)Interventional2003-03-31Completed
Prostaglandin Inhibition to Prevent Breast Cancer [NCT01769625]Phase 1/Phase 231 participants (Actual)Interventional2009-01-31Completed
A Randomized, Double-blind, Multicenter, Phase 3 Study of Pelubiprofen Tab. & Celebrex Cap. for Comparative Evaluation of Safety & Efficacy in Rheumatoid Arthritis Patients [NCT01781702]Phase 3120 participants (Actual)Interventional2010-10-31Completed
Use of Urinary Nerve Growth Factor as A Biomarker to Determine Complete Resolution of Bladder Inflammation After Acute Bacterial Cystitis in Women [NCT01800799]37 participants (Actual)Interventional2013-02-28Completed
A 26-week Single Site, Randomized, Double-blind, Active-controlled, Parallel Group, Human PoC Study to Evaluate Superiority of RK-01, Valsartan Plus Celecoxib Addon to Metformin Versus Metformin Alone in Type 2 Diabetes Patients [NCT03686657]Phase 1/Phase 2115 participants (Anticipated)Interventional2023-10-10Not yet recruiting
For 12 Weeks, the Multi-center, Randomized, Double-blinded, Clinical Study to Evaluate the Efficacy and Safety of Entelon Tab. 150mg Compared With Celebrex Capsule in Patients With Osteoarthritis of Knee (Phase III) [NCT01768520]Phase 3338 participants (Actual)Interventional2012-07-02Completed
A Prospective, Randomized Study Evaluating the Efficacy and Safety of Early Diuresis Following Colorectal Surgery [NCT02351934]Phase 4123 participants (Actual)Interventional2015-02-28Completed
A Pilot Study: Celecoxib Inhibition of Aromatase Expression and Inflammation in Adipose Tissue of Obese Postmenopausal Women [NCT01901679]Early Phase 110 participants (Actual)Interventional2013-07-31Completed
Evaluation of the Effect of Celecoxib on Angiogenesis Markers in Patients With Operable Head and Neck Squamous Cell Carcinoma [NCT00357617]Phase 1/Phase 224 participants (Anticipated)Interventional2006-06-30Active, not recruiting
A Multicenter Phase III Placebo-Controlled Trial of Celecoxib for Prevention of Capecitabine-Induced Palmar/Plantar (Hand/Foot) Syndrome in Patients With Metastatic Breast and Colorectal Cancer [NCT00305643]Phase 311 participants (Actual)Interventional2006-02-28Terminated(stopped due to Terminated due to low accrual. No data analyzed.)
A Single- and Multiple-Ascending Dose, Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Study of LY3127760 in Healthy Subjects [NCT01968070]Phase 180 participants (Actual)Interventional2013-10-31Completed
An Open-label, Phase I Trial With Expansion Cohort of Nab-Paclitaxel + Gemcitabine + Cisplatin + Botensilimab (AGEN1811) + Balsilimab (AGEN2034) + Chloroquine + Celecoxib in Patients With Previously Untreated Metastatic Pancreatic Cancer [NCT06076837]Phase 112 participants (Anticipated)Interventional2023-12-31Not yet recruiting
A Phase 2 Randomized, Single-blind, Placebo-controlled Study to Evaluate the Safety and Efficacy of the Combination of Famotidine and Celecoxib as a Treatment in Moderate-to-severe Patients Hospitalized for COVID-19 [NCT05085574]Phase 20 participants (Actual)Interventional2023-02-07Withdrawn(stopped due to COVID environment, lack of site confidence to enroll subjects, sites not suited to study procedures, decline of potential inpatient subjects at site)
Leidos-Enabled Adaptive Protocol for Clinical Trials (LEAP-CT) to Evaluate the Safety and Efficacy of Drug Combinations in COVID-19 Patients [NCT05077332]Phase 22,000 participants (Anticipated)Interventional2021-12-29Active, not recruiting
Multicenter, Double Blind, Randomized, Placebo Controlled Trial Of The Efficacy And Safety Of Usual Care Plus Celecoxib Compared To Placebo For Peri-Operative And Rehabilitation Pain Control And Return To Function In Osteoarthritis Patients Undergoing Tot [NCT00359151]Phase 422 participants (Actual)Interventional2006-11-30Terminated(stopped due to This study was terminated early due to slow enrollment.)
Efficacy of Pre-emptive Different Doses of Oral Pregabalin Versus Celecoxib on Sevoflurane and Analgesic Consumption in Patients Subjected for Elective Lumbar Spine Fixation Surgery: a Randomized Controlled Trial [NCT04342065]Phase 2/Phase 3200 participants (Actual)Interventional2019-01-01Completed
Molecular Targeting of 15-LOX-1 for Apoptosis Induction in Human Colorectal Cancers [NCT00503035]Phase 251 participants (Actual)Interventional2003-08-20Completed
A Phase 2, Randomized, Single-Blind, Active-Control, Parallel Group Study to Evaluate Safety and Activity of a Single Administration of F14 for Management of Postoperative Pain in Participants Undergoing Unilateral Total Knee Replacement [NCT03541655]Phase 220 participants (Actual)Interventional2018-05-04Completed
Vitamin D Plus Celecoxib Therapy to Stimulate Intratumoral Immune Reactivity [NCT00953849]Phase 1/Phase 221 participants (Actual)Interventional2009-11-30Completed
Randomized Placebo-Controlled Biomarker Modulation Trial Using Celecoxib in Premenopausal Women at High Risk for Breast Cancer [NCT00088972]Phase 28 participants (Actual)Interventional2004-11-30Terminated(stopped due to Study closed due to poor accrual.)
Pilot Study of Celecoxib Combined With Gemcitabine and Cisplatin for Neoadjuvant Treatment of Localized, Muscle-Invasive Bladder Cancer [NCT02885974]Phase 115 participants (Anticipated)Interventional2016-12-31Recruiting
CELECOXIB Plasma and Cerebral Spinal Fluid Pharmacokinetics in Children [NCT01344200]Phase 265 participants (Anticipated)Interventional2022-12-31Not yet recruiting
A Pilot, Open-Label, Randomized, Single-Dose, Three-Treatment, Three-Period Crossover Study to Evaluate the Effect of Food on the Bioavailability of PrimeC-ER Tablets and the Comparative Bioavailability of PrimeC-ER and Ciprofloxacin Tablets and Celecoxib [NCT05232461]Phase 112 participants (Actual)Interventional2022-04-08Completed
A Double-blind, Placebo-controlled, Crossover Pilot Study of the Efficacy of Celecoxib 200 mg qd in Relieving Pain and Walking Dysfunction in Osteoarthritis of the Knee [NCT00194090]Phase 440 participants (Actual)Interventional2004-06-30Completed
A PHASE 1-2 NEOADJUVANT DOSE FINDING, SAFETY, AND IMMUNOLOGIC EFFICACY TRIAL OF INTENSIVE LOCOREGIONAL CHEMOIMMUNOTHERAPY FOR RECURRENT OVARIAN CANCER AND TUMOR-SPECIFIC INTRANODAL AUTOLOGOUS ALPHA-DC1 VACCINES [NCT02432378]Phase 1/Phase 225 participants (Anticipated)Interventional2015-09-04Suspended
The Use of Celecoxib (Celebrex (c)) in Post-operative Pain Control After Microdissection Testicular Sperm Extraction [NCT01323595]78 participants (Actual)Interventional2011-01-31Terminated(stopped due to Interim analysis demonstrated significant benefit in intervention arm)
The Effect of a Non-hormonal Cox-2 Inhibitor (Celebrex) on Ovulation [NCT01129245]20 participants (Actual)Interventional2009-09-30Completed
Study of Parecoxib Versus Celecoxib Versus Oxycodone on Perioperative Pain Control of Transcatheter Chemoembolization Procedure for Patients With Hepatocelullar Carcinoma [NCT03059238]Phase 3213 participants (Actual)Interventional2016-09-30Completed
A Phase 2, Randomized, Double-Blind, Single-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Diclofenac [Test] Capsules for the Treatment of Pain After Surgical Removal of Impacted Third Molars [NCT00985439]Phase 2202 participants (Actual)Interventional2009-09-30Completed
Traditional vs. Nonopioid Analgesia After Labral Surgery [NCT03825809]Phase 2/Phase 3100 participants (Anticipated)Interventional2019-01-22Recruiting
Biologic and Clinical Role of COX-2 Inhibitor (Celecoxib)in the Management of MGUS and Smoldering Myeloma [NCT00099047]Phase 223 participants (Actual)Interventional2004-11-30Completed
A Phase II Trial of Maintenance ADAPT Therapy With Capecitabine and Celecoxib in Patients With Metastatic Colorectal Cancer [NCT01729923]Phase 227 participants (Actual)Interventional2013-03-31Terminated(stopped due to Funding ended)
A Phase II Trial of Exemestane (Aromasin) in Combination With Celecoxib (Celebrex) as Neoadjuvant Treatment in Postmenopausal Women With Stage II, III, and IV Breast Cancer [NCT00201773]Phase 222 participants (Actual)Interventional2003-07-31Completed
Optimal Multimodal Pain Management Package Versus Regular Bottled Pain Formulation for Outpatient Use Following Microdiscectomies , Foraminotomies, and Spinal Decompressions: A Randomized Control Trial Comparing Two Strategies [NCT05965492]Phase 3100 participants (Anticipated)Interventional2024-02-01Not yet recruiting
Possible Protective Effect of Celecoxib Against Capecitabine Induced Hand and Foot Syndrome in Patients With Colorectal Cancer [NCT05327751]Phase 344 participants (Anticipated)Interventional2022-04-01Recruiting
Effects and Mechanisms of Celecoxib on Intracerebral Hemorrhage [NCT05434065]Phase 260 participants (Anticipated)Interventional2023-01-01Recruiting
Pilot Open Label Clinical Trial Evaluating the Safety and Efficacy of Chemokine Modulation to Enhance the Effectiveness of Pembrolizumab in Patients With Metastatic Triple Negative Breast Cancer [NCT03599453]Early Phase 18 participants (Actual)Interventional2019-01-09Completed
Comparison Between Multimodal and Unimodal Analgesia in Cholecystectomy [NCT05547659]Phase 1/Phase 295 participants (Actual)Interventional2019-01-01Completed
A Phase III Multicentre Double Blind Randomised Trial of Celecoxib Versus Placebo in Primary Breast Cancer Patients [NCT02429427]Phase 32,639 participants (Actual)Interventional2005-12-31Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Efficacy, Tolerability, and Safety Study of DFN-15 in Episodic Migraine With or Without Aura [NCT03009019]Phase 3631 participants (Actual)Interventional2016-12-31Completed
A Randomized, Double-Blind, Multicenter, Placebo- and Active Comparator-Controlled Study to Evaluate Efficacy and Safety of MR308 in the Treatment of Acute Pain After Third Molar Tooth Extraction (STARDOM1). [NCT02982161]Phase 3818 participants (Actual)Interventional2016-12-28Completed
Double Blinded, Randomized, Active Drug Comparative, Multi-center, phase3 Clinical Study to Evaluate the Efficacy and Safety of PG201 in Osteoarthritis Patients [NCT01576419]Phase 3309 participants (Actual)Interventional2010-01-31Completed
Non-Inferiority Clinical Trial On The Efficacy And Safety Of Chondroitin Sulfate And Glucosamine Hydrochloride In Combination Versus Celecoxib In Patients With Knee Osteoarthritis [NCT01425853]Phase 4606 participants (Actual)Interventional2011-09-30Completed
A Phase 3, Randomized, Double-Blind, Multiple-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Indomethacin [Test] Capsules for the Treatment of Acute Postoperative Pain After Bunionectomy [NCT01543685]Phase 3462 participants (Actual)Interventional2012-02-29Completed
An International, Multicentre, Double-blind, Randomised Study of the Effect of Diacerein vs Celecoxib on Symptoms and Structural Changes in Symptomatic Knee Osteoarthritis Patients as Assessed by Magnetic Resonance Imaging [NCT02688400]Phase 3380 participants (Actual)Interventional2016-05-31Completed
MEASURES OF GAIT AND SELF-REPORTED PAIN IN PATIENTS WITH OSTEOARTHRITIS OF THE KNEE: A RANDOMIZED, SINGLE-BLIND WASHOUT, DOUBLE-BLIND TREATMENT, DOUBLE DUMMY CROSS-OVER PILOT TRIAL USING PLACEBO, OXYCODONE AND CELECOXIB (A9011030) [NCT00484718]Phase 46 participants (Actual)Interventional2008-01-17Terminated(stopped due to See termination reason in detailed description.)
The Safety of Celecoxib (Celebrex) in Patients With Crohn's Disease [NCT00177866]Phase 428 participants (Actual)Interventional2003-12-31Terminated(stopped due to We were unable to get additional funding to complete study.)
A Single-Dose, Dose-Escalation Study to Evaluate the Safety and Tolerability of LY3023703 in Healthy Subjects [NCT01632579]Phase 130 participants (Actual)Interventional2012-06-30Completed
Effectiveness of Two Different Doses of BI 1026706 on the Overall Peak-to-Peak (PtP) N2/P2-component Amplitude of Laser (Somatosensory, Radiant-heat) Evoked Potentials (LEP) in UVB (Ultraviolet)-Irradiated Skin in Healthy Male Volunteers (a Single-blinded [NCT02037165]Phase 125 participants (Actual)Interventional2014-01-21Completed
The Role of Cytokines as Inflammatory Mediators in Painful Temporomandibular Joints [NCT00001955]Phase 2150 participants Interventional1999-12-31Completed
Pain Treatment After Joint Surgery With a Combination of Aspirin, Ketorolac, and Celecoxib. [NCT05994287]105 participants (Actual)Interventional2021-01-01Completed
Comparing Pre-emptive Injection of Peri-Articular-Multimodal Drug With Oral Celecoxib for Postoperative Pain Management in Total Knee Arthroplasty: A Randomized Clinical Trial [NCT05324995]Phase 2146 participants (Actual)Interventional2021-01-01Completed
Celecoxib for Pain Management After Tonsillectomy [NCT02934191]Phase 2172 participants (Actual)Interventional2016-06-30Completed
Neoadjuvant Therapy and Biomarker Analysis of Stage II and III Breast Cancer With Docetaxel/Capecitabine and Celecoxib Followed by Doxorubicin/Cyclophosphamide and Celecoxib [NCT00665457]Phase 23 participants (Actual)Interventional2004-04-15Terminated(stopped due to study drug was removed from the market and low enrollment.)
A Randomized, Open-label, Multiple-dose, Crossover Clinical Trial to Investigate the Pharmacokinetic Drug Interactions and Safety After Co-administration of Ilaprazole and NSAID in Healthy Adults [NCT05237297]Phase 172 participants (Actual)Interventional2022-02-17Completed
MAST Trial: Multi-modal Analgesic Strategies in Trauma [NCT03472469]Phase 41,561 participants (Actual)Interventional2018-04-02Completed
The Effect of Celecoxib on Heterotopic Bone Formation Following Cementless Total Hip Arthroplasty [NCT05648916]200 participants (Anticipated)Observational2022-08-02Enrolling by invitation
Evaluation of Perioperative Celecoxib for Hip Arthroscopy [NCT02779166]98 participants (Actual)Interventional2012-08-31Completed
A Randomized, Double-blind, Active- (Tramadol and Celecoxib) and Placebo-controlled, Parallel Groups, Phase 3 Clinical Trial to Establish the Efficacy of Co-crystal E-58425 for the Management of Moderate to Severe Post-surgical Pain After Bunionectomy. [NCT03108482]Phase 3637 participants (Actual)Interventional2017-03-14Completed
Non-Steroidal Anti-inflammatory Drugs in Axial Spondyloarthritis: a Pilot Study [NCT03473665]Phase 49 participants (Actual)Interventional2018-03-01Terminated(stopped due to Slow recruitment)
A Prospective Randomized Blinded Placebo Controlled Comparison of Multimodal Pre-emptive Analgesia on Long Term Outcome Following Uterine Artery Embolization [NCT01555073]Phase 423 participants (Actual)Interventional2011-10-31Terminated(stopped due to Subjects did not meet inclusion criteria)
A Phase III, 12-Week, Randomized, Active-Comparator-Controlled, Parallel-Group, Double Blind Study in Korea to Assess the Safety and Efficacy of Etoricoxib 30 mg Versus Celecoxib 200 mg in Patients With Osteoarthritis [NCT01554163]Phase 3239 participants (Actual)Interventional2012-03-31Completed
An Open Label Safety Study of a Single Administration of F14 in Patients Undergoing Unilateral Total Knee Replacement [NCT04860635]Phase 2/Phase 3100 participants (Anticipated)Interventional2023-09-30Suspended(stopped due to Study superseded by alternative Phase 3 trial)
Effects of Nonsteroidal Anti-inflammatory Drug (NSAID) on Inflammatory Lesion of Axial Spondyloarthritis Results From MRI Finding [NCT03190603]Phase 412 participants (Actual)Interventional2018-06-01Completed
A Prospective Randomized Placebo Controlled Study to Evaluate the Effect of Celecoxib on the Efficacy and Safety of Amlodipine in Subjects With Hypertension Requiring Antihypertensive Therapy [NCT02172040]Phase 3152 participants (Actual)Interventional2014-06-26Completed
Celebrex and Metformin for Postoperative Hepatocellular Carcinoma [NCT03184493]Phase 3200 participants (Anticipated)Interventional2017-06-02Recruiting
An Open-Label Phase I Trial to Evaluate the Safety and Tolerability of ATRA, Celecoxib, and Itraconazole Administered As Maintenance Treatment Post-Autologous Transplantation in Relapsed Multiple Myeloma [NCT02401295]Phase 11 participants (Actual)Interventional2015-05-31Completed
Improvement in Pain, Function and Quality of Life With a Protocolized Exercise Program Compared With Non-steroidal Anti-inflammatory Analgesics in Patients With Subacute Low Back Pain in Medellín, Colombia, 2009-2010 [NCT01374269]Phase 490 participants (Actual)Interventional2009-06-30Completed
Biomarkers of Neuroinflammation and Anti-Inflammatory Treatments in Major Depressive Disorder [NCT02362529]Early Phase 1115 participants (Anticipated)Interventional2015-02-28Completed
Single Dose Preoperative Gabapentin Use in Minimally Invasive Hysterectomy for Acute Pain Management [NCT02703259]Phase 4137 participants (Actual)Interventional2016-06-30Completed
COX-2 Inhibitor Reduces Serum PSA Levels Might Predict a Lower Risk of Prostatic Cancer in Men With LUTS/BPH With an Elevated PSA Level [NCT01678313]Phase 2140 participants (Actual)Interventional2012-08-31Completed
Different Kinds of Acupuncture Treatment for Knee Osteoarthritis：a Multicentre Randomised Controlled Trial [NCT03563690]360 participants (Actual)Interventional2018-07-03Completed
Efficacy of Multimodal Analgesia Following Hip Arthroscopy [NCT03351439]100 participants (Actual)Interventional2018-04-06Completed
a Multicenter, Double-blind, Randomized, Active Drug Control, Parallel Design Phase 3 Clinical Trial to Evaluate the Efficacy and Safety of YYC301 in Patients With Osteoarthritis of the Knee Joint [NCT05362851]Phase 3692 participants (Anticipated)Interventional2021-11-11Recruiting
Comparative Study for Decrease of Pain Intensity and Pain Sensitivity Between Pregabalin + COX-2 Inhibitor and COX-2 Inhibitor in Patients With Lumbar Spinal Stenosis: Randomized Controlled Trial [NCT03584074]Phase 460 participants (Anticipated)Interventional2018-07-01Not yet recruiting
Pharmacoepidemiological Study on the Use of Arcoxia® Under Actual Conditions of Use in France [NCT01572675]547 participants (Actual)Observational2012-06-30Completed
A Randomized, Open-label, Negative and Positive Control, Crossover Clinical Study to Evaluate Effect on QT/QTc Interval After Multiple Dose of Celecoxib in Healthy Adult Volunteers [NCT03822520]Phase 128 participants (Actual)Interventional2017-06-30Completed
A Pharmacokinetic Study of the Interaction Between Celecoxib and Anticonvulsant Drugs in Patients With Newly Diagnosed Glioblastoma Multiforme Undergoing Radiation Therapy [NCT00068770]Phase 235 participants (Actual)Interventional2003-10-31Terminated(stopped due to EORTC trail showed TMZ & RT conferred significant survivial in this population)
A Multiple-Dose, Dose-Escalation Study to Evaluate the Safety and Tolerability of LY3031207 in Healthy Subjects [NCT01632566]Phase 139 participants (Actual)Interventional2012-06-30Terminated(stopped due to Elevation of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in some participants.)
Multimodal Opioid-free Anesthesia Versus Opioid-based Anesthesia for Patients Undergoing Cardiac Valve Surgeries: A Randomized Controlled Trial [NCT04648540]Early Phase 160 participants (Actual)Interventional2020-12-01Completed
A Double-blinded Phase II Study of the Expression of Ki-67/MIB-1 in Women With Hyperplasia of the Breast Randomized to Receive Daily Celecoxib 400 mg BID or Placebo [NCT00291694]Phase 272 participants (Actual)Interventional2003-04-30Completed
A Comparison of Non-Surgical Treatment Methods for Patients With Lumbar Spinal Stenosis [NCT01943435]259 participants (Actual)Interventional2013-11-20Completed
A Phase 1/2 Trial Evaluating αDC1 Vaccines Combined With Tumor-Selective Chemokine Modulation as Adjuvant Therapy After Surgical Resection of Peritoneal Surface Malignancies [NCT02151448]Phase 1/Phase 264 participants (Actual)Interventional2014-07-31Completed
Effectiveness and Safety of Different Doses of BI 1026706 in Patients With Postoperative Dental Pain (a Single-centre, Partially Double-blinded, Randomised, placebo-and Active Comparator-controlled, Single-dose, Parallel-group Study) [NCT02084511]Phase 180 participants (Actual)Interventional2014-03-31Completed
Lidocaine Spray Plus Oral Celecoxib for Pain Control During Hysterosalpingography: a Randomized Controlled Trial [NCT04505657]150 participants (Actual)Interventional2020-09-01Completed
A Prospective, Randomized, Controlled, Single Centre Trial to Assess the Efficacy and Safety of Radial Extracorporeal Shock Wave Therapy in Patients With Chronic Non-specific Low Back Pain [NCT03337607]150 participants (Anticipated)Interventional2017-11-13Recruiting
A Single-Dose, Dose-Escalation Study to Evaluate the Safety and Tolerability of LY3031207 in Healthy Subjects [NCT01449630]Phase 129 participants (Actual)Interventional2011-10-24Completed
Twenty-four Month Exploratory Study of the Effect of Chondroitin Sulphate on Structural Changes in Knee Osteoarthritis Patients as Assessed by MRI [NCT01354145]Phase 3194 participants (Actual)Interventional2011-06-30Completed
A Pilot Study of Toripalimab With or Without Celecoxib as Neoadjuvant Therapy in Resectable Non-metastatic Colorectal Cancer Patients With Mismatch Repair-deficient or Microsatellite Instability-high [NCT03926338]Phase 1/Phase 269 participants (Anticipated)Interventional2019-05-10Recruiting
A Randomized Double-blinded Study to Evaluate Preincisional Dextromethorphan in Patients Undergoing Total Knee Arthroplasty and Its Effect on Postoperative Opioid Use [NCT02987920]Phase 423 participants (Actual)Interventional2017-01-31Terminated(stopped due to The surgeon changed pain control protocol for all patients. Continued enrollment impossible under approved protocol.)
A Randomized, Double-blind, Placebo- and Active-controlled, Parallel-group Analgesic Efficacy Trial of Oral ARRY-371797 in Subjects Undergoing Third Molar Extraction [NCT00663767]Phase 2250 participants (Actual)Interventional2008-04-07Completed
Does Duloxetine Reduce Chronic Pain After Total Knee Arthroplasty? [NCT02307305]Phase 2168 participants (Anticipated)Interventional2014-08-31Recruiting
"Medical Treatment of High-Risk Neurofibromas in Patients With Type 1 Neurofibromatosis: A Clinical Trial of Sequential Medical Therapies" [NCT00846430]Phase 29 participants (Actual)Interventional2008-10-31Completed
Pain Management in Head and Neck Surgery Patients [NCT03121963]Phase 40 participants (Actual)Interventional2017-11-10Withdrawn(stopped due to This protocol was difficult to enroll into, and changes to personnel have made it difficult to main this study. Data collection was not completed and therefore, no data analysis was performed. The PI has made the decision to close this study.)
A Phase II Study of Type-1 Polarized Dendritic Cell (aDC1) -Based Treatment in Combination With Tumor-Selective Chemokine Modulation (CKM: Interferon Alpha 2b, Rintatolimod and Celecoxib) in Melanoma Patients With Primary PD-1/PD-L1 Resistance [NCT04093323]Phase 224 participants (Anticipated)Interventional2023-12-31Suspended(stopped due to IFNa2b supply shortage)
A PHASE 3 RANDOMIZED, DOUBLE-BLIND, ACTIVE-CONTROLLED, MULTICENTER STUDY OF THE LONG-TERM SAFETY AND EFFICACY OF SUBCUTANEOUS ADMINISTRATION OF TANEZUMAB IN JAPANESE ADULT SUBJECTS WITH CHRONIC LOW BACK PAIN [NCT02725411]Phase 3277 participants (Actual)Interventional2016-05-26Completed
A Pilot Study of Low-Dose Antiangiogenic Chemotherapy in Combination With Standard Multiagent Chemotherapy for Patients With Newly Diagnosed Metastatic Ewing Sarcoma Family of Tumors [NCT00061893]Phase 238 participants (Actual)Interventional2004-04-30Completed
A Phase II Trial of Celecoxib in Patients With IPMN [NCT00198081]Phase 28 participants (Actual)Interventional2005-09-30Terminated(stopped due to Lack of funding and personnel to conduct study.)
Phase II Combination Therapy Selection Trial in Amyotrophic Lateral Sclerosis [NCT00355576]Phase 286 participants (Actual)Interventional2006-07-31Completed
An Open Label Phase 2 Study to Evaluate the Effects of a Local Anesthetic, Anti-inflammatory Medications and Compression Garments on RZL-012-Induced Adverse Events [NCT05476679]Phase 1/Phase 248 participants (Actual)Interventional2022-09-25Completed
A Pilot, Randomized, Open-label, Single Dose Study to Evaluate the Safety and Efficacy of Celecoxib Plus Nucleos(t)Ide Analogues on the Hepatitis B Surface Antigen of Virally Suppressed Subjects With Chronic Hepatitis B(a Multicenter, Open-labelled, Rando [NCT05256823]Phase 247 participants (Actual)Interventional2022-02-24Active, not recruiting
Evaluation of the Acute Analgesic Efficacy of a Single Dose of LY3023703 in Patients With Postsurgical Dental Pain: A Parallel, Double-Blind, Randomized, Placebo and Positive Control Study [NCT01872910]Phase 2124 participants (Actual)Interventional2013-06-30Completed
A Randomized Double Blind Placebo Controlled Parallel Group Study Of The Efficacy And Safety Of Concomitant Administration Of Celecoxib And Pregabalin Compared With Celecoxib Monotherapy, In Patients With Chronic Low Back Pain Having A Neuropathic Compone [NCT01838044]Phase 4180 participants (Actual)Interventional2013-10-31Terminated(stopped due to Recruitment terminated on 3Apr2015 due to slow recruitment rate and lack of operational feasibility. Study was not terminated for reasons of safety/efficacy.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00033371 (3) [back to overview]Percent Change in the Number of Polyps Greater Than or Equal to 2mm in Diameter in Focal Area(s) of the Colorectum
NCT00033371 (3) [back to overview]Number of Participants With Adverse Events Occurring at a Frequency of 5% or Grade 3 and Higher
NCT00033371 (3) [back to overview]Percentage Change in Global Colorectal Polyps Burden
NCT00038103 (8) [back to overview]Time to Treatment Failure
NCT00038103 (8) [back to overview]Duration of Clinical Benefit
NCT00038103 (8) [back to overview]Duration of Long-Term SD
NCT00038103 (8) [back to overview]Duration of Objective Response (in Subjects With CR or PR)
NCT00038103 (8) [back to overview]Number of Subjects With Clinical Benefit
NCT00038103 (8) [back to overview]Number of Subjects With Objective Response
NCT00038103 (8) [back to overview]Survival
NCT00038103 (8) [back to overview]Time to Tumor Progression
NCT00046839 (2) [back to overview]Overall Survival
NCT00046839 (2) [back to overview]Maximum Tolerated Dose (MTD) of Celecoxib Combined With Radiation Therapy (RT)
NCT00061893 (2) [back to overview]Occurrence of Severe Toxicity
NCT00061893 (2) [back to overview]Event Free Survival
NCT00068770 (2) [back to overview]Overall Survival
NCT00068770 (2) [back to overview]Effects of Hepatic Enzyme Inducing Drugs Such as Anticonvulsants, on the PK of Celecoxib
NCT00081263 (2) [back to overview]Histologic Regression
NCT00081263 (2) [back to overview]Incidence of Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events Version 3.0
NCT00099047 (1) [back to overview]Changes in M-protein Levels
NCT00112502 (10) [back to overview]Overall Survival of Individual Arms
NCT00112502 (10) [back to overview]Median Progression-Free Survival (PFS) of Individual Arms
NCT00112502 (10) [back to overview]Median Progression-Free Survival (PFS) Comparison of Thalidomide Arms Versus no Thalidomide Arms
NCT00112502 (10) [back to overview]Median Progression-Free Survival (PFS) Comparison of Doublet Versus Triplet Therapy
NCT00112502 (10) [back to overview]Median Progression-Free Survival (PFS) Comparison of Isotretinoin Arms Versus no Isotretinoin Arms
NCT00112502 (10) [back to overview]Median Progression-Free Survival (PFS) Comparison of Celecoxib Arms Versus no Celecoxib Arms
NCT00112502 (10) [back to overview]Median Overall Survival (OS) Comparison of Doublet Versus Triplet Therapy
NCT00112502 (10) [back to overview]Median Overall Survival (OS) Comparison of Isotretinoin Arms Versus no Isotretinoin Arms
NCT00112502 (10) [back to overview]Median Overall Survival (OS) Comparison of Celecoxib Arms Versus no Celecoxib Arms
NCT00112502 (10) [back to overview]Median Overall Survival (OS) Comparison of Thalidomide Arms Versus no Thalidomide Arms
NCT00139776 (16) [back to overview]Area Under the Curve (AUCs) of Western Ontario and McMaster Universities (WOMAC) Osteoarthritis Scores
NCT00139776 (16) [back to overview]Arthritis Pain Numerical Rating Scale (NRS)
NCT00139776 (16) [back to overview]Change in Medical Outcomes Study Sleep Scale - All Assessments
NCT00139776 (16) [back to overview]Change in the Quality of Life Short Form-12v2 (SF-12v2) Scale Scores - All Assessments
NCT00139776 (16) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Osteoarthritis Scores
NCT00139776 (16) [back to overview]Medical Outcomes Study Sleep Scale - Number of Participants With Optimal, Mixed and Not Optimal Sleep
NCT00139776 (16) [back to overview]Patient's Global Assessment of Arthritis
NCT00139776 (16) [back to overview]Physician's Global Assessment of Arthritis at Final Visit
NCT00139776 (16) [back to overview]Serious Adverse Events in Open Label run-in Period
NCT00139776 (16) [back to overview]Total Rescue Medication Taken (Mean)
NCT00139776 (16) [back to overview]Days on Flare Medication
NCT00139776 (16) [back to overview]Number of Flare Events Per Time of Exposure to Study Medication
NCT00139776 (16) [back to overview]Proportion of Days in Osteoarthritis (OA) Flare
NCT00139776 (16) [back to overview]Time to Occurrence of First Osteoarthritis (OA) Flare
NCT00139776 (16) [back to overview]Proportion of Days on Rescue Medication
NCT00139776 (16) [back to overview]Proportion of Days Free From Osteoarthritis (OA) Flare
NCT00141102 (17) [back to overview]Change From Baseline in Hemoglobin at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Iron Binding Capacity to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)
NCT00141102 (17) [back to overview]Number of Subjects Alive at the Post Trial Interview
NCT00141102 (17) [back to overview]Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview
NCT00141102 (17) [back to overview]Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)
NCT00141102 (17) [back to overview]Number of Subjects With Moderate to Severe Abdominal Symptoms
NCT00141102 (17) [back to overview]Number of Subjects With SUs
NCT00141102 (17) [back to overview]Number of Subjects Withdrawn Due to GI Adverse Events (AEs)
NCT00141102 (17) [back to overview]Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIEs by History of GD Ulceration
NCT00141102 (17) [back to overview]Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)
NCT00141102 (17) [back to overview]Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)
NCT00141102 (17) [back to overview]Change From Baseline in Hematocrit at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in C-Reactive Protein to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Ferretin to Month 6/ET
NCT00151476 (12) [back to overview]Duodenal Adenoma Burden as Measured by Polyp Counts
NCT00151476 (12) [back to overview]Time From Ileopouch Anal Anastomosis (IPAA) to Time of First Excisional Polypectomy of a Rectal Polyp Post IPAA
NCT00151476 (12) [back to overview]Time From Ileorectal Anastomosis (IRA) to Time of First Excisional Polypectomy of a Rectal Polyp Post IRA
NCT00151476 (12) [back to overview]Time From Most Recent Prior FAP-related Surgical Event or Onset of FAP Phenotype to Time of First Excisional or Ablational Event for Rectal, Colonic, Pouch, or Duodenal Adenomas (Duodenal Adenomatous Polyps)
NCT00151476 (12) [back to overview]Time From Most Recent Prior FAP-related Surgical Event or Onset of FAP Phenotype to Time of First FAP-related Adverse Event
NCT00151476 (12) [back to overview]Time From Post IRA to Time of Conversion From IRA to IPAA
NCT00151476 (12) [back to overview]Time From Start of Study Follow-up to the Time of First Excisional Polypectomy of a Rectal Polyp Post IRA
NCT00151476 (12) [back to overview]Time From Start of Study Follow-up to Time of Conversion From IRA to IPAA
NCT00151476 (12) [back to overview]Time From Start of Study Follow-up to Time of First Excisional or Ablational Event for Rectal, Colonic, Pouch, or Duodenal Adenomas
NCT00151476 (12) [back to overview]Time From Start of Study Follow-up to Time of First Excisional Polypectomy of a Rectal Polyp Post IPAA
NCT00151476 (12) [back to overview]Time From Start of Study Follow-up to Time of First FAP-related Adverse Event
NCT00151476 (12) [back to overview]Rectal or Pouch Adenoma Burden Based on Polyp Counts
NCT00198081 (4) [back to overview]Concentration of PGE2 in Serum at Baseline, Surgery, 1 wk, 4wks, and 6 Months
NCT00198081 (4) [back to overview]Concentration of PGE2 in Urine at Baseline, Surgery, 1 wk, 4wks, and 6 Months
NCT00198081 (4) [back to overview]Concentration of PGEM in Serum at Baseline, Surgery, 1 wk, 4wks, and 6 Months
NCT00198081 (4) [back to overview]Concentration of PGEM in Urine at Baseline, Surgery, 1 wk, 4wks, and 6 Months
NCT00201773 (2) [back to overview]Number of Patients With Decreased Gene Expression of CYP19 in Breast Cancer by Adding COX-2 Inhibitor to Exemestane
NCT00201773 (2) [back to overview]Evaluate Response Rate of Neoadjuvant Exemestane and Celecoxib in Postmenopausal Women.
NCT00250835 (6) [back to overview]Toxicity
NCT00250835 (6) [back to overview]Surgical Downstaging Rate
NCT00250835 (6) [back to overview]Progression-free Survival (PFS)
NCT00250835 (6) [back to overview]Pelvic Local Control Rate
NCT00250835 (6) [back to overview]Incidence of Sphincter-sparing Surgery
NCT00250835 (6) [back to overview]Pathologic Complete Response (PCR)
NCT00291694 (5) [back to overview]Serum Sex Hormone Binding Globulin (SHBG) Concentration
NCT00291694 (5) [back to overview]Serum Estradiol Concentration
NCT00291694 (5) [back to overview]Molecular Ratio of Serum Concentration of IGF-1 to IGFBP3
NCT00291694 (5) [back to overview]Mammographic Breast Density
NCT00291694 (5) [back to overview]Change in Percent of Breast Epithelial Cells Staining Positive for Ki-67
NCT00314262 (3) [back to overview]Clinical Outcome: Documented Progression
NCT00314262 (3) [back to overview]Dose Escalation and Toxicity: Toxicities Including Grades 1 to 4
NCT00314262 (3) [back to overview]Clinical Outcome: Progression to a Higher-grade Dysplasia or Carcinoma
NCT00346216 (4) [back to overview]The First Occurrence of Clinically Significant Gastrointestinal Events (CSGIE)
NCT00346216 (4) [back to overview]Change From Baseline in Patient's Assessment of Arthritis Pain (VAS)
NCT00346216 (4) [back to overview]The First Occurrence of a Major Adverse Cardiovascular Events (MACE)
NCT00346216 (4) [back to overview]The First Occurrence of Antiplatelet Trialists Collaboration (APTC) Composite Endpoint, Confirmed by the Clinical Events Committee (CEC).
NCT00357500 (4) [back to overview]Best Response
NCT00357500 (4) [back to overview]27-Week Progression-Free Survival
NCT00357500 (4) [back to overview]Therapy Completion Rate
NCT00357500 (4) [back to overview]27-Week Overall Survival
NCT00373685 (15) [back to overview]Change From Baseline Hct at Week 24
NCT00373685 (15) [back to overview]Percentage of Participants With Proton Pump Inhibitor (PPI) and Other Gastric Protective Drug Utilization
NCT00373685 (15) [back to overview]Change From Baseline Hb at Week 24
NCT00373685 (15) [back to overview]Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Time to Pain Relief
NCT00373685 (15) [back to overview]Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Duration of Pain Relief
NCT00373685 (15) [back to overview]Percentage of Participants With Non-study Medication Utilization
NCT00373685 (15) [back to overview]Percentage of Participants With Clinically Significant Decrease in Hct and/or Hb From Baseline
NCT00373685 (15) [back to overview]Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Amount of Pain Relief
NCT00373685 (15) [back to overview]Percentage of Participants With Moderate to Severe Abdominal Symptoms
NCT00373685 (15) [back to overview]Percentage of Participants With Positive Blood Fecal Occult
NCT00373685 (15) [back to overview]Percentage of Participants With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)
NCT00373685 (15) [back to overview]Percentage of Participants Who Withdrew Due to GI Adverse Events (AEs)
NCT00373685 (15) [back to overview]Hemoglobin (Hb) at Baseline
NCT00373685 (15) [back to overview]Hematocrit (Hct) at Baseline
NCT00373685 (15) [back to overview]Percentage of Participants Satisfied With Efficacy of Current Pain Medication Overall
NCT00402987 (45) [back to overview]Sore Throat Relief Rating Scale (STRRS) - 'Moderate Relief' at 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects Taking Rescue Medication
NCT00402987 (45) [back to overview]Subjects With >= 50% Total Pain Relief (TOTPAR) at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects With >= 50% Total Pain Relief (TOTPAR) at 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Sore Throat Pain Intensity Difference (SPID2) as Measured by Difficulty Swallowing Scale (DSS) at 2 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Sore Throat Pain Intensity Difference (SPID2) on Swallowing at 2 Hours Post-First Dose
NCT00402987 (45) [back to overview]Time to Meaningful Pain Relief
NCT00402987 (45) [back to overview]Time to Perceptible Pain Relief
NCT00402987 (45) [back to overview]Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]First Perceptible Relief
NCT00402987 (45) [back to overview]No Perceptible Relief
NCT00402987 (45) [back to overview]Patient's Global Evaluation of Study Medication at 12 and 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Patient's Global Evaluation of Study Medication at 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Pain Intensity Difference (PID) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Pain Intensity Difference (PID) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Relief Rating Scale (STRRS) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Relief Rating Scale (STRRS) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects Who Achieved Their Own Level of 'Meaningful Relief' and 'Much Improvement' at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects Who Achieved Their Own Level of 'Meaningful Relief' and 'Much Improvement' at 2 and 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Who Had Perceptible Relief Onset Time Within 1 Hour
NCT00402987 (45) [back to overview]Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Who Still Had Perceptible Relief at 12 and 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects With Sore Throat Pain at Least 35% Gone and at Least 50% Gone at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Number Needed to Treat (NNT) to Achieve at Least 50% of Maximum Total Pain Relief (TOTPAR) at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Subjects With Sore Throat Pain at Least 35% Gone and at Least 50% Gone at 2 and 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Sore Throat Pain Intensity Difference (SPID) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Sore Throat Pain Intensity Difference (SPID) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Throat Soreness Difference as Measured by Throat Soreness Scale (TSS) From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sum of Throat Soreness Difference as Measured by Throat Soreness Scale (TSS) Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Throat Soreness Scale (TSS) Difference From 7 to 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Throat Soreness Scale (TSS) Difference Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Total Pain Relief (TOTPAR) at 12 and 24 Hours Post-First Dose
NCT00402987 (45) [back to overview]Total Pain Relief (TOTPAR) at 2 and 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Treatment Failures on STRRS Questionnaire
NCT00402987 (45) [back to overview]Treatment Satisfaction Questionnaire for Medication (TSQM vII)
NCT00402987 (45) [back to overview]Time to Onset of Analgesia
NCT00402987 (45) [back to overview]Number Needed to Treat (NNT) to Achieve at Least 50% of Maximum Total Pain Relief (TOTPAR) at 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Pain Intensity Difference (SPID2) as Measured by Throat Soreness Scale (TSS) at 2 Hours Post-First Dose
NCT00402987 (45) [back to overview]Sore Throat Relief Rating Scale (STRRS) - 'Moderate Relief' at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Difficulty Swallowing Scale (DSS) Difference at Least 50% Gone at 12 Hours Post-First Dose
NCT00402987 (45) [back to overview]Difficulty Swallowing Scale (DSS) Difference at Least 50% Gone at 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Median Offset Time of No Perceptible Relief in Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Post-First Dose
NCT00402987 (45) [back to overview]Median Onset Time of First Perceptible Relief in Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Post-First Dose
NCT00424294 (21) [back to overview]Change From Baseline in Swollen Joint Count (SJC) at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Patient's Global Assessment of Arthritis at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Patient's Assessment of Arthritis Pain at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Percentage of Participants Achieving American College of Rheumatology 20% (ACR20) Response at Week 12
NCT00424294 (21) [back to overview]Change From Baseline in Heart Rate Day 7, 14, 21, 28, 42, 56, 84 and 91
NCT00424294 (21) [back to overview]Change From Baseline in Health Assessment Questionnaire-Disability Index (HAQ-DI) Score at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Duration of Morning Stiffness at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Disease Activity Score Based on 28-Joints Count and C-Reactive Protein (3 Variables) (DAS28-3 [CRP]) at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Physician's Global Assessment of Arthritis at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in C-Reactive Protein (CRP) at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Number of Participants Who Withdrew From Study Due to Lack of Efficacy
NCT00424294 (21) [back to overview]Number of Participants With Clinical Laboratory Abnormalities
NCT00424294 (21) [back to overview]Percentage of Participants Achieving American College of Rheumatology 70% (ACR70) Response
NCT00424294 (21) [back to overview]Percentage of Participants Achieving American College of Rheumatology 50% (ACR50) Response
NCT00424294 (21) [back to overview]Percentage of Participants Achieving American College of Rheumatology 20% (ACR20) Response at Week 1, 2, 4 and 8
NCT00424294 (21) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00424294 (21) [back to overview]Number of Participants With Categorical Vital Signs Data
NCT00424294 (21) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG)
NCT00424294 (21) [back to overview]Number of Adverse Events by Severity
NCT00424294 (21) [back to overview]Change From Baseline in Tender/Painful Joint Count (TJC) at Week 1, 2, 4, 8 and 12
NCT00424294 (21) [back to overview]Change From Baseline in Systolic and Diastolic Blood Pressure at Day 7, 14, 21, 28, 42, 56, 84 and 91
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Index
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 1
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 2
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 3
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 4
NCT00446797 (20) [back to overview]Number of Subjects Responding (Improving) - MITT Population
NCT00446797 (20) [back to overview]Pain Relief - MITT Population
NCT00446797 (20) [back to overview]Physician Global Assessment of Ankle Injury
NCT00446797 (20) [back to overview]Subject's Global Assessment of Ankle Injury
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5G
NCT00446797 (20) [back to overview]Subject Assessment of Normal Function / Activity
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Index
NCT00446797 (20) [back to overview]Change From Baseline at Day 3 in Pain Visual Analog Scale (VAS) - Per Protocol Population
NCT00446797 (20) [back to overview]Change From Baseline in Pain Visual Analog Scale (VAS) - Modified Intent to Treat Population
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5A
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5B
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5C
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5D
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5E
NCT00446797 (20) [back to overview]Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5F
NCT00466505 (9) [back to overview]One Year Survival Rate
NCT00466505 (9) [back to overview]Urinary PGE-M : Treatment Cycle 2
NCT00466505 (9) [back to overview]Urinary PGE-M : Treatment Cycle 1
NCT00466505 (9) [back to overview]Serum TGF-alpha: Treatment Cycle 2
NCT00466505 (9) [back to overview]Patient Response to Treatment
NCT00466505 (9) [back to overview]Number of Patients With Each Worst-grade Toxicity Response
NCT00466505 (9) [back to overview]Progression-free Survival (PFS)
NCT00466505 (9) [back to overview]Overall Survival
NCT00466505 (9) [back to overview]Serum TGF-alpha: Treatment Cycle 1
NCT00499655 (5) [back to overview]Progression-free Survival - Low PGEM
NCT00499655 (5) [back to overview]Number of Participants With Overall Response
NCT00499655 (5) [back to overview]Progression-free Survival
NCT00499655 (5) [back to overview]Progression-free Survival - EGRF
NCT00499655 (5) [back to overview]Progression-free Survival - Elevated PGEM
NCT00503035 (2) [back to overview]13-HODE Colonic Tissue Levels
NCT00503035 (2) [back to overview]PGE2 Colonic Tissue Levels
NCT00504660 (2) [back to overview]6 Month Progression-free Survival for Participants With Glioblastoma
NCT00504660 (2) [back to overview]12 Month-progression-free Survival for Participants With Anaplastic Tumors
NCT00520845 (3) [back to overview]Time to Progression
NCT00520845 (3) [back to overview]Overall Response Rate
NCT00520845 (3) [back to overview]Median Survival
NCT00538031 (3) [back to overview]Overall Response
NCT00538031 (3) [back to overview]Overall Survival
NCT00538031 (3) [back to overview]Time to Treatment Failure
NCT00549549 (15) [back to overview]Number of Participants With Pre-specified Gastrointestinal (GI) Adverse Events
NCT00549549 (15) [back to overview]Participant's Assessment of Pain Intensity for the Average Pain Intensity at Baseline
NCT00549549 (15) [back to overview]Participants Global Evaluation of Study Medication Score
NCT00549549 (15) [back to overview]Change From Baseline in Patient's Assessment of Pain Intensity
NCT00549549 (15) [back to overview]Change From Baseline in Patient's Assessment of Pain Intensity on Day 1
NCT00549549 (15) [back to overview]Change From Baseline in Physician's Assessment of the Index Joint on Days 5, 9, and 14/Early Termination: Swelling
NCT00549549 (15) [back to overview]Change From Baseline in Physician's Assessment of the Index Joint on Days 5, 9, and 14/Early Termination: Tenderness
NCT00549549 (15) [back to overview]Change From Baseline in Time Weighted Average of Patient's Assessment of Pain Intensity Over 8, 12, and 24 Hours
NCT00549549 (15) [back to overview]Change From Baseline to Day 2 in Patient's Assessment of Pain Intensity
NCT00549549 (15) [back to overview]Number of Participants With ≥30% and ≥50% Reduction From Baseline to Day 2 in Patient's Assessment of Pain Intensity
NCT00549549 (15) [back to overview]Number of Participants With Redness Present According to Physician's Assessment of the Index Joint on Day 5, Day 9, and Day 14/Early Termination
NCT00549549 (15) [back to overview]Number of Participants With Warmth Present According to Physician's Assessment of the Index Joint on Day 5, Day 9, and Day 14
NCT00549549 (15) [back to overview]Percentage Change From Baseline in the Patient's Assessment of Pain Intensity for the Average Pain Intensity on Days 2-4, Days 2-8 and Days 2-13
NCT00549549 (15) [back to overview]Number of Participants With Withdrawal From Treatment Due to Lack of Efficacy
NCT00549549 (15) [back to overview]Number of Participants With Moderate or Severe Central Nervous System (CNS) Adverse Events
NCT00571701 (7) [back to overview]Maintenance of Response Following Discontinuation of Celecoxib
NCT00571701 (7) [back to overview]Effect of Juvenile Versus Adult Disease Onset on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%.
NCT00571701 (7) [back to overview]Effect of Gender on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%.
NCT00571701 (7) [back to overview]Correlation Between Mean Plasma Level of Celecoxib and Response.
NCT00571701 (7) [back to overview]Mean Percent Change in Papilloma Growth Rate at 12 Month Measurement Compared to Baseline
NCT00571701 (7) [back to overview]Percent of Patients With Positive Response to Treatment
NCT00571701 (7) [back to overview]Effect of HPV 6 Versus HPV 11 on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%
NCT00581971 (2) [back to overview]Toxicity of Celecoxib With Concurrent Weekly Chemotherapy and Radiotherapy in the Treatment of Locally Advanced or Recurrent Squamous Cell Carcinoma of the Head and Neck.
NCT00581971 (2) [back to overview]Response as Evaluated by Recurrence of Diseases
NCT00582660 (2) [back to overview]Number of Subjects Witha Change (IMPROVEMENT) in Colo-rectal Adenocarcinoma as Measured by Cyclooxygenase-2 Activity After 7 Days of Celecoxib
NCT00582660 (2) [back to overview]Subjects With Positive Response 72 Hours After Administration of Study Treatment as Measured by Immunoblot
NCT00583453 (5) [back to overview]Acetaminophen Equivalent Use
NCT00583453 (5) [back to overview]Total Morphine Equivalent
NCT00583453 (5) [back to overview]Self-reported Pain Score
NCT00583453 (5) [back to overview]Self-reported Activity Level
NCT00583453 (5) [back to overview]Incidence of Post-operative Hemorrhage
NCT00585312 (4) [back to overview]Time to Treatment Failure
NCT00585312 (4) [back to overview]Total Number of Colorectal Polyps
NCT00585312 (4) [back to overview]Colorectal Polyp Burden
NCT00585312 (4) [back to overview]Time to Disease Progression
NCT00592319 (2) [back to overview]Number of Case With Papilloma Recurrence During a 12-month Follow up
NCT00592319 (2) [back to overview]Time Course (Month) With Papilloma Recurrence During 12-month Follow up
NCT00614406 (1) [back to overview]Menstrual Cycle Length
NCT00624559 (2) [back to overview]Mean Arterial Pressure
NCT00624559 (2) [back to overview]Urinary Sodium Excretion
NCT00662558 (14) [back to overview]Treatment Responders Based on the Numerical Rating Scale-Pain (NRS-Pain)
NCT00662558 (14) [back to overview]Patient's Satisfaction Questionnaire (With Walking and Bending Ability Scale)
NCT00662558 (14) [back to overview]Physician's Global Assessment of Disease Activity
NCT00662558 (14) [back to overview]Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Score
NCT00662558 (14) [back to overview]Change From Baseline in Severity of Chronic Low Back Pain as Measured by NRS-Pain
NCT00662558 (14) [back to overview]Change From Baseline in Severity of Low Back Pain as Measured by Visual Analogue Scale (VAS)
NCT00662558 (14) [back to overview]Change From Baseline in Medical Outcomes Study (MOS) Sleep Scale
NCT00662558 (14) [back to overview]Change From Baseline in Modified Brief Pain Inventory (m-BPI-sf)
NCT00662558 (14) [back to overview]Change From Baseline in Work Limitations Questionnaire (WLQ)
NCT00662558 (14) [back to overview]Chronic Low Back Pain Responders Based on VAS, Patient's Global, and RMDQ
NCT00662558 (14) [back to overview]Number of Subjects With Change From Baseline in MOS Optimal Sleep Scale Scores
NCT00662558 (14) [back to overview]Patient's Global Assessment of Disease Activity
NCT00662558 (14) [back to overview]Patient's Global Evaluation of Study Medication
NCT00662558 (14) [back to overview]Patient's Satisfaction Questionnaire (With Pain Relief Scale)
NCT00664560 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline
NCT00664560 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline
NCT00664560 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline
NCT00664560 (12) [back to overview]Number of Participants Reporting Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal (UGI) Symptoms
NCT00664560 (12) [back to overview]Modified Severity of Dyspepsia Assessment (mSODA)
NCT00664560 (12) [back to overview]Change in Patient Global Assessment (PGA) Subscore From Baseline
NCT00664560 (12) [back to overview]Antacid Tablet Use
NCT00664560 (12) [back to overview]American Pain Society Patient Outcome Questionnaire (APS-POQ)Total Interference Caused by Pain.
NCT00664560 (12) [back to overview]Percent of Days With no Heartburn (Heartburn Resolution)
NCT00664560 (12) [back to overview]The Number of Subjects Who Discontinued From the Study Due to Any Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal Adverse Event
NCT00664560 (12) [back to overview]Change in Patient Global Assessment (PGA) Subscore From Baseline
NCT00664560 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline
NCT00665431 (12) [back to overview]Change in Patient Global Assessment (PGA) Subscore From Baseline
NCT00665431 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline
NCT00665431 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline
NCT00665431 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline
NCT00665431 (12) [back to overview]Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline
NCT00665431 (12) [back to overview]Mean Change From Baseline in American Pain Society Patient Outcome Questionnaire (APS-POQ)Total Interference Caused by Pain.
NCT00665431 (12) [back to overview]Number of Participants Reporting Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal (UGI) Symptoms
NCT00665431 (12) [back to overview]The Number of Subjects Who Discontinued From the Study Due to Any Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal Adverse Event
NCT00665431 (12) [back to overview]Modified Severity of Dyspepsia Assessment (mSODA)
NCT00665431 (12) [back to overview]Percent of Days With no Heartburn (Heartburn Resolution)
NCT00665431 (12) [back to overview]Antacid Tablet Use
NCT00665431 (12) [back to overview]Change in Patient Global Assessment (PGA) Subscore From Baseline
NCT00665457 (1) [back to overview]Number of Participants With Grade 4 Adverse Events
NCT00688545 (2) [back to overview]JIA Concomitant Medications
NCT00688545 (2) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00698204 (2) [back to overview]Clinical Oral Mucosal Injury Score at Cumulative Radiation Dose of 5000 cGy
NCT00698204 (2) [back to overview]Evaluation of Pain Severity at 5000 cGy Radiation
NCT00762463 (26) [back to overview]Percentages of Participants Responding to Assessment in Ankylosing Spondylitis (ASAS)-20
NCT00762463 (26) [back to overview]Change From Baseline in Physician's Global Assessment of Disease Activity at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Physician's Global Assessment of Disease Activity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Global Assessment of Disease Activity at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Global Assessment of Disease Activity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Weeks 2 and 4
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Nocturnal Pain at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Chest Expansion at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Paracetamol Tablets Taken Per Day by Participant
NCT00762463 (26) [back to overview]Participant's Assessment of Global Pain Intensity at Baseline
NCT00762463 (26) [back to overview]Percentage of Days With Concomitant Administration of Paracetamol
NCT00762463 (26) [back to overview]Percentage of Participants With Concomitant Use of Paracetamol
NCT00762463 (26) [back to overview]Change From Baseline in BASDAI at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in BASFI at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Bath Ankylosing Spondylitis Functional Index (BASFI) at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Chest Expansion at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 6
NCT00762463 (26) [back to overview]Change From Baseline in CRP at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Fingertips to Floor Distance at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Fingertips to Floor Distance at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in C-Reactive Protein (CRP) at Week 6
NCT00762463 (26) [back to overview]Change From Baseline in Nocturnal Pain at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in ESR at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Erythrocyte Sedimentation Rate (ESR) at Week 6
NCT00807846 (14) [back to overview]Change From Baseline in Assessment of ABPM for SBP and DBP Pressure at Week 6/Final Visit (Sensitivity Analysis Excluding One Participant)
NCT00807846 (14) [back to overview]Change From Baseline in Assessment of Ambulatory Blood Pressure Monitoring (ABPM) for SBP and DBP at Week 6/Final Visit
NCT00807846 (14) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) at Week 6/Final Visit
NCT00807846 (14) [back to overview]Number of Participants With >= 30% Improvement in the Parent's Global Assessment of Overall Well-being at Week 6/Final Visit.
NCT00807846 (14) [back to overview]Change From Baseline in Assessment of ABPM for Heart Rate at Week 6/Final Visit
NCT00807846 (14) [back to overview]Change From Baseline in Assessment of ABPM for Heart Rate at Week 6/Final Visit (Sensitivity Analysis Excluding One Participant)
NCT00807846 (14) [back to overview]Change From Baseline in DBP at Week 4.
NCT00807846 (14) [back to overview]Change From Baseline in DBP at Week 6/Final Visit
NCT00807846 (14) [back to overview]Change From Baseline in Diastolic Blood Pressure (DBP) at Week 2.
NCT00807846 (14) [back to overview]Change From Baseline in Parent's Assessment of Overall Well-being at Week 6/Final Visit.
NCT00807846 (14) [back to overview]Change From Baseline in Participant's Assessment of Overall Well-being at Week 6/Final Visit.
NCT00807846 (14) [back to overview]Change From Baseline in SBP at Week 4.
NCT00807846 (14) [back to overview]Change From Baseline to Week 2 in SBP.
NCT00807846 (14) [back to overview]Number of Participants With >= 30% Improvement in the Participant's Global Assessment of Overall Well-being at Week 6/Final Visit.
NCT00846430 (4) [back to overview]At Least 50% Shrinkage in Tumor Measurements by Physical Examination
NCT00846430 (4) [back to overview]Improvement of Symptoms and Pain
NCT00846430 (4) [back to overview]No Reported Psychological Toxicity Based Upon Psychological Evaluations
NCT00846430 (4) [back to overview]Response by MRI Measurements
NCT00953849 (4) [back to overview]Change in GM-CSF
NCT00953849 (4) [back to overview]Change in IFN-gamma Levels
NCT00953849 (4) [back to overview]Change in IL-2 Levels
NCT00953849 (4) [back to overview]Change in IL-6 Levels.
NCT00964431 (1) [back to overview]Total Patient Pain Relief Over 0 to 8 Hours.
NCT00970502 (4) [back to overview]Toxicity
NCT00970502 (4) [back to overview]Clinical Response
NCT00970502 (4) [back to overview]Locoregional Control, Progression-free Survival, Overall Survival and Late Toxicity
NCT00970502 (4) [back to overview]Locoregional Progression
NCT00976716 (13) [back to overview]"Patient Impressions Within 8 Days Post-first Dose (the Number of Subjects Who Have Rated Excellent and Good)"
NCT00976716 (13) [back to overview]Withdrawal Due to Lack of Efficacy
NCT00976716 (13) [back to overview]"Patient Impressions at Final Visit (the Number of Participants Who Have Rated Excellent and Good)"
NCT00976716 (13) [back to overview]Pain Intensity Differences (PID) in Pain at Rest (Spontaneous Pain) Within 8 Days Post-first Dose
NCT00976716 (13) [back to overview]Summary of Adverse Events
NCT00976716 (13) [back to overview]Sum of Pain Intensity Differences (SPID) for Pain at Rest (Spontaneous Pain) and on Active Movement Until 6 Hours Post-first Dose
NCT00976716 (13) [back to overview]Severity of Inflammatory Symptoms (Swelling) Within 8 Days Post-first Dose
NCT00976716 (13) [back to overview]Severity of Inflammatory Symptoms (Redness) Within 8 Days Post-first Dose
NCT00976716 (13) [back to overview]Severity of Inflammatory Symptoms (Localized Warmth) Within 8 Days Post First Dose
NCT00976716 (13) [back to overview]PID in Pain on Active Movement Within 8 Days Post-first Dose
NCT00976716 (13) [back to overview]PI of Pain on Active Movement as Measured by VAS Within 8 Days Post-first Dose
NCT00976716 (13) [back to overview]Peak Pain Intensity Difference (PPID) for Pain at Rest (Spontaneous Pain) and on Active Movement Until 6 Hours Post-first Dose
NCT00976716 (13) [back to overview]Pain Intensity (PI) of Pain at Rest (Spontaneous Pain) as Measured by Visual Analog Scale (VAS) Within 8 Days Post-first Dose
NCT00985439 (1) [back to overview]Total Patient Pain Relief Over 0 to 12 Hours.
NCT00994461 (7) [back to overview]Incidence of Any Gastric, and Duodenal Ulcers
NCT00994461 (7) [back to overview]Incidence of Any Gastroduodenal, Gastric, and Duodenal Ulcers and/or Erosions
NCT00994461 (7) [back to overview]Number of Gastroduodenal Erosions in Each Subject
NCT00994461 (7) [back to overview]Number of Gastroduodenal Ulcers in Each Subject
NCT00994461 (7) [back to overview]Post-treatment Gastroduodenal Endoscopic Scores (According to Mucosal Grading Scale)
NCT00994461 (7) [back to overview]Incidence of Gastroduodenal Ulcers
NCT00994461 (7) [back to overview]Incidence of Treatment-emergent, All-causality GI Body System Adverse Events
NCT01021215 (3) [back to overview]Median Urinary LTE4 Levels (Pre and Post Treatment)
NCT01021215 (3) [back to overview]Proportion of Cases With a Post-treatment Increase in Urinary PGE-M Levels
NCT01021215 (3) [back to overview]Median Urinary PGE-M Levels (Pre and Post Treatment)
NCT01041781 (7) [back to overview]Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the Median Quartile (Q2)
NCT01041781 (7) [back to overview]Response Rate
NCT01041781 (7) [back to overview]Progression-free Survival
NCT01041781 (7) [back to overview]Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the Third Quartile (Q3)
NCT01041781 (7) [back to overview]Overall Survival
NCT01041781 (7) [back to overview]Incidence of Toxicities as Assessed by NCI CTCAE v. 4.0
NCT01041781 (7) [back to overview]Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the First Quartile (Q1)
NCT01062113 (4) [back to overview]Number of Participants in Each Pain Intensity (PI) With 4 Categories
NCT01062113 (4) [back to overview]Pain Intensity Measured by Visual Analog Scale (VAS)
NCT01062113 (4) [back to overview]Efficacy Rate (Percentage) of Patient's Impression
NCT01062113 (4) [back to overview]Differences in Pain Intensity (PI) Measured by VAS Among Participants
NCT01129245 (3) [back to overview]Peak Estradiol Level
NCT01129245 (3) [back to overview]Peak Hormone Levels
NCT01129245 (3) [back to overview]Number of Cycles With Ovulation Dysfunction When Taken After Ovulation: Extended Luteal Phase
NCT01150045 (2) [back to overview]Disease-free Survival
NCT01150045 (2) [back to overview]Overall Survival
NCT01158534 (5) [back to overview]Duration of Response
NCT01158534 (5) [back to overview]Overall Survival
NCT01158534 (5) [back to overview]Progression-free Survival
NCT01158534 (5) [back to overview]Objective Response Rate Assessed by RECIST Criteria.
NCT01158534 (5) [back to overview]Number of Patients With Statistically Significant Change in Cellular Immune Parameters From Baseline to 2 Months
NCT01220973 (1) [back to overview]PSA Response
NCT01323595 (2) [back to overview]Level of Pain
NCT01323595 (2) [back to overview]Number of Participants With Bleeding Complications
NCT01341405 (4) [back to overview]Change of WOMAC-Stiffness Subscale at Day 28 From Baseline
NCT01341405 (4) [back to overview]Change of WOMAC-Physical Function Subscale at Day 28 From Baseline
NCT01341405 (4) [back to overview]Change of the WOMAC Pain Subscale at Day 28 From Baseline
NCT01341405 (4) [back to overview]Change of the Sum of WOMAC OA Index at Day 28 From Baseline
NCT01354145 (14) [back to overview]Percentage of Participants With Presence of Joint Swelling and Effusion
NCT01354145 (14) [back to overview]WOMAC Pain Subscale
NCT01354145 (14) [back to overview]Visual Analog Scale (VAS)
NCT01354145 (14) [back to overview]Synovial Membrane Thickness
NCT01354145 (14) [back to overview]Synovial Fluid Volume
NCT01354145 (14) [back to overview]Short Form (SF-36) Health Survey
NCT01354145 (14) [back to overview]Percentage of Participants With the Presence of Extrusion in the Meniscus
NCT01354145 (14) [back to overview]Cartilage Volume Loss of the Global Knee
NCT01354145 (14) [back to overview]WOMAC Stiffness Subscale
NCT01354145 (14) [back to overview]WOMAC Function Subscale
NCT01354145 (14) [back to overview]Use of Acetaminophen
NCT01354145 (14) [back to overview]Bone Marrow Lesions Score
NCT01354145 (14) [back to overview]Cartilage Volume in the Medial Compartment
NCT01354145 (14) [back to overview]Cartilage Volume Loss of the Lateral Compartment
NCT01374269 (62) [back to overview]Quality of Life, Social Function.
NCT01374269 (62) [back to overview]Quality of Life, Physical Performance.
NCT01374269 (62) [back to overview]Quality of Life, Physical Performance.
NCT01374269 (62) [back to overview]Quality of Life, Physical Performance.
NCT01374269 (62) [back to overview]Quality of Life, Physical Performance.
NCT01374269 (62) [back to overview]Quality of Life, Physical Function.
NCT01374269 (62) [back to overview]Quality of Life, Physical Function.
NCT01374269 (62) [back to overview]Quality of Life, Physical Function.
NCT01374269 (62) [back to overview]Quality of Life, Physical Function.
NCT01374269 (62) [back to overview]Quality of Life, Mental Health.
NCT01374269 (62) [back to overview]Quality of Life, Mental Health.
NCT01374269 (62) [back to overview]Quality of Life, Mental Health.
NCT01374269 (62) [back to overview]Quality of Life, General Health Perceptions.
NCT01374269 (62) [back to overview]Quality of Life, General Health Perceptions.
NCT01374269 (62) [back to overview]Quality of Life, Emotional Performance.
NCT01374269 (62) [back to overview]Quality of Life, General Health Perceptions.
NCT01374269 (62) [back to overview]Quality of Life, General Health Perceptions.
NCT01374269 (62) [back to overview]Quality of Life, Mental Health.
NCT01374269 (62) [back to overview]Quality of Life, Emotional Performance.
NCT01374269 (62) [back to overview]Quality of Life, Emotional Performance.
NCT01374269 (62) [back to overview]Quality of Life, Emotional Performance.
NCT01374269 (62) [back to overview]Quality of Life, Change in Health
NCT01374269 (62) [back to overview]Quality of Life, Change in Health
NCT01374269 (62) [back to overview]Quality of Life, Change in Health
NCT01374269 (62) [back to overview]Quality of Life, Change in Health
NCT01374269 (62) [back to overview]Quality of Life, Bodily Pain
NCT01374269 (62) [back to overview]Quality of Life, Bodily Pain
NCT01374269 (62) [back to overview]Quality of Life, Bodily Pain
NCT01374269 (62) [back to overview]Quality of Life, Bodily Pain
NCT01374269 (62) [back to overview]PHQ-9 Patient Health Questionnaire (PHQ-9) Depression
NCT01374269 (62) [back to overview]Quality of Life, Social Function.
NCT01374269 (62) [back to overview]PHQ-9 Patient Health Questionnaire (PHQ-9) Depression
NCT01374269 (62) [back to overview]PHQ-9 Patient Health Questionnaire (PHQ-9) Depression
NCT01374269 (62) [back to overview]Visual Analogue Scale of Pain
NCT01374269 (62) [back to overview]Oswestry Disability Index
NCT01374269 (62) [back to overview]Oswestry Disability Index
NCT01374269 (62) [back to overview]Oswestry Disability Index
NCT01374269 (62) [back to overview]Missing Workdays
NCT01374269 (62) [back to overview]Missing Workdays
NCT01374269 (62) [back to overview]Missing Workdays
NCT01374269 (62) [back to overview]Missing Workdays
NCT01374269 (62) [back to overview]Medical Consultations.
NCT01374269 (62) [back to overview]Medical Consultations.
NCT01374269 (62) [back to overview]Medical Consultations.
NCT01374269 (62) [back to overview]Visual Analogue Scale of Pain
NCT01374269 (62) [back to overview]Visual Analogue Scale of Pain
NCT01374269 (62) [back to overview]Visual Analogue Scale of Pain
NCT01374269 (62) [back to overview]Oswestry Disability Index
NCT01374269 (62) [back to overview]Treatments Associated With Low Back Pain at 6 Months
NCT01374269 (62) [back to overview]Roland-Morris Questionnaire
NCT01374269 (62) [back to overview]Roland-Morris Questionnaire
NCT01374269 (62) [back to overview]Roland-Morris Questionnaire
NCT01374269 (62) [back to overview]Roland-Morris Questionnaire
NCT01374269 (62) [back to overview]Relapses of Lumbar Pain
NCT01374269 (62) [back to overview]Relapses of Lumbar Pain
NCT01374269 (62) [back to overview]Quality of Life, Vitality.
NCT01374269 (62) [back to overview]Quality of Life, Vitality.
NCT01374269 (62) [back to overview]Quality of Life, Vitality.
NCT01374269 (62) [back to overview]Quality of Life, Vitality.
NCT01374269 (62) [back to overview]Quality of Life, Social Function.
NCT01374269 (62) [back to overview]Quality of Life, Social Function.
NCT01374269 (62) [back to overview]PHQ-9 Patient Health Questionnaire (PHQ-9) Depression
NCT01425853 (13) [back to overview]Health Status According to EuroQoL
NCT01425853 (13) [back to overview]WOMAC Pain Subscale
NCT01425853 (13) [back to overview]Percentage of Participants With Response as Defined by Outcome Variables for Osteoarthritis Clinical Trials - Osteoarthritis Research Society International (OMERACT-OARSI)
NCT01425853 (13) [back to overview]Number of Participants With at Least One Adverse Events
NCT01425853 (13) [back to overview]Consumption of Rescue Medication
NCT01425853 (13) [back to overview]Percentage of Presence of Joint Effusion
NCT01425853 (13) [back to overview]Percentage of Presence of Joint Swelling
NCT01425853 (13) [back to overview]WOMAC Stiffness Subscale
NCT01425853 (13) [back to overview]WOMAC Function Subscale
NCT01425853 (13) [back to overview]Patient's Global Assessment (PGA) and Investigator's Global Assessment (IGA) of Disease Activity
NCT01425853 (13) [back to overview]Patient's and Investigator's Global Assessment of Response to Therapy
NCT01425853 (13) [back to overview]Number of Adverse Events Defined by Relationship With Treatment
NCT01425853 (13) [back to overview]Huskisson's VAS
NCT01449630 (7) [back to overview]Number of Participants With 1 or More Drug Related Adverse Events (AE) or Any Serious AE
NCT01449630 (7) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of LY3031207
NCT01449630 (7) [back to overview]Pharmacokinetics: Area Under the Concentration-Time Curve (AUC) of LY3031207
NCT01449630 (7) [back to overview]Pharmacodynamics: Percent Change From Baseline of Ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation
NCT01449630 (7) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Thromboxane A Metabolite (TXAM)
NCT01449630 (7) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostaglandin E(2) Metabolite (PGEM)
NCT01449630 (7) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostacyclin Metabolite (PGIM)
NCT01462435 (8) [back to overview]Total Pain Relief (TOTPAR) Over 0 to 4 Hours. TOTPAR-4.
NCT01462435 (8) [back to overview]The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48), ANCOVA Model.
NCT01462435 (8) [back to overview]TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours
NCT01462435 (8) [back to overview]TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours
NCT01462435 (8) [back to overview]TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours
NCT01462435 (8) [back to overview]VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry.
NCT01462435 (8) [back to overview]VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.
NCT01462435 (8) [back to overview]VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.
NCT01543685 (8) [back to overview]The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48)
NCT01543685 (8) [back to overview]Total Pain Relief (TOTPAR) Over 0 to 4 Hours (TOTPAR-4).
NCT01543685 (8) [back to overview]VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry
NCT01543685 (8) [back to overview]TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours
NCT01543685 (8) [back to overview]TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours
NCT01543685 (8) [back to overview]TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours
NCT01543685 (8) [back to overview]VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.
NCT01543685 (8) [back to overview]VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.
NCT01545141 (1) [back to overview]Treatment Related Adverse Events
NCT01554163 (7) [back to overview]Time-Weighted Mean Response in the Participant Global Assessment of Response to Therapy
NCT01554163 (7) [back to overview]Time-Weighted Mean Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale
NCT01554163 (7) [back to overview]Time-Weighted Mean Change From Baseline in the WOMAC Stiffness Subscale
NCT01554163 (7) [back to overview]Time-Weighted Mean Change From Baseline in the WOMAC Physical Function Subscale
NCT01554163 (7) [back to overview]Time-Weighted Mean Change From Baseline in the Participant Global Assessment of Disease Status
NCT01554163 (7) [back to overview]Time-Weighted Mean Change From Baseline in the Investigator Global Assessment of Disease Status
NCT01554163 (7) [back to overview]Time-Weighted Mean Response on the Investigator Global Assessment of Response to Therapy
NCT01572675 (25) [back to overview]Number of Participants Switching to Another Treatment With the Same Reason for Prescription
NCT01572675 (25) [back to overview]Duration of Prescription for Arcoxia® and Celebrex® at Enrollment
NCT01572675 (25) [back to overview]Number of Participants With Contraindications for Use of Arcoxia®
NCT01572675 (25) [back to overview]Reasons for Discontinuation of Treatment With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Reasons for Misuse of Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Significant Past Treatments Prior to Initiating Treatment With Arcoxia® or Celebrex®
NCT01572675 (25) [back to overview]Total Duration of Treatment With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Type of Arcoxia® and Celebrex® Use
NCT01572675 (25) [back to overview]Type of Arcoxia® and Celebrex® Use According to Duration of Treatment
NCT01572675 (25) [back to overview]Maximum Dosage Prescribed During Treatment With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Number of Participants Treated With Other Agents Prior to Initiation of Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Mean Dosage of Arcoxia® and Celebrex® During Treatment
NCT01572675 (25) [back to overview]Number of Participants Demonstrating Proper Use of Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Number of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT01572675 (25) [back to overview]Number of Participants Who Experienced at Least One Adverse Event
NCT01572675 (25) [back to overview]Blood Pressure at Study Entry in Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Co-morbidities in Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Medications Co-Prescribed at Study Entry in Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Dosage of Arcoxia® and Celebrex® at Initiation
NCT01572675 (25) [back to overview]Indications for Which Arcoxia® and Celebrex® Were Prescribed
NCT01572675 (25) [back to overview]Mean Systolic and Diastolic Blood Pressure (BP) at Study Entry in Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Medical History of Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Mean Body Mass Index (BMI) at Study Entry in Participants Treated With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Medications Co-Prescribed Over the Course of Follow-up With Arcoxia® and Celebrex®
NCT01572675 (25) [back to overview]Number of Participants Requiring Dose Modification of Arcoxia® and Celebrex®
NCT01632566 (7) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Simvastatin
NCT01632566 (7) [back to overview]Pharmacokinetics: Time of Maximum Concentration (Tmax) of Simvastatin
NCT01632566 (7) [back to overview]Number of Participants With One or More Drug Related Adverse Events (AEs) or Any Serious AEs
NCT01632566 (7) [back to overview]Pharmacokinetics: Time of Maximum Concentration (Tmax) of LY3031207
NCT01632566 (7) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY3031207
NCT01632566 (7) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) of Simvastatin
NCT01632566 (7) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of LY3031207
NCT01632579 (8) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostacyclin Metabolite (PGIM)
NCT01632579 (8) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Thromboxane A Metabolite (TXAM)
NCT01632579 (8) [back to overview]Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostaglandin E(2) Metabolite (PGEM)
NCT01632579 (8) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY3023703
NCT01632579 (8) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of LY3023703
NCT01632579 (8) [back to overview]Number of Participants With One or More Drug Related Adverse Events (AEs) or Any Serious AE
NCT01632579 (8) [back to overview]Pharmacodynamics: Percent Change From Baseline of ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation
NCT01632579 (8) [back to overview]Pharmacodynamics: Percent Change From Baseline of ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation
NCT01678313 (6) [back to overview]Change From Baseline in the Maximum Flow Rate (Qmax)
NCT01678313 (6) [back to overview]Change From Baseline in the Serum Prostate Specific Antigen (PSA) Level
NCT01678313 (6) [back to overview]Change From Baseline in the Void Volume (VV)
NCT01678313 (6) [back to overview]Change From Baseline in the IPSS Subscore (IPSS Storage) Questionnaires
NCT01678313 (6) [back to overview]Change From Baseline in the IPSS Subscore (IPSS Voiding) Questionnaires
NCT01678313 (6) [back to overview]Change From Baseline in the International Prostate Symptom Score (IPSS) Questionnaires
NCT01729923 (5) [back to overview]Best Overall Response Rate Among All Patients Who Had RECIST Measurements at Baseline and at Least One Subsequent Occasion
NCT01729923 (5) [back to overview]Best Overall Response Rate Among All Patients Who Had RECIST Measurements at Baseline and at Least One Subsequent Occasion and Did Not Have Surgery or Radiation Therapy
NCT01729923 (5) [back to overview]Overall Survival
NCT01729923 (5) [back to overview]Rate of CR, Assessed According to CEA and CA 19-9 Measurements and Response Evaluation Criteria in Solid Tumors (RECIST) 1.1
NCT01729923 (5) [back to overview]Relapse Free Survival in Patients Achieving CR
NCT01765296 (2) [back to overview]Change in WOMAC-Pain Subscale
NCT01765296 (2) [back to overview]Change of the WOMAC-physical Function Subscale at Week 3 and 6 From Pre-dose Baseline
NCT01768520 (2) [back to overview]the Change of Numeric Rating Scale
NCT01768520 (2) [back to overview]the Change of Total Sum of K-WOMAC(Korean The Western Ontario and McMaster Universities Arthritis Index)
NCT01838044 (14) [back to overview]Percentage of Participants With PGIC for Each Arm Compared at Week 5 (Visit 4) and at Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Change From Baseline in the Weekly Mean Pain Numeric Rating Scale (NRS) Score at Week 5 (ie, Visit 4) Compared Between the Two Study Arms
NCT01838044 (14) [back to overview]Change in the Weekly Mean Pain NRS Score in Arm B, Compared Between Week 5 (Visit 4) and Week 10 (Visit 6).
NCT01838044 (14) [back to overview]Change From Baseline in Benefit, Satisfaction, and Willingness to Continue Measure Scores Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Change From Baseline in Hospital Anxiety and Depression Scale (HADS-A) Anxiety Scores at Week 5 (Visit 4) and Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Change From Baseline in Hospital Anxiety and Depression Scale (HADS-D) Depression Scores at Week 5 (Visit 4) and Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Change From Baseline in Medical Outcomes Study (MOS) Sleep Scale - Sleep Disturbance Subscale at Week 5 and Week 10
NCT01838044 (14) [back to overview]Change From Baseline in Weekly Mean of Daily Sleep Interference Rating Scale (SIRS) Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Patient Global Impression of Change (PGIC) Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)
NCT01838044 (14) [back to overview]Percentage of Days in Mild, Moderate and Severe Pain at Period 1 and Period 2
NCT01838044 (14) [back to overview]Percentage of Participants With >= 30% Reduction From Baseline in the Weekly Mean Pain NRS Score at Week 5 and Week 10
NCT01838044 (14) [back to overview]Change From Baseline in Brief Pain Inventory Short Form (BPI sf) - Pain Severity Index Score at Week 5 and Week 10
NCT01838044 (14) [back to overview]Percentage of Participants With >= 50% Reduction From Baseline in the Weekly Mean Pain NRS Score at Week 5 and Week 10
NCT01838044 (14) [back to overview]Change From Baseline in the Weekly Mean Pain NRS Score at Week 10 (Visit 6) Compared Between the Two Study Arms
NCT01849055 (5) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve [AUC(0-24)] of LY3023703
NCT01849055 (5) [back to overview]Change From Baseline to Day 27 in Blood Pressure (BP)
NCT01849055 (5) [back to overview]Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
NCT01849055 (5) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of LY3023703
NCT01849055 (5) [back to overview]Pharmacokinetics: Time of Maximum Concentration (Tmax) of LY3023703
NCT01872910 (8) [back to overview]Part A: Weighted Mean Change From Baseline in Pain Intensity Over the First 8 Hours Post-Dose Using VAS
NCT01872910 (8) [back to overview]Time to First Use of Rescue Medication
NCT01872910 (8) [back to overview]Part A: Patient Global Impression of Improvement (PGI-I) Scale Score
NCT01872910 (8) [back to overview]Summed Pain Intensity Difference (SPID) Over the First 24 Hours Post-Dose as Measured by a 4-point Categorical Scale
NCT01872910 (8) [back to overview]Total Pain Relief (TOPAR) Score at 4, 6, 8, 12 and 24 Hours Post-Dose
NCT01872910 (8) [back to overview]Part A: Time to Onset of Meaningful Pain Relief
NCT01872910 (8) [back to overview]Weighted Mean Change From Baseline in Pain Intensity Over the First 24 Hours Post-Dose as Measured by VAS
NCT01872910 (8) [back to overview]Part A: Time to Onset of First Perceptible Pain Relief
NCT01943435 (3) [back to overview]Self Paced Walking Test (SPWT)
NCT01943435 (3) [back to overview]Sense Wear Armband
NCT01943435 (3) [back to overview]Swiss Spinal Stenosis (SSS) Questionnaire Score
NCT01968070 (7) [back to overview]Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
NCT01968070 (7) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Curve Versus Time Curve From Zero to Infinity (AUC 0-∞) of Single Dose LY3127760
NCT01968070 (7) [back to overview]PK: Maximum Observed Concentration (Cmax) of Single Dose LY3127760
NCT01968070 (7) [back to overview]PK: Area Under the Concentration Versus Time Curve During One Dosing Interval [AUC-tau (τ)] of Multiple Doses LY3127760
NCT01968070 (7) [back to overview]PK: Cmax of Multiple Doses LY3127760
NCT01968070 (7) [back to overview]PK: Time of Maximum Observed Concentration (Tmax) of Single Dose LY3127760
NCT01968070 (7) [back to overview]PK: Tmax of Multiple Doses LY3127760
NCT02037165 (9) [back to overview]Weighted Needle (Pain) Threshold (WNT) in the Secondary Flare Area of Capsaicin-irritated Skin
NCT02037165 (9) [back to overview]Overall Peak-to-Peak(PtP) N2/P2-component Amplitude of Laser (Somatosensory/Radiant Heat) Evoked Potentials (LEP) in Ultraviolet B (UVB) -Irradiated Skin
NCT02037165 (9) [back to overview]"Electronic Visual Analogue Scale (100mm VAS Post Laser Pain Scales) - Measured in the Capsaicin-irritated Skin Type."
NCT02037165 (9) [back to overview]"Electronic Visual Analogue Scale (VAS) (100mm VAS Post Laser Pain Scales) - Measured in the UVB-irradiated Skin Type"
NCT02037165 (9) [back to overview]Overall Peak-to-Peak (PtP) N2/P2-component Amplitude of (LEP) in Capsaicin-irritated Skin
NCT02037165 (9) [back to overview]"Single Peripheral N2-component Amplitudes - Measured in UVB-irradiated Skin Type"
NCT02037165 (9) [back to overview]"Single Central P2-component Amplitudes - Measured in Capsaicin-irritated Skin Type"
NCT02037165 (9) [back to overview]"Single Peripheral N2-component Amplitudes - Measured in Capsaicin-irritated Skin Type"
NCT02037165 (9) [back to overview]"Single Central P2-component Amplitudes - Measured in UVB-irradiated Skin Type"
NCT02054104 (4) [back to overview]Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0)
NCT02054104 (4) [back to overview]Fold Change From Baseline of Intensity of Programmed Cell Death Protein 1(PD-1) Expression on Tregs
NCT02054104 (4) [back to overview]Fold Change From Baseline of Percent Tregs
NCT02054104 (4) [back to overview]Number of Participants With an Immunologic Responses
NCT02084511 (6) [back to overview]Percentage of Patients With Drug-related Adverse Events
NCT02084511 (6) [back to overview]SPID0-8h
NCT02084511 (6) [back to overview]Time to First Dose of Rescue Medication
NCT02084511 (6) [back to overview]Time to Meaningful Pain Relief
NCT02084511 (6) [back to overview]TOTPAR0-8h
NCT02084511 (6) [back to overview]SPID0-2h
NCT02151448 (11) [back to overview]Overall Survival (OS)
NCT02151448 (11) [back to overview]Time to Progression (TTP)
NCT02151448 (11) [back to overview]CXCL10 (Interferon Gamma-induced Protein 10) Levels
NCT02151448 (11) [back to overview]CXCL11 (C-X-C Motif Chemokine 11) Levels
NCT02151448 (11) [back to overview]Interleukin 10 (IL-10) Levels
NCT02151448 (11) [back to overview]Interleukin-8 (IL-8) Cytokine Levels
NCT02151448 (11) [back to overview]Interleukin 6 (IL-6) Cytokine Levels
NCT02151448 (11) [back to overview]Adverse Events Possibly, Probably or Definitely Related to Study Treatment
NCT02151448 (11) [back to overview]Stromal Derived Factor 1 Alpha (SDF-1A/CXCL-12) Chemokine Levels
NCT02151448 (11) [back to overview]Progression-free Survival (PFS)
NCT02151448 (11) [back to overview]Tumor Necrosis Factor (TFNα) Cytokine Levels
NCT02172040 (12) [back to overview]Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Diastolic Blood Pressure (DBPday)
NCT02172040 (12) [back to overview]Frequency of Adverse Events (Number of Participants Affected/Number of Participants at Risk)
NCT02172040 (12) [back to overview]Mean Change in Average 24-hour Ambulatory Diastolic Blood Pressure (DBP24h)
NCT02172040 (12) [back to overview]Mean Change in Average 24-hour Ambulatory Systolic Blood Pressure (SBP24h)
NCT02172040 (12) [back to overview]Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday) - Primary Endpoint
NCT02172040 (12) [back to overview]Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday) - Secondary Endpoint
NCT02172040 (12) [back to overview]Mean Change in Average Night-time (01:00 to 06:00) Ambulatory Systolic Blood Pressure (SBPnight)
NCT02172040 (12) [back to overview]Mean Log-transformed Amlodipine Plasma Concentration
NCT02172040 (12) [back to overview]Mean Log-transformed Celecoxib Plasma Concentration
NCT02172040 (12) [back to overview]Mean Non-transformed Amlodipine Plasma Concentration
NCT02172040 (12) [back to overview]Mean Non-transformed Celecoxib Plasma Concentration
NCT02172040 (12) [back to overview]Mean Change in Average Night-time (01:00 to 06:00) Ambulatory Diastolic Blood Pressure (DBPnight)
NCT02192190 (6) [back to overview]Change From Baseline to 8 Weeks in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale
NCT02192190 (6) [back to overview]Change From Baseline to 8 Weeks in the WOMAC Physical Function Subscale
NCT02192190 (6) [back to overview]Change From Baseline to 8 Weeks in the WOMAC Stiffness Subscale
NCT02192190 (6) [back to overview]Change From Baseline to 8 Weeks in the WOMAC Total Score
NCT02192190 (6) [back to overview]Change in Baseline to 8 Weeks in Patient's Global Assessment of Osteoarthritis
NCT02192190 (6) [back to overview]Number of Participants With a Response Rate Measured by the Outcome Measures for Rheumatology Committee and Osteoarthritis Research Society International Standing Committee for Clinical Trials Response Criteria Initiative (OMERACT-OARSI)
NCT02351934 (6) [back to overview]Length of Hospital Stay
NCT02351934 (6) [back to overview]Number of Participants Readmitted to Mayo Clinic Within 30-days
NCT02351934 (6) [back to overview]Number of Participants Requiring Nasogastric Tube Placement
NCT02351934 (6) [back to overview]Time to Stool Output
NCT02351934 (6) [back to overview]Number of Participants With Acute Kidney Injury
NCT02351934 (6) [back to overview]Number of Participants With Hypokalemia
NCT02389465 (3) [back to overview]Montgomery Asberg Depression Rating Scale (MADRS)
NCT02389465 (3) [back to overview]IL-6 Levels
NCT02389465 (3) [back to overview]IL10 Levels
NCT02413203 (8) [back to overview]Quantification of Plasma Lipids in the Whole Blood: 15-Hydroxyeicosatetraenoic Acid (15-HETE)
NCT02413203 (8) [back to overview]Quantification of Plasma Lipids in the Whole Blood: Prostaglandin E2 (PGE2)
NCT02413203 (8) [back to overview]Quantification of Plasma Lipids in the Whole Blood: Prostaglandin F2a (PGF2a)
NCT02413203 (8) [back to overview]Quantification of Plasma Lipids in the Whole Blood: Thromboxane B2 (TxB2)
NCT02413203 (8) [back to overview]Urinary Lipid Metabolites: PGE2 Metabolite (PGE-M)
NCT02413203 (8) [back to overview]Celecoxib Plasma Concentration
NCT02413203 (8) [back to overview]Urinary Lipid Metabolites: PGI2 Metabolite (PGI-M)
NCT02413203 (8) [back to overview]Urinary Lipid Metabolites: TxB2 Metabolite (Tx-M)
NCT02429427 (4) [back to overview]Overall Survival
NCT02429427 (4) [back to overview]Disease Free Survival (DFS) Benefit of Two Years Adjuvant Therapy With the COX-2 Inhibitor Celecoxib Compared With Placebo in Primary Breast Cancer Patients.
NCT02429427 (4) [back to overview]Number of Participants With Incidence of Second Primary Breast Cancers
NCT02429427 (4) [back to overview]Cardiovascular Mortality
NCT02484664 (5) [back to overview]St. George's Respiratory Questionnaire
NCT02484664 (5) [back to overview]Number of Participants With Adverse Events as a Measure of Safety and Tolerability
NCT02484664 (5) [back to overview]FEV1
NCT02484664 (5) [back to overview]Angiomyolipoma Size Measured Volumetrically on MRI
NCT02484664 (5) [back to overview]VEGF-D Serum Levels
NCT02502006 (7) [back to overview]COX-2 Activity in Vivo
NCT02502006 (7) [back to overview]Diastolic Blood Pressure
NCT02502006 (7) [back to overview]Mean Arterial Pressure
NCT02502006 (7) [back to overview]Systolic Blood Pressure
NCT02502006 (7) [back to overview]COX-1 Activity in Vivo
NCT02502006 (7) [back to overview]COX-1 Activity ex Vivo
NCT02502006 (7) [back to overview]COX-2 Activity ex Vivo
NCT02688400 (15) [back to overview]Assessment of Joint Swelling, Effusion or Both
NCT02688400 (15) [back to overview]OARSI Responders
NCT02688400 (15) [back to overview]Change From Baseline in WOMAC A Pain Subscale
NCT02688400 (15) [back to overview]Change From Baseline in Patient's Global Assessment of Disease Activity
NCT02688400 (15) [back to overview]Change From Baseline in WOMAC OA Scores
NCT02688400 (15) [back to overview]Global Assessment of Response to Therapy
NCT02688400 (15) [back to overview]Quality of Life SF-36
NCT02688400 (15) [back to overview]Change From Baseline in Visual Analogue Scale Pain (VAS-Huskisson's)
NCT02688400 (15) [back to overview]Change From Baseline in Synovitis (Synovial Membrane Thickness) Using MRI
NCT02688400 (15) [back to overview]Change From Baseline in Global Stiffness Using WOMAC Subscale
NCT02688400 (15) [back to overview]Change Form Baseline in WOMAC A Pain Subscale
NCT02688400 (15) [back to overview]Consumption of Acetaminophen
NCT02688400 (15) [back to overview]Cartilage Volume Loss From Baseline in the Medial Compartment Using MRI
NCT02688400 (15) [back to overview]Cartilage Volume Loss From Baseline in the Lateral Compartment Using MRI
NCT02688400 (15) [back to overview]Absolute Changes From Baseline in Pain Visual Analogue Scale
NCT02703259 (6) [back to overview]Narcotic Use at 2 Weeks Postop
NCT02703259 (6) [back to overview]Narcotic Use at 24 Hours Postop
NCT02703259 (6) [back to overview]Subjective Pain at 2 Weeks Postop
NCT02703259 (6) [back to overview]Subjective Pain at 24 Hours Postoperative
NCT02703259 (6) [back to overview]Number of Patient With Gabapentin Adverse Effects at 2 Weeks Postoperatively
NCT02703259 (6) [back to overview]Number of Patient With Gabapentin Adverse Effects at 24 Hours Postoperatively
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Visits of Services Received Directly Related to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Visits of Services Received Directly Related to Low Back Pain
NCT02725411 (74) [back to overview]Number of Days of Rescue Medication Use During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64: Observed Data
NCT02725411 (74) [back to overview]Number of Participants Who Took Rescue Medication During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56: Last Observation Carried Forward (LOCF)
NCT02725411 (74) [back to overview]Number of Participants Who Took Rescue Medication During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64: Observed Data
NCT02725411 (74) [back to overview]Number of Participants With Abnormal Physical Examination Findings
NCT02725411 (74) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT02725411 (74) [back to overview]Number of Participants With Treatment-Emergent Treatment Related Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT02725411 (74) [back to overview]Observation Time-Adjusted Event Rate for an Individual Adjudicated Joint Safety Outcome/Event
NCT02725411 (74) [back to overview]Percentage of Participants Achieving Change of >=2 Points From Baseline in Patient's Global Assessment (PGA) of Low Back Pain at Weeks 16, 24, 40 and 56
NCT02725411 (74) [back to overview]Percentage of Participants With >=30 Percent (%), >=50%, >=70% and >=90% Reduction From Baseline in Weekly Average Low Back Pain Intensity (LBPI) Score at Weeks 16, 24, 40 and 56
NCT02725411 (74) [back to overview]Percentage of Participants With Chronic Low Back Pain Responders Index at Weeks 16, 24, 40 and 56
NCT02725411 (74) [back to overview]Percentage of Participants With Cumulative Percent Change From Baseline in Average Low Back Pain Intensity (LBPI) Score at Weeks 16, 24 and 56
NCT02725411 (74) [back to overview]Percentage of Participants With Individual Adjudicated Joint Safety Outcome/Event
NCT02725411 (74) [back to overview]Time to Discontinuation Due to Lack of Efficacy
NCT02725411 (74) [back to overview]Treatment Satisfaction Questionnaire for Medication Version II (TSQM v II) Scores at Weeks 16 and 56
NCT02725411 (74) [back to overview]Treatment Satisfaction Questionnaire for Medication Version II (TSQM v II) Scores at Weeks 16 and 56
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Participants Who Used Any Aids/Devices for Doing Things
NCT02725411 (74) [back to overview]Number of Participants Responding to Patient Reported Treatment Impact Assessment-Modified (mPRTI) at Weeks 16 and 56 for Preference of Study Drug Versus Prior Treatment
NCT02725411 (74) [back to overview]Number of Participants Responding to Patient Reported Treatment Impact Assessment-Modified (mPRTI) at Weeks 16 and 56 for Willingness to Use Study Drug Again
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 48
NCT02725411 (74) [back to overview]Number of Days of Rescue Medication Use During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56: LOCF
NCT02725411 (74) [back to overview]Change From Baseline in Average Low Back Pain Intensity (LBPI) at Week 64: Observed Data
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 16
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 24
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 32
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 4
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 40
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 56
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 64
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 8
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 80
NCT02725411 (74) [back to overview]Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Score at Week 64: Observed Data
NCT02725411 (74) [back to overview]Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Early Termination Follow-up Visit 1
NCT02725411 (74) [back to overview]Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Week 56
NCT02725411 (74) [back to overview]Change From Screening in Mean Total Symptom Impact Scores as Per Survey of Autonomic Symptoms (SAS) at Early Termination Follow-up Visit 3
NCT02725411 (74) [back to overview]Change From Screening in Mean Total Symptom Impact Scores as Per Survey of Autonomic Symptoms (SAS) at Week 80
NCT02725411 (74) [back to overview]Largest Change From Baseline in Neuropathy Impairment Score (NIS) to Any Post-baseline Visit
NCT02725411 (74) [back to overview]Number of Participants Who Discontinued Due to Lack of Efficacy
NCT02725411 (74) [back to overview]Number of Participants With Anti Tanezumab Antibodies From Baseline up to Week 80
NCT02725411 (74) [back to overview]Number of Participants With Clinically Significant Electrocardiogram (ECG) Assessments
NCT02725411 (74) [back to overview]Number of Participants With Clinically Significant Laboratory Test Abnormalities
NCT02725411 (74) [back to overview]Number of Participants With Clinically Significant Vital Signs Abnormalities
NCT02725411 (74) [back to overview]Number of Participants With Confirmed Orthostatic Hypotension From Baseline up to Week 80
NCT02725411 (74) [back to overview]Observation Time-Adjusted Event Rate for Total Joint Replacement (TJR) Event
NCT02725411 (74) [back to overview]Percentage of Participants With At Least 1 Total Joint Replacement
NCT02725411 (74) [back to overview]Amount of Rescue Medication Used in Weeks 2, 4, 8, 12, and 16: LOCF
NCT02725411 (74) [back to overview]Amount of Rescue Medication Used in Weeks 2, 4, 8, 12, and 16: Observed Data
NCT02725411 (74) [back to overview]Change From Baseline in Average Low Back Pain Intensity (LBPI) at Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, and 56: Multiple Imputation
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Average Pain at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference Index at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With General Activity at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Normal Work at Weeks 2, 4, 8, 16, 24, 40, 56 and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Sleep at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Walking Ability at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Worst Pain at Weeks 2, 4, 8, 16, 24, 40, 56, and 64
NCT02725411 (74) [back to overview]Change From Baseline in in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Impairment While Working Due to Chronic Low Back Pain at Weeks 16, 56 and 64
NCT02725411 (74) [back to overview]Change From Baseline in Neuropathy Impairment Score (NIS) at Week 2
NCT02725411 (74) [back to overview]Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Scores at Weeks 2, 4, 8, 16, 24, 32, 40, 48, and 56: Multiple Imputation
NCT02725411 (74) [back to overview]Change From Baseline in the Patient's Global Assessment (PGA) of Low Back Pain at Weeks 2, 4, 8, 16, 24, 32, 40, 48, 56 and 64
NCT02725411 (74) [back to overview]Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Activity Impairment Due to Chronic Low Back Pain at Weeks 16, 56 and 64
NCT02725411 (74) [back to overview]Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Overall Work Impairment Due to Chronic Low Back Pain at Weeks 16, 56 and 64
NCT02725411 (74) [back to overview]Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Work Time Missed Due to Chronic Low Back Pain at Weeks 16, 56 and 64
NCT02725411 (74) [back to overview]Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Week 24
NCT02725411 (74) [back to overview]European Quality of Life-5 Dimension-5 Levels (EQ-5D-5L): Dimensions Scores at Baseline, Weeks 16 and 56
NCT02725411 (74) [back to overview]European Quality of Life-5 Dimension-5 Levels (EQ-5D-5L): Overall Health Utility Score/ Index Value
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Duration Since Quitting Job Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Duration Since Quitting Job Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Nights Stayed in the Hospital Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Nights Stayed in the Hospital Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Participants Hospitalized Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Participants Visited to the Emergency Room Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Participants Who Quit Job Due to Low Back Pain
NCT02725411 (74) [back to overview]Health Care Resource Utilization (HCRU): Number of Visits of Services Received Directly Related to Low Back Pain
NCT02739035 (19) [back to overview]Knee Society Functional Score
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcome Score (KOOS): Pain Score
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcome Score (KOOS): Activities of Daily Living (ADL) Score
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcome Score (KOOS) for Joint Replacement (JR)
NCT02739035 (19) [back to overview]Short Form Survey 12-item Version 2 (SF-12v2): Physical Health
NCT02739035 (19) [back to overview]Short Form Survey 12-item Version 2 (SF-12v2): Mental Health
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Social Activities
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Sleep Disturbance
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Physical Function
NCT02739035 (19) [back to overview]Knee Range of Motion After Manipulation Under Anesthesia
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcome Score (KOOS): Sport and Recreation Score
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Pain Interference
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Fatigue
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Anxiety
NCT02739035 (19) [back to overview]PROMIS-29 Outcome Form: Depression
NCT02739035 (19) [back to overview]Knee Society Knee Score
NCT02739035 (19) [back to overview]Knee Range of Motion After Manipulation Under Anesthesia
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcomes Score (KOOS): Quality of Life
NCT02739035 (19) [back to overview]Knee Injury and Osteoarthritis Outcome Score (KOOS): Symptom Score
NCT02779166 (3) [back to overview]Visual Analog Score for Pain (VAS) in the Immediate Post Operative Period
NCT02779166 (3) [back to overview]Time to Discharge Following Surgery
NCT02779166 (3) [back to overview]Total Narcotic Consumption in the Post Anesthesia Care Unit (PACU)
NCT02845336 (9) [back to overview]Eyelid Retraction as Measured in Millimeters (Right Eye)
NCT02845336 (9) [back to overview]Number of Participants With Ocular Misalignment
NCT02845336 (9) [back to overview]Number of Participants With Ocular Misalignment
NCT02845336 (9) [back to overview]Number of Participants With Ocular Misalignment
NCT02845336 (9) [back to overview]Number of Participants With Ocular Misalignment
NCT02845336 (9) [back to overview]Eyelid Retraction as Measured in Millimeters (Left Eye)
NCT02845336 (9) [back to overview]Proptosis as Measured in Millimeters With an Exophthalmometer (Left Eye)
NCT02845336 (9) [back to overview]Proptosis as Measured in Millimeters With an Exophthalmometer (Right Eye)
NCT02845336 (9) [back to overview]Thyroid Eye Disease Clinical Activity Score
NCT02934191 (2) [back to overview]Difference in Amount of Rescue Pain Medication Consumed
NCT02934191 (2) [back to overview]Difference in Number of Days Requiring Rescue Pain Medication
NCT02979197 (9) [back to overview]Log-transformed Plasma Concentration of Amlodipine
NCT02979197 (9) [back to overview]Non-transformed Plasma Concentration of Amlodipine
NCT02979197 (9) [back to overview]Occurrence of Treatment Emergent Adverse Events
NCT02979197 (9) [back to overview]Change in Average 24-hour Ambulatory Diastolic Blood Pressure (DBP24h)
NCT02979197 (9) [back to overview]Change in Average 24-hour Ambulatory Systolic Blood Pressure (SBP24h)
NCT02979197 (9) [back to overview]Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday)
NCT02979197 (9) [back to overview]Change in Body Weight
NCT02979197 (9) [back to overview]Change in Creatinine Clearance
NCT02979197 (9) [back to overview]Change in Serum Creatinine
NCT03006276 (18) [back to overview]Subject-Rated Treatment Satisfaction at 24 Hours Postdose - PPMQ-R (DB1 and DB2)
NCT03006276 (18) [back to overview]Headache Pain Freedom Among BMI Category (DB1 and DB2)
NCT03006276 (18) [back to overview]Absence of Screening MBS at Time Points Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Headache Pain Freedom Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Headache Pain Relief Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Use of Rescue Medication Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Subject-Rated Treatment Satisfaction Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Freedom From Nausea, Photophobia, and Phonophobia Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Change in Functional Disability Score Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Headache Pain Freedom Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Time to Headache Pain Freedom Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Headache Pain Freedom Among Subjects With Cutaneous Allodynia (DB1 and DB2)
NCT03006276 (18) [back to overview]Sustained Headache Pain Relief Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Sustained Headache Pain Freedom Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Percentage of Subjects Who Are Pain-free at 2 Hours Postdose (DB1)
NCT03006276 (18) [back to overview]Percentage of Subjects Who Are Free From Their MBS at 2 Hours Postdose (DB1)
NCT03006276 (18) [back to overview]Headache Pain Recurrence Postdose (DB1 and DB2)
NCT03006276 (18) [back to overview]Time to Headache Pain Relief Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Percentage of Subjects Who Are Pain-free at 2 Hours Postdose (First Treated Double-blind Treatment Period)
NCT03009019 (19) [back to overview]Sustained Headache Pain Freedom Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Sustained Headache Pain Relief Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Time to Headache Pain Freedom Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Time to Headache Pain Relief Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Use of Rescue Medication Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]The Number of Subjects With TEAEs After Study Drug Compared Between DFN-15 and Placebo
NCT03009019 (19) [back to overview]Headache Pain Freedom Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Headache Pain Recurrence Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Subject-Rated Treatment Satisfaction Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Percentage of Subjects Who Are Free From Their MBS at 2 Hours Postdose
NCT03009019 (19) [back to overview]Subject-Rated Treatment Satisfaction at 24 Hours Postdose - PPMQ-R (DB1 and DB2)
NCT03009019 (19) [back to overview]Headache Pain Relief Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Headache Pain Freedom Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Headache Pain Freedom Among Subjects With Cutaneous Allodynia (DB1 and DB2)
NCT03009019 (19) [back to overview]Headache Pain Freedom Among BMI Category (DB1 and DB2)
NCT03009019 (19) [back to overview]Freedom From Nausea, Photophobia, and Phonophobia Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Change in Functional Disability Score Postdose (DB1 and DB2)
NCT03009019 (19) [back to overview]Absence of Screening MBS at Time Points Postdose (DB1 and DB2)
NCT03084536 (5) [back to overview]Interference as Measured by the Brief Pain Inventory (BPI) at 1 Year
NCT03084536 (5) [back to overview]Worst Pain as Measured by the Brief Pain Inventory (BPI) at 1 Year
NCT03084536 (5) [back to overview]Change in Quality of Life as Measured by the Veterans RAND12 Questionnaire Physical Health Summary Measure
NCT03084536 (5) [back to overview]Average Pain as Measured by the Brief Pain Inventory (BPI) at 1 Year
NCT03084536 (5) [back to overview]Change in Quality of Life as Measured by the Veterans RAND12 Questionnaire Mental Health Summary Measure
NCT03108482 (1) [back to overview]Sum of Pain Intensity Differences (SPID)
NCT03304379 (18) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT03304379 (18) [back to overview]Serum Concentrations of Functional Fasinumab
NCT03304379 (18) [back to overview]Number of Participants With At-least One Positive Anti-Drug Antibody (ADA) Development
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Number of Participants With Sympathetic Nervous System (SNS) Dysfunction Events
NCT03304379 (18) [back to overview]Number of Participants With Joint Replacement (JR) Surgery Reported at End of Study (EOS) (Week 72)
NCT03304379 (18) [back to overview]Number of Participants With At-least One Peripheral Sensory Adverse Events (AEs)
NCT03304379 (18) [back to overview]Number of Participants With Adjudicated Arthropathy (AA) Events
NCT03304379 (18) [back to overview]Number of Participants With AA Events Meeting Destructive Arthropathy (DA) Criteria
NCT03304379 (18) [back to overview]Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 44
NCT03304379 (18) [back to overview]Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 24
NCT03304379 (18) [back to overview]Change From Baseline in Weekly Average Walking Index Joint Pain Score up to Week 24 by Using the Numeric Rating Scale (NRS) Pain Scale
NCT03304379 (18) [back to overview]Change From Baseline in PGA Score up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in Patient Global Assessment (PGA) Score up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Percentage of Participants With Greater Than or Equal to (≥) 30 Percent (%) Reduction From Baseline up to Week 24 in WOMAC Pain Subscale Score in Participants Treated With Fasinumab Compared to Placebo
NCT03331315 (8) [back to overview]Average Inpatient Hydromorphone Use
NCT03331315 (8) [back to overview]Average Inpatient Ondansetron Use
NCT03331315 (8) [back to overview]Average Inpatient Postoperative Pain Score
NCT03331315 (8) [back to overview]Days of Oral Narcotic Use After Discharge
NCT03331315 (8) [back to overview]Total Hospital Stay
NCT03331315 (8) [back to overview]Return to Activities of Daily Living
NCT03331315 (8) [back to overview]Number of Participants With Perioperative Complications
NCT03331315 (8) [back to overview]Number of Oral Narcotic Pills Used After Discharge
NCT03403634 (4) [back to overview]Objective Response Rate (ORR) Assessed by Response Evaluation Criteria in Solid Tumors Version (RECIST) 1.1
NCT03403634 (4) [back to overview]Change in Tumor-infiltrating Lymphocytes (TILs) in the Colorectal Cancer Lesions
NCT03403634 (4) [back to overview]Overall Survival
NCT03403634 (4) [back to overview]Progression Free Survival
NCT03472469 (10) [back to overview]Pharmacy Costs
NCT03472469 (10) [back to overview]Pain as Assessed by Score on the Numeric Rating Scale (NRS)
NCT03472469 (10) [back to overview]Pain as Assessed by Score on the Behavioral Pain Scale (BPS)
NCT03472469 (10) [back to overview]Overall Costs
NCT03472469 (10) [back to overview]Number of Participants With Any Opioid-related Complications
NCT03472469 (10) [back to overview]Opioid Use Per Day
NCT03472469 (10) [back to overview]Number of Ventilator Days
NCT03472469 (10) [back to overview]Number of Participants Discharged From the Hospital With an Opioid Prescription
NCT03472469 (10) [back to overview]Number of Intensive Care Unti (ICU) Days
NCT03472469 (10) [back to overview]Number of Hospital Days
NCT03473665 (4) [back to overview]Change of Pain Score
NCT03473665 (4) [back to overview]Change of Bath Ankylosing Spondylitis Function Index (BASFI)
NCT03473665 (4) [back to overview]Change of Bath Ankylosing Spondylitis Disease Activity Index (BASDAI)
NCT03473665 (4) [back to overview]Change of ASAS Endorsed Disease Activity Score (ASDAS)
NCT03540030 (16) [back to overview]Nausea
NCT03540030 (16) [back to overview]Pain Satisfaction
NCT03540030 (16) [back to overview]Pain Satisfaction
NCT03540030 (16) [back to overview]Veterans RAND 12 Item Health Survey (VR-12©) Physical Health Subscore, and Mental Health Subscore
NCT03540030 (16) [back to overview]Veterans RAND 12 Item Health Survey (VR-12©) Physical Health Subscore, and Mental Health Subscore
NCT03540030 (16) [back to overview]Constipation
NCT03540030 (16) [back to overview]Morphine Use
NCT03540030 (16) [back to overview]Post Op Pain
NCT03540030 (16) [back to overview]Simple Shoulder Test
NCT03540030 (16) [back to overview]Simple Shoulder Test
NCT03540030 (16) [back to overview]Nausea
NCT03540030 (16) [back to overview]Additional Post Op Pain
NCT03540030 (16) [back to overview]Constipation
NCT03540030 (16) [back to overview]Falls
NCT03540030 (16) [back to overview]Falls
NCT03540030 (16) [back to overview]ASES
NCT03554772 (1) [back to overview]Summed Pain Intensity Difference Over the First Six Hours
NCT03570554 (3) [back to overview]Change From Baseline in Brief Arthritis Stiffness Scale (BASS) Score at Day 4
NCT03570554 (3) [back to overview]Absolute Brief Arthritis Stiffness Scale (BASS) Score at Each Time Point
NCT03570554 (3) [back to overview]Sum of Change in Brief Arthritis Stiffness Scale (BASS) Scores Over the 4-day Treatment Period
NCT03885596 (5) [back to overview]Pain Intensity Scores at 24 Hours at Rest Using Numerical Rating Scale (NRS)
NCT03885596 (5) [back to overview]Pain Intensity Scores at 48 Hours at Rest Using Numerical Rating Scale (NRS)
NCT03885596 (5) [back to overview]Area Under the Curve (AUC) of Numerical Rating Scale (NRS) Scores (at Rest) Over 72h
NCT03885596 (5) [back to overview]Opioid Consumption
NCT03885596 (5) [back to overview]Pain Intensity Scores at 72 Hours at Rest Using Numerical Rating Scale (NRS)
NCT03892707 (11) [back to overview]Change of Pain Intensity After 5, 24 and 38 Days of Treatment
NCT03892707 (11) [back to overview]Patient Satisfaction With Treatment
NCT03892707 (11) [back to overview]Percentage of Patients With 30% Low Back Pain Relief After 5, 10, 24 and 38 Days of Treatment.
NCT03892707 (11) [back to overview]Percentage of Patients With at Least One Pain Flare-up Resulting in Consultancy With Physician, Resulting in Disruption of Daily Activity, and Resulting in NSAIDs Intake
NCT03892707 (11) [back to overview]Prescribed and Actual Number of Milgamma® Injections
NCT03892707 (11) [back to overview]Prescribed and Actual Number of Treatment Days With Milgamma® Compositum
NCT03892707 (11) [back to overview]Change in Pain-related Disability After 10 Days of Treatment
NCT03892707 (11) [back to overview]Change of Pain Intensity After 10 Days of Treatment
NCT03892707 (11) [back to overview]Change of Pain Intensity Over Time
NCT03892707 (11) [back to overview]Number of Treatment Days With NSAIDs
NCT03892707 (11) [back to overview]Percentage of Patients With at Least One Pain Flare-up During the Study
NCT03949673 (3) [back to overview]Number of Participants by Degree of Synovial Lymphocytic Inflammation
NCT03949673 (3) [back to overview]Number of Participants by Degree of Bony Changes
NCT03949673 (3) [back to overview]Number of Participants by Degree of Cartilage Loss
NCT03974932 (19) [back to overview]Median Time to First Ambulation Postsurgery.
NCT03974932 (19) [back to overview]Median Time to First Opioid Rescue Medication.
NCT03974932 (19) [back to overview]Percentage of Subjects Unable to Participate in Each Rehabilitation Session Because of Pain.
NCT03974932 (19) [back to overview]Percentage of Subjects Who Are Opioid-free
NCT03974932 (19) [back to overview]Percentage of Subjects Who Are Opioid-free Through 72 Hours Who Remain Opioid-free Through Day 11.
NCT03974932 (19) [back to overview]Percentage of Subjects Who do Not Receive an Opioid Prescription at Discharge.
NCT03974932 (19) [back to overview]Percentage of Subjects Who do Not Receive an Opioid Prescription Between Discharge and the Day 11 Visit.
NCT03974932 (19) [back to overview]1) Pain Control Based on Patient Global Assessment (PGA)."-NCT03974932">"Percentage of Subjects Achieving a Score of Good or Better (>1) Pain Control Based on Patient Global Assessment (PGA)."
NCT03974932 (19) [back to overview]Maximum Concentration (Cmax)
NCT03974932 (19) [back to overview]Mean AUC of the NRS of Pain Intensity at Rest (NRS-R).
NCT03974932 (19) [back to overview]Mean Area Under the Curve (AUC) of the Visual Analogue Scale (VAS).
NCT03974932 (19) [back to overview]Time of Occurrence of Maximum Concentration (Tmax)
NCT03974932 (19) [back to overview]Percentage of Subjects Who Are Discharged Home vs to a Skilled Nursing Facility.
NCT03974932 (19) [back to overview]Mean Overall Benefit of Analgesia Score (OBAS).
NCT03974932 (19) [back to overview]Mean Total TSQM-9 Score
NCT03974932 (19) [back to overview]Percentage of Subjects Who First Achieve an MPADSS Score ≥9.
NCT03974932 (19) [back to overview]Percentage of Subjects With Severe Pain.
NCT03974932 (19) [back to overview]Mean Total Postoperative Opioid Consumption (in IV Morphine Milligram Equivalents [MME]).
NCT03974932 (19) [back to overview]Mean AUC of VAS Scores.
NCT04081389 (4) [back to overview]Recurrence-free Survival (RFS)
NCT04081389 (4) [back to overview]Overall Survival (OS)
NCT04081389 (4) [back to overview]Number of Patients With Dose Limiting Toxicities
NCT04081389 (4) [back to overview]Number of Patients With Pathological Complete Response (pCR)
NCT04429022 (8) [back to overview]Estimated Blood Loss
NCT04429022 (8) [back to overview]Length of Stay in Hours
NCT04429022 (8) [back to overview]Number of Patients With Return to the Clinic, Emergency Department Due to Post Operative Pain Within a 2 Week Period
NCT04429022 (8) [back to overview]Operative Time
NCT04429022 (8) [back to overview]Pain Scores
NCT04429022 (8) [back to overview]Pain Scores
NCT04429022 (8) [back to overview]Total Opioid Pain Medications Required 0-3h Post op in Morphine Milligram Equivalents (MME)
NCT04429022 (8) [back to overview]Total Opioid Pain Medications Required Through 3-24h Post op in MME
NCT04526197 (6) [back to overview]Cmax Of Molybdenum With Coadministration Of Celecoxib
NCT04526197 (6) [back to overview]AUCinf Of Molybdenum With Coadministration Of Celecoxib
NCT04526197 (6) [back to overview]AUCt Of Molybdenum With Coadministration Of Celecoxib
NCT04526197 (6) [back to overview]Area Under The Plasma Concentration Versus Time Curve From Time 0 To Infinity (AUCinf) Of Celecoxib With And Without The Coadministration Of ALXN1840
NCT04526197 (6) [back to overview]Area Under The Plasma Concentration Versus Time Curve From Time 0 To The Last Quantifiable Concentration (AUCt) Of Celecoxib With And Without The Coadministration Of ALXN1840
NCT04526197 (6) [back to overview]Maximum Observed Plasma Concentration (Cmax) Of Celecoxib With And Without The Coadministration Of ALXN1840

Percent Change in the Number of Polyps Greater Than or Equal to 2mm in Diameter in Focal Area(s) of the Colorectum

Differences between average treatment effects of two study arms tested using two-sided type I error rate of 5% in two-sample t-test. If model assumptions not met by data or transformations of data, appropriate nonparametric tests (e.g. Wilcoxon rank sums test) were used to compare treatment arms - Percent change of polyp counts from baseline to 6 months, ie [(6 months - baseline) x 100]/baseline (%). For each participant, first were matched polyps between baseline & 6 months by region and landmark and summed over all matched regions on number of polyps >2 mm to calculate total number of polyps >2 mm at baseline & 6 months, respectively. For participants refusing exit colonoscopy, 0% change entered as primary endpoint. Defined ITT All: All patients; if 6-month polyp counts missing = 0% change; ITT Measurable: All participants with baseline & 6 month polyp counts; ITT Evaluable: ITT Measurable participants who also took 80% of treatment, both overall as well as during final 60 days. (NCT00033371)
Timeframe: Baseline up to 6 months

,
Interventionpercentage change in polyp count (Mean)
ITT AllITT MeasurableITT Evaluable
Arm I: Celecoxib and Placebo-1-110
Arm II: Celecoxib and Eflornithine-11-13-8

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Number of Participants With Adverse Events Occurring at a Frequency of 5% or Grade 3 and Higher

To determine the relative tolerability and safety of celecoxib + DFMO in FAP study participants. Includes only adverse events that occurred in at least 5% of the patients or a patient exhibited at least 1 grade 3 toxicity. (NCT00033371)
Timeframe: 6 months

,
InterventionParticipants (Count of Participants)
High-frequency hearing lossFatigueDiarrhoeaHeartburn/dyspepsiaMucositis/stomatitisNausea/vomitingGoutHeadache
Arm I:Celecoxib, 400 mg p.o. BID Plus DFMO Placebo ( 60 Partic4116411605
Arm II: Celecoxib, 400 mg p.o. BID Plus DFMO 0.5 gm/m2/Day Rou734215711

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Percentage Change in Global Colorectal Polyps Burden

Percentage Change in Global Colorectal Polyps burden (NCT00033371)
Timeframe: 6 months

Interventionpercentage change of total Polyps burden (Mean)
Arm I: Celecoxib and Placebo-27
Arm II: Celecoxib and Eflornithine-40

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Time to Treatment Failure

Time from randomization to first objective tumor recurrence or progression or death due to any cause or withdrawal from study treatment due to any reason, whichever was the earliest. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks from Week 24 up to Week 108, and every 24 weeks thereafter until 9 months following LSLV

InterventionWeeks (Median)
Exemestane (Exemestane Alone)18.1
Combination (Exemestane + Celecoxib)20.4

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Duration of Clinical Benefit

Time from randomization date to first objective documentation of tumor progression or death due to tumor progression in the absence of previous documentation of tumor progression. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks from Week 24 up to Week 108, and every 24 weeks thereafter until 9 months following LSLV

Interventionweeks (Median)
Exemestane (Exemestane Alone)49.1
Combination (Exemestane + Celecoxib)96.6

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Duration of Long-Term SD

Time from start of treatment until the first objective documentation of tumor progression or death due to tumor progression in the absence of previous documentation of tumor progression in subjects with long-term SD. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks from Week 24 up to Week 108, and every 24 weeks thereafter until 9 months LSLV

Interventionweeks (Median)
Exemestane (Exemestane Alone)52.9
Combination (Exemestane + Celecoxib)109.7

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Duration of Objective Response (in Subjects With CR or PR)

Time from the first objective documentation of response until the first objective documentation of tumor progression. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks beyond 24 up to Week 108, and every 24 weeks thereafter until 9 months following LSLV

Interventionweeks (Median)
Exemestane (Exemestane Alone)32.7
Combination (Exemestane + Celecoxib)40.1

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Number of Subjects With Clinical Benefit

Clinical benefit was based on objective tumor assessments made according to Response Evaluation Criteria (RECIST) system of unidimensional evaluation. Includes subjects with complete response (CR), partial response (PR), and long term disease stabilization (SD) for at least 24 weeks. (NCT00038103)
Timeframe: Baseline, Week 8, 16, 24, and every 12 weeks beyond 24 up to Week 108 and every 24 weeks thereafter until 9 months following last subject last visit (LSLV)

Interventionparticipants (Number)
Exemestane (Exemestane Alone)24
Combination (Exemestane + Celecoxib)24

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Number of Subjects With Objective Response

Objective tumor response includes subjects with CR or PR according to RECIST. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks from Week 24 up to Week 108, and every 24 weeks thereafter until 9 months following LSLV

Interventionparticipants (Number)
Exemestane (Exemestane Alone)11
Combination (Exemestane + Celecoxib)12

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Survival

Time from randomization to date of death (any cause). (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks from Week 24 up to Week 108, and every 24 weeks thereafter until 9 months following LSLV or death

Interventionweeks (Median)
Exemestane (Exemestane Alone)74.4
Combination (Exemestane + Celecoxib)73.9

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Time to Tumor Progression

Time from randomization to first objective tumor recurrence or progression or death due to tumor progression in the absence of previous documentation of tumor progression. (NCT00038103)
Timeframe: Baseline, Weeks 8, 16, 24, every 12 weeks beyond Week 24 up to Week 108 and every 24 weeks thereafter until 9 months following LSLV

Interventionweeks (Median)
Exemestane (Exemestane Alone)20
Combination (Exemestane + Celecoxib)23.4

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Overall Survival

Because only 21 patients (18 analyzable) out of 128 planned were accrued on this study, all analyzable patients were combined to report overall survival. The original study design planned for a comparison to a historical control, but due to the small number of patients, survival time is only reported, not tested. (NCT00046839)
Timeframe: From randomization to date of death or last follow-up. Analysis occurs after all patients have been potentially followed for 12 months.

Interventionyears (Median)
Experimental: Phase I/II: Celecoxib 200 or 400mg BID + RT10.0

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Maximum Tolerated Dose (MTD) of Celecoxib Combined With Radiation Therapy (RT)

"Patients were followed for at least 90 days from start of RT and carefully evaluated with respect to treatment morbidity. A dose limiting toxicity (DLT) was defined as grade 3 or 4 nonhematologic (excluding nausea, vomiting, and alopecia) and grade 4 hematologic toxicities. Six patients were to be accrued at each dose level. If no more than three of the six patients experienced a DLT then that dose level was considered acceptable and dose escalation occurred by accruing six more patients at the next dose level. Otherwise, the preceding dose level, if any, would be declared the MTD. The MTD would be used for the Phase II arm. At a given dose, the probability of halting dose escalation when the true toxicity is 50% or higher is at least 66% (power). In addition, if the true DLT rate is instead 20%, there will still be a 10% probability of halting dose escalation at a given dose level (type I error).~Rating scale: 0 = not the MTD, 1 = MTD" (NCT00046839)
Timeframe: Start of treatment to 90 days

Interventionunits on a scale (Number)
Phase I: Celecoxib 200mg BID + RT0
Phase I: Celecoxib 400mg BID + RT1

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Occurrence of Severe Toxicity

An incidence of severe toxicity is defined to be the occurrence of grade 3 or higher infection or grade 3 or higher sensory neuropathy during cycles 1-2 of protocol therapy. If 12 or more patients experience grade 3 or higher infection or five or more patients experience grade 3 or higher sensory neuropathy during cycles 1-2 of protocol therapy, the regimen will be flagged as being associated with an excessive rate of severe toxicity. (NCT00061893)
Timeframe: The first two cycles (6 weeks) of protocol chemotherapy

Interventionparticipants (Number)
Grade 3 or Higher InfectionGrade 3 or Higher Sensory Neuropathy
Combination Chemotherapy11

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Event Free Survival

(NCT00061893)
Timeframe: 24 months after start of protocol therapy

Interventionpercentage of participants (Number)
Combination Chemotherapy35

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Overall Survival

duration of survival when celecoxib is administered concurrently with radiation in pts with newly diagnosed glioblastoma multiforme (NCT00068770)
Timeframe: date pt started treatment to date pt last known alive

Interventionmonths (Mean)
p450 ( +EIASD)11.5
nonp450 (-EIASD)16

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Effects of Hepatic Enzyme Inducing Drugs Such as Anticonvulsants, on the PK of Celecoxib

subjects will take one dose of celecoxib and will then have 6 hours of blood draws, day 2 subject will take 2 doses of celecoxib 8 hours apart with 2 additional blood samples, one hour apart. Subject, will continue to take 2 doses of celecoxib for 6 weeks, with a sample (PK) drawn every week prior to the first dose of the week. Comparison of Cmax of Celecoxib is reported (NCT00068770)
Timeframe: First dose of celecoxib through completion of radiation, 6 weeks.

Intervention(ng/ml) (Geometric Mean)
nonp4501752
p4501813

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Histologic Regression

Whether or not patients with CIN 2/3 or CIN 3 upon entry experience a complete remission (or partial regression to CIN 1) in the post-treatment excisional biopsy. (NCT00081263)
Timeframe: Post treatment evaluation was done 14 to 18 weeks after treatment randomization

Interventionpercentage of participants (Number)
Arm I (Celecoxib)40
Arm II (Placebo)34.1

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Incidence of Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events Version 3.0

Number of participants with a grade of 3 or higher during the treatment period. (NCT00081263)
Timeframe: Assessed every cycle while on treatment, 30 days after the last cycle of treatment

,
Interventionparticipants (Number)
GastrointestinalPain
Arm I (Celecoxib)10
Arm II (Placebo)01

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Changes in M-protein Levels

For a given biomarker (or a suitable transformation of it, e.g. log transform) t-tests and Wilcoxon tests (2-sample t-test and Wilcoxon rank sum test for between treatment comparisons, and paired 1-sample t-test and Wilcoxon signed rank test for within treatment comparisons) will be used to detect statistically significant differences between (or within) treatments. (NCT00099047)
Timeframe: Baseline and 6 months

Interventiong/dL (Median)
Arm I (Celecoxib)1.65
Arm II (Placebo)2.24

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Overall Survival of Individual Arms

Overall Survival (OS) was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 3 months from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Arm I: TMZ21.2
Arm II: TMZ + Thalidomide17.4
Arm III: TMZ + Celecoxib18.1
Arm IV: TMZ + Isotretinoin11.7
Arm V: TMZ + Isotretinoin + Celecoxib23.1
Arm VI: TMZ + Thalidomide + Celecoxib20.2
Arm VII: TMZ + Thalidomide + Isotretinoin17.9
Arm VIII: TMZ + Thalidomide + Isotretinoin + Celecoxib18.5

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Median Progression-Free Survival (PFS) of Individual Arms

Median PFS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 2 cycles (1 cycle = 28 days) from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Arm I: TMZ10.5
Arm II: TMZ + Thalidomide7.7
Arm III: TMZ + Celecoxib13.4
Arm IV: TMZ + Isotretinoin6.5
Arm V: TMZ + Isotretinoin + Celecoxib11.6
Arm VI: TMZ + Thalidomide + Celecoxib7.9
Arm VII: TMZ + Thalidomide + Isotretinoin6.2
Arm VIII: TMZ + Thalidomide + Isotretinoin + Celecoxib5.8

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Median Progression-Free Survival (PFS) Comparison of Thalidomide Arms Versus no Thalidomide Arms

Thalidomide versus not Thalidomide analysis: Comparison of median PFS outcome of participants in arms II, VI, VII and VIII, versus participants in arms I, III, IV and V. Median PFS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 2 cycles (1 cycle = 28 days) from randomization until progression of disease, death or last follow-up, up to one year (12 study cycles).

Interventionmonths (Median)
Thalidomide: Arm II, Arm VI, Arm VII and Arm VIII7.6
No Thalidomide: Arm I, Arm III, Arm IV and Arm V8.7

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Median Progression-Free Survival (PFS) Comparison of Doublet Versus Triplet Therapy

Doublet (2 agents) versus Triplet (3 agents) therapy analysis: We compared the median PFS outcome of participants in arms II, III, IV, versus participants in arms V, VI and VII. Median PFS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 2 cycles (1 cycle = 28 days) from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Doublet (2 Agents): Arm II, Arm III and Arm IV8.3
Triplet (3 Agents): Arm V, Arm VI and Arm VII8.2

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Median Progression-Free Survival (PFS) Comparison of Isotretinoin Arms Versus no Isotretinoin Arms

Isotretinoin versus not Isotretinoin analysis: We compared the median PFS outcome of participants in arms IV, V, VII and VIII, versus participants in arms I, II, III and VI. Median PFS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 2 cycles (1 cycle = 28 days) from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Isotretinoin: Arm IV, Arm V, Arm VII and Arm VIII6.6
No Isotretinoin: Arm I, Arm II, Arm III and Arm VI9.1

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Median Progression-Free Survival (PFS) Comparison of Celecoxib Arms Versus no Celecoxib Arms

Celecoxib versus not Celecoxib analysis: We compared the median PFS outcome of participants in arms III, V, VI and VIII, versus participants in arms I, II, IV and VII. Median PFS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 2 cycles (1 cycle = 28 days) from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Celecoxib: Arm III, Arm V, Arm VI and Arm VIII8.3
No Celecoxib: Arm I, Arm II, Arm IV and Arm VII7.4

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Median Overall Survival (OS) Comparison of Doublet Versus Triplet Therapy

Doublet (2 agents) versus Triplet (3 agents) therapy analysis: We compared the median OS outcome of participants in arms II, III, IV, versus participants in arms V, VI and VII. Median OS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 3 months from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Doublet (2 Agents): Arm II, Arm III and Arm IV17.0
Triplet (3 Agents): Arm V, Arm VI and Arm VII20.1

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Median Overall Survival (OS) Comparison of Isotretinoin Arms Versus no Isotretinoin Arms

Isotretinoin versus not Isotretinoin analysis: We compared the median OS outcome of participants in arms IV, V, VII and VIII, versus participants in arms I, II, III and VI. Median OS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 3 months from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Isotretinoin: Arm IV, Arm V, Arm VII and ARM VIII17.1
No Isotretinoin: Arm I, Arm II, Arm III and ARM VI19.9

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Median Overall Survival (OS) Comparison of Celecoxib Arms Versus no Celecoxib Arms

Celecoxib versus not Celecoxib analysis: We compared the median OS outcome of participants in arms III, V, VI and VIII, versus participants in arms I, II, IV and VII. Median OS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 3 months from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Celecoxib: Arm III, Arm V, Arm VI and Arm VIII20.2
No Celecoxib: Arm I, Arm II, Arm IV and Arm VII17.1

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Median Overall Survival (OS) Comparison of Thalidomide Arms Versus no Thalidomide Arms

Thalidomide versus not Thalidomide analysis: We compared the median OS outcome of participants in arms II, VI, VII and VIII, versus participants in arms I, III, IV and V. Median OS was estimated using the Kaplan-Meier method from time of randomization to time of progression, death, or last follow-up. Progression defined as 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) using the same techniques as baseline, OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR failure to return for evaluation due to death or deteriorating condition (unless clearly unrelated to this cancer). (NCT00112502)
Timeframe: Every 3 months from randomization until progression of disease, death or last follow-up.

Interventionmonths (Median)
Thalidomide: Arm II, Arm VI, Arm VII and Arm VIII18.3
No Thalidomide: Arm I, Arm III, Arm IV and Arm V17.4

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Area Under the Curve (AUCs) of Western Ontario and McMaster Universities (WOMAC) Osteoarthritis Scores

WOMAC assesses subject responses to 24 components regarding subscales of pain, stiffness and physical function (score range: 0=none to 4= extreme). Total score is sum of the 3 subscale scores. Scores analyzed as area under the curve (AUC) of participant's WOMAC scores from each assessment in Period III. (NCT00139776)
Timeframe: Period III (22 weeks)

,
Interventionscores on a scale * weeks (Mean)
Total WOMAC scoreWOMAC pain subscaleWOMAC stiffness subscaleWOMAC physical function subscale
Celecoxib 200mg Continuous Use604.9119.254.5431.4
Celecoxib 200mg Intermittent Use693.6138.462.1493.6

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Arthritis Pain Numerical Rating Scale (NRS)

Participant rated intensity of osteoarthritis pain on categorical scale from 0 (no pain) to 10 (worst pain). Scores analyzed as area under the curve (AUC) of participant's scores from each assessment in Period III. (NCT00139776)
Timeframe: Period III

,
Interventionscores on a scale * weeks (Least Squares Mean)
Week 4 (n=415 cont; n=414 inter)Week 8 (n=401 cont; n=395 inter)Week 12 (n=383 cont; n=363 inter)Week 16 (n=373 cont; n=339 inter)Week 20 (n=362; n=323 inter)Week 24 (n=350 cont; n=403 inter)
Celecoxib 200mg Continuous Use81.7148.8212.6272.7335.9378.1
Celecoxib 200mg Intermittent Use90.5167.0234.3297.6361.1403.9

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Change in Medical Outcomes Study Sleep Scale - All Assessments

Subject assessment on 7 sleep associated categories. Raw scores are transformed to a 0-100 scale. Higher score indicates more of the outcome (e.g. more snoring, more adequate sleep). Score at end of Period III minus score at start of Period III. (NCT00139776)
Timeframe: Period III

,
Interventionscores on a scale (Mean)
Sleep disturbance (n=415 cont; n=410 inter)Snoring (n=415 cont; n=412 inter)Awaken short of breath (n=417 cont; n=411 inter)Quantity of sleep (n=417 cont; n=413 inter)Sleep adequacy (n=416 cont; n=413 inter)Somnolence (n=416 cont; n=413 inter)Sleep problems index I (n=416 cont; n=410 inter)Sleep problems index II (n=413 cont; n=408 inter)
Celecoxib 200mg Continuous Use0.50.91.9-0.10.11.40.90.7
Celecoxib 200mg Intermittent Use-1.40.71.1-0.1-1.30.60.5-0.1

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Change in the Quality of Life Short Form-12v2 (SF-12v2) Scale Scores - All Assessments

SF-12v2 is a 12 item health survey covering 7 topics. Raw scores are transformed to a 0 to 100 scale. Higher scores indicate better state of health. Score at end of Period III minus score at start of Period III. (NCT00139776)
Timeframe: Period III

,
Interventionscores on a scale (Mean)
Physical function (n=417 cont; n=413 inter)Role physical (n=416 cont; n=412 inter)Bodily pain (n=417 cont; n=414 inter)General health (n=417 cont; n=414 inter)Vitality (n=416 cont; n=414 inter)Social functioning (n=416 cont; n=414 inter)Role emotional (n=417 cont; n=413 inter)Mental health (n=416 cont; n=413 inter)Physical component summary(n=416 cont;n=411 inter)Mental component summary (n=416 cont;n=411 inter)
Celecoxib 200mg Continuous Use1.83.53.8-0.30.3-1.9-0.7-0.99.0-3.1
Celecoxib 200mg Intermittent Use-3.2-1.1-0.3-0.8-3.5-3.5-2.1-1.3-5.2-10.5

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Change in Western Ontario and McMaster Universities (WOMAC) Osteoarthritis Scores

Score at end of Period III minus score at start of Period III. WOMAC assesses subject responses to 24 components regarding subscales of pain, stiffness and physical function (score range: 0=none to 4= extreme). Total score is sum of the 3 subscale scores. Negative change indicates improvement. (NCT00139776)
Timeframe: Period III (22 weeks)

,
Interventionscores on a scale (Least Squares Mean)
Total WOMAC scoreWOMAC pain subscaleWOMAC stiffness subscaleWOMAC physical function subscale
Celecoxib 200mg Continuous Use1.600.370.121.13
Celecoxib 200mg Intermittent Use4.991.180.403.43

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Medical Outcomes Study Sleep Scale - Number of Participants With Optimal, Mixed and Not Optimal Sleep

Transformed score scale: 1=optimal; 0=not optimal; mixed = both optimal and non-optimal sleep during Period III (NCT00139776)
Timeframe: Period III

,
Interventionparticipants (Number)
Optimal (all scores are 1)Mixed (scores are both 1 and 0)Not optimal (all scores are 0)
Celecoxib 200mg Continuous Use139166115
Celecoxib 200mg Intermittent Use123165132

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Patient's Global Assessment of Arthritis

"Participant's response to question Considering all the ways the osteoarthritis in your hip or knee affects you, how are you doing today? on scale from 1 (very good) to 5 (very poor). Scores analyzed as area under the curve (AUC) of participant's scores from each assessment in Period III." (NCT00139776)
Timeframe: Period III

,
Interventionscores on a scale * weeks (Least Squares Mean)
Week 4 (n=415 cont; n=414 inter)Week 8 (n=401 cont; n=395 inter)Week 12 (n=383 cont; n=363 inter)Week 16 (n=373 cont; n=339 inter)Week 20 (n=362 cont; n=323 inter)Week 24 (n=350 cont; n=309 inter)
Celecoxib 200mg Continuous Use67.9126.0182.8236.3292.4329.2
Celecoxib 200mg Intermittent Use71.7133.2188.7241.2293.8328.9

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Physician's Global Assessment of Arthritis at Final Visit

Physician assessed each participant's disease symptoms on a categorical scale from 1 (very good) to 5 (very poor). (NCT00139776)
Timeframe: Period III (22 weeks)

,
Interventionparticipants (Number)
Grade 1 (very good)Grade 2 (good)Grade 3 (fair)Grade 4 (poor)Grade 5 (very poor)
Celecoxib 200mg Continuous Use6824291232
Celecoxib 200mg Intermittent Use39244113272

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Serious Adverse Events in Open Label run-in Period

Serious adverse events occuring during the 2 week run-in period (Period II) when all participants were dosed with celecoxib 200 mg daily (NCT00139776)
Timeframe: 2 weeks prior to double blind dosing

Interventionparticipants (Number)
AnaemiaVitreous haemorrhage
Celecoxib 200mg Open Label11

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Total Rescue Medication Taken (Mean)

Total amount of rescue medication (acetaminophen in milligrams [mg]) taken per month per participant (NCT00139776)
Timeframe: Period III (22 weeks)

Interventionmg taken per month per participant (Mean)
Celecoxib 200mg Continuous Use1566
Celecoxib 200mg Intermittent Use2428

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Days on Flare Medication

Number of days on flare medication per month per subject calculated as number of days on flare medication divided by the number of days on study medication in Period III (NCT00139776)
Timeframe: Period III (22 weeks)

Interventiondays on medication per month per subject (Mean)
Celecoxib 200mg Continuous Use6.589
Celecoxib 200mg Intermittent Use9.793

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Number of Flare Events Per Time of Exposure to Study Medication

Number of flare events per month during Period III (calculated as number of flares divided by number of months participant was enrolled during Period III). Flare was determined using pre-defined criteria, using an interactive voice response system. (NCT00139776)
Timeframe: Period III (22 weeks)

Interventionflare events per month (Mean)
Celecoxib 200mg Continuous Use0.54
Celecoxib 200mg Intermittent Use0.93

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Proportion of Days in Osteoarthritis (OA) Flare

Number of days subject was in OA flare divided by number of days on study medication in Period III. Subjects may have more than one flare. Flare was determined using pre-defined criteria, using an interactive voice response system. (NCT00139776)
Timeframe: Period III (22 weeks)

Interventionproportion of days in OA flare (Mean)
Celecoxib 200mg Continuous Use0.23
Celecoxib 200mg Intermittent Use0.33

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Time to Occurrence of First Osteoarthritis (OA) Flare

Time from first dose of double blind medication (start of Period III) to occurrence of first OA flare. Flare was determined using pre-defined criteria, using an interactive voice response system (NCT00139776)
Timeframe: Period III (22 weeks)

Interventiondays (Median)
Celecoxib 200mg Continuous Use16.0
Celecoxib 200mg Intermittent Use8.0

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Proportion of Days on Rescue Medication

Days on rescue medication divided by number of days on study medication in Period III (NCT00139776)
Timeframe: Period III (22 weeks)

Interventionproportion of days (Mean)
Celecoxib 200mg Continuous Use0.044
Celecoxib 200mg Intermittent Use0.069

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Proportion of Days Free From Osteoarthritis (OA) Flare

Number of days subject was free from OA flare divided by number of days on study medication in Period III. Flare was determined using pre-defined criteria, using an interactive voice response system. (NCT00139776)
Timeframe: Period III (22 weeks)

Interventionproportion of days free from OA flare (Mean)
Celecoxib 200mg Continuous Use0.77
Celecoxib 200mg Intermittent Use0.67

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Change From Baseline in Hemoglobin at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventiongrams (g)/deciliter (dL) (Least Squares Mean)
Celecoxib-0.017
Oral Diclofenac Plus Omeprazole-0.423

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Change From Baseline in Iron Binding Capacity to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmicrogram (ug)/dL (Least Squares Mean)
Celecoxib2.517
Oral Diclofenac Plus Omeprazole1.952

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Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)

"Subjects rated response to question: Considering all the ways the osteoarthritis or rheumatoid arthritis affects you, how are you doing today? using a 1 to 5 grading scale where 1=very good and 5=very poor." (NCT00141102)
Timeframe: Month 6/Early Termination (ET)

Interventionscores on a scale (Least Squares Mean)
Celecoxib0.754
Oral Diclofenac Plus Omeprazole0.773

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Number of Subjects Alive at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib2018
Oral Diclofenac Plus Omeprazole2023

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Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib82
Oral Diclofenac Plus Omeprazole79

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Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin

A clinically significant decrease from baseline was defined as a fall in hematocrit > = 10 percentage points and/or hemoglobin > = 2 g/dL. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib45
Oral Diclofenac Plus Omeprazole123

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Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)

CSULGIE=any of the following: GD hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib25
Oral Diclofenac Plus Omeprazole92

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Number of Subjects With Moderate to Severe Abdominal Symptoms

"Abdominal symptoms were defined by the Medical Dictionary for Regulatory Activities MedDRA System Organ Class (SOC) 'Gastrointestinal Disorders' and keeping high level group term (HLGT) equal to Gastrointestinal Signs and Symptoms." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib132
Oral Diclofenac Plus Omeprazole162

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Number of Subjects With SUs

Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib5
Oral Diclofenac Plus Omeprazole11

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Number of Subjects Withdrawn Due to GI Adverse Events (AEs)

"GI AEs were defined using MedDRA SOC Gastrointestinal Disorders but excluding the following HLGTs: Benign Neoplasms Gastrointestinal; Dental and Gingival Conditions; Oral Soft Tissue Conditions; Salivary Gland Conditions; and Tongue Conditions." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib114
Oral Diclofenac Plus Omeprazole167

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Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

,
InterventionIU/L (Least Squares Mean)
GGTASTALT
Celecoxib-2.689-0.901-1.151
Oral Diclofenac Plus Omeprazole7.4551.4905.213

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Number of Subjects With CSULGIEs by History of GD Ulceration

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
History of GD Ulceration (n=395, 400)No History of GD Ulceration (n=1843, 1846)
Celecoxib713
Oral Diclofenac Plus Omeprazole1368

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Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)

GGT ULN was 49 international units (IU)/liter (L) for females and 61 IU/L for males, AST ULN was 37 IU/L for females and 39 IU/L for males, and ALT ULN was 43 IU/L for females and 45 IU/L for males. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
GGTASTALT
Celecoxib26813
Oral Diclofenac Plus Omeprazole861227

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Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib20
Oral Diclofenac Plus Omeprazole81

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Change From Baseline in Hematocrit at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionpercent (Least Squares Mean)
Celecoxib-0.306
Oral Diclofenac Plus Omeprazole-1.425

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Change From Baseline in C-Reactive Protein to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmg/dL (Least Squares Mean)
Celecoxib0.058
Oral Diclofenac Plus Omeprazole0.073

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Change From Baseline in Ferretin to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionug/dL (Least Squares Mean)
Celecoxib-3.396
Oral Diclofenac Plus Omeprazole-1.990

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Duodenal Adenoma Burden as Measured by Polyp Counts

Number of subjects with polyp burden as assessed in most recent prior polyps evaluation: attenuated: <100 polyps, mild: between 100 to 1000 polyps, severe: >1000 polyps. EOS: endoscopic examination closest to end of on-study celecoxib or index period (within 6 months of end of celecoxib or index period and prior to intake of any exclusionary medications after baseline). Post-hoc analysis of duodenal polyp burden in terms of severity categories and based on polyp numbers; Spigelman Stage not completed as staging data largely missing (see: Duodenal adenoma burden as measured by Spigelman Stage) (NCT00151476)
Timeframe: Baseline, 6 to 14 months post-baseline, End of study (EOS)

,,,
Interventionparticipants (Number)
Baseline attenuatedBaseline mildBaseline severeBaseline unknownBaseline no polypsBaseline not assessedPost-baseline attenuatedPost-baseline mildPost-baseline severePost-baseline unknownPost-baseline no polypsPost-baseline not assessedEOS attenuatedEOS mildEOS severeEOS unknownEOS no polypsEOS not assessed
All Celecoxib Treated2300136121300313719003329
Matched Celecoxib Treated500314100318200119
Matched Control1002553000372000110
Not Matched Celecoxib Treated180010581200002917002220

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Time From Ileopouch Anal Anastomosis (IPAA) to Time of First Excisional Polypectomy of a Rectal Polyp Post IPAA

Time (months): [date of first excisional polypectomy of a rectal polyp post IPAA minus date of prior IPAA plus 1] divided by 30.44. Baseline = start of study follow-up: start of on-study celecoxib treatment period for celecoxib-treated subjects and comparable to index date for control subjects. Index date calculated as Matched Celecoxib-treated patients: number of days from most recent FAP-related surgery (IRA or IPAA) to start of study follow-up; add this number of days to matched control patient's most recent FAP-related surgery date=index date for Matched Control. (NCT00151476)
Timeframe: Up to 15 years prior to baseline

Interventionmonths (Mean)
Matched Celecoxib Treated152.7
All Celecoxib Treated152.7

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Time From Ileorectal Anastomosis (IRA) to Time of First Excisional Polypectomy of a Rectal Polyp Post IRA

Time(months): [date of first excisional polypectomy of rectal polyp post IRA minus date of prior IRA plus 1] divided by 30.44. Baseline = start of study follow-up: start of on-study celecoxib treatment period for celecoxib-treated subjects and comparable to index date for control subjects. Index date calculated as Matched Celecoxib-treated patients: number of days from most recent FAP-related surgery (IRA or IPAA) to start of study follow-up; add this number of days to matched control patient's most recent FAP-related surgery date=index date for Matched Control. (NCT00151476)
Timeframe: Up to 8 years prior to baseline

Interventionmonths (Mean)
Matched Celecoxib Treated86.4
Matched Control4.0
Not Matched Celecoxib Treated78.4
All Celecoxib Treated79.5

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Time From Post IRA to Time of Conversion From IRA to IPAA

Time (months): [date of IPAA minus date of prior IRA plus 1] divided by 30.44. (NCT00151476)
Timeframe: Up to 15 years prior to baseline

Interventionmonths (Median)
Matched Celecoxib Treated301.6
Not Matched Celecoxib Treated129.7
All Celecoxib Treated175.8

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Time From Start of Study Follow-up to the Time of First Excisional Polypectomy of a Rectal Polyp Post IRA

Time(months): [date of first excisional polypectomy of rectal polyp post IRA minus date of start of study follow-up plus 1] divided by 30.44. (NCT00151476)
Timeframe: Baseline, Up to 60 months post-baseline

Interventionmonths (Median)
Matched Celecoxib Treated19.8
Not Matched Celecoxib Treated32.1
All Celecoxib Treated25.9

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Time From Start of Study Follow-up to Time of Conversion From IRA to IPAA

Time (months): [date of IPAA minus date of start of study follow-up plus 1] divided by 30.44. (NCT00151476)
Timeframe: Baseline, Up to 60 months post-baseline

Interventionmonths (Median)
Not Matched Celecoxib Treated4.8
All Celecoxib Treated4.8

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Time From Start of Study Follow-up to Time of First Excisional or Ablational Event for Rectal, Colonic, Pouch, or Duodenal Adenomas

Time (months): [date of first excisional or ablational event for colonic, pouch, or duodenal adenomas, occurring after date of most recent prior FAP-related surgical event, or date of FAP diagnosis minus date of start of study follow-up plus 1] divided by 30.44. (NCT00151476)
Timeframe: Baseline, Up to 60 months post-baseline

Interventionmonths (Mean)
Matched Celecoxib Treated0.0
Matched Control41.7
Not Matched Celecoxib Treated21.4
All Celecoxib Treated12.9

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Time From Start of Study Follow-up to Time of First Excisional Polypectomy of a Rectal Polyp Post IPAA

Time (months): [date of first excisional polypectomy of rectal polyp post IPAA minus date of start of study follow-up plus 1] divided by 30.44. (NCT00151476)
Timeframe: Baseline, Up to 60 months post-baseline

Interventionmonths (Mean)
Matched Celecoxib Treated20.3
All Celecoxib Treated20.3

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Rectal or Pouch Adenoma Burden Based on Polyp Counts

Number of subjects with polyp burden as assessed in most recent prior polyps evaluation: attenuated: <100 polyps, mild: between 100 to 1000 polyps, severe: >1000 polyps. EOS: endoscopic examination closest to end of on-study celecoxib or index period (within 6 months of end of celecoxib or index period and prior to intake of any exclusionary medications after baseline). (NCT00151476)
Timeframe: Baseline, 6 to 14 months post-baseline, EOS

,,,
Interventionparticpants (Number)
Baseline attenuatedBaseline mildBaseline severeBaseline unknownBaseline no polypsBaseline not assessedPost-baseline attenuatedPost-baseline mildPost-baseline severePost-baseline unknownPost-baseline no polypsPost-baseline not assessedEOS attenuatedEOS mildEOS severeEOS unknownEOS no polypsEOS not assessed
All Celecoxib Treated274013551610053220004426
Matched Celecoxib Treated920110600043800320
Matched Control420061300055200065
Not Matched Celecoxib Treated182012451010012912001226

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Concentration of PGE2 in Serum at Baseline, Surgery, 1 wk, 4wks, and 6 Months

Measured by Elisa at participant level - only participant level data available; not summarized across group (NCT00198081)
Timeframe: Baseline, surgery, 1 wk, 4 wks, and 6 months

,,,,
Interventionpg/ml (Number)
IPMN Adenoma-Part 1IPMN low-Part 2IPMN Invasive-Part 3IPMN NOS-Part 4
Surgery Candidate Surgery709030140
Surgical Candidate 4 Weeks130401080
Surgical Candidate 6 Months100107030
Surgical Candidate Baseline6017070100
Surgical Candidate One Week70106020

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Concentration of PGE2 in Urine at Baseline, Surgery, 1 wk, 4wks, and 6 Months

Measured by Elisa at participant level - only participant level data available; not summarized across group (NCT00198081)
Timeframe: Baseline, surgery, 1 wk, 4 wks, and 6 months

,,,,
Interventionpg/ml (Number)
IPMN Adenoma-Part 1IPMN low-Part 2IPMN Invasive-Part 3IPMN NOS-Part 4
Surgery Candidate Surgery1330013400300008700
Surgical Candidate 4 Weeks19600363002480040300
Surgical Candidate 6 Months240001600036007500
Surgical Candidate Baseline118002100080010100
Surgical Candidate One Week121004700154009500

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Concentration of PGEM in Serum at Baseline, Surgery, 1 wk, 4wks, and 6 Months

Measured by Elisa at participant level - only participant level data available; not summarized across group (NCT00198081)
Timeframe: Baseline, surgery, 1 wk, 4 wks, and 6 months

,,,,
Interventionpg/ml (Number)
IPMN Adenoma-Part 1IPMN low-Part 2IPMN Invasive-Part 3IPMN NOS-Part 4
Surgery Candidate Surgery44.333.4
Surgical Candidate 4 Weeks5.45.95.14.3
Surgical Candidate 6 Months6.78.78.31.8
Surgical Candidate Baseline20729
Surgical Candidate One Week6.49.311.87.2

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Concentration of PGEM in Urine at Baseline, Surgery, 1 wk, 4wks, and 6 Months

Measured by Elisa at participant level - only participant level data available; not summarized across group (NCT00198081)
Timeframe: Baseline, surgery, 1 wk, 4 wks, and 6 months

,,,,
Interventionpg/ml (Number)
IPMN Adenoma-Part 1IPMN low-Part 2IPMN Invasive-Part 3IPMN NOS-Part 4
Surgery Candidate Surgery177201NA100
Surgical Candidate 4 Weeks431594453417
Surgical Candidate 6 Months52236618488
Surgical Candidate Baseline196257128131
Surgical Candidate One Week354153850184

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Number of Patients With Decreased Gene Expression of CYP19 in Breast Cancer by Adding COX-2 Inhibitor to Exemestane

Collected from postmenopausal women that receive neoadjuvant exemestane. (NCT00201773)
Timeframe: up to 16 weeks

Interventionpatients (Number)
Exemestane + Celecoxib0
Exemestane0

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Evaluate Response Rate of Neoadjuvant Exemestane and Celecoxib in Postmenopausal Women.

Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response, Disappearance of all target lesions; Partial Response, >=30% decrease in the sum of the longest diameter of target lesions; Stable Disease, <30% decrease in the sum of the longest diameter of target lesions; Progressive Disease, 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. (NCT00201773)
Timeframe: up to 16 weeks

Interventionpatients (Number)
Complete ResponsePartial ResponseStable DiseaseProgressive DiseaseNon-measurable
Exemestane & Celecoxib051115

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Toxicity

"All toxicities encountered during the study will be evaluated according to the grading system (0-5) NCI CTCAE (Common Terminology Criteria for Adverse Events) version 3.0.~Toxicity will be reported as the proportion of subjects experiencing Grades 3,4, and 5 adverse events (AEs) out of all evaluable patients" (NCT00250835)
Timeframe: Up to 3 years

Interventionpercentage of participants (Number)
Grade 3 and 4 diarrheaGrade 3 and 4 abnormal liver function testsGrade 3 and 4 abdominal painDeath (from severe infection)
Chemotherapy, Celecoxib, and Radiation9966

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Surgical Downstaging Rate

Downstaging rate after neoadjuvant treatment with combination oxaliplatin, capecitabine, celecoxib and concurrent radiation is defined as the proportion of patients whose pathological stage (stage at surgery) is different from their clinical stage (stage at baseline) (NCT00250835)
Timeframe: At surgery (up to 6 weeks after treatment)

Interventionpercentage of evaluable participants (Number)
Chemotherapy, Celecoxib, and Radiation75

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Progression-free Survival (PFS)

"The Response Evaluation Criteria In Solid Tumors (RECIST) guidelines (Version 1.0) will be used to determine tumor response and progression. Progressive disease (PD) for target lesions: >= 20% increase in the sum of diameters of the target lesions taking as reference the smallest sum on study, and an absolute increase of at least 5 mm. The appearance of one or more new lesions is also considered . PD for non-target lesions is defined as unequivocal appearance of one or more new malignant lesions or unequivocal progression of existing non-target lesions. Time to progression will be measured from the time of surgery or clinically documented down staging if surgery for whatever reason is not carried in the subject until there is evidence of PD.~Progression-free survival is reported as the percentage of patients who have not experienced progression of disease at three years post-surgery" (NCT00250835)
Timeframe: 3 years after surgery

Interventionpercentage of evaluable participants (Number)
Chemotherapy, Celecoxib, and Radiation84

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Pelvic Local Control Rate

Pelvic local control rate is defined as the proportion of subjects who have no evidence of pelvic recurrence (by standard clinical assessment, including CT scan and clinical examination) at the final follow-up evaluation, out of all evaluable patients (NCT00250835)
Timeframe: Up to 3 years after surgery

Interventionpercentage of evaluable participants (Number)
Chemotherapy, Celecoxib, and Radiation6

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Incidence of Sphincter-sparing Surgery

Incidence of sphincter-saving surgery is defined as the proportion of subjects who do not have permanent colostomy at the final follow-up out of all evaluable patients. (NCT00250835)
Timeframe: At surgery (up to 6 weeks after end of treatment)

Interventionpercentage of evaluable participants (Number)
Chemotherapy, Celecoxib, and Radiation56

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Pathologic Complete Response (PCR)

The pathologic complete response (PCR) rate will be calculated as the proportion of patients who achieve complete response out of all evaluable patients. PCR is defined as the total absence of residual tumor cells by microscopic examination of the resected surgical specimen, including all of the sampled lymph nodes. (NCT00250835)
Timeframe: At surgery (up to 6 weeks after end of treatment)

Interventionpercentage of evaluable participants (Number)
Chemotherapy, Celecoxib, and Radiation31

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Serum Sex Hormone Binding Globulin (SHBG) Concentration

Change in serum concentration (NCT00291694)
Timeframe: Baseline to 12 months

Interventionnmol/L (Median)
Celecoxib-0.70
Placebo3.05

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Serum Estradiol Concentration

Change in serum estradiol concentration (NCT00291694)
Timeframe: Baseline to 12 months

Interventionpg/ml (Median)
Celecoxib-6.6
Placebo-5.7

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Molecular Ratio of Serum Concentration of IGF-1 to IGFBP3

Change ion ratio. (NCT00291694)
Timeframe: baseline to 12 months

Interventionratio (Median)
Celecoxib-0.012
Placebo-0.011

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Mammographic Breast Density

The percent of mammographic breast area that is considered to be at increased density. Evaluated using the semi-automated computer program Cumulus. (NCT00291694)
Timeframe: Baseline and 12 months

Interventionpercentage of breast area at increased d (Median)
Celecoxib-1.3
Placebo0.3

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Change in Percent of Breast Epithelial Cells Staining Positive for Ki-67

Immunocytochemical staining of breast epithelial cells. Positive cells reflect proliferative activity. (NCT00291694)
Timeframe: Baseline and 12 months

Interventionpercentage of cells staining positive (Median)
Celecoxib-1.2
Placebo-2.0

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Clinical Outcome: Documented Progression

Response evaluation was based on pathologic examination of the degree of dysplasia observed and recorded by an expert head and neck pathologist. Pathologic complete response was defined as complete disappearance of dysplasia from the epithelium. Pathologic partial response was defined as improvement of dysplasia by at least one degree (i.e., severe dysplasia becomes moderate dysplasia). Pathologic minor response or stable disease was defined as minor focal improvement without change of degree of dysplasia (i.e., focal improvement from moderate to mild dysplasia with still moderate dysplasia overall) or no pathologic changes after treatment. Pathologic progressive disease was defined as worsening by at least one degree of dysplasia (i.e., mild to moderate dysplasia) or development of invasive cancer on or following treatment. (NCT00314262)
Timeframe: 12 months from time of enrollment

Interventionparticipants (Number)
Complete remission (CR)Partial remission (PR)Progressive disease (PD)Stable disease (SDi)
Erlotinib & Celecoxib3112

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Dose Escalation and Toxicity: Toxicities Including Grades 1 to 4

Participants received a fixed dose of celecoxib 400 mg orally BID continuously for 6 months. Erlotinib was dose escalated at 3 dose levels of 50, 75, and 100 mg orally every day for 6 months. Dose escalation followed a standard 3+3 escalation design. (NCT00314262)
Timeframe: 12 months from time of enrollment

Interventionparticipants (Number)
Abdominal cramping, Grade 1Alopecia, Grade 1Anemia, Grade 1Anemia, Grade 2Anxiety, Grade 1Decreased protein, Grade 1Leukopenia, Grade 1Leukopenia, Grade 2Depression, Grade 1Diarrhea, Grade 1Dry eyes, Grade 1Dry skin, Grade 1Elevated LDH, Grade 1Elevated serum creatinine, Grade 1Elevated serum creatinine, Grade 2Elevated alkaline phosphatase, Grade 1Elevated ALT, Grade 1Elevated AST, Grade 4Fatigue, Grade 1Hyperbilirubinemia, Grade 1Hypercholesterolemia, Grade 1Hyperglycemia, Grade 1Hyperglycemia, Grade 2Hypoalbuminemia, Grade 1Hypoalbuminemia, Grade 2Hypocalcemia, Grade 1Hypoglycemia, Grade 1Hypoglycemia, Grade 2Hypokalemia, Grade 1Hyponatremia, Grade 1Mouth sores, Grade 1Mouth sores, Grade 2Mucositis, Grade 1Mucositis, Grade 3Nausea, Grade 1Neuropathy, Grade 1Pruritis, Grade 1Rash, Grade 1Rash, Grade 3Shortness of breath, Grade 1Strep throat, Grade 2Urosepsis, Grade 3Vomiting, Grade 1
Erlotinib & Celecoxib2221221135463413546227231411239331432823112

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Clinical Outcome: Progression to a Higher-grade Dysplasia or Carcinoma

Response evaluation was based on pathologic examination of the degree of dysplasia observed and recorded by an expert head and neck pathologist. Pathologic complete response was defined as complete disappearance of dysplasia from the epithelium. Pathologic partial response was defined as improvement of dysplasia by at least one degree (i.e., severe dysplasia becomes moderate dysplasia). Pathologic minor response or stable disease was defined as minor focal improvement without change of degree of dysplasia (i.e., focal improvement from moderate to mild dysplasia with still moderate dysplasia overall) or no pathologic changes after treatment. Pathologic progressive disease was defined as worsening by at least one degree of dysplasia (i.e., mild to moderate dysplasia) or development of invasive cancer on or following treatment. (NCT00314262)
Timeframe: Up to 55 months from initiation of therapy. Median duration of follow-up was 36 months.

Interventionparticipants (Number)
Stage I invasive carcinomaStage II oral cavity carcinomaInvasive squamous cell carcinomaRecurrent moderate dysplasiaRecurrent severe dysplasiaRecurrent high-grade dysplasiaComplete remission
Erlotinib & Celecoxib1111111

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The First Occurrence of Clinically Significant Gastrointestinal Events (CSGIE)

CSGIE include: Gastroduodenal (GD) hemorrhage, Gastric outlet obstruction, Gastroduodenal, small bowel or large bowel perforation, Large bowel hemorrhage, Small bowel hemorrhage, Acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage, Symptomatic gastric or duodenal ulcer (NCT00346216)
Timeframe: ITT Population - 30 months; MITT Population - 42 months

,,
InterventionPercentage of Participants (Number)
ITT (N = 8072, 8040, 7969)MITT (N = 8030, 7990, 7933)
Celecoxib0.70.3
Ibuprofen0.90.7
Naproxen0.70.7

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Change From Baseline in Patient's Assessment of Arthritis Pain (VAS)

"VAS question How much pain do you have was graded on a scale from 0 to 100 with 0 indicating No pain and 100 indicating Worst possible pain." (NCT00346216)
Timeframe: ITT and MITT Population - Baseline to 42 months

,,
InterventionNumber of participants (Mean)
Baseline (ITT) N= 8014, 8001, 7928Change-Baseline to Mon1 (ITT) N=7382, 7379, 7325Change-Baseline to Mon2 (ITT) N=7180, 7090, 7149Change-Baseline to Mon4 (ITT) N=6777, 6696, 6740Change-Baseline to Mon8 (ITT) N=6230, 6137, 6159Change-Baseline to Mon12 (ITT) N=5792, 5696, 5846Change-Baseline to Mon18 (ITT) N=5310, 5181. 5246Change-Baseline to Mon24 (ITT) N=4818, 4776, 4785Change-Baseline to Mon30 (ITT) N=4140, 4069, 4086Change-Baseline to Mon36 (ITT) N=3692, 3627, 3635Change-Baseline to Mon42 (ITT) N=3469, 3406, 3439Baseline (MITT) N=7974, 7954, 7894Change-Baseline to Mon1 MITT N=7372, 7367, 7321Change-Baseline to Mon2 MITT N=7170, 7078, 7142Change-Baseline to Mon4 MITT N=6772, 6686, 6732Change-Baseline to Mon8 MITT N=6224, 6128, 6155Change-Baseline to Mon12 MITT N=5787, 5689, 5844Change-Baseline to Mon18 MITT N=5305, 5175, 5242Change-Baseline to Mon24 MITT N=4815, 4769, 4782Change-Baseline to Mon30 MITT N=4139, 4067, 4085Change-Baseline to Mon36 MITT N=3691, 3623, 3635Change-Baseline to Mon42 MITT N=3468, 3404, 3438
Celecoxib54.0-8.2-10.5-11.4-11.7-11.0-11.3-11.3-10.5-10.1-11.454.0-8.2-10.5-11.4-11.7-11.0-11.3-11.4-10.5-10.2-11.4
Ibuprofen54.1-9.0-10.6-11.7-12.1-11.6-11.3-11.5-11.2-10.7-11.154.1-9.0-10.6-11.7-12.1-11.6-11.3-11.5-11.2-10.7-11.1
Naproxen54.1-9.9-11.1-12.3-12.1-11.9-11.7-11.4-11.3-11.6-12.154.1-9.9-11.1-12.3-12.1-11.9-11.7-11.3-11.3-11.6-12.1

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The First Occurrence of a Major Adverse Cardiovascular Events (MACE)

MACE defined as the composite of CV death (including hemorrhagic death), non-fatal MI, non-fatal stroke, hospitalization for UA, revascularization or hospitalization for TIA (NCT00346216)
Timeframe: ITT Population - 30 months; MITT Population - 42 months

,,
InterventionPercentage of Participants (Number)
ITT (N = 8072, 8040, 7969)MITT (N = 8030, 7990, 7933)
Celecoxib4.23.1
Ibuprofen4.83.6
Naproxen4.33.2

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The First Occurrence of Antiplatelet Trialists Collaboration (APTC) Composite Endpoint, Confirmed by the Clinical Events Committee (CEC).

APTC events are defined as a composite of any of the following events: Death due to CV causes (including cardiac, cerebrovascular, venous thromboembolic, haemorrhagic, other vascular, or unknown cause); Non-fatal MI; Non-fatal stroke (including intracranial hemorrhages, stroke of ischemic or unknown etiology). (NCT00346216)
Timeframe: Intent to Treat (ITT) Population - 30 months; Modified ITT (MITT) Population - 42 months

,,
InterventionPercentage of Partcipants (Number)
ITT (N = 8072, 8040, 7969)MITT (N = 8030, 7990, 7933)
Celecoxib2.31.7
Ibuprofen2.71.9
Naproxen2.51.8

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Best Response

As appropriate for tumor type and location, gadolinium-enhanced MRI and other imaging modalites were used to assess response. Best response was regarded as best response at any single assessment. Response was defined as follows: complete resolution of all demonstrable tumor, complete response (CR); >/=50% decrease in the product of the 2 maximum perpendicular diameters relative to the baseline evaluation, partial response (PR); <50% decrease and <25% increase in product of diameters, stable disease (SD); and >/=25% increase in product of diameters, development of new areas of disease, or disease-attributable clinical deterioration or death, progressive disease (PD). For patients with leukemia PD was defined as >/=25% or >/=5,000 cells/mm3 increase in number of circulating cells, development of extramedullary disease, or other clinical evidence of progression. (NCT00357500)
Timeframe: Assessed at study entry, every 9 weeks on treatment and at treatment discontinuation, up to 27 weeks.

Interventionparticipants (Number)
Complete ResponsePartial ResponseStable DiseaseProgressive DiseaseNot Evaluable
5-drug Metronomic Antiangiogenic Regimen11236471

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27-Week Progression-Free Survival

27-week progression-free survival is the probability of patients remaining alive and progression-free at 27-weeks from study entry estimated using Kaplan-Meier methods. As appropriate for tumor type and location, gadolinium-enhanced MRI and other imaging modalites were used to assess response. Progressive disease was defined as >/=25% increase in product of diameters, development of new areas of disease, or disease-attributable clinical deterioration or death, progressive disease. For patients with leukemia PD was defined as >/=25% or >/=5,000 cells/mm3 increase in number of circulating cells, development of extramedullary disease, or other clinical evidence of progression. (NCT00357500)
Timeframe: Assessed every 9 weeks on treatment and annually until death or initiation of new therapy, up to 27 weeks.

InterventionProbability (Number)
5-drug Metronomic Antiangiogenic Regimen0.31

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Therapy Completion Rate

Proportion of patients alive at 27 weeks without progressive disease (PD) and having tolerated therapy. As appropriate for tumor type and location, gadolinium-enhanced MRI and other imaging modalites were used to assess response. Progressive disease was defined as >/=25% increase in product of diameters, development of new areas of disease, or disease-attributable clinical deterioration or death, progressive disease. For patients with leukemia PD was defined as >/=25% or >/=5,000 cells/mm3 increase in number of circulating cells, development of extramedullary disease, or other clinical evidence of progression. (NCT00357500)
Timeframe: 27 weeks

Interventionproportion of patients (Number)
5-drug Metronomic Antiangiogenic Regimen.25

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27-Week Overall Survival

27-week overall survival is the probability of patients remaining alive at 27-weeks from study entry estimated using with Kaplan-Meier methods. (NCT00357500)
Timeframe: Assessed every 9 weeks on treatment and annually until death or initiation of new therapy, up to 27 weeks.

InterventionProbability (Number)
5-drug Metronomic Antiangiogenic Regimen0.61

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Change From Baseline Hct at Week 24

(NCT00373685)
Timeframe: Baseline and Week 24 or ET

InterventionPercent (Least Squares Mean)
Celecoxib-0.330
nsNSAIDs-0.716

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Percentage of Participants With Proton Pump Inhibitor (PPI) and Other Gastric Protective Drug Utilization

PPI and other gastric protective drug (defined as Histamine-2 receptor antagonists [H2RA], misoprostol, sucralfate, and others such as antacids) utilization. (NCT00373685)
Timeframe: Baseline through week 24 or ET

,
InterventionPercentage of participants (Number)
PPIsH2RAsGastric protective agents
Celecoxib23.05.00.9
nsNSAIDs24.25.71.0

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Change From Baseline Hb at Week 24

(NCT00373685)
Timeframe: Baseline and Week 24 or ET

Interventiong/dL (Least Squares Mean)
Celecoxib-0.109
nsNSAIDs-0.241

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Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Time to Pain Relief

Percentage of participants who reported Very Satisfied or Satisfied with efficacy of current pain medication questions on the PTSS Efficacy subscale for the time it took medication to work, scale ranged from Very Satisfied (1) to Very Dissatisfied (5). Possible range of scores 1 to 15. (NCT00373685)
Timeframe: Baseline, Weeks 8, 16, 24 or ET

,
InterventionPercentage of participants (Number)
Baseline (n=3890, 3905)Week 8 (n=3185, 3202)Week 16 (n=2784,2777)Week 24 or ET (n=3386,3362)Week 24/LOCF (n=3672, 3653)
Celecoxib43.280.283.276.276.0
nsNSAIDs43.771.677.773.873.3

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Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Duration of Pain Relief

Percentage of participants who reported Very Satisfied or Satisfied with efficacy of current pain medication questions on the PTSS Efficacy, subscale for duration of pain relief provided by medication, scale ranged from Very Satisfied (1) to Very Dissatisfied (5). Possible range of scores 1 to 15. (NCT00373685)
Timeframe: Baseline, Weeks 8, 16, 24 or ET

,
InterventionPercentage of participants (Number)
Baseline (n=3886, 3905)Week 8 (n=3182, 3202)Week 16 (n=2780,2778)Week 24 or ET (n=3383,3361)Week 24/LOCF (n=3671, 3653)
Celecoxib37.875.477.872.272.2
nsNSAIDs36.666.871.668.868.2

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Percentage of Participants With Non-study Medication Utilization

Non-study medication utilization associated with initial treatment defined as narcotic analgesics and acetaminophen use. (NCT00373685)
Timeframe: Baseline through week 24 or ET

,
InterventionPercentage of participants (Number)
AcetaminophenAcetylsalicylic acid (ASA)NSAIDsOpioids
Celecoxib6.83.512.814.2
nsNSAIDs6.53.013.315.6

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Percentage of Participants With Clinically Significant Decrease in Hct and/or Hb From Baseline

Clinically significant decrease in Hct (greater than or equal to 10 percent [≥10%]) and/or decrease in Hb (≥ 2 g/dL). (NCT00373685)
Timeframe: Baseline, Weeks 8, 16, 24 or ET

,
InterventionPercentage of participants (Number)
Week 8 (n= 3043, 3086)Week 16 (n=2687, 2675)Week 24 (n=3278, 3207)Week 24 LOCF (n=3604, 3574)
Celecoxib0.70.80.91.8
nsNSAIDs0.91.61.52.9

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Percentage of Participants Satisfied With Efficacy of Current Pain Medication - Amount of Pain Relief

Percentage of participants who reported Very Satisfied or Satisfied with efficacy of current pain medication questions on the PTSS Efficacy subscale for the amount of pain relief medication provided, scale ranged from Very Satisfied (1) to Very Dissatisfied (5). Possible range of scores 1 to 15. (NCT00373685)
Timeframe: Baseline, Weeks 8, 16, 24 or ET

,
InterventionPercentage of participants (Number)
Baseline (n=3888, 3905)Week 8 (n=3185, 3203)Week 16 (n=2783, 2778)Week 24 or ET (n=3385, 3362)Week 24/LOCF (n=3671, 3653)
Celecoxib41.477.480.574.074.0
nsNSAIDs40.569.274.571.370.8

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Percentage of Participants With Moderate to Severe Abdominal Symptoms

"Abdominal symptoms coded using the Medical Dictionary for Regulatory Activities (MedDRA) System Organ Class (SOC) 'Gastrointestinal Disorders' high level group term (HLGT) equal to Gastrointestinal Signs and Symptoms; where moderate indicated the gastrointestinal adverse event (GI AE) interfered to some extent with the participants' usual function and severe indicated the GI AE interfered significantly with participants' usual function." (NCT00373685)
Timeframe: Baseline through week 24 or ET

InterventionPercentage of participants (Number)
Celecoxib2.3
nsNSAIDs3.4

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Percentage of Participants With Positive Blood Fecal Occult

Positive blood fecal occult; blood in feces that is not visibly apparent (NCT00373685)
Timeframe: Week 24 or ET

InterventionPercentage of participants (Number)
Celecoxib1.1
nsNSAIDs1.4

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Percentage of Participants With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)

CSULGIE defined as any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; acute gastrointestinal (GI) hemorrhage of unknown origin; small bowel obstruction; clinically significant anemia/blood loss of defined GI origin or presumed occult GI origin. (NCT00373685)
Timeframe: Baseline through week 24 or Early Termination (ET)

InterventionPercentage of participants (Number)
Celecoxib1.3
nsNSAIDs2.4

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Percentage of Participants Who Withdrew Due to GI Adverse Events (AEs)

GI AEs defined using MedDRA SOC 'Gastrointestinal Disorders' but excluding HLGT's: Benign Neoplasms Gastrointestinal, Dental and Gingival Conditions, Oral Soft Tissue Conditions, Salivary Gland Conditions and Tongue Conditions (NCT00373685)
Timeframe: Baseline through week 24 or ET

InterventionPercentage of participants (Number)
Celecoxib2.8
nsNSAIDs3.0

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Hemoglobin (Hb) at Baseline

(NCT00373685)
Timeframe: Baseline

Interventiongram per deciliter (g/dL) (Mean)
Celecoxib13.6
nsNSAIDs13.6

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Hematocrit (Hct) at Baseline

(NCT00373685)
Timeframe: Baseline

InterventionPercent (Mean)
Celecoxib40.8
nsNSAIDs40.9

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Percentage of Participants Satisfied With Efficacy of Current Pain Medication Overall

Percentage of participants who reported Very Satisfied or Satisfied with current pain medication question on the Patient Treatment Satisfaction Scale (PTSS), scale ranged from Very Satisfied (1) to Very Dissatisfied (5). (NCT00373685)
Timeframe: Baseline, Weeks 8, 16, 24 or ET

,
InterventionPercentage of participants (Number)
Baseline (n=3887, 3904)Week 8 (n=3181, 3199)Week 16 (n=2784, 2772)Week 24 or ET (n=3383, 3361)Week 24/LOCF (n=3672, 3651)
Celecoxib39.878.581.974.674.5
nsNSAIDs38.069.574.670.870.3

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Sore Throat Relief Rating Scale (STRRS) - 'Moderate Relief' at 6 Hours Post-First Dose

Subjects Achieving at Least 'Moderate Relief' as Measured by STRRS (range: 0=no relief to 6=complete relief); Moderate relief is defined as STRRS = 3). (NCT00402987)
Timeframe: at 6 hours

Interventionsubjects (Number)
Celecoxib 50mg/50mg28
Celecoxib 100 mg (Pooled)31
Placebo13

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Subjects Taking Rescue Medication

Subjects were allowed to use rescue medication at any time during the trial, but were discouraged from taking rescue medication within 2 hours of administration of the first dose of study drug. (NCT00402987)
Timeframe: Within 24 hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg22
Celecoxib 100mg /Placebo15
Celecoxib 100mg/50mg13
Placebo39

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Subjects With >= 50% Total Pain Relief (TOTPAR) at 12 Hours Post-First Dose

TOTPAR is time-interval-weighted sum of accumulated Sore Throat Relief Rating Scale (STRRS) scores (scale: 0 no relief to 6 complete relief). Maximum TOTPAR over 12 hours is 72. If the subject calculated TOTPAR is greater than or equal to 50% of the maximum TOTPAR then the subject is said to have achieved >=50% TOTPAR. (NCT00402987)
Timeframe: 12 hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg18
Celecoxib 100mg/Placebo12
Celecoxib 100mg/50mg8
Placebo6

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Subjects With >= 50% Total Pain Relief (TOTPAR) at 6 Hours Post-First Dose

TOTPAR is time-interval-weighted sum of accumulated Sore Throat Relief Rating Scale (STRRS) scores (scale: 0 no relief to 6 complete relief). Maximum TOTPAR over 6 hours is 36. If the subject calculated TOTPAR is greater than or equal to 50% of the maximum TOTPAR then the subject is said to have achieved >=50% TOTPAR. (NCT00402987)
Timeframe: 6 hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg18
Celecoxib 100mg (Pooled)19
Placebo7

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Sum of Sore Throat Pain Intensity Difference (SPID2) as Measured by Difficulty Swallowing Scale (DSS) at 2 Hours Post-First Dose

SPID2 was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Difficulty Swallowing PID was calculated as the difference between the pain intensity (DSS scale: 0mm=not difficult, 100mm=very difficult) at 2 hours post dose and at baseline. (NCT00402987)
Timeframe: Over 2 hour Period Post-First Dose

Interventionunits on a scale * hours (Least Squares Mean)
Celecoxib 50mg/50mg22.0
Celecoxib 100mg (Pooled)16.0
Placebo5.8

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Sum of Sore Throat Pain Intensity Difference (SPID2) on Swallowing at 2 Hours Post-First Dose

Based on the Pain Intensity scores measured on a Visual Analogue Scale (PI-VAS: 0mm=no pain,100mm=worst possible pain), assessed by the subjects, the SPID2 is the area under the curve (AUC) over the 2-hour period post-first dose of the Pain Intensity Difference (PID) scores using the trapezoidal rule. (NCT00402987)
Timeframe: 2 hours Post-First Dose

Interventionunits on a scale * hours (Least Squares Mean)
Celecoxib 100mg (Pooled)21.0
Placebo9.4

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Time to Meaningful Pain Relief

The time (measured by stopwatch) when the subject felt their pain relief was meaningful to them was not estimable thus the number of subjects experiencing meaningful pain relief within 2 hours of first dose is reported (NCT00402987)
Timeframe: Within 2 Hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg36
Celecoxib 100 mg (Pooled)33
Placebo15

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Time to Perceptible Pain Relief

Defined as time (measured by stopwatch) when subject began to feel any pain relieving effect from the drug (NCT00402987)
Timeframe: Within 2 Hours Post-First Dose

Interventionminutes (Median)
Celecoxib 50mg/50mg49
Celecoxib 100 mg (Pooled)61
Placebo97

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Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) From 7 to 24 Hours Post-First Dose

The Difficulty Swallowing Pain Intensity Difference (PID) was calculated as the difference between the pain intensity (DSS range: 0mm=not difficult, 100mm=very difficult) at the time and at baseline. (NCT00402987)
Timeframe: 7 to 24 hours Post-First Dose

,,,
Interventionunits on a scale (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100mg/50mg11.3813.4012.6811.6813.1313.4113.24
Celecoxib 100mg/Placebo18.1117.2915.1014.3212.9911.4413.67
Celecoxib 50mg/50mg16.9116.5316.5916.6115.0115.4014.25
Placebo4.864.885.465.855.225.308.79

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Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) Within 6 Hours Post-First Dose

The Difficulty Swallowing Pain Intensity Difference (PID) was calculated as the difference between the pain intensity (DSS range: 0mm=not difficult, 100mm=very difficult) at the time and at baseline. (NCT00402987)
Timeframe: Within 6 hours Post-First Dose

,,
Interventionunits on a scale (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)1.163.145.758.0210.4712.2115.1516.5018.3918.2718.1116.43
Celecoxib 50mg/50mg1.694.856.9911.2114.3117.4020.5221.7622.2020.5318.4016.62
Placebo0.811.112.853.533.953.974.454.994.207.286.025.70

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First Perceptible Relief

Subjects having First Perceptible Relief at each time point. Perceptible relief is score >0 on Sore Throat Relief Rating Scale(STRRS)(range: 0=no relief to 6=complete relief). (NCT00402987)
Timeframe: up to 24 hours

,,,
Interventionsubjects (Number)
1 hour - Onset subjects in hour1 hour - No onset subjects in hour2 hour - Onset subjects in hour2 hour-No onset subjects in hour3 hour - Onset subjects in hour3 hour-No onset subjects in hour4 hour - Onset subjects in hour4 hour- No onset subjects in hour5 hour - Onset subjects in hour5 hour-No onset subjects in hour6 hour - Onset subjects in hour6 hour-No onset subjects in hour7 hour - Onset subjects in hour7 hour-No onset subjects in hour8 hour - Onset subjects in hour8 hour-No onset subjects in hour9 hour - Onset subjects in hour9 hour-No onset subjects in hour10 hour - Onset subjects in hour10 hour-No onset subjects in hour11 hour - Onset subjects in hour11 hour-No onset subjects in hour (12 hour - Onset subjects in hour12 hour-No onset subjects in hour24 hour - Onset subjects in hour24 hour-No onset subjects in hour
Celecoxib 100mg/50mg22239140142121113817160606060606
Celecoxib 100mg/Placebo29161062404041303030303030303
Celecoxib 50mg/50mg68221391808080808082606060615
Placebo40491138236432428127126224222022121120218

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No Perceptible Relief

Subjects having No Perceptible Relief at each time point. No Perceptible relief is score = 0 on Sore Throat Relief Rating Scale (STRRS)(range: 0=no relief to 6=complete relief). (NCT00402987)
Timeframe: up to 24 hours

,,,
Interventionsubjects (Number)
1 hour - Offset subjects in hour1 hour-No offset subjects in hour2 hour- Offset subjects in hour2 hour-No offset subjects in hr3 hour- Offset subjects in hour3 hour-No offset subjects in hr4 hour- Offset subjects in hour4 hour-No offset subjects in hr5 hour- Offset subjects in hour5 hour-No offset subjects in hr6 hour- Offset subjects in hour6 hour-No offset subjects in hr7 hour- Offset subjects in hour7 hour-No offset subjects in hr8 hour- Offset subjects in hour8 hour-No offset subjects in hr9 hour- Offset subjects in hour9 hour-No offset subjects in hr10 hour-Offset subjects in hour10 hour-No offset subjects in hr11 hour-Offset subjects in hour11 hour-No offset subjects in hr12 hour-Offset subjects in hour12 hour-No offset subjects in hr24 hour-Offset subjects in hour (N=78,37, 41, 81)24 hour-No offset subjects in hr (N=78,37,41, 81)
Celecoxib 100mg/50mg045045144044044044242042141041041041338
Celecoxib 100mg/Placebo045144044044044044242240337037037037037
Celecoxib 50mg/50mg090090189089188088484183182280179178375
Placebo089188088088088187186086086383083281081

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Patient's Global Evaluation of Study Medication at 12 and 24 Hours Post-First Dose

Subject assessment of overall impression of study drug on 4 point scale from 1 (poor) to 4 (excellent) (NCT00402987)
Timeframe: 12 and 24 hours Post-First Dose

,,,
Interventionsubjects (Number)
Excellent (4) - 12 hoursGood (3) - 12 hoursFair (2) - 12 hoursPoor (1) - 12 hoursExcellent (4) - 24 hoursGood (3) - 24 hoursFair (2) - 24 hoursPoor (1) - 24 hours
Celecoxib 100 mg / Placebo5101118413721
Celecoxib 100mg / 50mg0131120291518
Celecoxib 50mg/50mg82321377202537
Placebo11018562131557

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Patient's Global Evaluation of Study Medication at 6 Hours Post-First Dose

Subject assessment of overall impression of study drug on 4 point scale from 1 (poor) to 4 (excellent) (NCT00402987)
Timeframe: 6 Hours Post-First Dose

,,
Interventionsubjects (Number)
Excellent (4)Good (3)Fair (2)Poor (1)
Celecoxib 100 mg (Pooled)4252733
Celecoxib 50mg/50mg5242535
Placebo252260

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Sore Throat Pain Intensity Difference (PID) From 7 to 24 Hours Post-First Dose

Pain intensity (PI) on Swallowing as Measured by PI-VAS scale: 0mm=no pain, 100mm=worst possible pain. PID score was obtained by subtracting the PI at each time point from the Baseline PI score. An increase in scores indicated a lessening of subjects' pain as compared to Baseline scores, thus, higher scores indicated a greater reduction in pain. (NCT00402987)
Timeframe: 7 to 24 hours

,,,
Interventionunits on a scale (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100mg/50mg18.3419.9318.8718.0618.9920.2219.44
Celecoxib 100mg/Placebo22.0120.8119.1818.0217.4315.0116.50
Celecoxib 50mg/50mg20.8220.3921.3921.2619.6519.0118.43
Placebo9.328.129.929.569.298.6012.81

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Sore Throat Pain Intensity Difference (PID) Within 6 Hours Post-First Dose

Pain intensity (PI) on Swallowing as Measured by PI-VAS scale: 0mm=no pain, 100mm=worst possible pain. Sore throat PID score was obtained by subtracting the PI at each time point from the Baseline PI score. Increase in scores indicated a lessening of subjects' pain compared to baseline scores; higher scores indicated a greater reduction in pain. (NCT00402987)
Timeframe: Within First 6 hours Post-First Dose

,,
Interventionunits on a scale (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)1.924.937.0511.4313.2417.0018.8021.5122.2123.1523.5620.59
Celecoxib 50mg/50mg1.624.709.5712.1817.2422.3924.6826.6327.9025.5224.1221.42
Placebo0.402.143.855.346.606.757.418.069.0610.3510.479.04

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Sore Throat Relief Rating Scale (STRRS) From 7 to 24 Hours Post-First Dose

STRRS score (scale: 0 no relief to 6 complete relief); a higher score indicated a greater reduction in pain. (NCT00402987)
Timeframe: 7 to 24 hours

,,,
Interventionscores on a scale (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100 mg / Placebo2.001.801.761.671.581.421.62
Celecoxib 100mg / 50mg1.671.711.561.511.601.531.60
Celecoxib 50mg/50mg1.711.681.691.741.671.561.69
Placebo0.930.971.081.081.101.071.31

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Sore Throat Relief Rating Scale (STRRS) Within 6 Hours Post-First Dose

STRRS score (scale: 0 no relief to 6 complete relief); a higher pain score indicated a greater reduction in pain. (NCT00402987)
Timeframe: within the first 6 hours

,,
Interventionscores on a scale (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100 mg (Pooled)0.090.340.691.011.271.611.741.931.921.961.971.86
Celecoxib 50mg/50mg0.120.410.741.221.581.882.102.222.132.082.001.81
Placebo0.160.340.520.640.790.880.930.920.921.101.070.96

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Subjects Who Achieved Their Own Level of 'Meaningful Relief' and 'Much Improvement' at 12 Hours Post-First Dose

Symptom relief measured as self-directed endpoints defined by each individual at end of study using Sore Throat Relief Rating Scale (STRRS); STRRS score ranges from 0=no relief to 6=complete relief. If subject scored same or greater in their STRRS during the study then they achieved their 'Meaningful Relief' or 'Much Improvement'. (NCT00402987)
Timeframe: 12 hours Post-First Dose

,,,
Interventionsubjects (Number)
Meaningful Relief - achievedMeaningful Relief - not achievedMuch Improvement - achievedMuch Improvement - not achieved
Celecoxib 100mg /Placebo26192223
Celecoxib 100mg/50mg20241232
Celecoxib 50mg/50mg44463852
Placebo20691673

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Subjects Who Achieved Their Own Level of 'Meaningful Relief' and 'Much Improvement' at 2 and 6 Hours Post-First Dose

Symptom relief measured as self-directed endpoints defined by each individual at end of study using Sore Throat Relief Rating Scale (STRRS); STRRS score ranges from 0=no relief to 6=complete relief. If subject scored same or greater in their STRRS during the study then they achieved their 'Meaningful Relief' or 'Much Improvement'. (NCT00402987)
Timeframe: 2 and 6 hours Post-First Dose

,,
Interventionsubjects (Number)
meaningful relief - 2 hours- achievedmeaningful relief- 2 hours- not achievedmeaningful relief - 6 hours- achievedmeaningful relief- 6 hours- not achievedmuch improvement - 2 hours- achievedmuch improvement - 2 hours- not achievedmuch improvement - 6 hours- achievedmuch improvement - 6 hours- not achieved
Celecoxib 100mg (Pooled)2663385122673158
Celecoxib 50mg/50mg3159405022683357
Placebo1277177210791277

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Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Who Had Perceptible Relief Onset Time Within 1 Hour

At end of study subjects defined meaningful pain relief by completing Meaningful Relief Scale. Meaningful relief was achieved if Sore Throat Relief Rating Scale (STRRS) score (range: 0=no relief to 6=complete relief) at end of the study was the same or higher than individually defined relief score during the study. Perceptible relief is STRRS >0. (NCT00402987)
Timeframe: Within 6 hours Post-First Dose

,,
Interventionsubjects (Number)
AchievedNot achieved
Celecoxib 100mg (Pooled)2762
Celecoxib 50mg/50mg3159
Placebo1277

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Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Who Still Had Perceptible Relief at 12 and 24 Hours Post-First Dose

At end of study subjects defined meaningful pain relief by completing the Meaningful Relief Scale. Meaningful relief was achieved if Sore Throat Relief Rating Scale (STRRS)(range: 0=no relief to 6=complete relief) score at end of the study was the same or higher than individually defined relief score during the study. Perceptible relief is STRRS >0 (NCT00402987)
Timeframe: 12 and 24 hours Post-First Dose

,,,
Interventionsubjects (Number)
at 12 hours - Achievedat 12 hours - Not Achievedat 24 hours - Achievedat 24 hours - Not Achieved
Celecoxib 100mg/50mg1232935
Celecoxib 100mg/Placebo16291629
Celecoxib 50mg/50mg32582862
Placebo11781178

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Subjects With Sore Throat Pain at Least 35% Gone and at Least 50% Gone at 12 Hours Post-First Dose

>= 35% and 50% Pain Intensity Difference (PID) on the Pain Intensity-Visual Analog Scale (PI-VAS) (scale: 0mm=no pain, 100mm=worst possible pain). The PID was calculated as the difference between the pain intensity at 12 hours and at baseline. (NCT00402987)
Timeframe: 12 hours Post-First Dose

,,,
Interventionsubjects (Number)
12 hours >=35% gone12 hours >=50% gone
Celecoxib 100mg/50mg1210
Celecoxib 100mg/Placebo1312
Celecoxib 50mg/50mg3022
Placebo139

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Number Needed to Treat (NNT) to Achieve at Least 50% of Maximum Total Pain Relief (TOTPAR) at 12 Hours Post-First Dose

NNT is number of subjects needed to treat to have one subject report a 50% or better pain relief over 12 hours based on maximum possible pain relief on Sore Throat Relief Rating Scale. Maximum TOTPAR over 12 hours is 72. If the subject TOTPAR is greater than or equal to 50% of the maximum TOTPAR then the subject has achieved >=50% TOTPAR. (NCT00402987)
Timeframe: 12 hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg18
Celecoxib 100mg/Placebo12
Celecoxib 100mg/50mg8
Placebo6

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Subjects With Sore Throat Pain at Least 35% Gone and at Least 50% Gone at 2 and 6 Hours Post-First Dose

>= 35% and 50% Pain Intensity Difference (PID) on the Pain Intensity-Visual Analog Scale (PI-VAS) (scale: 0mm=no pain, 100mm=worst possible pain). The PID was calculated as the difference between the pain intensity at the time and at baseline. (NCT00402987)
Timeframe: 2 and 6 hours Post-First Dose

,,
Interventionsubjects (Number)
2 hours >=35% gone6 hours >=35% gone2 hours >=50% gone6 hours >=50% gone
Celecoxib 100mg (Pooled)32292422
Celecoxib 50mg/50mg39312823
Placebo151289

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Sum of Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) From 7 to 24 Hours Post-First Dose

The sum of pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Difficulty Swallowing PID was calculated as the difference between the pain intensity (DSS range: 0mm=not difficult, 100mm=very difficult) at the time and at baseline. (NCT00402987)
Timeframe: 7 to 24 hours Post-First Dose

,,,
Interventionunits on a scale * hours (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100mg/50mg72.284.597.6109.8122.2135.4295.3
Celecoxib 100mg/Placebo133.6151.3167.5182.2195.8208.0358.7
Celecoxib 50mg/50mg119.1135.8152.3168.9184.7200.0377.9
Placebo33.938.843.949.655.160.4144.9

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Sum of Difficulty Swallowing Difference as Measured by Difficulty Swallowing Scale (DSS) Within 6 Hours Post-First Dose

The sum of pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Difficulty Swallowing PID was calculated as the difference between the pain intensity (DSS range: 0mm=not difficult, 100mm=very difficult) at the time and at baseline. (NCT00402987)
Timeframe: Within 6 hours Post-First Dose

,,
Interventionunits on a scale * hours (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)0.10.71.83.55.88.712.116.033.551.870.087.3
Celecoxib 50mg/50mg0.21.02.54.88.011.916.722.043.965.384.8102.3
Placebo0.10.30.81.62.63.64.65.810.416.122.828.6

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Sum of Sore Throat Pain Intensity Difference (SPID) From 7 to 24 Hours Post-First Dose

The sum of pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The PID [based on PI-VAS scale: 0mm=no pain, 100mm=worst possible pain] was calculated as the difference between the pain intensity at the time and at baseline. (NCT00402987)
Timeframe: 7 to 24 hours

,,,
Interventionunits on a scale * hours (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100 mg / Placebo151.8173.2193.2211.8229.5245.7434.8
Celecoxib 100mg / 50mg111.6130.8150.2168.6187.2206.8444.7
Celecoxib 50mg/50mg149.2169.8190.7212.0232.4251.8476.4
Placebo56.665.474.484.193.5102.5231.0

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Sum of Sore Throat Pain Intensity Difference (SPID) Within 6 Hours Post-First Dose

The sum of pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The PID [based on PI-VAS scale: 0mm=no pain, 100mm=worst possible pain] was calculated as the difference between the pain intensity at the time and at baseline. (NCT00402987)
Timeframe: up to 6 hours

,,
Interventionunits on a scale * hours (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)0.21.12.64.98.011.816.221.343.165.889.2111.2
Celecoxib 50mg/50mg0.21.02.85.59.214.120.026.453.780.4105.2128.0
Placebo0.10.41.12.33.85.47.29.117.727.437.847.6

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Sum of Throat Soreness Difference as Measured by Throat Soreness Scale (TSS) From 7 to 24 Hours Post-First Dose

The sum of sore throat pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Sore Throat PID was calculated as the difference between the pain intensity (TSS range: 0=not sore to 10=very sore) at the time and at baseline. (NCT00402987)
Timeframe: 7 to 24 hours Post-First Dose

,,,
Interventionunits on a scale * hours (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100mg/50mg9.911.613.314.916.618.439.8
Celecoxib 100mg/Placebo14.216.017.719.320.822.339.2
Celecoxib 50mg/50mg12.814.516.218.019.721.440.3
Placebo5.66.37.28.18.99.821.7

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Sum of Throat Soreness Difference as Measured by Throat Soreness Scale (TSS) Within 6 Hours Post-First Dose

The sum of sore throat pain intensity differences (SPID) was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Sore Throat PID was calculated as the difference between the pain intensity (TSS range: 0=not sore to 10=very sore) at the time and at baseline. (NCT00402987)
Timeframe: Within 6 hours Post-First Dose

,,
Interventionunits on a scale * hours (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)0.010.060.190.390.671.041.481.964.026.128.2110.20
Celecoxib 50mg/50mg0.010.070.210.450.801.241.772.354.767.059.1311.07
Placebo0.010.050.140.270.440.630.821.021.832.763.794.75

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Throat Soreness Scale (TSS) Difference From 7 to 24 Hours Post-First Dose

The Pain Intensity Difference (PID) based on TSS (scale: 0=not sore to 10=very sore) was calculated as the difference between the pain intensity at the time and at baseline. (NCT00402987)
Timeframe: 7 to 24 hours post-first dose

,,,
Interventionscores on a scale (Least Squares Mean)
7 hours8 hours9 hours10 hours11 hours12 hours24 hours
Celecoxib 100mg/50mg1.681.701.651.631.761.801.78
Celecoxib 100mg/Placebo1.951.651.601.581.531.371.46
Celecoxib 50mg/50mg1.651.671.761.801.761.531.62
Placebo0.780.760.900.870.870.821.17

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Throat Soreness Scale (TSS) Difference Within 6 Hours Post-First Dose

The Pain Intensity Difference (PID) based on TSS (scale: 0=not sore to 10=very sore) was calculated as the difference between the pain intensity at the time and at baseline. (NCT00402987)
Timeframe: Within first 6 hours post-first dose

,,
Interventionscores on a scale (Least Squares Mean)
15 min30 min45 min60 min75 min90 min1.75 hours2 hours3 hours4 hours5 hours6 hours
Celecoxib 100mg (Pooled)0.060.360.660.971.291.641.862.032.092.122.061.90
Celecoxib 50mg/50mg0.060.390.741.171.621.972.242.392.432.142.031.83
Placebo0.060.290.430.600.750.760.790.780.851.011.040.90

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Total Pain Relief (TOTPAR) at 12 and 24 Hours Post-First Dose

TOTPAR is time-interval-weighted sum of accumulated Sore Throat Relief Rating Scale (STRRS) scores (scale: 0 no relief to 6 complete relief). (NCT00402987)
Timeframe: 12 and 24 hours Post-First Dose

,,,
Interventionscores on a scale (Least Squares Mean)
12 hours24 hours
Celecoxib 100mg /Placebo22.041.5
Celecoxib 100mg/50mg17.536.7
Celecoxib 50mg/50mg20.640.9
Placebo11.627.3

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Total Pain Relief (TOTPAR) at 2 and 6 Hours Post-First Dose

TOTPAR is time-interval-weighted sum of accumulated Sore Throat Relief Rating Scale (STRRS) scores (scale: 0 no relief to 6 complete relief). (NCT00402987)
Timeframe: 2 and 6 hours Post-First Dose

,,
Interventionscores on a scale (Least Squares Mean)
2 hours6 hours
Celecoxib 100mg (Pooled)2.29.9
Celecoxib 50mg/50mg2.610.6
Placebo1.35.3

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Treatment Failures on STRRS Questionnaire

Subjects were considered treatment failures if all of the STRRS scores were less than each individual's 'meaningful relief' scores. STRRS score ranges from 0=no relief to 6=complete relief. (NCT00402987)
Timeframe: 24 hours Post-First Dose

,,,
Interventionsubjects (Number)
Not treatment failuresTreatment failures
Celecoxib 100mg/50mg2024
Celecoxib 100mg/Placebo2718
Celecoxib 50mg/50mg4644
Placebo2366

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Treatment Satisfaction Questionnaire for Medication (TSQM vII)

11 questions scored on factors: effectiveness, side effects, convenience, overall satisfaction. TSQM vII scores range 0 to 100, with higher scores indicating a higher level of global satisfaction with treatment. (NCT00402987)
Timeframe: 24 hours or immediately prior to taking rescue medication

,,,
Interventionscores on a scale (Mean)
EffectivenessSide EffectsConvenienceGlobal Satisfaction
Celecoxib 100mg /Placebo40.696.773.047.8
Celecoxib 100mg/50mg34.397.969.342.2
Celecoxib 50mg/50mg41.596.377.249.1
Placebo26.198.671.336.0

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Time to Onset of Analgesia

Equal to time of perceptible pain relief when both perceptible pain relief and meaningful pain relief were experienced- the median time was not estimable thus the number of subjects with onset of analgesia within 2 hours of first dose is reported (NCT00402987)
Timeframe: Within 2 Hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg36
Celecoxib 100 mg (Pooled)34
Placebo15

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Number Needed to Treat (NNT) to Achieve at Least 50% of Maximum Total Pain Relief (TOTPAR) at 6 Hours Post-First Dose

NNT is number of subjects needed to treat to have one extra subject report a 50% or better pain relief over 6 hours based on maximum possible pain relief on Sore Throat Relief Rating Scale. Maximum TOTPAR over 6 hours is 36. If the subject TOTPAR is greater than or equal to 50% of the maximum TOTPAR then the subject has achieved >=50% TOTPAR. (NCT00402987)
Timeframe: 6 hours Post-First Dose

Interventionsubjects (Number)
Celecoxib 50mg/50mg18
Celecoxib 100mg (Pooled)19
Placebo7

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Sore Throat Pain Intensity Difference (SPID2) as Measured by Throat Soreness Scale (TSS) at 2 Hours Post-First Dose

SPID2 was calculated as the AUC of the Pain Intensity Difference (PID) scores. The Sore Throat PID was calculated as the difference between the pain intensity (TSS scale: 0=not sore to 10=very sore) at 2 hours post dose and at baseline. (NCT00402987)
Timeframe: 2 hour period Post-First Dose

Interventionunits on a scale * hours (Least Squares Mean)
Celecoxib 50mg/50mg2.4
Celecoxib 100mg (Pooled)2.0
Placebo1.0

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Sore Throat Relief Rating Scale (STRRS) - 'Moderate Relief' at 12 Hours Post-First Dose

Subjects Achieving at Least 'Moderate Relief' as Measured by STRRS (range: 0=no relief to 6=complete relief); Moderate relief is defined as STRRS = 3). (NCT00402987)
Timeframe: 12 hours

Interventionsubjects (Number)
Celecoxib 50mg/50mg21
Celecoxib 100 mg / Placebo13
Celecoxib 100mg / 50mg12
Placebo14

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Difficulty Swallowing Scale (DSS) Difference at Least 50% Gone at 12 Hours Post-First Dose

Number of Subjects with >= 50% Pain Intensity Difference (PID) on the DSS. The Difficulty Swallowing PID was calculated as the difference between the pain intensity (DSS scale: 0mm=not difficult, 100mm=very difficult) at 12 hours and at baseline. (NCT00402987)
Timeframe: At 12 Hours

Interventionsubjects (Number)
Celecoxib 50mg/50mg24
Celecoxib 100mg/Placebo12
Celecoxib 100mg/50mg10
Placebo12

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Difficulty Swallowing Scale (DSS) Difference at Least 50% Gone at 6 Hours Post-First Dose

Number of Subjects with >= 50% Pain Intensity Difference (PID) on the DSS. The Difficulty Swallowing PID was calculated as the difference between the pain intensity (DSS scale: 0mm=not difficult, 100mm=very difficult) at 6 hours and at baseline. (NCT00402987)
Timeframe: At 6 hours

Interventionsubjects (Number)
Celecoxib 50mg/50mg22
Celecoxib 100mg (Pooled)24
Placebo14

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Median Offset Time of No Perceptible Relief in Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Post-First Dose

Offset time is time of first no perceptible relief (STRRS score=0) with meaningful relief (score>0) at earlier time. STRRS score ranges from 0=no relief to 6=complete relief. (NCT00402987)
Timeframe: 24 Hours

Interventionhours (Median)
Celecoxib 50mg/50mg8.00
Celecoxib 100mg/Placebo8.00
Celecoxib 100mg/50mg8.00
Placebo10.00

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Median Onset Time of First Perceptible Relief in Subjects Who Achieved Their Own Level of 'Meaningful Relief' Within 6 Hours Post-First Dose

Perceptible Relief is score >0 on STRRS. Individual level of meaningful relief had to be reached within 6 hours. Meaningful Relief was achieved if Sore Throat Relief Rating Scale (STRRS)(range: 0=no relief to 6=complete relief)score at the end of the study was the same or higher than individually defined meaningful relief score during the study. (NCT00402987)
Timeframe: 24 Hours

Interventionhours (Median)
Celecoxib 50mg/50mg0.75
Celecoxib 100mg (Pooled)0.63
Placebo0.50

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Change From Baseline in Swollen Joint Count (SJC) at Week 1, 2, 4, 8 and 12

Participants were assessed for swollen joints using a 28-joint count comprised of left and right shoulders, elbows, wrists, proximal interphalangeal joints, metacarpophalangeal joints and knees. Artificial joints were not assessed. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionswollen joints (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 31)Change at Week 2 (n=34, 31)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib12.00-4.35-5.97-6.32-6.71-6.38
Placebo and Celecoxib11.49-3.18-2.74-3.45-2.79-3.80

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Change From Baseline in Patient's Global Assessment of Arthritis at Week 1, 2, 4, 8 and 12

Patient's global assessment of arthritic condition assessed all the ways participants' illness and health conditions affect them at the time of assessment. The response was scored on a 5-point scale: 1 = Very Good (Asymptomatic and no limitation of normal activities), 2 = Good (Mild symptoms and no limitation of normal activities), 3 = Fair (Moderate symptoms and limitation of some normal activities), 4 = Poor (Severe symptoms and inability to carry out most normal activities) and 5 = Very Poor (Very severe symptoms which are intolerable and inability to carry out all normal activities). (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionunits on a scale (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 31)Change at Week 2 (n=34, 31)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib3.24-0.48-0.61-0.68-0.46-0.57
Placebo and Celecoxib3.14-0.58-0.38-0.39-0.58-0.40

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Change From Baseline in Patient's Assessment of Arthritis Pain at Week 1, 2, 4, 8 and 12

Patient's assessment of arthritis pain was assessed using a 100 millimeter (mm) visual analogue scale (VAS) with range: 0 = no pain to 100 = worst possible pain. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionmm (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 30)Change at Week 2 (n=34, 32)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib54.74-11.33-9.50-14.12-12.04-21.43
Placebo and Celecoxib50.94-13.27-9.53-8.16-14.06-11.50

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Percentage of Participants Achieving American College of Rheumatology 20% (ACR20) Response at Week 12

ACR20 response: greater than or equal to (>=) 20 percent (%) improvement in tender joint count; >=20% improvement in swollen joint count; and >=20% improvement in at least 3 of 5 remaining ACR core measures: participant assessment of pain; participant global assessment of disease activity; physician global assessment of disease activity; self-assessed disability (disability index of the Health Assessment Questionnaire [HAQ]); and C-Reactive Protein (CRP). (NCT00424294)
Timeframe: Week 12

Interventionpercentage of participants (Number)
Placebo and Celecoxib31.43
CP-195543 and Celecoxib35.29

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Change From Baseline in Heart Rate Day 7, 14, 21, 28, 42, 56, 84 and 91

(NCT00424294)
Timeframe: Baseline, Day 7, 14, 21, 28, 42, 56, 84, 91

,
Interventionbeats per minute (Mean)
Baseline (n=35, 34)Change at Day 7 (n=33, 30)Change at Day 14 (n=5, 1)Change at Day 21 (n=0, 1)Change at Day 28 (n=1, 2)Change at Day 42 (n=4, 2)Change at Day 56 (n=0, 3)Change at Day 84 (n=27, 17)Change at Day 91 (n=3, 3)
CP-195543 and Celecoxib74.52.2-6.42.02.0-3.07.75.1-2.0
Placebo and Celecoxib74.3-1.0-3.0NA-2.03.3NA0.81.0

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Change From Baseline in Health Assessment Questionnaire-Disability Index (HAQ-DI) Score at Week 1, 2, 4, 8 and 12

Health Assessment Questionnaire-Disability Index (HAQ-DI): participant-reported assessment of ability to perform tasks in 8 categories of daily living activities: dress/groom; arise; eat; walk; reach; grip; hygiene; and common activities over past week. Each item scored on 4-point scale from 0 to 3: 0=no difficulty; 1=some difficulty; 2=much difficulty; 3=unable to do. Overall score was computed as the sum of domain scores and divided by the number of domains answered. Total possible score range 0-3, where 0 = least difficulty and 3 = extreme difficulty. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionunits on a scale (Mean)
Baseline (n=34, 34)Change at Week 1 (n=32, 30)Change at Week 2 (n=31, 29)Change at Week 4 (n=30, 25)Change at Week 8 (n=32, 24)Change at Week 12 (n=29, 20)
CP-195543 and Celecoxib1.65-0.18-0.24-0.29-0.30-0.44
Placebo and Celecoxib1.650.34-0.18-0.34-0.38-0.38

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Change From Baseline in Duration of Morning Stiffness at Week 1, 2, 4, 8 and 12

Duration of morning stiffness was defined as the time elapsed between the time participant woke up and was able to resume normal activities without stiffness in hours (duration was recorded in hours to the nearest quarter. For those participants with unrelenting stiffness, duration was recorded as 24 hours). (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionhour (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 31)Change at Week 2 (n=34, 31)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib3.22-0.61-1.34-1.51-1.03-1.65
Placebo and Celecoxib2.83-0.110.03-0.760.341.05

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Change From Baseline in Disease Activity Score Based on 28-Joints Count and C-Reactive Protein (3 Variables) (DAS28-3 [CRP]) at Week 1, 2, 4, 8 and 12

DAS28-3 (CRP) was calculated from the SJC and TJC using the 28 joints count and CRP. It was calculated as DAS28-3 (CRP) = 1.15 + 1.10 * ([0.56 * square root of TJC] + [0.28 * square root of SJC] + [0.36 * natural logarithm of {CRP+1}]). Total score range: 0 to 9.4, higher score indicated more disease activity. DAS28-3 (CRP) <= 3.2 implied low disease activity and >3.2 to 5.1 implied moderate to high disease activity, and DAS28-3 (CRP) <2.6 = remission. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionunits on a scale (Mean)
Baseline (n=34, 34)Change at Week 1 (n=32, 31)Change at Week 2 (n=32, 31)Change at Week 4 (n=29, 25)Change at Week 8 (n=32, 24)Change at Week 12 (n=29, 21)
CP-195543 and Celecoxib4.68-0.71-0.86-0.83-1.04-1.19
Placebo and Celecoxib4.78-0.65-0.56-0.82-0.84-0.98

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Change From Baseline in Physician's Global Assessment of Arthritis at Week 1, 2, 4, 8 and 12

Investigator assessed overall appearance of arthritis at the time of the visit. The response was scored on a 5-point scale: 1 = Very Good (Asymptomatic and no limitation of normal activities), 2 = Good (Mild symptoms and no limitation of normal activities), 3 = Fair (Moderate symptoms and limitation of some normal activities), 4 = Poor (Severe symptoms and inability to carry out most normal activities) and 5 = Very Poor (Very severe symptoms which are intolerable and inability to carry out all normal activities). (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionunits on a scale (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 31)Change at Week 2 (n=34, 31)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib3.32-0.58-0.58-0.60-0.71-0.67
Placebo and Celecoxib3.37-0.76-0.74-0.71-0.67-0.67

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Change From Baseline in C-Reactive Protein (CRP) at Week 1, 2, 4, 8 and 12

The test for CRP is a laboratory measurement for evaluation of an acute phase reactant of inflammation through the use of an ultrasensitive assay. A decrease in the level of CRP indicates reduction in inflammation and therefore improvement. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventionmilligram per deciliter (mg/dL) (Mean)
Baseline (n=34, 34)Change at Week 1 (n=32, 31)Change at Week 2 (n=32, 31)Change at Week 4 (n=29, 25)Change at Week 8 (n=32, 24)Change at Week 12 (n=29, 21)
CP-195543 and Celecoxib1.360.150.610.160.410.03
Placebo and Celecoxib0.93-0.060.080.670.150.60

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Number of Participants Who Withdrew From Study Due to Lack of Efficacy

(NCT00424294)
Timeframe: Baseline up to Week 12

Interventionparticipants (Number)
Placebo and Celecoxib2
CP-195543 and Celecoxib1

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Number of Participants With Clinical Laboratory Abnormalities

Following parameters were analyzed for laboratory examination: hematology (hemoglobin, hematocrit, red blood cell count, platelet count, white blood cell count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes); liver function (aspartate aminotransferase, alanine aminotransferase, total bilirubin, lactate dehydrogenase, alkaline phosphatase, albumin, total protein); renal function (blood urea nitrogen, creatinine, uric acid); electrolytes (sodium, potassium, chloride, calcium, phosphate, bicarbonate); clinical chemistry (glucose, creatine kinase); immunology (CRP); urinalysis (dipstick [urine specific gravity, decimal logarithm of reciprocal of hydrogen ion activity {pH} of urine, glucose, protein, blood, ketones, bilirubin], microscopy [urine RBC, WBC, urate crystals, calcium, oxalate, miscellaneous [urine mucus and leucocytes]). (NCT00424294)
Timeframe: Baseline up to Week 13

Interventionparticipants (Number)
Placebo and Celecoxib15
CP-195543 and Celecoxib14

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Percentage of Participants Achieving American College of Rheumatology 70% (ACR70) Response

ACR70 response: >=70% improvement in tender joint count; >=70% improvement in swollen joint count; and >=70% improvement in at least 3 of 5 remaining ACR core measures: participant assessment of pain; participant global assessment of disease activity; physician global assessment of disease activity; self-assessed disability (disability index of the Health Assessment Questionnaire [HAQ]); and C-Reactive Protein (CRP). (NCT00424294)
Timeframe: Week 1, 2, 4, 8, 12

,
Interventionpercentage of participants (Number)
Week 1Week 2Week 4Week 8Week 12
CP-195543 and Celecoxib0.00.00.00.02.94
Placebo and Celecoxib0.00.00.00.02.86

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Percentage of Participants Achieving American College of Rheumatology 50% (ACR50) Response

ACR50 response: >=50% improvement in tender joint count; >=50% improvement in swollen joint count; and >=50% improvement in at least 3 of 5 remaining ACR core measures: participant assessment of pain; participant global assessment of disease activity; physician global assessment of disease activity; self-assessed disability (disability index of the Health Assessment Questionnaire [HAQ]); and C-Reactive Protein (CRP). (NCT00424294)
Timeframe: Week 1, 2, 4, 8, 12

,
Interventionpercentage of participants (Number)
Week 1Week 2Week 4Week 8Week 12
CP-195543 and Celecoxib0.00.02.9411.7614.71
Placebo and Celecoxib0.00.08.575.718.57

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Percentage of Participants Achieving American College of Rheumatology 20% (ACR20) Response at Week 1, 2, 4 and 8

ACR20 response: >=20% improvement in tender joint count; >=20% improvement in swollen joint count; and >=20% improvement in at least 3 of 5 remaining ACR core measures: participant assessment of pain; participant global assessment of disease activity; physician global assessment of disease activity; self-assessed disability (disability index of the Health Assessment Questionnaire [HAQ]); and C-Reactive Protein (CRP). (NCT00424294)
Timeframe: Week 1, 2, 4, 8

,
Interventionpercentage of participants (Number)
Week 1Week 2Week 4Week 8
CP-195543 and Celecoxib23.5335.2941.1838.24
Placebo and Celecoxib31.4328.5728.5725.71

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Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence attributed to study drug in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pretreatment state. (NCT00424294)
Timeframe: Baseline up to 28 days after last dose

,
Interventionparticipants (Number)
AEsSAEs
CP-195543 and Celecoxib312
Placebo and Celecoxib291

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Number of Participants With Categorical Vital Signs Data

Number of participants with maximum increase from Baseline in sitting SBP and DBP of greater than or equal to 30 mmHg at Week 12 was reported. (NCT00424294)
Timeframe: Baseline, Week 12

,
Interventionparticipants (Number)
SBP: >=30 mmHg IncreaseDBP: >=30 mmHg Increase
CP-195543 and Celecoxib13
Placebo and Celecoxib11

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Number of Participants With Abnormal Electrocardiogram (ECG)

Criteria for potential clinical concern in ECG parameters: Maximum corrected QT interval (QTc) in range of 450 to less than 480 millisecond (msec), Maximum QTcB interval (Bazett's Correction) (msec) in range of 450 to less than 480 msec, Maximum QTcF interval (Fridericia's Correction) in range of 450 to less than 480 msec, maximum QTc interval increase from baseline in range of 30 to less than 60 msec and >=60 msec. (NCT00424294)
Timeframe: Baseline up to Week 12

,
Interventionparticipants (Number)
Maximum QTc Interval (msec)Maximum QTcB Interval (Bazett's Correction)Maximum QTcF Interval (Fridericia's Correction)QTcF interval 30 to <60 msec IncreaseQTcF interval >=60 msec Increase
CP-195543 and Celecoxib79220
Placebo and Celecoxib03010

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Number of Adverse Events by Severity

An AE was any untoward medical occurrence attributed to study drug in a participant who received study drug. AEs are classified according to the severity in 3 categories a) mild - AEs does not interfere with participant's usual function b) moderate - AEs interferes to some extent with participant's usual function c) severe - AEs interferes significantly with participant's usual function. (NCT00424294)
Timeframe: Baseline up to 28 days after last dose

,
Interventionadverse events (Number)
MildModerateSevere
CP-195543 and Celecoxib41255
Placebo and Celecoxib40260

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Change From Baseline in Tender/Painful Joint Count (TJC) at Week 1, 2, 4, 8 and 12

Participants were assessed for tender/painful joints using a 28-joint count comprised of left and right shoulders, elbows, wrists, proximal interphalangeal joints, metacarpophalangeal joints and knees. Artificial joints were not assessed. (NCT00424294)
Timeframe: Baseline, Week 1, 2, 4, 8, 12

,
Interventiontender/painful joints (Mean)
Baseline (n=35, 34)Change at Week 1 (n=33, 31)Change at Week 2 (n=34, 31)Change at Week 4 (n=31, 25)Change at Week 8 (n=33, 24)Change at Week 12 (n=30, 21)
CP-195543 and Celecoxib13.74-4.68-6.13-5.04-6.00-5.95
Placebo and Celecoxib15.54-4.45-3.82-5.68-5.15-5.67

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Change From Baseline in Systolic and Diastolic Blood Pressure at Day 7, 14, 21, 28, 42, 56, 84 and 91

Systolic blood pressure (SBP) and diastolic blood pressure (DBP) were evaluated in sitting position. (NCT00424294)
Timeframe: Baseline, Day 7, 14, 21, 28, 42, 56, 84, 91

,
Interventionmillimeter of mercury (mmHg) (Mean)
Baseline: SBP (n=35, 34)Change at Day 7: SBP (n=33, 30)Change at Day 14: SBP (n=1, 5)Change at Day 21: SBP (n=0, 1)Change at Day 28: SBP (n=1, 2)Change at Day 42: SBP (n=4, 2)Change at Day 56: SBP (n=0, 3)Change at Day 84: SBP (n=27, 17)Change at Day 91: SBP (n=3, 3)Baseline: DBP (n=35, 34)Change at Day 7: DBP (n=33, 30)Change at Day 14: DBP (n=1, 5)Change at Day 21: DBP (n=0, 1)Change at Day 28: DBP (n=1, 2)Change at Day 42: DBP (n=4, 2)Change at Day 56: DBP (n=0, 3)Change at Day 84: DBP (n=27, 17)Change at Day 91: DBP (n=3, 3)
CP-195543 and Celecoxib124.60.53.20.00.00.0-2.06.8-15.775.81.41.216.08.0-2.0-4.0-0.5-5.3
Placebo and Celecoxib123.7-0.25.0NA18.03.3NA4.73.377.9-1.3-1.0NA-4.0-1.8NA1.42.7

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Index

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Pain severity index is the average of the pain severity questions 1 to 4. Scale: 0 = no pain to 10 = pain as bad as you can imagine" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib4.242.841.37
nsNSAIDs4.483.261.68

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 1

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q1: Subject response to 'describe your pain at its worst in the last 24 hours'. Scale: 0 = no pain to 10 = pain as bad as you can imagine" (NCT00446797)
Timeframe: Days 1, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib5.713.812.08
nsNSAIDs5.904.442.38

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 2

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q2: Subject response to 'describe your pain at its least in the last 24 hours'. Scale: 0 = no pain to 10 = pain as bad as you can imagine" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 133, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib3.252.070.83
nsNSAIDs3.362.401.16

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 3

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q3: Subject response to 'describe your pain on the average'. Scale: 0 = no pain to 10 = pain as bad as you can imagine" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib4.342.901.41
nsNSAIDs4.413.261.74

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Severity Question 4

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q4: Subject response to 'how much pain you have right now'. Scale: 0 = no pain to 10 = pain as bad as you can imagine" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N =135, 131)Day 7 (N = 133, 125)
Celecoxib3.642.581.14
nsNSAIDs4.232.921.43

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Number of Subjects Responding (Improving) - MITT Population

The number of subjects showing a response: a decrease of at least 20 mm (that is improvement) on the pain visual analog scale (VAS) scale (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionparticipants (Number)
Day 2 - response (N=134, 133)Day 2 - no responseDay 3 - response (N=135, 131)Day 3 - no responseDay 7 - response (N=133, 125)Day 7 - no response
Celecoxib9143124111294
nsNSAIDs7954116151205

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Pain Relief - MITT Population

"Subject's response to the statement My relief from starting pain is. Scale from 0 = None to 4 = Complete." (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionparticipants (Number)
Day 2 - None (N=135, 132)Day 2 - A littleDay 2 - SomeDay 2 - A lotDay 2 -CompleteDay 3 - None (N=135, 131)Day 3 - A littleDay 3 - SomeDay 3 - A lotDay 3 -CompleteDay 7 - None (N=133, 125)Day 7 - A littleDay 7 - SomeDay 7 - A lotDay 7 -Complete
Celecoxib82549521015338431677742
nsNSAIDs533524201214660313158026

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Physician Global Assessment of Ankle Injury

Investigator evaluation of overall severity of ankle injury. Scale: 5 point from 1 = Very mild (very mild signs and symptoms of ankle sprain) to 5 =Very severe (very severe signs and symptoms of ankle sprain) (NCT00446797)
Timeframe: Days 3 and 7

,
Interventionparticipants (Number)
Day 3 - very mild (N=134, 131)Day 3 - mildDay 3 - moderateDay 3 - severeDay 3 - very severeDay 7 - very mild (N=132, 125)Day 7 - mildDay 7 - moderateDay 7 - severeDay 7 - very severe
Celecoxib207140218738700
nsNSAIDs127938207047710

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Subject's Global Assessment of Ankle Injury

"Subject response to question: Considering all the ways your ankle injury affects you, how are you doing today? Scale: 5 point from 1 = very good (no symptoms and no limitation of normal activities) to 5 = very poor (very severe symptoms which are intolerable and inability to carry out all normal activities)." (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionparticipants (Number)
Day 2 - Very good (no symptoms) (N=135, 133)Day 2 - Good (mild symptoms)Day 2 - Fair (moderate symptoms)Day 2 - Poor (severe symptoms)Day 2- Very poor (very severe symptoms)Day 3 - Very good (no symptoms) (N=135, 131)Day 3 - Good (mild symptoms)Day 3 - Fair (moderate symptoms)Day 3 - Poor (severe symptoms)Day 3 - Very poor (very severe symptoms)Day 7 - Very good (no symptoms) (N=133, 125)Day 7 - Good (mild symptoms)Day 7 - Fair (moderate symptoms)Day 7 - Poor (severe symptoms)Day 7 - Very poor (very severe symptoms)
Celecoxib14076171868545053611720
nsNSAIDs13180192655637037632140

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5G

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5G: Subject response to 'how, during the past 24 hours, pain has interfered with your enjoyment of life'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib3.332.131.07
nsNSAIDs2.992.061.10

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Subject Assessment of Normal Function / Activity

"Subject response to question: How does your ankle injury affect your walking and normal activity? Scale from 1 = Normal walking/activity and no pain to 5 = Severely restricted walking due to pain and can't resume normal activities (normal activities defined as all activity that a subject did on a routine basis, including work and recreation)" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionparticipants (Number)
Day 2 - normal no pain (N =135, 133)Day 2 - normal with painDay 2 - mildly restrictedDay 2 - moderately restrictedDay 2 - severely restrictedDay 3 - normal no pain (N = 135, 131)Day 3 - normal with painDay 3 - mildly restrictedDay 3 - moderately restrictedDay 3 - severely restrictedDay 7 - normal no pain (N = 133, 125)Day 7 - normal with painDay 7 - mildly restrictedDay 7 - moderately restrictedDay 7 - severely restricted
Celecoxib54059191218524914262551141
nsNSAIDs230553971346571144368833

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Index

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~The pain interference index is the average of pain interference questions 5A to 5G. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib4.072.791.28
nsNSAIDs4.012.831.33

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Change From Baseline at Day 3 in Pain Visual Analog Scale (VAS) - Per Protocol Population

"Assessment of ankle pain by VAS: 100 mm horizontal line with left end being No Pain & right end being Worst Possible Pain. Participants drew vertical line on horizontal scale to best reflect current pain on full weight bearing of injured ankle. Distance from left end of line to mark. Change: mean score at day 3 minus mean score at baseline" (NCT00446797)
Timeframe: Baseline and day 3

Interventionscores on a scale (Mean)
Celecoxib-44.88
nsNSAIDs-40.76

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Change From Baseline in Pain Visual Analog Scale (VAS) - Modified Intent to Treat Population

"Assessment of ankle pain by VAS: 100 mm horizontal line, left end being No Pain & right end being Worst Possible Pain. Participants drew vertical line on horizontal scale to best reflect current pain on full weight bearing of injured ankle. Distance from left end of line to mark. Change: mean score at observation minus mean score at baseline" (NCT00446797)
Timeframe: Baseline and days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2Day 3Day 7
Celecoxib-29.25-44.87-61.17
nsNSAIDs-25.98-40.75-57.89

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5A

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5A: Subject response to 'how, during the past 24 hours, pain has interfered with your general activity. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib5.403.651.78
nsNSAIDs5.374.071.90

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5B

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5B: Subject response to 'how, during the past 24 hours, pain has interfered with your mood'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib3.722.431.17
nsNSAIDs3.642.381.26

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5C

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5C: Subject response to 'how, during the past 24 hours, pain has interfered with your walking ability'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib5.103.581.65
nsNSAIDs5.113.691.62

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5D

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5D: Subject response to 'how, during the past 24 hours, pain has interfered with your normal work (work outside the home and housework)'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib5.294.041.84
nsNSAIDs5.394.041.87

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5E

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5E: Subject response to 'how, during the past 24 hours, pain has interfered with your relations with other people'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib2.701.810.80
nsNSAIDs2.671.690.78

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Modified Brief Pain Inventory Short Form (m-BPI-sf) - Pain Interference Question 5F

"m-BPI-sf questionnaire assessed pain severity and pain interference with functional activities during the 24 hour follow-up period.~Q5F: Subject response to 'how, during the past 24 hours, pain has interfered with your sleep'. Scale: 0 = does not interfere to 10 = completely interferes" (NCT00446797)
Timeframe: Days 2, 3 and 7

,
Interventionscores on a scale (Mean)
Day 2 (N = 134, 133)Day 3 (N = 135, 131)Day 7 (N = 133, 125)
Celecoxib2.971.900.68
nsNSAIDs2.871.860.82

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One Year Survival Rate

Percent of patients who remain alive one year from on-study date (NCT00466505)
Timeframe: 1 year from on-study date

InterventionPercentage of participants (Number)
Therapeutic Intervention17.6

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Urinary PGE-M : Treatment Cycle 2

Measurement in ng/mL of a stable metabolite of prostaglandin E2 (PGE-M) in urine during treatment cycle 2 (NCT00466505)
Timeframe: on-study week 9

Interventionng/mL (Mean)
Stable or PR (n=6)Progressive Disease (n=4)
Therapeutic Intervention28.4229.76

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Urinary PGE-M : Treatment Cycle 1

Measurement in ng/mL of a stable metabolite of prostaglandin E2 (PGE-M) in urine during treatment cycle 1 (NCT00466505)
Timeframe: on-study week 5

Interventionng/mL (Mean)
Stable or PR (n=6)Progressive Disease (n=11)
Therapeutic Intervention30.4221.94

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Serum TGF-alpha: Treatment Cycle 2

Measurement in ng/mL of tumor growth factor-alpha (TGF-alpha) in serum samples during treatment cycle 2 (NCT00466505)
Timeframe: on-study week 9

Interventionng/mL (Mean)
Stable or PR (n=6)Progressive Disease (n=4)
Therapeutic Intervention48.0249.95

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Patient Response to Treatment

Number of patients in each response category according to RECIST criteria: Progressive disease (PD): >=20% increase in sum of longest diameter (LD) of target lesion(s), taking as reference smallest sum LD recorded since treatment started. Complete response (CR): disappearance of all target lesions. Partial response (PR): >=30% decrease in sum of LD of target lesion(s), taking as reference baseline sum LD. Stable disease (SD): neither sufficient shrinkage to qualify as PR nor sufficient increase to qualify as PD. (NCT00466505)
Timeframe: On study date to off study date in this study with median 9.76 months

Interventionparticipants (Number)
Partial ResponseProgressive DiseaseStable DiseaseUnknown
Therapeutic Intervention2744

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Number of Patients With Each Worst-grade Toxicity Response

Number of patients with worst-grade toxicity response of each grade (grade 1 to 5) following NCI Common Toxicity Criteria, with grade 1=mild adverse event; 2=moderate adverse event; 3=severe and undesirable adverse event; 4=life-threatening or disabling adverse event; 5=death. (NCT00466505)
Timeframe: On study date to off study date in this study with median 9.76 months

Interventionpatients (Number)
No. of patients with worst-grade toxicity of 1No. of patients with worst-grade toxicity of 2No. of patients with worst-grade toxicity of 3No. of patients with worst-grade toxicity of 4No. of patients with worst-grade toxicity of 5
Therapeutic Intervention00110

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Progression-free Survival (PFS)

Number of days from study enrollment to evidence of progressive disease radiographically, with progression defined under RECIST criteria as at least 20% increase in sum of longest diameter of target lesions (NCT00466505)
Timeframe: On study date to off study date in this study with median 9.76 months

InterventionDays (Median)
Therapeutic Intervention55

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Overall Survival

Median survival time in months, from on-study date to date of death (NCT00466505)
Timeframe: On study date to off study date in this study with median 9.76 months

InterventionMonths (Median)
Therapeutic Intervention8.54

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Serum TGF-alpha: Treatment Cycle 1

Measurement in ng/mL of tumor growth factor-alpha (TGF-alpha) in serum samples during treatment cycle 1 (NCT00466505)
Timeframe: on-study week 5

Interventionng/mL (Mean)
Stable or PR (n=5)Progressive Disease (n=10)
Therapeutic Intervention26.3825.90

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Progression-free Survival - Low PGEM

Estimated using the product-limit method of Kaplan and Meier.Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of one or more new lesions. (NCT00499655)
Timeframe: Until disease progression, up to 5 years.

InterventionMonths (Median)
ErlotinibPlacebo5.4
ErlotinibCelecoxib6.8

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Number of Participants With Overall Response

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR (NCT00499655)
Timeframe: 16 weeks post start of treatment

InterventionParticipants (Count of Participants)
ErlotinibPlacebo17
ErlotinibCelecoxib12

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Progression-free Survival

Estimated using the product-limit method of Kaplan and Meier.Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of one or more new lesions. (NCT00499655)
Timeframe: Until disease progression, up to 5 years.

InterventionMonths (Median)
ErlotinibPlacebo3.5
ErlotinibCelecoxib5.4

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Progression-free Survival - EGRF

Estimated using the product-limit method of Kaplan and Meier.Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of one or more new lesions. (NCT00499655)
Timeframe: Until disease progression, up to 5 years.

InterventionMonths (Median)
ErlotinibPlacebo1.8
ErlotinibCelecoxib3.2

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Progression-free Survival - Elevated PGEM

Estimated using the product-limit method of Kaplan and Meier.Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of one or more new lesions. (NCT00499655)
Timeframe: Until disease progression, up to 5 years.

InterventionMonths (Median)
ErlotinibPlacebo2.2
ErlotinibCelecoxib5.4

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13-HODE Colonic Tissue Levels

13-HODE colonic tissue levels measured by Liquid chromatography and tandem mass spectrometry measurements (LC/MS/MS) in colorectal normal and polyp tissues (NCT00503035)
Timeframe: Baseline to post 6 months of celecoxib treatment

Interventionng/mg tissue protein (Mean)
polyps before celecoxib treatmentpolyps after celecoxib treatmentNormal: before celecoxib treatmentNormal: after celecoxib treatment
Celecoxib14.5618.8323.0220.03

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PGE2 Colonic Tissue Levels

PGE2 colonic tissue levels measured by Liquid chromatography and tandem mass spectrometry measurements (LC/MS/MS) in colorectal normal and polyp tissues (NCT00503035)
Timeframe: at the baseline colonoscopy (or sigmoidoscopy in patients who had undergone colectomy) before the initiation of celecoxib, and the follow-up colonoscopy or sigmoidoscopy was performed after celecoxib treatment (month 6)

Interventionng/mg tissue protein (Mean)
Polyps: before celecoxib treatmentPolyps: after celecoxib treatmentNormal: before celecoxib treatmentNormal: after celecoxib treatment
Celecoxib14.7120.6221.4824.99

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6 Month Progression-free Survival for Participants With Glioblastoma

Progression-free Survival (PFS) at 6 months measured as percentage of participants that are alive and progression-free at 6 months (glioblastoma multiforme). A combination of neurological examination and MRI brain scan used to define overall response or progression. (NCT00504660)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Participants With Glioblastoma Multiforme14

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12 Month-progression-free Survival for Participants With Anaplastic Tumors

Progression-free Survival (PFS) at 12 months measured as percentage of participants that are alive and progression-free at 12 months (anaplastic tumors). A combination of neurological examination and MRI brain scan used to define overall response or progression. (NCT00504660)
Timeframe: 12 months

Interventionpercentage of participants (Number)
Participants With Recurrent Anaplastic Glioma44

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Time to Progression

Estimated probable duration from on-study date to date of disease progression, using the Kaplan-Meier method with censoring (see analysis population description for additional details). Disease progression is defined under RECIST v1.1 as >=20% increase in sum of longest diameters of target lesions, unequivocal progression of non-target lesions, or appearance of new lesions. (NCT00520845)
Timeframe: 2 years from date of registration

Interventiondays (Median)
Treatment Arm89

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Overall Response Rate

Overall response rate is measured by complete response + partial response. Number of patients in each response category, per RECIST v1.1, summarized as follows for target lesion criteria (see RECIST v1.1 for additional details): complete response (CR),disappearance of target lesions; partial response (PR), >=30% decrease in sum of longest diameter of target lesions; progressive disease (PD), >=20% increase in sum of LD of target lesions or appearance of new lesions; stable disease (SD), insufficient change in target lesions or new lesions to qualify as either PD or SD. Patients are categorized according to the best response achieved prior to occurrence of progressive disease, where best response hierarchy is CR>PR>SD>PD. (NCT00520845)
Timeframe: On-treatment date to date of disease progression (assessed at 6 weeks up to 2 years)

Interventionparticipants (Number)
Treatment Arm0

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Median Survival

Estimated probable duration of life from on-study date to date of death from any cause, using the Kaplan-Meier method with censoring (see analysis population description for additional details) (NCT00520845)
Timeframe: 2 years from date of registration

Interventiondays (Median)
Treatment Arm184

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Overall Response

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR (NCT00538031)
Timeframe: Up to 3 years

InterventionParticipants (Count of Participants)
Arm I (Cyclophosphamide Alone)1
Arm II (Cyclophosphamide + Celecoxib)1

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Overall Survival

Estimated using the product-limit method of Kaplan and Meier. From time of initial treatment to death from any cause. (NCT00538031)
Timeframe: Up to 5 years

InterventionMonths (Median)
Arm I (Cyclophosphamide Alone)9.69
Arm II (Cyclophosphamide + Celecoxib)12.55

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Time to Treatment Failure

"Estimated using the product-limit method of Kaplan and Meier. Time to treatment failure is defined as the time from initial treatment to discontinuation of treatment for any reason, including progression of disease, treatment toxicity, and death.~Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions." (NCT00538031)
Timeframe: Up to 3 years

InterventionMonths (Median)
Arm I (Cyclophosphamide Alone)1.84
Arm II (Cyclophosphamide + Celecoxib)1.92

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Number of Participants With Pre-specified Gastrointestinal (GI) Adverse Events

The gastrointestinal tolerability was measured by incidence of moderate or severe GI adverse events (nausea, abdominal pain and dyspepsia) (NCT00549549)
Timeframe: Baseline to Day 14/Early Termination

InterventionParticipants (Number)
Celecoxib 50 mg1
Celecoxib 400/200 mg0
Celecoxib 800/400 mg2
Indomethacin 50 mg3

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Participant's Assessment of Pain Intensity for the Average Pain Intensity at Baseline

The participant's assessment of pain was assessed by completion of the following 5 point scale: My pain has been: None (0), Mild (1), Moderate, (2), Severe (3), and Extreme (4). (NCT00549549)
Timeframe: Baseline

InterventionUnits on a scale (Mean)
Celecoxib 50 mg3.03
Celecoxib 400/200 mg2.73
Celecoxib 800/400 mg2.84
Indomethacin 50 mg2.83

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Participants Global Evaluation of Study Medication Score

"The participant rated the study medication that they received during the study by completing the following question:~How would you rate the study medication you received for pain? 4=Excellent, 3=Good, 2=Fair, 1=Poor" (NCT00549549)
Timeframe: Day 9

InterventionScores on a scale (Mean)
Celecoxib 50 mg3.04
Celecoxib 400/200 mg3.11
Celecoxib 800/400 mg3.27
Indomethacin 50 mg3.33

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Change From Baseline in Patient's Assessment of Pain Intensity

The Patient's assessment of pain for the prior 24 hours was assessed by completion of the following 5 point scale: My pain over the past 24 hours has been: None (0), Mild (1), Moderate, (2), Severe (3), and Extreme (4). (NCT00549549)
Timeframe: Baseline, Day 2 to Day 13

,,,
InterventionScores on a scale (Mean)
BaselineChange at Day 1Change at Day 2Change at Day 3Change at Day 4Change at Day 5Change at Day 6Change at Day 7Change at Day 8Change at Day 9Change at Day 10Change at Day 11Change at Day 12Change at Day 13/Early termination
Celecoxib 400/200 mg2.73-0.85-1.23-1.42-1.60-1.67-1.84-1.90-1.95-1.96-1.99-1.94-1.95-1.95
Celecoxib 50 mg3.03-0.65-1.14-1.32-1.52-1.52-1.68-1.79-1.88-1.86-1.90-1.89-1.93-1.91
Celecoxib 800/400 mg2.84-1.06-1.51-1.78-1.96-2.05-2.12-2.29-2.30-2.24-2.23-2.22-2.27-2.27
Indomethacin 50 mg2.83-1.10-1.62-1.84-2.02-2.04-2.11-2.15-2.16-2.19-2.17-2.15-2.07-1.98

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Change From Baseline in Patient's Assessment of Pain Intensity on Day 1

The patient's assessment of pain was assessed by completion of the following 5 point scale: my pain at this time is none (0), mild (1), moderate, (2), severe (3), and extreme (4). (NCT00549549)
Timeframe: Baseline, 2, 4, 8, 12 hours postdose Day 1, Day 2 (24 hours and 32 hours post first dose)

,,,
InterventionScores on a scale (Mean)
BaselineChange at Day 1, 2 HRChange at Day 1, 4 HRChange at Day 1, 8 HRChange at Day 1, 12 HRChange at Day 2, 0 HRChange at Day 2, 8 HR
Celecoxib 400/200 mg2.73-0.28-0.54-0.58-0.75-0.98-1.07
Celecoxib 50 mg3.03-0.32-0.53-0.64-0.73-0.93-1.08
Celecoxib 800/400 mg2.84-0.45-0.70-0.87-1.02-1.15-1.31
Indomethacin 50 mg2.83-0.57-0.81-0.98-1.09-1.26-1.46

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Change From Baseline in Physician's Assessment of the Index Joint on Days 5, 9, and 14/Early Termination: Swelling

Swelling was assessed using a 4 point scale with the following ratings: none (0), palpable (1), visible (2), and bulging beyond joint margins (3) (NCT00549549)
Timeframe: Baseline, Days 5, 9 and 14/Early Termination

,,,
InterventionScores on a scale (Mean)
BaselineChange at Day 5Change at Day 9Change at Day 14/Early Termination
Celecoxib 400/200 mg2.08-1.21-1.54-1.63
Celecoxib 50 mg2.16-1.22-1.47-1.55
Celecoxib 800/400 mg2.09-1.27-1.62-1.78
Indomethacin 50 mg2.01-1.20-1.58-1.58

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Change From Baseline in Physician's Assessment of the Index Joint on Days 5, 9, and 14/Early Termination: Tenderness

Tenderness was assessed on the basis of palpation or passive motion using a 4 point scale with the following ratings: the patient had no tenderness (0), the patient complained of pain (1), the patient complained of pain and winced (2) and the patient complained of pain, winced, and withdrew (3). (NCT00549549)
Timeframe: Baseline, Day 5, Day 9, and Day 14/Early Termination

,,,
InterventionScores on a scale (Mean)
BaselineChange at Day 5Change at Day 9Change at Day 14/Early Termination
Celecoxib 400/200 mg2.15-1.39-1.64-1.66
Celecoxib 50 mg2.39-1.44-1.75-1.74
Celecoxib 800/400 mg2.26-1.58-1.84-1.94
Indomethacin 50 mg2.13-1.52-1.65-1.64

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Change From Baseline in Time Weighted Average of Patient's Assessment of Pain Intensity Over 8, 12, and 24 Hours

Time weighted average over 8 (TWA-8), 12 (TWA-12) and 24 (TWA-24) hours post first dose of study medication on Day 1. Positive TWA values represent a reduction in pain intensity (NCT00549549)
Timeframe: Baseline, 8, 12, and 24 hours post first dose

,,,
InterventionScores on a scale (Mean)
BaselineChange at 8 HRChange at 12 HRChange at 24 HR
Celecoxib 400/200 mg2.730.420.500.68
Celecoxib 50 mg3.030.440.520.67
Celecoxib 800/400 mg2.840.590.710.89
Indomethacin 50 mg2.830.690.810.99

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Change From Baseline to Day 2 in Patient's Assessment of Pain Intensity

The Patient's Pain Intensity in the Index Joint for the prior 24 hours was assessed by completion of the following 5 point scale: My pain over the past 24 hours has been: None (0), Mild (1), Moderate (2), Severe (3), or Extreme (4). (NCT00549549)
Timeframe: Baseline and Day 2

,,,
InterventionScores on a scale (Mean)
BaselineChange at Day 2
Celecoxib 400/200 mg2.73-1.23
Celecoxib 50 mg3.03-1.14
Celecoxib 800/400 mg2.84-1.51
Indomethacin 50 mg2.83-1.62

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Number of Participants With ≥30% and ≥50% Reduction From Baseline to Day 2 in Patient's Assessment of Pain Intensity

The Patient's assessment of pain was assessed by completion of the following 5 point scale: My pain over the past 24 hours has been: None (0), Mild (1), Moderate, (2), Severe (3), and Extreme (4). (NCT00549549)
Timeframe: Baseline, Day 2

,,,
InterventionParticipants (Number)
Reduction in Pain Intensity >= 30%Reduction in Pain Intensity >= 50%
Celecoxib 400/200 mg6957
Celecoxib 50 mg5843
Celecoxib 800/400 mg7563
Indomethacin 50 mg8271

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Number of Participants With Redness Present According to Physician's Assessment of the Index Joint on Day 5, Day 9, and Day 14/Early Termination

Redness was assessed by the physician as present or absent. (NCT00549549)
Timeframe: Baseline, Day 5, Day 9 and Day 14/Early Termination

,,,
InterventionParticipants (Number)
BaselineDay 5Day 9Day 14/Early termination
Celecoxib 400/200 mg88291515
Celecoxib 50 mg84271215
Celecoxib 800/400 mg7926137
Indomethacin 50 mg85231113

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Number of Participants With Warmth Present According to Physician's Assessment of the Index Joint on Day 5, Day 9, and Day 14

Warmth was assessed by the physician as present or absent. (NCT00549549)
Timeframe: Baseline, Day 5, Day 9 and Day 14

,,,
InterventionParticipants (Number)
BaselineDay 5Day 9DAY 14/E_TERM
Celecoxib 400/200 mg911687
Celecoxib 50 mg89251319
Celecoxib 800/400 mg9122911
Indomethacin 50 mg88211115

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Percentage Change From Baseline in the Patient's Assessment of Pain Intensity for the Average Pain Intensity on Days 2-4, Days 2-8 and Days 2-13

The participant's assessment of pain was assessed by completion of the following 5 point scale: My change in pain has been: None (0), Mild (1), Moderate, (2), Severe (3), and Extreme (4). Average change over days was calculated by taking the change from Baseline to the average Pain Intensity score over the days for each patient. (NCT00549549)
Timeframe: Baseline to Day 13

,,,
InterventionPercentage change (Mean)
Average change over days 2 - 4Average change over days 2 - 8Average change over days 2 - 13
Celecoxib 400/200 mg-53.15-61.83-66.26
Celecoxib 50 mg-44.13-51.36-56.11
Celecoxib 800/400 mg-60.11-69.41-73.59
Indomethacin 50 mg2.83-70.05-72.35

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Number of Participants With Withdrawal From Treatment Due to Lack of Efficacy

Withdrawal due to lack of efficacy was assessed from Days 1 to 8 (NCT00549549)
Timeframe: Day 1 to Day 8

,,,
InterventionParticipants (Number)
Day 1Any time during treatmentAny time during study
Celecoxib 400/200 mg189
Celecoxib 50 mg21011
Celecoxib 800/400 mg045
Indomethacin 50 mg034

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Number of Participants With Moderate or Severe Central Nervous System (CNS) Adverse Events

The pre-specfied CNS AEs were headache, nausea, dizziness, vertigo, vomiting and somnolence. (NCT00549549)
Timeframe: Baseline to Day 14/Early Termination

InterventionParticipants (Number)
Celecoxib 50 mg3
Celecoxib 400/200 mg2
Celecoxib 800/400 mg1
Indomethacin 50 mg5

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Maintenance of Response Following Discontinuation of Celecoxib

Percent of patients who responded to celecoxib with increase in papilloma growth rate of no greater than 0.01 at end of second treatment period compared to growth rate at end of first treatment period. (NCT00571701)
Timeframe: End of first treatment period (month 12) to end of second treatment period (month 24)

Interventionpercent of patients (Number)
Celecoxib Responders-maintained100

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Effect of Juvenile Versus Adult Disease Onset on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%.

Percent of juvenile versus adult onset patients with reduction in papilloma growth rate greater than 50% during the last 3 months of first treatment period compared to baseline. (NCT00571701)
Timeframe: Baseline to 12 months

Interventionpercentage of responders (Number)
Celecoxib First- Juvenile Onset12.50
Placebo First- Juvenile-onsent7.69
Celecoxib First - Adult Onset12.50
Placebo First- Adult-onset33.33

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Effect of Gender on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%.

Percent of patients of each gender with reduction in papilloma growth rate greater than 50% during the last 3 months of first treatment period compared to baseline (NCT00571701)
Timeframe: Baseline to12 months

Interventionpercent responders (Number)
Celecoxib First - Males12.50
Placebo First- Males40.00
Celecoxib First- Females12.50
Placebo First- Females0.00

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Correlation Between Mean Plasma Level of Celecoxib and Response.

Mean plasma levels of celecoxib over months 3-12 in first treatment period correlated with reduction in papilloma growth rate greater than 50% during the last 3 months of first treatment period compared to baseline. (NCT00571701)
Timeframe: Baseline to 12 months

Interventionpg. celecoxib/ml. plasma (Mean)
Responders151.3
Non-responders543.41

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Mean Percent Change in Papilloma Growth Rate at 12 Month Measurement Compared to Baseline

Change in mean growth rates during the last 3 months of the first treatment period compared to the mean values at baseline. Endoscopy and removal of all tumor was done every 3 months. Growth rate is calculated as the scored amount of papilloma recurrence in a 3 month period divided by the exact number of days since last endoscopy and removal of all tumor. (NCT00571701)
Timeframe: Baseline to 12 months

Interventionpercent change in mean growth rate (Mean)
Celecoxib First, Then Placebo-5.4
Placebo First, Then Celecoxib-15.2

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Percent of Patients With Positive Response to Treatment

Percent of patients with reduction in papilloma growth rate greater than 50% during the last 3 months of first treatment period compared to baseline (NCT00571701)
Timeframe: Baseline to 12 months

Interventionpercent responders (Number)
Celecoxib First (12 Months), Then Placebo (12 Months)12.5
Placebo First (12 Months), Then Celecoxib (12 Months)28.6

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Effect of HPV 6 Versus HPV 11 on Percent of Patients With Reduction in Papilloma Growth Rate Greater Than 50%

Percent of patients with HPV 6 versus patients with HPV 11 with reduction in papilloma growth rate greater than 50% during the last 3 months of first treatment period compared to baseline. (NCT00571701)
Timeframe: Baseline to 12 months

Interventionpercent of responders (Number)
Celecoxib First - HPV 69.09
Placebo First- HPV 642.86
Celecoxib First- HPV 1125.00
Placebo First- HPV 110.00

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Toxicity of Celecoxib With Concurrent Weekly Chemotherapy and Radiotherapy in the Treatment of Locally Advanced or Recurrent Squamous Cell Carcinoma of the Head and Neck.

Particpants experiencing Acute Toxicities > Grade 3 (NCT00581971)
Timeframe: 2 years from radiation therapy

Interventionparticipants (Number)
HematologicDermatitisMucositis/Dysphagia
Acute Toxicity12716

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Response as Evaluated by Recurrence of Diseases

Evaluate the response to concurrent celecoxib, carboplatin, paclitaxel, and radiotherapy in the treatment of locally advanced SSC of the head and neck. Response is determined by local control only, local and distant metastasis, distant metastasis only, second primary, and surgical salvage. (NCT00581971)
Timeframe: 2 years from end of treatment (Radiation therapy)

InterventionParticipants (Number)
Local Control OnlyLocal Control and Distant MetastasisDistant Metastatsis OnlySecondary Primary - Site UnknownSurgical Salvage
Recurrence62123

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Number of Subjects Witha Change (IMPROVEMENT) in Colo-rectal Adenocarcinoma as Measured by Cyclooxygenase-2 Activity After 7 Days of Celecoxib

"The Colo-Rectal adenocarcinoma will be measured by cyclooxygenase-2(COX-2) activity at 7 days post baseline. Cox-2 activity is measured by assessing tumors and normal tissue using Electron microscope and Tandem mass Spectrometry methodology though the UAB shared Mass Spectrometry facility. Improvement was measured by 2-fold increase in COX-2 activity from baseline. The methodology used was High Performance Liquid Chromatography(HPLC). additional studies include expression of genes thought to be important in colorectal carcinogenesis: COX-1 and 2, MMP, 2 7, and 9, tissue inhibitor of metalloproteinases(TIMPs) 1 ans 2 and beta-catenin." (NCT00582660)
Timeframe: baseline to 7 days

InterventionParticipant (Number)
Celecoxib2.0
Placebo2.0

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Subjects With Positive Response 72 Hours After Administration of Study Treatment as Measured by Immunoblot

At 72 hours after start of treatment, the number of subjects with immunoblot demonstrated a 1.5 to 2 fold increase in 15-LOX-1 protein expression in human colorectal adenocarcinoma cell line with epithelial morphology(HT-29) and dihydrolipoamide dehydrogenase(DLD)-1 cells. (NCT00582660)
Timeframe: baseline to 72 hours

InterventionParticipants (Number)
Celecoxib3.0
Placebo0

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Acetaminophen Equivalent Use

Participant reported acetaminophen use and its equivalent. Medication use was collected from reported participant journals. (NCT00583453)
Timeframe: From operative day through 10 days post-operative

,
Interventionmg (Mean)
Day 1Average, days 2 to 4Average, days 5 to 7Average, days 8 to 10
Celecoxib as Experimerimental Intervention2074224520281418
Placebo Control, Active Comparator3006293436102483

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Total Morphine Equivalent

Participant reported mophine equivalent use (NCT00583453)
Timeframe: From operative day through 10 days post-operative

,
Interventionmg (Mean)
Day 1Average, days 2 to 4Average, days 5 to 7Average, days 8 to 10
Celecoxib as Experimerimental Intervention28.930.427.813.2
Placebo Control, Active Comparator55.072.469.738.3

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Self-reported Pain Score

Pain score as reported by participant, measured on a 10 point scale, where 0 = none and 10 = unbearable, collected once daily. (NCT00583453)
Timeframe: day of procedure through post-operative day 10

,
Interventionpain score (units on a scale) (Mean)
Maximum pain, day 1maximum pain, averaged across days 2 to 4maximum pain, averaged across days 5 to 7maximum pain, averaged across days 8 to 10Average pain, day 1Average pain, averaged across days 2 to 4Average pain, averaged across days 5 to 7Average pain, averaged across days 8 to 10Pain with drinking, day 1Pain with drinking, averaged across days 2 to 4Pain with drinking, averaged across days 5 to 7Pain with drinking, averaged across days 8 to 10Activity, day 1
Celecoxib 200 mg Tablets5.05.14.43.66.16.26.14.95.75.44.93.92.8
Placebo With Same Dosing Schedule as the Active Comparator Arm6.06.05.94.07.37.67.45.76.76.65.94.14.5

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Self-reported Activity Level

Activity level, reported by participant utilizing a 10-point ordinal scale (0 = no activity, 10 = return to normal activities). Activity level was measured was collected once daily. (NCT00583453)
Timeframe: From operative day through 10 days post-operative

,
InterventionActivity score (units on a scale) (Mean)
Day 1Average, days 2 to 4Average, days 5 to 7Average, days 8 to 10
Celecoxib as Experimerimental Intervention2.83.15.47.4
Placebo Control, Active Comparator4.54.13.75.7

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Incidence of Post-operative Hemorrhage

The incidence of post-operative hemorrhage, defined as post-operative bleeding requiring medical intervention or hospitalization during the 10 day post-operative follow-up period. (NCT00583453)
Timeframe: From operative day through 10 days post-operative

InterventionParticipants (Count of Participants)
Celecoxib 200 mg Tablets0
Placebo With Same Dosing Schedule as the Active Comparator Arm0

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Time to Treatment Failure

"Time to treatment failure was defined as time from randomization to the earliest occurrence of one or more of the following:~Appearance of ≥20 polyps (>2 mm in size) at any colonoscopy during the study (Polyps), or~Diagnosis of colorectal malignancy (ColMal), or~Treatment related dropout (DO). The treatment related dropout was defined as insufficient clinical response, progression of disease, death, adverse event, treatment-related laboratory abnormality, subject no longer willing to participate in study, and other reasons that might be related to treatment as determined by treating physicians in a blind fashion before database release." (NCT00585312)
Timeframe: 5 years

Interventionyears (Mean)
Celecoxib2.0
Placebo1.7

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Total Number of Colorectal Polyps

"Total number of colorectal polyps >2 mm in size, that were detected over Years 1 - 5 cumulatively.~Weighted total number of colorectal polyps over Years 1 - 5 cumulatively was defined as the total number of colorectal polyps >2 mm in size, that were detected over Years 1 - 5, divided by the number of colonoscopies that the participant had during the study." (NCT00585312)
Timeframe: Years 1 - 5

,
Interventionpolyps (Mean)
Year 1 (N: 27, 30)Year 2 (N: 21, 25)Year 3 (N: 16, 14)Year 4 (N: 8, 7)Year 5 (N: 2, 2)Years 1 - 5 cumulatively (N: 33, 36)
Celecoxib3.08.813.418.630.54.3
Placebo8.113.722.336.446.58.6

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Colorectal Polyp Burden

"The polyp burden was defined as the sum of the largest diameters of all polyps (>2 mm in size) over Years 1 - 5 cumulatively.~Weighted colorectal polyp burden over Years 1 - 5 cumulatively was defined as the polyp burden over Years 1 - 5 divided by the number of colonoscopies that the participant had during the study." (NCT00585312)
Timeframe: Years 1 - 5

,
Interventionmm (Mean)
Year 1 (N: 27, 30)Year 2 (N: 21, 25)Year 3 (N: 16, 14)Year 4 (N: 8, 7)Year 5 (N: 2, 2)Year 1 - 5 cumulatively (N: 33, 36)
Celecoxib4.06.99.612.920.04.1
Placebo4.28.111.618.720.04.3

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Time to Disease Progression

"Time to disease progression was defined as the time from randomization to the earliest occurrence of one or more of the following events:~Appearance of ≥20 polyps (>2 mm in size) at any colonoscopy during the study (Polyps); or~Diagnosis of colorectal malignancy (ColMal)." (NCT00585312)
Timeframe: 5 years

Interventionyears (Mean)
Celecoxib2.2
Placebo1.8

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Number of Case With Papilloma Recurrence During a 12-month Follow up

Criteria for the recurrence: the site scoring >4, plus visible lesion found in >50% of the treated tissue area, after surgery Description: The caculation of the site scoring is based on a called Derkay's scoring system: to indicate how many anatomic site involved, from the 0 (the best)to 13 (the worst),among a total of 13 laryngeal sites such as epiglottis or right true vocal cords. (NCT00592319)
Timeframe: 12-month follow up

Interventioncase (Number)
Control2
Experienment5

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Time Course (Month) With Papilloma Recurrence During 12-month Follow up

The measuer is reported as time course (i.e., how many month) to see papilloma recurrence if there is any such recurrence. (NCT00592319)
Timeframe: 12 months

Interventionmonth (Mean)
Control3.5
Experiment5.2

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Menstrual Cycle Length

Menstrual cycle length was measured by the number of days subjects noted menstruating in their diary entry. (NCT00614406)
Timeframe: 3 months

InterventionDays (Mean)
Active Drug28.5
Placebo27.2

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Mean Arterial Pressure

Blood pressure was measured on the last day of each 7 day sodium diet for 24 hours using an ambulatory blood pressure monitor (NCT00624559)
Timeframe: 24 hours

Interventionmm Hg (Mean)
Celebrex, Low Sodium Diet88
Celebrex, High Sodium Diet87
Placebo, Low Sodium Diet87
Placebo, High Sodium Diet87

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Urinary Sodium Excretion

Urine collected over 24 hour period on last day of each different sodium diet (NCT00624559)
Timeframe: 24 hour

Interventionmmol Na+/24 hr (Mean)
Celebrex, Low Sodium Diet17
Celebrex, High Sodium Diet281
Placebo, Low Sodium Diet14
Placebo, High Sodium Diet253

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Treatment Responders Based on the Numerical Rating Scale-Pain (NRS-Pain)

A subject who met the following criteria was considered as a successful responder at Week 6: completed 6 weeks of treatment with study medication and had a 30% improvement from Baseline to Week 6/ET on the NRS-Pain. NRS-Pain scale assessed the severity of a subject's lower back pain on a scale of 0 (No pain) and 10 (Worst possible pain). (NCT00662558)
Timeframe: Week 6 or Early Termination (ET)

,
Interventionparticipants (Number)
RespondersNon-responders
Celecoxib254142
Tramadol HCL218178

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Patient's Satisfaction Questionnaire (With Walking and Bending Ability Scale)

Number of subjects at varying levels of pain relief (1 = very dissatisfied to 10 = very satisfied). (NCT00662558)
Timeframe: Week 6/ET

,
Interventionparticipants (Number)
12345678910
Celecoxib24161931353235555670
Tramadol HCL15222033403037467744

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Physician's Global Assessment of Disease Activity

"Number of subjects with a physician's grading of disease activity using the Physician's Global Assessment of Disease Activity 5-point scale ((1=very good, 2=good, 3=fair, 4=poor, and 5=very poor). Subjects were classified as Improved if their assessment reduced at least 2 grades from baseline or if their assessment changed to Grade 1 (Very Good). Subjects were classified as Worsened if their assessment increased at least 2 grades from baseline or if their assessment changed to Grade 5 (Very Poor). Subjects were classified as No Change otherwise." (NCT00662558)
Timeframe: Week 6/ET

,
Interventionparticipants (Number)
ImprovedNo ChangeWorsened
Celecoxib1132532
Tramadol HCL1022581

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Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Score

Each subject assessed his/her own disability due to low back pain using the RMDQ worksheet, which consisted of 24 statements of disability. The RMDQ total score was calculated as the total number of statements that were checked; the RMDQ total scores could have ranged from 0 to 24, with higher scores indicating greater disability. RMDQ: Change = mean score at Week 6/ET minus mean score at Baseline. (NCT00662558)
Timeframe: Baseline, Week 6/ET

Interventionscores on a scale (Mean)
Celecoxib-4.90
Tramadol HCL-4.45

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Change From Baseline in Severity of Chronic Low Back Pain as Measured by NRS-Pain

NRS-Pain scale assessed the severity of a subject's lower back pain on a scale of 0 (No pain) and 10 (Worst possible pain). NRS-Pain scale: Change = mean score at Week 6/ET minus mean score at Baseline. (NCT00662558)
Timeframe: Baseline, Week 6/ET

Interventionscores on a scale (Mean)
Celecoxib-3.38
Tramadol HCL-3.25

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Change From Baseline in Severity of Low Back Pain as Measured by Visual Analogue Scale (VAS)

"VAS was a 100 millimeter (mm) scale that subjects used to assess the severity of their lower back pain. Based on the following question, During the past day, how much back pain did you have?, the subject was instructed to place a vertical line on the VAS to indicate the magnitude of his/her lower back pain. 0 mm = no pain and 100 mm = worst possible pain. VAS: Change = mean score at Week 6/ET minus mean score at Baseline." (NCT00662558)
Timeframe: Baseline, Week 6/ET

Interventionmm (Mean)
Celecoxib-34.78
Tramadol HCL-34.27

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Change From Baseline in Medical Outcomes Study (MOS) Sleep Scale

MOS sleep scale included the following attributes: sleep disturbance, snoring, awaken shortness of breath or headache, quantity of sleep, sleep adequacy, somnolence, Sleep Problem Index I, and Sleep Problem Index II. Score ranged from 0-100, with a higher score indicating more of the scale attribute (e.g., more sleep disturbance, etc.). A negative change indicated subject improvement. MOS sleep scale: Change = mean score at Week 6/ET minus mean score at Baseline. (NCT00662558)
Timeframe: Baseline, Week 6/ET

,
Interventionscores on a scale (Mean)
Sleep Disturbance (n=374, 367)Snoring (n=372, 365)Awaken Shortness of Breath, Headache (n=374, 367)Quantity of Sleep (n=373, 365)Sleep Adequacy (n=373, 367)Somnolence (n=374, 366)Sleep Problem Index I (n=373, 367)Sleep Problem Index II (n=373, 367)
Celecoxib-17.91-7.53-8.610.007.32-9.63-11.59-12.97
Tramadol HCL-16.34-5.10-6.210.589.67-7.01-10.54-11.82

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Change From Baseline in Modified Brief Pain Inventory (m-BPI-sf)

m-BPI-sf scale assessed pain severity (0 = no pain to 10 = worst possible pain), and pain interference of functional activities (0 = does not interfere to 10 = completely interferes) during the 24 hour follow-up period. Subjects indicated: how much pain now; worst pain; average level of pain; how much pain interfered with general activity, mood, walking ability, relations with other people, sleep, normal work (including housework), and enjoyment of life. m-BPI-sf: Change = mean score at Week 6/ET minus mean score at Baseline. (NCT00662558)
Timeframe: Baseline, Week 6/ET

,
Interventionscores on a scale (Mean)
How Much Pain NowWorst Pain in Past 24 HoursAverage Pain in Past 24 HoursPain Interfered With General ActivityPain Interfered With MoodPain Interfered With Walking ActivityPain Interfered With Relations With OthersPain Interfered With SleepPain Interfered With Normal WorkPain Interfered With Enjoyment of LifePain Interference Subscale
Celecoxib-2.87-2.84-2.64-2.62-2.38-2.26-1.79-2.52-2.57-2.43-2.37
Tramadol HCL-2.88-2.87-2.59-2.57-2.25-2.36-1.74-2.51-2.46-2.43-2.33

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Change From Baseline in Work Limitations Questionnaire (WLQ)

The WLQ included the following: Time Scale, Physical Scale, Output Scale, Mental-Interpersonal Scale, and Index Scale. The scales ranged from 0 (Limited none of the time) to 100 (Limited all of the time). A negative change indicated subject improvement. (NCT00662558)
Timeframe: Baseline, Week 6/ET

,
Interventionscores on a scale (Mean)
Time Scale (n=241, 239)Physical Scale (n=270, 254)Output Scale (n=256, 246)Mental-Interpersonal Scale (n=266, 252)Index Scale (n=223, 220)
Celecoxib-11.55-13.68-11.44-9.06-3.10
Tramadol HCL-13.58-12.65-11.69-9.54-3.14

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Chronic Low Back Pain Responders Based on VAS, Patient's Global, and RMDQ

Subjects were successful responders if they had: > = 30% improvement from baseline to final visit in VAS assessment (as identified by 100 millimeter scale); > = 30% improvement from baseline to final visit in Patient's Global assessment (classified as improved if assessment reduced at least 2 grades from baseline or if assessment changed to Grade 1, worsened if assessment increased at least 2 grades from baseline or if assessment changed to Grade 5, or no change; and < 20% worsening from baseline to final visit in RMDQ assessment (lower scores indicated greater disability). (NCT00662558)
Timeframe: Week 6/ET

,
Interventionparticipants (Number)
RespondersNon-responders
Celecoxib213183
Tramadol HCL196200

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Number of Subjects With Change From Baseline in MOS Optimal Sleep Scale Scores

The Optimal Scale is scaled from 0 or 1 with 1 indicating 7 or 8 hours of sleep per night and 0 otherwise. Number of subjects with change of improvement (0 to 1), no change (1 to 1 or 0 to 0), or worsening (1 to 0) from baseline as indicated by the MOS Optimal sleep scale. (NCT00662558)
Timeframe: Baseline, Week 6/ET

,
Interventionparticipants (Number)
0 to 1 (Improvement)1 to 1 (No change)0 to 0 (No change)1 to 0 (worsening)
Celecoxib829417126
Tramadol HCL747019229

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Patient's Global Assessment of Disease Activity

"Number of subjects with a graded level of disease activity using the Patient's Global Assessment of Disease Activity 5-point scale (1=very good, 2=good, 3=fair, 4=poor, and 5=very poor). Subjects were classified as Improved if their assessment reduced at least 2 grades from baseline or if their assessment changed to Grade 1 (Very Good). Subjects were classified as Worsened if their assessment increased at least 2 grades from baseline or if their assessment changed to Grade 5 (Very Poor). Subjects were classified as No Change otherwise." (NCT00662558)
Timeframe: Week 6/ET

,
Interventionparticipants (Number)
ImprovedNo ChangeWorsened
Celecoxib1082643
Tramadol HCL1072591

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Patient's Global Evaluation of Study Medication

Number of subjects with an overall response to study medication of poor, fair, good, very good, and excellent. (NCT00662558)
Timeframe: Weeks 1, 3, and 6/ET

,
Interventionparticipants (Number)
Week 1, ExcellentWeek 1, Very GoodWeek 1, GoodWeek 1, FairWeek 1, PoorWeek 3, ExcellentWeek 3, Very GoodWeek 3, GoodWeek 3, FairWeek 3, PoorWeek 6/ET, ExcellentWeek 6/ET, Very GoodWeek 6/ET, GoodWeek 6/ET, FairWeek 6/ET, Poor
Celecoxib4697126782352104122532391123765132
Tramadol HCL388313757184197105511468112905144

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Patient's Satisfaction Questionnaire (With Pain Relief Scale)

Number of subjects at varying levels of pain relief (1 = very dissatisfied to 10 = very satisfied). (NCT00662558)
Timeframe: Week 6/ET

,
Interventionparticipants (Number)
12345678910
Celecoxib23152222442321635387
Tramadol HCL22181920302939566269

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Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline

"Western Ontario and McMaster Universities (WOMAC) pain questionnaire has 5 questions on pain all use visual analog scale (VAS) of 100 mm, with 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain at 12 weeks from baseline (in mm). WOMAC is a self-administered, patient-reported health status questionnaire designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. It consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00664560)
Timeframe: Baseline and 12 weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-43.4
(Celebrex 200 mg Once Daily)-41.1
(Placebo Twice Daily)-34.0

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Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline

"WOMAC function questionnaire (VAS). The 17 questions about function all use visual analog scale (VAS) of 100 mm; 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain from baseline (in mm).~The Western Ontario and McMaster Universities (WOMAC) is a self-administered, patient-reported health status questionnaire that is designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. The index consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00664560)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-35.3
(Celebrex 200 mg Once Daily)-33.9
(Placebo Twice Daily)-27.3

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Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline

"WOMAC function questionnaire (VAS). The 17 questions about function all use visual analog scale (VAS) of 100 mm; 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain from baseline (in mm).~The Western Ontario and McMaster Universities (WOMAC) is a self-administered, patient-reported health status questionnaire that is designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. The index consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00664560)
Timeframe: 12 weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-37.5
(Celebrex 200 mg Once Daily)-36.0
(Placebo Twice Daily)-28.9

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Number of Participants Reporting Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal (UGI) Symptoms

Number of participants reporting pre-specified non-steroidal antiinflammatory drug-associated (NSAID) upper gastrointestinal (UGI) symptoms. Pre-specified NSAID-associated UGI symptoms include adverse events such as dyspepsia, abdominal pain or discomfort, nausea, vomiting. (NCT00664560)
Timeframe: daily during 12 weeks

Interventionparticipants (Number)
(PN 400 (VIMOVO) Twice Daily)41
(Celebrex 200 mg Once Daily)41
(Placebo Twice Daily)24

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Modified Severity of Dyspepsia Assessment (mSODA)

Change from Baseline in the Modified Severity of Dyspepsia Assessment (mSODA) average daily pain intensity converted total score at Week 12. The mSODA instruments consists of 6 questions about abdominal discomfort during the past 24 hours, with a converted score of 2 through 47. Lower score equals less pain. (NCT00664560)
Timeframe: Baseline to 12 weeks

InterventionScores on a scale (Mean)
(PN 400 (VIMOVO) Twice Daily)-3.5
(Celebrex 200 mg Once Daily)-4.8
(Placebo Twice Daily)-4.0

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Change in Patient Global Assessment (PGA) Subscore From Baseline

PGA questionnaire. The patient global assessment (PGA) question asks about how the subject is doing considering his/her arthritis and is measured by a visual analog scale (VAS); 0 mm (very poor) 100 mm (excellent). The outcome measures a change from baseline PGA in mm. (NCT00664560)
Timeframe: 12 weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)21.5
(Celebrex 200 mg Once Daily)22.4
(Placebo Twice Daily)12.4

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Antacid Tablet Use

Tablet pill count (NCT00664560)
Timeframe: 12 weeks

InterventionTablets per subject (Mean)
(PN 400 (VIMOVO) Twice Daily)9.3
(Celebrex 200 mg Once Daily)13.9
(Placebo Twice Daily)15.4

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American Pain Society Patient Outcome Questionnaire (APS-POQ)Total Interference Caused by Pain.

Mean change from Baseline scores calculated for each subject through Day 7. Scale 0 through 70, where 0=no pain interference and 70=complete interference. (NCT00664560)
Timeframe: Baseline and Day 7

InterventionUnits on a scale (Mean)
(PN 400 (VIMOVO) Twice Daily)-17.8
(Celebrex 200 mg Once Daily)-17.7
(Placebo Twice Daily)-12.8

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Percent of Days With no Heartburn (Heartburn Resolution)

During 12 weeks, daily heartburn question with ratings none, mild, moderate, or severe. Percent of days with Heartburn resolution (heartburn is none). (NCT00664560)
Timeframe: 12 weeks

Interventionpercent days (Mean)
(PN 400 (VIMOVO) Twice Daily)83.9
(Celebrex 200 mg Once Daily)75.8
(Placebo Twice Daily)68.5

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The Number of Subjects Who Discontinued From the Study Due to Any Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal Adverse Event

The number of subjects who discontinued from the study due to any pre-specified non-steroidal antiinflammatory drug (NSAID)-associated upper gastrointestinal (UGI) adverse event (as classified by MedDRA). Pre-specified NSAID-associated UGI symptoms include adverse events such as dyspepsia, abdominal pain or discomfort, nausea, vomiting. (NCT00664560)
Timeframe: daily during 12 weeks

Interventionparticipants (Number)
(PN 400 (VIMOVO) Twice Daily)3
(Celebrex 200 mg Once Daily)4
(Placebo Twice Daily)3

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Change in Patient Global Assessment (PGA) Subscore From Baseline

PGA questionnaire. The patient global assessment (PGA) question asks about how the subject is doing considering his/her arthritis and is measured by a visual analog scale (VAS); 0 mm (very poor) 100 mm (excellent). The outcome measures a change from baseline PGA in mm. (NCT00664560)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)22.6
(Celebrex 200 mg Once Daily)20.7
(Placebo Twice Daily)14.7

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Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline

"Western Ontario and McMaster Universities (WOMAC) pain questionnaire has 5 questions on pain all use visual analog scale (VAS) of 100 mm, with 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain at 6 weeks from baseline (in mm). WOMAC is a self-administered, patient-reported health status questionnaire designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. It consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00664560)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-40.9
(Celebrex 200 mg Once Daily)-39.4
(Placebo Twice Daily)-30.7

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Change in Patient Global Assessment (PGA) Subscore From Baseline

PGA questionnaire. The patient global assessment (PGA) question asks about how the subject is doing considering his/her arthritis and is measured by a visual analog scale (VAS); 0 mm (very poor) 100 mm (excellent). The outcome measures a change from baseline PGA in mm. (NCT00665431)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)25.9
(Celebrex 200 mg Once Daily)24.4
(Placebo Twice Daily)22.3

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Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline

"WOMAC function questionnaire (VAS). The 17 questions about function all use visual analog scale (VAS) of 100 mm; 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain from baseline (in mm).~The Western Ontario and McMaster Universities (WOMAC) is a self-administered, patient-reported health status questionnaire that is designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. The index consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00665431)
Timeframe: 12 Weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-38.7
(Celebrex 200 mg Once Daily)-37.7
(Placebo Twice Daily)-30.9

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Change in Western Ontario and McMaster Universities (WOMAC) Function Questionnaire Subscore From Baseline

"WOMAC function questionnaire (VAS). The 17 questions about function all use visual analog scale (VAS) of 100 mm; 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain from baseline (in mm).~The Western Ontario and McMaster Universities (WOMAC) is a self-administered, patient-reported health status questionnaire that is designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. The index consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00665431)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-38.5
(Celebrex 200 mg Once Daily)-34.6
(Placebo Twice Daily)-29.0

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Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline

"Western Ontario and McMaster Universities (WOMAC) pain questionnaire has 5 questions on pain all use visual analog scale (VAS) of 100 mm, with 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain at 12 weeks from baseline (in mm). WOMAC is a self-administered, patient-reported health status questionnaire designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. It consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00665431)
Timeframe: Baseline and 12 Weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-44.1
(Celebrex 200 mg Once Daily)-43.6
(Placebo Twice Daily)-37.3

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Change in Western Ontario and McMaster Universities (WOMAC) Pain Questionnaire Subscore From Baseline

"Western Ontario and McMaster Universities (WOMAC) pain questionnaire has 5 questions on pain all use visual analog scale (VAS) of 100 mm, with 0 mm being no pain and 100 mm being extreme pain. The outcome measures a change in WOMAC pain at 6 weeks from baseline (in mm). WOMAC is a self-administered, patient-reported health status questionnaire designed to capture elements of pain, stiffness and physical disability in patients with OA of the knee and/or hip joints. It consists of 24 questions (5 questions about pain, 2 on stiffness and 17 about physical function)." (NCT00665431)
Timeframe: Week 6

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)-44.3
(Celebrex 200 mg Once Daily)-39.6
(Placebo Twice Daily)-33.9

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Mean Change From Baseline in American Pain Society Patient Outcome Questionnaire (APS-POQ)Total Interference Caused by Pain.

For APS-POQ score is the change from Baseline scores calculated for each subject through Day 7. Scale 0 through 70, where 0=no pain interference and 70=complete interference. (NCT00665431)
Timeframe: Baseline and Day 7

InterventionUnits on a scale (Mean)
(PN 400 (VIMOVO) Twice Daily)-18.8
(Celebrex 200 mg Once Daily)-16.6
(Placebo Twice Daily)-11.6

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Number of Participants Reporting Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal (UGI) Symptoms

Number of participants reporting pre-specified non-steroidal antiinflammatory drug-associated (NSAID) upper gastrointestinal (UGI) symptoms. Pre-specified NSAID-associated UGI symptoms include adverse events such as dyspepsia, abdominal pain or discomfort, nausea, vomiting. (NCT00665431)
Timeframe: daily during 12 weeks

Interventionparticipants (Number)
(PN 400 (VIMOVO) Twice Daily)46
(Celebrex 200 mg Once Daily)53
(Placebo Twice Daily)25

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The Number of Subjects Who Discontinued From the Study Due to Any Pre-specified Non-steroidal Antiinflammatory Drug-associated Upper Gastrointestinal Adverse Event

The number of subjects who discontinued from the study due to any pre-specified non-steroidal antiinflammatory drug (NSAID)-associated upper gastrointestinal (UGI) adverse event (as classified by MedDRA). Pre-specified NSAID-associated UGI symptoms include adverse events such as dyspepsia, abdominal pain or discomfort, nausea, vomiting. (NCT00665431)
Timeframe: daily during 12 weeks

Interventionparticipants (Number)
(PN 400 (VIMOVO) Twice Daily)2
(Celebrex 200 mg Once Daily)9
(Placebo Twice Daily)3

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Modified Severity of Dyspepsia Assessment (mSODA)

Change from Baseline in the Modified Severity of Dyspepsia Assessment (mSODA) average daily pain intensity converted total score at Week 12. The mSODA instruments consists of 6 questions about abdominal discomfort during the past 24 hours, with a converted score of 2 through 47. Lower score equals less pain. (NCT00665431)
Timeframe: 12 weeks

InterventionScores on a scale (Mean)
(PN 400 (VIMOVO) Twice Daily)-4.5
(Celebrex 200 mg Once Daily)-3.3
(Placebo Twice Daily)-3.5

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Percent of Days With no Heartburn (Heartburn Resolution)

During 12 weeks, daily heartburn question with ratings none, mild, moderate, or severe. Percent of days with Heartburn resolution (heartburn is none). (NCT00665431)
Timeframe: 12 weeks

Interventionpercent days (Mean)
(PN 400 (VIMOVO) Twice Daily)78.4
(Celebrex 200 mg Once Daily)72.1
(Placebo Twice Daily)71.1

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Antacid Tablet Use

Tablet pill count (NCT00665431)
Timeframe: 12 weeks

InterventionTablets per subject (Mean)
(PN 400 (VIMOVO) Twice Daily)13.4
(Celebrex 200 mg Once Daily)20.9
(Placebo Twice Daily)27.3

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Change in Patient Global Assessment (PGA) Subscore From Baseline

PGA questionnaire. The patient global assessment (PGA) question asks about how the subject is doing considering his/her arthritis and is measured by a visual analog scale (VAS); 0 mm (very poor) 100 mm (excellent). The outcome measures a change from baseline PGA in mm. (NCT00665431)
Timeframe: 12 Weeks

Interventionmm (Mean)
(PN 400 (VIMOVO) Twice Daily)27.7
(Celebrex 200 mg Once Daily)26.4
(Placebo Twice Daily)22.4

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Number of Participants With Grade 4 Adverse Events

Grading of adverse events was determine by the principal investigator according to NCI common toxicity criteria (CTC version 3.0). Safety analysis is based on any participant experiencing a grade 4 AE. (NCT00665457)
Timeframe: every 3 weeks X 4, then every 2 weeks X4

InterventionParticipants (Count of Participants)
Celecoxib1

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JIA Concomitant Medications

JIA medications by class: GI protective agents (eg, proton-pump inhibitors, antacids, surcalfate), other GI, DMARDs, biologics, antihypertensives, NSAIDs (Celecoxib, Diclofenac, Ibuprofen, Meloxicam, Naproxen, other NSAIDs), corticosteroids (oral, IV, intra-articular, other forms), analgesics Acetaminophen, Opioids, other). Participants could receive more than 1 medication. (NCT00688545)
Timeframe: Year 2 or early termination

,
InterventionParticipants (Number)
GI protective agentsOther GIDMARDsBiologicsAntihypertensivesNSAIDs (Celecoxib)NSAIDs (Diclofenac)NSAIDs (Ibuprofen)NSAIDs (Meloxicam)NSAIDs (Naproxen)NSAIDs (Other)Corticosteroids (oral, IV, intra-articular)Corticosteroids (Other)Analgesics (Acetaminophen, Opioids, Other)
Celecoxib205241317011004211
nsNSAIDs54810260420987315619

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Counts of participants who had treatment-emergent adverse events (TEAEs), defined as newly occurring or worsening after first dose. Participants with multiple occurrences of an AE within a category were counted once within the category. AEs attributed to the NSAID (celecoxib or nsNSAID) utilized at time of event, regardless of the initial NSAID treatment at Registry entry. (NCT00688545)
Timeframe: Baseline up to 2 years

,
InterventionParticipants (Number)
AEsSAEs
Celecoxib362
nsNSAIDs1179

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Clinical Oral Mucosal Injury Score at Cumulative Radiation Dose of 5000 cGy

"Oral Mucositis Assessment Scale (OMAS) was used to assess oral mucosal injury during the period of radiation therapy. This validated scale scores ulceration and erythema independently at nine specified sites in the oral cavity. Ulceration is scored from 0-3 based on size of lesion and erythema is scored from 0-2 based on severity of erythema. The sum of scores is then divided by 9.~The mean OMAS score at a cumulative radiation dose of 5000 cGy (approximately 5 weeks of treatment) was compared between groups." (NCT00698204)
Timeframe: 5 weeks from start of radiation therapy (5000 cGy)

Interventionunits on a scale (Mean)
I- Celecoxib1.42
II- Placebo1.36

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Evaluation of Pain Severity at 5000 cGy Radiation

Mean worst pain at 5000 cGy on 0-10 scale, 0 = no pain, 10 = worst pain imaginable (NCT00698204)
Timeframe: 5 weeks from start of radiation therapy (cumulative dose of 5000 cGy)

Interventionunits on a scale (Mean)
I- Celecoxib4.47
II- Placebo3.70

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Percentages of Participants Responding to Assessment in Ankylosing Spondylitis (ASAS)-20

Percentages of participants who demonstrated an improvement of greater than or equal to (≥) 20% from baseline and an absolute improvement of ≥10 mm from baseline on a 100-mm VAS in ≥3 of the 4 domains proposed by the Ankylosing Spondylitis Assessment Working Group (ASAS-20). (NCT00762463)
Timeframe: Weeks 2, 4, 6, 12

,,,
Interventionpercentage of participants (Number)
Week 2 (n=115, 114)Week 4 (n=116, 114)Week 6 (n=54, 54, 54, 54)Week 12 (n=51, 53, 46, 51)
Celecoxib 200 mg23.526.740.749.0
Celecoxib 200 mg, Then Celecoxib 400 mg0022.232.6
Diclofenac 75 mg, Then Celecoxib 400 mg0029.637.3
Diclofenac SR 75 mg25.431.642.647.2

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Change From Baseline in Physician's Global Assessment of Disease Activity at Weeks 2, 4, and 6

5-point Likert scale scores specified physician's subjective assessment on how overall ankylosing spondylitis appeared at the time of participant's visit and participant's disease signs. 1=very good to 5=very poor. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionunits on a scale (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.4-0.4-0.5
Diclofenac SR 75 mg-0.4-0.5-0.5

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Change From Baseline in Physician's Global Assessment of Disease Activity at Week 12

5-point Likert scale scores specified physician's subjective assessment on how the overall ankylosing spondylitis appeared at the time of the participant's visit and participant's disease signs. 1=very good to 5=very poor. Lower scores indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionunits on a scale (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.2-0.7
Celecoxib 200 mg, Then Celecoxib 400 mg3.2-0.5
Diclofenac SR 75 mg3.0-0.5
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.3-0.7

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Change From Baseline in Participant's Global Assessment of Disease Activity at Weeks 2, 4, and 6

"5-point Likert scale scores specified participant's current situation in response to the following question Considering all the ways your Ankylosing Spondylitis affects you, how are you doing today? 1=very good to 5=very poor. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionunits on a scale (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.4-0.3-0.3
Diclofenac SR 75 mg-0.4-0.4-0.4

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Change From Baseline in Participant's Global Assessment of Disease Activity at Week 12

"5-point Likert scale scores specified participant's current situation in response to the following question Considering all the ways your Ankylosing Spondylitis affects you, how are you doing today? 1=very good to 5=very poor. Lower scores indicated better health. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionunits on a scale (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.1-0.6
Celecoxib 200 mg, Then Celecoxib 400 mg3.2-0.4
Diclofenac SR 75 mg3.0-0.6
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.2-0.6

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Weeks 2 and 4

"100-mm VAS score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Change from baseline of <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)
Celecoxib 200 mg-18.6-20.7
Diclofenac SR 75 mg-17.9-23.3

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 12

"100-mm VAS score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Lower scores indicated less pain. Change from baseline of <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg63.4-28.4
Celecoxib 200 mg, Then Celecoxib 400 mg63.4-20.8
Diclofenac SR 75 mg61.1-30.9
Diclofenac SR 75 mg, Then Celecoxib 400 mg65.6-28.1

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Change From Baseline in Nocturnal Pain at Weeks 2, 4, and 6

"100-mm VAS scores specified participant's nocturnal pain in response to the following question Did you have any pain in the neck, back or hips during the previous night? 0=no pain to 100=worst pain possible. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-12.0-14.5-15.4
Diclofenac SR 75 mg-16.3-17.1-19.4

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Change From Baseline in Chest Expansion at Weeks 2, 4, and 6

Chest expansion, measured in cm, is defined as the difference in thoracic circumference during full expiration versus full inspiration, measured at the fourth intercostal space (nipple line). The better of 2 tries was recorded. Change from baseline greater than (>) 0 represented improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventioncm (Least Squares Mean)
Week 2 (n=117, 115)Week 4 (n=118, 115)Week 6 (n=118, 115)
Celecoxib 200 mg0.20.60.7
Diclofenac SR 75 mg0.30.40.6

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Paracetamol Tablets Taken Per Day by Participant

Calculated as the total number of paracetamol tablets taken divided by days of exposure in the study. (NCT00762463)
Timeframe: Week 6

Interventiontablets per day (Mean)
Celecoxib 200 mg0.2
Diclofenac SR 75 mg0.0

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Participant's Assessment of Global Pain Intensity at Baseline

"100-mm VAS scores specified participant's assessment of global pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Lower scores indicated less pain." (NCT00762463)
Timeframe: Baseline

Interventionmm (Mean)
Celecoxib 200 mg62.9
Diclofenac SR 75 mg63.6

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Percentage of Days With Concomitant Administration of Paracetamol

Calculated as days on rescue medication divided by days of exposure in the study at the end of Week 6. (NCT00762463)
Timeframe: Week 6

Interventionpercentage of days (Mean)
Celecoxib 200 mg0.1
Diclofenac SR 75 mg0.0

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Percentage of Participants With Concomitant Use of Paracetamol

Percentage of participants who concomitantly took at least 1 paracetamol tablet as rescue medication at Week 6 (NCT00762463)
Timeframe: Week 6

Interventionpercentage of participants (Number)
Celecoxib 200 mg2.5
Diclofenac SR 75 mg0.0

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Change From Baseline in BASDAI at Week 12

BASDAI is comprised of 6 specific questions, each answered on a 10-mm VAS. Scores for the first 5 questions: 0=none to 10=severe. Score for the sixth question: 0=0 hours to 10=2 hours. BASDAI score was defined as the mean of the scaled responses to these 6 questions. Lower scores indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg4.71-1.7
Celecoxib 200 mg, Then Celecoxib 400 mg4.7-0.6
Diclofenac SR 75 mg4.9-2.1
Diclofenac SR 75 mg, Then Celecoxib 400 mg4.9-1.4

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Change From Baseline in BASFI at Week 12

BASFI was comprised of 10 specific questions, each answered on a 10-mm VAS scale. 0=easy to 10=impossible. BASFI score was defined as the mean of the scaled responses to these 10 questions. Lower scores indicated better functional health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.4-0.9
Celecoxib 200 mg, Then Celecoxib 400 mg3.5-0.6
Diclofenac SR 75 mg3.5-1.0
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.5-1.0

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Change From Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) at Weeks 2, 4, and 6

Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) was comprised of 6 specific questions, each answered on a 10-mm VAS scale. Scores for the first 5 questions: 0=none to 10=severe. Score for the sixth question: 0=0 hours to 10=2 hours. BASDAI score was defined as the mean of the scaled responses to these 6 questions. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.8-0.9-1.1
Diclofenac SR 75 mg-0.9-1.1-1.4

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Change From Baseline in Bath Ankylosing Spondylitis Functional Index (BASFI) at Weeks 2, 4, and 6

Bath Ankylosing Spondylitis Functional Index (BASFI) was comprised of 10 specific questions, each answered on a 10-mm VAS scale. 0=easy to 10=impossible. BASFI score was defined as the mean of the scaled responses to these 10 questions. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.3-0.4-0.5
Diclofenac SR 75 mg-0.3-0.6-0.8

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Change From Baseline in Chest Expansion at Week 12

Chest expansion, measured in cm, is defined as the difference in thoracic circumference during full expiration versus full inspiration, measured at the fourth intercostal space (nipple line). The better of 2 tries was recorded. Higher scores indicate better health. Change from baseline greater than (>) 0 represented improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventioncm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.90.8
Celecoxib 200 mg, Then Celecoxib 400 mg3.60.8
Diclofenac SR 75 mg3.80.8
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.80.8

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 6

"100-millimeter (mm) Visual Analog Scale (VAS) score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Change from baseline of less than (<) 0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 6

Interventionmm (Least Squares Mean)
Celecoxib 200 mg-23.8
Diclofenac SR 75 mg-27.1

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Change From Baseline in CRP at Week 12

CRP was a marker of inflammation. Lower values indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmg/L (Mean)
Baseline (n=53, 55, 53, 54)Change from Baseline at Week 12 (n=47, 49, 42, 47)
Celecoxib 200 mg18.53-4.58
Celecoxib 200 mg, Then Celecoxib 400 mg18.80-4.77
Diclofenac SR 75 mg15.84-2.99
Diclofenac SR 75 mg, Then Celecoxib 400 mg21.01-2.13

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Change From Baseline in Fingertips to Floor Distance at Week 12

Fingertips to floor distance measured in cm from the tip of the fingers to the floor with participant standing erect and feet together, knees as straight as possible, then bending forward as far as possible with fingers reaching towards the floor. The better of 2 tries was recorded. Lower scores indicated better health. Change from baseline <0 represented improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventioncm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg14.8-3.0
Celecoxib 200 mg, Then Celecoxib 400 mg22.9-3.1
Diclofenac SR 75 mg17.6-3.7
Diclofenac SR 75 mg, Then Celecoxib 400 mg14.6-1.3

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Change From Baseline in Fingertips to Floor Distance at Weeks 2, 4, and 6

Fingertips to floor distance measured in centimeter (cm) from the tip of the fingers to the floor with participants standing erect and feet together, knees as straight as possible, then bending forward as far as possible with fingers reaching towards the floor. The better of 2 tries was recorded. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventioncm (Least Squares Mean)
Week 2 (n=117, 115)Week 4 (n=118, 115)Week 6 (n=118, 115)
Celecoxib 200 mg-1.6-1.9-2.8
Diclofenac SR 75 mg-1.6-2.2-3.1

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Change From Baseline in C-Reactive Protein (CRP) at Week 6

C-Reactive Protein (CRP) was a marker of inflammation, measured in milligram per liter (mg/L). Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, 6 Weeks

Interventionmg/L (Least Squares Mean)
Celecoxib 200 mg-4.16
Diclofenac SR 75 mg-2.72

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Change From Baseline in Nocturnal Pain at Week 12

"100-mm VAS scores specified participant's nocturnal pain in response to the following question Did you have any pain in the neck, back or hips during the previous night? 0=no pain to 100=worst pain possible. Lower scores indicated less pain. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg52.2-19.4
Celecoxib 200 mg, Then Celecoxib 400 mg54.5-12.5
Diclofenac SR 75 mg55.1-27.5
Diclofenac SR 75 mg, Then Celecoxib 400 mg61.5-22.6

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Change From Baseline in ESR at Week 12

ESR was a laboratory test that provided a non-specific measure of inflammation. The test assessed the rate at which red blood cells fell in a test tube. Lower values indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm/h (Mean)
Baseline (n=54, 54, 52, 54)Change from Baseline at Week 12 (n=45, 44, 41, 43)
Celecoxib 200 mg20.9-3.5
Celecoxib 200 mg, Then Celecoxib 400 mg22.8-6.3
Diclofenac SR 75 mg20.8-1.3
Diclofenac SR 75 mg, Then Celecoxib 400 mg23.6-0.7

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Change From Baseline in Erythrocyte Sedimentation Rate (ESR) at Week 6

Erythrocyte Sedimentation Rate (ESR) was a laboratory test that providee a non-specific measure of inflammation. The test assessed the rate at which red blood cells fell in a test tube and was measured in millimeter per hour (mm/h). Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 6

Interventionmm/h (Least Squares Mean)
Celecoxib 200 mg-2.5
Diclofenac SR 75 mg-1.8

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Change From Baseline in Assessment of ABPM for SBP and DBP Pressure at Week 6/Final Visit (Sensitivity Analysis Excluding One Participant)

A summary of ABPM 24-hour averages for SBP and DBP are presented in this Outcome Measure. One of the participant in the Naproxen ABPM Arm had clinically implausible high BP values at Baseline. Due to the low number of participants in each Arm (12 and 11) these values had a significant impact on the mean baseline values for the Naproxen Arm. As a result, an additional sensitivity analysis was conducted, excluding this participant (Participant ID 10031002). (NCT00807846)
Timeframe: 6 weeks/Final Visit

,
InterventionmmHg (Mean)
SBPDBP
Celecoxib2.40.9
Naproxen1.90.3

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Change From Baseline in Assessment of Ambulatory Blood Pressure Monitoring (ABPM) for SBP and DBP at Week 6/Final Visit

Ambulatory BP measurements were obtained from 24 participants(in addition to the BP measurements obtained by the cuff technique) participating in the exploratory 24-hour ABPM sub-study. BP was monitored by a 24 hour Ambulatory BP device provided by a central vendor. (NCT00807846)
Timeframe: 6 weeks/Final Visit

,
InterventionmmHg (Mean)
SBPDBP
Celecoxib2.40.9
Naproxen-1.7-1.1

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Change From Baseline in Systolic Blood Pressure (SBP) at Week 6/Final Visit

Value at 6 weeks minus value at baseline. (NCT00807846)
Timeframe: 6 Weeks/Final Visit

InterventionmmHg (millimeter of mercury) (Least Squares Mean)
Celecoxib0.366
Naproxen-0.734

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Number of Participants With >= 30% Improvement in the Parent's Global Assessment of Overall Well-being at Week 6/Final Visit.

The parent/legal guardian evaluated the participant's overall well-being at Baseline and at Week 6 (or Final Visit) by placing one vertical line on the visual analog scale (VAS). The VAS ranged from 0 to 100, with 0 being 'very well' and 100 being 'very poor. (NCT00807846)
Timeframe: Week 6/Final Visit

InterventionParticipants (Number)
Celecoxib47
Naproxen54

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Change From Baseline in Assessment of ABPM for Heart Rate at Week 6/Final Visit

Ambulatory BP measurements were obtained from 24 participants (in addition to the BP measurements obtained by the cuff technique) participating in the exploratory 24-hour ABPM sub-study. A summary of ABPM 24-hour averages for heart rate is presented in this Outcome Measure. (NCT00807846)
Timeframe: 6 weeks/Final Visit

Interventionbpm (beats per minute) (Mean)
Celecoxib2.5
Naproxen3.7

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Change From Baseline in Assessment of ABPM for Heart Rate at Week 6/Final Visit (Sensitivity Analysis Excluding One Participant)

A summary of ABPM 24-hour averages for heart rate is presented in this Outcome Measure. One of the participant in the Naproxen ABPM Arm had clinically implausible high BP values at Baseline. Due to the low number of participants in each Arm (12 and 11) these values had a significant impact on the mean baseline values for the Naproxen Arm. As a result, an additional sensitivity analysis was conducted, excluding this participant (Participant ID 10031002). (NCT00807846)
Timeframe: 6 weeks/Final Visit

Interventionbpm (Mean)
Celecoxib2.5
Naproxen3.3

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Change From Baseline in DBP at Week 4.

Value at 4 weeks minus value at baseline. (NCT00807846)
Timeframe: 4 weeks

InterventionmmHg (Least Squares Mean)
Celecoxib-0.628
Naproxen-0.848

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Change From Baseline in DBP at Week 6/Final Visit

Value at 6 weeks/Final Visit minus value at baseline. (NCT00807846)
Timeframe: 6 weeks

InterventionmmHg (Least Squares Mean)
Celecoxib-0.535
Naproxen-0.356

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Change From Baseline in Diastolic Blood Pressure (DBP) at Week 2.

Value at 2 weeks minus value at baseline. (NCT00807846)
Timeframe: 2 weeks

InterventionmmHg (Least Squares Mean)
Celecoxib-1.346
Naproxen-0.139

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Change From Baseline in Parent's Assessment of Overall Well-being at Week 6/Final Visit.

The parent/legal guardian evaluated the participant's overall well-being at Baseline and at Week 6 (or Final Visit) by placing one vertical line on the visual analog scale (VAS). The VAS ranged from 0 to 100, with 0 being 'very well' and 100 being 'very poor. (NCT00807846)
Timeframe: 6 weeks

Interventionmm (millimeter) (Least Squares Mean)
Celecoxib-10.581
Naproxen-13.614

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Change From Baseline in Participant's Assessment of Overall Well-being at Week 6/Final Visit.

Participants, ≥8 years of age at the baseline, evaluated their own overall well-being at Baseline and at Week 6 (or Final Visit) by placing one vertical line on the VAS. The VAS ranges from 0 to 100, with 0 being 'very well' and 100 being 'very poor'. (NCT00807846)
Timeframe: 6 weeks

Interventionmm (Least Squares Mean)
Celecoxib-12.990
Naproxen-12.588

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Change From Baseline in SBP at Week 4.

Value at 4 weeks minus value at baseline. (NCT00807846)
Timeframe: 4 weeks

InterventionmmHg (Least Squares Mean)
Celecoxib-0.170
Naproxen-2.007

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Change From Baseline to Week 2 in SBP.

Value at 2 weeks minus value at baseline. (NCT00807846)
Timeframe: 2 weeks

InterventionmmHg (Least Squares Mean)
Celecoxib-0.202
Naproxen-1.290

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Number of Participants With >= 30% Improvement in the Participant's Global Assessment of Overall Well-being at Week 6/Final Visit.

Participants, ≥8 years of age at the baseline, evaluated their own overall well-being at Baseline and at Week 6 (or Final Visit) by placing one vertical line on the VAS. The VAS ranges from 0 to 100, with 0 being 'very well' and 100 being 'very poor'. (NCT00807846)
Timeframe: Week 6/Final Visit

InterventionParticipants (Number)
Celecoxib33
Naproxen45

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At Least 50% Shrinkage in Tumor Measurements by Physical Examination

(NCT00846430)
Timeframe: Monthly physical exam first three months and then every three months after, for up to 36 months

InterventionParticipants (Count of Participants)
Open-Label Intervention7

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Improvement of Symptoms and Pain

Subjects will be evaluated for pain and Quality of Life scores (NCT00846430)
Timeframe: Monthly physical exam first three months and then every three months after, for up to 36 months

InterventionParticipants (Count of Participants)
Open-Label Intervention9

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No Reported Psychological Toxicity Based Upon Psychological Evaluations

Psychological toxicity defined as suicidal ideation (NCT00846430)
Timeframe: Psychological evaluation at 24 months

InterventionParticipants (Count of Participants)
Open-Label Intervention8

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Response by MRI Measurements

partial response by RICST criteria is defined as >50% tumor shrinkage (NCT00846430)
Timeframe: evaluated 6, 12 and 24 months compared to baseline

Interventionparticipants (Number)
Partial Response at 6 monthsComplete Response at 6 monthsLess than Partial Response at 6 monthsPartial Response at 12 monthsComplete Response at 12 monthsLess than Partial Response at 12 monthsPartial Response at 24 monthsComplete Response at 24 monthsLess than Partial Response at 24 monthsno longer participating at 24 months
Open-Label Intervention0182164113

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Change in GM-CSF

Change in GM-CSF stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib3.8
Arm 2: Calcitriol8.1
Arm 3: Celecoxib Plus Calcitriol14.3
Arm 4: No Treatment3.2

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Change in IFN-gamma Levels

Change in IFN-gamma stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib1.9
Arm 2: Calcitriol2.8
Arm 3: Celecoxib Plus Calcitriol6.3
Arm 4: No Treatment2.0

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Change in IL-2 Levels

Change in IL-2 stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib1.8
Arm 2: Calcitriol4.0
Arm 3: Celecoxib Plus Calcitriol7.9
Arm 4: No Treatment2.1

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Change in IL-6 Levels.

Change in levels of immune inhibitory/inflammatory mediator IL-6 in tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib39
Arm 2: Calcitriol46
Arm 3: Celecoxib Plus Calcitriol29
Arm 4: No Treatment132

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Total Patient Pain Relief Over 0 to 8 Hours.

"Total patient pain relief was assessed as a time-weighted sum of the patient pain assessments at each individual time point from 0-8 hours.~Values for TOTPAR are measured from 0 to 4 on the Pain Relief Scale 0 None Min; 1 A little; 2 Some; 3 A lot; 4 Complete Max~The TOTPAR is a weighted measure of the observations; the minimum possible value is 0 and the maximum possible value is 32." (NCT00964431)
Timeframe: 8 hours

Interventionunits on a scale (Least Squares Mean)
Indomethacin Test (Lower Dose)10.794
Indomethacin Test (Upper Dose)12.564
Celecoxib 400 mg14.822
Placebo3.019

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Toxicity

Number of participants with acute and late toxicity (NCT00970502)
Timeframe: 30 DAYS

Interventionparticipants (Number)
Celecoxib 200mg0
Celecoxib 400mg1
Celecoxib 600mg2

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Clinical Response

Response to Concurrent Erlotinib, Celecoxib, and Reirradiation according to Response Evaluation Criteria in Solid Tumors - Complete Response (CR): Disappearance of all target lesions Partial Response (PR): At least a 30% decrease in the sum of the LD of target lesions, taking as reference the baseline sum LD Progressive Disease (PD): At least a 20% increase in the sum of the LD of target lesions, taking as reference the smallest sum LD recorded since the treatment started or the appearance of one or more new lesions (NCT00970502)
Timeframe: 20 months

InterventionParticipants (Count of Participants)
Complete Response(CR)Pathologic partial response (pPR)Progressive disease (PD)No evidence of disease (NED)
Erlotinib + Celecoxib6152

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Locoregional Control, Progression-free Survival, Overall Survival and Late Toxicity

At a median follow-up of 11 months, the 1 year locoregional control, progression-free survival, and overall survival rates. (NCT00970502)
Timeframe: 1 year

Interventionpercentage of participants (Number)
locoregional controlprogress-free survivaloverall survival rateslong term toxicity
Erlotinib + Celecoxib6037550

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Locoregional Progression

Patients with locoregional and/or distant progression (NCT00970502)
Timeframe: 20 months

Interventionparticipants (Number)
free of diseaseisolated locoregional progressionisolated distant progressionboth locoregional and distant progressionno evidence of disease, died of comorbid illness
Erlotinib + Celecoxib44213

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"Patient Impressions Within 8 Days Post-first Dose (the Number of Subjects Who Have Rated Excellent and Good)"

"The patient impression of the study medication was entered in the patient diary based on the following categories: excellent, good, fair and poor.~Efficacy was based on the patient impression of the study medication (excellent and good) from the first study medication until each time point." (NCT00976716)
Timeframe: 6 hours post first dose and before sleep on Day 1, before sleep on Day 2, Day 4 (Visit 2) and Day 8 (Visit 3)

InterventionParticipants (Number)
Day 1, 6 hours post first dose (n=80)Day 1, before sleep (n=80)Day 2, before sleep (n=80)Visit 2 (Day 4), (n=80)Visit 3 (Day 8), (n=68)
Celecoxib4448556060

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Withdrawal Due to Lack of Efficacy

The number of subjects who withdrew due to insufficient clinical response was evaluated. (NCT00976716)
Timeframe: 8 days

InterventionParticipants (Number)
Celecoxib0

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"Patient Impressions at Final Visit (the Number of Participants Who Have Rated Excellent and Good)"

"The patient impression of the study medication was entered in the patient diary based on the following categories: excellent, good, fair and poor.~Efficacy was based on the patient impression of the study medication (excellent and good) from the first study medication until Final Visit." (NCT00976716)
Timeframe: 8 days

InterventionParticipants (Number)
Celecoxib70

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Pain Intensity Differences (PID) in Pain at Rest (Spontaneous Pain) Within 8 Days Post-first Dose

The PID score was obtained by subtracting the PI (by VAS: 0 mm=no pain, 100 mm=worst possible pain) at each time point from the Baseline PI score. Increase in PID scores indicated a lessening of subjects' pain compared to baseline scores; higher scores indicated a greater reduction in pain. (NCT00976716)
Timeframe: Two, 4 and 6 hours post first dose, and before sleep on Day 1, on awakening and before sleep on Days 2 to 7, on awakening on Day 8 and Visit 3 (Day 8)

Interventionmm (Mean)
Day 1, 2 hours post first dose (n=80)Day 1, 4 hours post first dose (n=80)Day 1, 6 hours post first dose (n=80)Day 1, before sleep (n=80)Day 2, on awakening (n=80)Day 2, before sleep (n=80)Day 3, on awakening (n=80)Day 3, before sleep (n=78)Day 4, on awakening (n=78)Day 4, before sleep (n=73)Day 5, on awakening (n=73)Day 5, before sleep (n=68)Day 6, on awakening (n=68)Day 6, before sleep (n=68)Day 7, on awakening (n=68)Day 7, before sleep (n=55)Day 8, on awakening (n=55)Visit 3 (Day 8) (n=73)Final Visit (LOCF, n=80)
Celecoxib12.617.419.621.825.130.935.137.941.341.844.345.448.048.849.250.251.352.452.6

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Summary of Adverse Events

The number of subjects who experienced adverse events (AEs; all-causality and treatment-related) based on safety assessment was summarized. The severity and seriousness of treatment-emergent AEs as well as discontinuations, dose reductions and temporary discontinuations (DR/TD) due to treatment-emergent AEs were also summarized. (NCT00976716)
Timeframe: 8 days

InterventionParticipants (Number)
AEs: all-causalityAEs: treatment-relatedSevere AEs: all-causalitySevere AEs: treatment-realtedSerious AEs: all-causalitySerious AEs: treatment-relatedDiscontinuation due to all-causality AEsDiscontinuation due to treatment-related AEsDR/TD due to all-causality AEsDR/TD due to treatment-related AEs
Celecoxib10800001100

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Sum of Pain Intensity Differences (SPID) for Pain at Rest (Spontaneous Pain) and on Active Movement Until 6 Hours Post-first Dose

The SPID was derived according to the following rule: each PID was weighted by the width of time interval between previous and current time points in hours and summed up to 6 hours post-first dose (NCT00976716)
Timeframe: 6 hours

Interventionmm (Mean)
Pain at rest (n=80)Pain on active movement (n=77)
Celecoxib99.3118.2

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Severity of Inflammatory Symptoms (Swelling) Within 8 Days Post-first Dose

"The investigator assessed the swelling, using the categories None, Mild, Moderate, and Severe at Baseline, Visit 2 (Day 4), Visit 3 (Day 8) and Final Visit." (NCT00976716)
Timeframe: Baseline, Days 4 (Visit 2) and 8 (Visit 3)

InterventionParticipants (Number)
None at Baseline (n=80)None at Visit 2 (Day 4) (n=80)None at Visit 3 (Day 8) (n=68)None at Final Visit (n=80)Mild at Baseline (n=80)Mild at Visit 2 (Day 4) (n=80)Mild at Visit 3 (Day 8) (n=68)Mild at Final Visit (n=80)Moderate at Baseline (n=80)Moderate at Visit 2 (Day 4) (n=80)Moderate at Visit 3 (Day 8) (n=68)Moderate at Final Visit (n=80)Severe at Baseline (n=80)Severe at Visit 2 (Day 4) (n=80)Severe at Visit 3 (Day 8) (n=68)Severe at Final Visit (n=80)
Celecoxib05384124692635485448100

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Severity of Inflammatory Symptoms (Redness) Within 8 Days Post-first Dose

"The investigator assessed the redness, using the categories None, Mild, Moderate, and Severe at Baseline, Visit 2 (Day 4), Visit 3 (Day 8) and Final Visit." (NCT00976716)
Timeframe: Baseline, Days 4 (Visit 2) and 8 (Visit 3)

InterventionParticipants (Number)
None at Baseline (n=80)None at Visit 2 (Day 4) (n=80)None at Visit 3 (Day 8) (n=68)None at Final Visit (n=80)Mild at Baseline (n=80)Mild at Visit 2 (Day 4) (n=80)Mild at Visit 3 (Day 8) (n=68)Mild at Final Visit (n=80)Moderate at Baseline (n=80)Moderate at Visit 2 (Day 4) (n=80)Moderate at Visit 3 (Day 8) (n=68)Moderate at Final Visit (n=80)Severe at Baseline (n=80)Severe at Visit 2 (Day 4) (n=80)Severe at Visit 3 (Day 8) (n=68)Severe at Final Visit (n=80)
Celecoxib16516473402847191005000

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Severity of Inflammatory Symptoms (Localized Warmth) Within 8 Days Post First Dose

"The investigator assessed the localized warmth, using the categories None, Mild, Moderate, and Severe at Baseline, Visit 2 (Day 4), Visit 3 (Day 8) and Final Visit." (NCT00976716)
Timeframe: Baseline, Days 4 (Visit 2) and 8 (Visit 3)

InterventionParticipants (Number)
None at Baseine (n=80)None at Visit 2 (Day 4) (n=80)None at Visit 3 (Day 8) (n=68)None at Final Visit (n=80)Mild at Baseine (n=80)Mild at Visit 2 (Day 4) (n=80)Mild at Visit 3 (Day 8) (n=68)Mild at Final Visit (n=80)Moderate at Baseine (n=80)Moderate at Visit 2 (Day 4) (n=80)Moderate at Visit 3 (Day 8) (n=68)Moderate at Final Visit (n=80)Severe at Baseine (n=80)Severe at Visit 2 (Day 4) (n=80)Severe at Visit 3 (Day 8) (n=68)Severe at Final Visit (n=80)
Celecoxib8636676431724230006000

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PID in Pain on Active Movement Within 8 Days Post-first Dose

The PID score was obtained by subtracting the PI at each time point from the Baseline PI score. Increase in scores indicated a lessening of subjects' pain compared to baseline scores; higher scores indicated a greater reduction in pain. (NCT00976716)
Timeframe: 2, 4 and 6 hours post first dose, and before sleep on Day 1, on awakening and before sleep on Days 2 to 7, on awakening on Day 8 and Visit 3 (Day 8)

Interventionmm (Mean)
Day 1, 2 hours post first dose (n=77)Day 1, 4 hours post first dose (n=77)Day 1, 6 hours post first dose (n=77)Day 1, before sleep (n=77)Day 2, on awakening (n=77)Day 2, before sleep (n=77)Day 3, on awakening (n=77)Day 3, before sleep (n=75)Day 4, on awakening (n=75)Day 4, before sleep (n=70)Day 5, on awakening (n=70)Day 5, before sleep (n=66)Day 6, on awakening (n=66)Day 6, before sleep (n=66)Day 7, on awakening (n=66)Day 7, before sleep (n=55)Day 8, on awakening (n=55)Visit 3 (Day 8) (n=71)Final Visit (LOCF, n=78)
Celecoxib14.320.424.326.530.336.140.243.248.549.552.553.557.558.459.662.163.363.663.7

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PI of Pain on Active Movement as Measured by VAS Within 8 Days Post-first Dose

The PI of pain on active movement was recorded on the 100 mm VAS in the patient diary, where 0 mm=no pain, 100 mm=worst possible pain. (NCT00976716)
Timeframe: Baseline, 2, 4 and 6 hours post first dose, and before sleep on Day 1, on awakening and before sleep on Days 2 to 7, on awakening on Day 8 and Visit 3 (Day 8)

Interventionmm (Mean)
Baseline (n=79)Day 1, 2 hours post first dose (n=77)Day 1, 4 hours post first dose (n=77)Day 1, 6 hours post first dose (n=77)Day 1, before sleep (n=77)Day 2, on awakening (n=77)Day 2, before sleep (n=77)Day 3, on awakening (n=77)Day 3, before sleep (n=75)Day 4, on awakening (n=75)Day 4, before sleep (n=70)Day 5, on awakening (n=70)Day 5, before sleep (n=66)Day 6, on awakening (n=66)Day 6, before sleep (n=66)Day 7, on awakening (n=66)Day 7, before sleep (n=55)Day 8, on awakening (n=55)Visit 3 (Day8) (n=71)Final Visit (LOCF, n=78)
Celecoxib75.561.455.351.549.345.539.735.532.427.226.423.523.219.218.217.115.514.312.111.8

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Peak Pain Intensity Difference (PPID) for Pain at Rest (Spontaneous Pain) and on Active Movement Until 6 Hours Post-first Dose

The PPID was obtained by subtracting the maximum value of pain intensity (PI) at a time point among 2 to 6 hours post first dose from baseline value of PI for each patient. (NCT00976716)
Timeframe: Two, 4 and 6 hours post first dose

Interventionmm (Mean)
Pain at rest (n=80)Pain on active movement (n=77)
Celecoxib22.226.7

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Pain Intensity (PI) of Pain at Rest (Spontaneous Pain) as Measured by Visual Analog Scale (VAS) Within 8 Days Post-first Dose

The PI of pain at rest (spontaneous pain) was recorded on the 100 mm VAS in the patient diary, where 0 mm=no pain, 100 mm=worst possible pain. (NCT00976716)
Timeframe: Baseline, 2, 4 and 6 hours post first dose, and before sleep on Day 1, on awakening and before sleep on Days 2 to 7, on awakening on Day 8 and Visit 3 (Day 8)

Interventionmm (Mean)
Baseline (n=80)Day 1, 2 hours post first dose (n=80)Day 1, 4 hours post first dose (n=80)Day 1, 6 hours post first dose (n=80)Day 1, before sleep (n=80)Day 2, on awakening (n=80)Day 2, before sleep (n=80)Day 3, on awakening (n=80)Day 3, before sleep (n=78)Day 4, on awakening (n=78)Day 4, before sleep (n=73)Day 5, on awakening (n=73)Day 5, before sleep (n=68)Day 6, on awakening (n=68)Day 6, before sleep (n=68)Day 7, on awakening (n=68)Day 7, before sleep (n=55)Day 8, on awakening (n=55)Visit 3 (Day 8) (n=73)Final Visit (LOCF, n=80)
Celecoxib59.947.342.540.338.134.829.024.821.818.417.815.315.012.411.611.39.78.67.27.3

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Total Patient Pain Relief Over 0 to 12 Hours.

"Total patient pain relief was assessed as a time-weighted sum of the patient pain assessments at each individual time point from 0-12 hours.~Values for TOTPAR are measured from 0 to 4 on the Pain Relief Scale 0 None Min; 1 A little; 2 Some; 3 A lot; 4 Complete Max~The TOTPAR is a weighted measure of the observations; the minimum possible value is 0 and the maximum possible value is 60." (NCT00985439)
Timeframe: 12 hours.

Interventionunits on a scale (Least Squares Mean)
Diclofenac Test (Lower Dose)17.770
Diclofenac Test (Upper Dose)16.893
Celecoxib 400 mg14.685
Placebo5.486

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Incidence of Any Gastric, and Duodenal Ulcers

The percentage of subjects who had gastric and duodenal endoscopic ulcers after 2 weeks treatment (The number of subjects who had gastric and duodenal endoscopic ulcers after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. (NCT00994461)
Timeframe: 2 weeks

,,
InterventionPercent (Number)
Gastric ulcersDuodenal ulcers
Celecoxib01.4
Loxoprofen25.05.3
Placebo2.70

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Incidence of Any Gastroduodenal, Gastric, and Duodenal Ulcers and/or Erosions

The percentage of subjects who had gastroduodenal, gastric, and duodenal endoscopic ulcers and/or erosions after 2 weeks treatment (The number of subjects who had gastroduodenal, gastric, and duodenal endoscopic ulcers and/or erosions after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. An erosion is defined as a lesion producing a definite break in the mucosa with equivocal depth. (NCT00994461)
Timeframe: 2 weeks

,,
InterventionPercent (Number)
Gastroduodenal ulcers and/or erosionsGastric ulcers and/or erosionsDuodenal ulcers and/or erosions
Celecoxib36.535.14.1
Loxoprofen53.953.95.3
Placebo24.324.30

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Number of Gastroduodenal Erosions in Each Subject

Number of subjects for each number of gastroduodenal endoscopic erosions after 2 weeks treatment (An erosion is defined as a lesion producing a definite break in the mucosa with equivocal depth.) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
0 erosion1 erosion2 erosions3 erosions4 erosions5 erosions6 erosions7 erosions8 erosions9 erosions10 or more erosions
Celecoxib4714450021001
Loxoprofen4113394311100
Placebo295120000000

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Number of Gastroduodenal Ulcers in Each Subject

Number of subjects for each number of gastroduodenal endoscopic ulcers after 2 weeks treatment (An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth.) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
0 ulcer1 ulcer2 ulcers3 ulcers4 ulcers5 ulcers6 ulcers7 ulcers8 ulcers9 ulcers10 or more ulcers
Celecoxib731000000000
Loxoprofen5510520012100
Placebo361000000000

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Post-treatment Gastroduodenal Endoscopic Scores (According to Mucosal Grading Scale)

Number of subjects for each gastroduodenal endoscopic score (according to Mucosal Grading Scale) after 2 weeks treatment (Score 0 = normal mucosa (no visible lesions); Score 1 = 1 to 10 petechiae; Score 2 = more than 10 petechiae; Score 3 = 1 to 5 erosions; Score 4 = 6 to 10 erosions; Score 5 = 11 to 25 erosions; Score 6 = more than 25 erosions; Score 7 = ulcer) (NCT00994461)
Timeframe: 2 weeks

,,
InterventionParticipants (Number)
Score 0Score 1Score 2Score 3Score 4Score 5Score 6Score 7
Celecoxib3881224001
Loxoprofen33201910021
Placebo226080001

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Incidence of Gastroduodenal Ulcers

The percentage of subjects who had gastroduodenal endoscopic ulcers after 2 weeks treatment (The number of subjects who had gastroduodenal endoscopic ulcers after 2 weeks treatment divided by participants multiplied by 100.) An ulcer is defined as any break in the mucosa at least 3 mm in diameter with unequivocal depth. (NCT00994461)
Timeframe: 2 weeks

InterventionPercent (Number)
Celecoxib1.4
Loxoprofen27.6
Placebo2.7

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Incidence of Treatment-emergent, All-causality GI Body System Adverse Events

The percentage of subjects who had treatment-emergent, all-causality gastrointestinal body system adverse events after 2 weeks treatment (The number of subjects who had treatment-emergent, all-causality gastrointestinal body system adverse events after 2 weeks treatment divided by participants multiplied by 100.) (NCT00994461)
Timeframe: 2 weeks

InterventionPercent (Number)
Celecoxib24.3
Loxoprofen47.4
Placebo16.2

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Median Urinary LTE4 Levels (Pre and Post Treatment)

Pre and Post treatment differences in urinary LTE4 levels measured in each treatment arm compared using paired t-test should the data conform to the normality assumption or one-sample Wilcoxon rank-sum test. LTE4 levels reported as median with full range (pg/mg creatinine) for Pre treatment versus Post treatment LTE4 levels among study participants compliant to treatment with evaluable urine samples at both time points (baseline and Day 6 +/- 1 day). (NCT01021215)
Timeframe: Baseline and day 6

,
Interventionpg/mg creatinine (Median)
Pre LTE4 levelsPost LTE4 levels
Arm I: Zileuton10742
Arm II: Zileuton and Celecoxib8630

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Proportion of Cases With a Post-treatment Increase in Urinary PGE-M Levels

Proportion of cases with a post-treatment increase in urinary PGE-M levels by comparing those treated with Zileuton and Celecoxib combined therapy compared to those treated with Zileuton alone. Pre/postchange in levels (Increase) derived from baseline level to Day 6 +/- 1 day. Differences in baseline levels between 2 treatment arms were examined using the Wilcoxon rank-sum test. (NCT01021215)
Timeframe: Baseline to Day 6

Interventionproportion of participants (Number)
Arm I: Zileuton.37
Arm II: Zileuton and Celecoxib.06

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Median Urinary PGE-M Levels (Pre and Post Treatment)

Pre and Post treatment differences in urinary PGE-M levels measured in each treatment arm. PGE-M levels reported as median with full range (ng/mg creatinine) for Pre treatment versus Post treatment PGE-M levels among study participants compliant to treatment with evaluable urine samples at both time points (baseline and Day 6 +/- 1 day). (NCT01021215)
Timeframe: Baseline and Day 6

,
Interventionng/mg creatinine (Median)
Pre PGE-M LevelsPost PGE-M Levels
Arm I: Zileuton12.810.5
Arm II: Zileuton and Celecoxib13.43.9

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Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the Median Quartile (Q2)

prognostic value of urinary prostaglandin metabolites (PGE-M) levels for worse PFS for patients who had baseline urinary PGE-M above/below the median quartile (Q2, 15.38). Progression free survival (PFS) is defined as the time from the date of randomization to the date of disease progression or death resulting from any cause, whichever comes first. Progression is defined according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. The median and 95% confidence intervals are estimated using the Kaplan-Meier estimator. (NCT01041781)
Timeframe: Up to 5 years

Interventionmonths (Median)
PGE-M < Q26.2
PGE-M >= Q24.2

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Response Rate

The response rate (percentage) is the percent of patients whose best response was Complete Response (CR) or Partial Response (PR) as defined by RECIST 1.1 criteria. Percentage of successes will be estimated by 100 times the number of successes divided by the total number of evaluable patients. Response rates (including complete and partial response) will be tested using Fisher's exact test (NCT01041781)
Timeframe: Up to 5 years

Interventionpercentage of patients (Number)
Arm I (Arm A: Celecoxib + Standard Chemotherapy)40
Arm II (Arm B: Placebo + Standard Chemotherapy)35

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Progression-free Survival

Progression free survival (PFS) is defined as the time from the date of randomization to the date of disease progression or death resulting from any cause, whichever comes first. Progression is defined according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. The median and 95% confidence intervals are estimated using the Kaplan-Meier estimator. (NCT01041781)
Timeframe: Time between randomization and disease relapse or death from any cause, assessed up to 5 years

Interventionmonths (Median)
Arm I (Arm A: Celecoxib + Standard Chemotherapy)5.16
Arm II (Arm B: Placebo + Standard Chemotherapy)5.26

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Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the Third Quartile (Q3)

Prognostic value of urinary prostaglandin metabolites (PGE-M) levels for worse PFS for patients who had baseline urinary PGE-M above/below the median quartile (Q3, 27.86). Progression free survival (PFS) is defined as the time from the date of randomization to the date of disease progression or death resulting from any cause, whichever comes first. Progression is defined according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. The median and 95% confidence intervals are estimated using the Kaplan-Meier estimator. (NCT01041781)
Timeframe: Up to 5 years

Interventionmonths (Median)
PGE-M < Q36.0
PGE-M >= Q33.0

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Overall Survival

Overall survival time is defined as the time from randomization to death due to any cause. The median and 95% confidence intervals are estimated using the Kaplan-Meier estimator. (NCT01041781)
Timeframe: Time between randomization and death from any cause, assessed up to 5 years

Interventionmonths (Median)
Arm I (Arm A: Celecoxib + Standard Chemotherapy)11.4
Arm II (Arm B: Placebo + Standard Chemotherapy)12.5

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Incidence of Toxicities as Assessed by NCI CTCAE v. 4.0

The overall toxicity rates (percentages) for grade 3 or higher adverse events considered at least possibly related to treatment (NCT01041781)
Timeframe: Up to 5 years

Interventionpercentage of patients (Number)
Arm I (Arm A: Celecoxib + Standard Chemotherapy)61.04
Arm II (Arm B: Placebo + Standard Chemotherapy)55.06

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Prognostic Value of Urinary Prostaglandin Metabolites (PGE-M) Levels for Worse PFS for Patients Who Had Baseline Urinary PGE-M Above/Below the First Quartile (Q1)

Prognostic value of urinary prostaglandin metabolites (PGE-M) levels for worse PFS for patients who had baseline urinary PGE-M above/below the first quartile (Q1, 10.09). Progression free survival (PFS) is defined as the time from the date of randomization to the date of disease progression or death resulting from any cause, whichever comes first. Progression is defined according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. The median and 95% confidence intervals are estimated using the Kaplan-Meier estimator. (NCT01041781)
Timeframe: Up to 5 years

Interventionmonths (Median)
PGE-M < Q17.7
PGE-M >= Q14.9

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Number of Participants in Each Pain Intensity (PI) With 4 Categories

"Pain intensity was entered in the patient diary on the following categories: No pain, Mild pain, Moderate pain and Severe pain." (NCT01062113)
Timeframe: 2 hours after additional dose

,
Interventionparticipants (Number)
NoneMildModerateSevere
Additional Dose Celecoxib 200mg1134181
Additional Dose Placebo324283

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Pain Intensity Measured by Visual Analog Scale (VAS)

The Pain intensity was recorded on the 100 mm VAS in the patient diary, where 0 mm=no pain, 100 mm=unbearable maximal pain. (NCT01062113)
Timeframe: 2 hours post-additional dose

Interventionmm (Mean)
Additional Dose Celecoxib 200 mg35.8
Additional Dose Placebo51.9

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Efficacy Rate (Percentage) of Patient's Impression

"Patient's impression was assessed by self-report and was entered in the patient diary, based on the following categories: Excellent, Good, Fair and Poor.~Efficacy rate was calculated from the following formula, The number of participants assessed as Excellent or Good over total participants multiplied by 100." (NCT01062113)
Timeframe: 2 hours post-additional dose

Interventionpercentage of participants (Number)
Additional Dose Celecoxib 200 mg64.1
Additional Dose Placebo25.9

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Differences in Pain Intensity (PI) Measured by VAS Among Participants

The differences in PI were obtained by subtracting the PI at each time point from the Baseline PI score. (NCT01062113)
Timeframe: Pre-additional dose (baseline) and 2 hours post-additional dose

Interventionmm (Mean)
Additional Dose Celecoxib 200 mg33.4
Additional Dose Placebo12.3

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Peak Estradiol Level

Average serum levels of estradiol (pg/mL) normalized to days of the luteal phase of menstrual cycle. (NCT01129245)
Timeframe: 4 cycles (approximately 4 months)

Interventionpg/mL (Mean)
Control Cycle274
Pre-LH Celecoxib289.4
Post-LH Surge Celecoxib282.2

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Peak Hormone Levels

Average serum levels of progesterone (ng/mL) and luteinizing hormone (ng/mL) normalized to days of the luteal phase of menstrual cycle. (NCT01129245)
Timeframe: 4 cycles (approximately 4 months)

,,
Interventionng/mL (Mean)
LH (luteinizing hormone)P (progesterone)
Control Cycle39.713.3
Post-LH Surge Celecoxib42.612.3
Pre-LH Celecoxib46.213.5

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Number of Cycles With Ovulation Dysfunction When Taken After Ovulation: Extended Luteal Phase

One cycle corresponds to one participant (NCT01129245)
Timeframe: 4 cycles (approximately 4 months)

InterventionParticipants (Count of Participants)
Control Cycle1
Pre-LH Celecoxib6
Post-LH Surge Celecoxib5

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Disease-free Survival

Disease-Free Survival (DFS) is defined as the time of randomization until documented progression or death from any cause. The endpoint of this trial is to compare disease-free survival of patients with stage III colon cancer randomized to standard chemotherapy only (FOLFOX; Arm A and Arm C) or standard chemotherapy (FOLFOX) with 3 years of celecoxib 400 mg daily (Arm B and Arm D). The percentage of patients who were alive and disease free after 3 years are reported here. A log-rank test stratified with the stratification factors was used to compare disease-free survival (celecoxib vs placebo) (NCT01150045)
Timeframe: At 3 years of follow-up

Interventionpercentage of participants (Number)
FOLFOX and Placebo (Arms A +C)73.4
FOLFOX Plus Celecoxib Daily (Arms B + D)76.3

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Overall Survival

Overall Survival (DFS) is defined as the time of randomization until documented death from any cause. The endpoint is to compare overall survival of patients with stage III colon cancer randomized to standard chemotherapy only (FOLFOX; Arm A and Arm C) or standard chemotherapy (FOLFOX) with 5 years of celecoxib 400 mg daily (Arm B and Arm D). The percentage of patients who were alive after 3 years are reported here. (NCT01150045)
Timeframe: up to 3 years from registration

Interventionpercentage of participants (Number)
FOLFOX and Placebo (Arms A +C)81.6
FOLFOX Plus Celecoxib Daily (Arms B + D)84.3

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Duration of Response

The duration of overall response is measured from the time measurement criteria are met for CR or PR (whichever is first recorded) until the first date that recurrent or progressive disease is objectively documented (taking as reference for progressive disease the smallest measurements recorded since the treatment started, including baseline). The duration of overall CR is measured from the time measurement criteria are first met for CR until the first date that recurrent disease is objectively documented. (NCT01158534)
Timeframe: end of study

Interventionmonths (Median)
Celecoxib and Recombinant Interferon Alpha-2b8.7

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Overall Survival

Overall survival measured in months and summarized using the Kaplan-Meier method. (NCT01158534)
Timeframe: death

Interventionmonths (Median)
Celecoxib and Recombinant Interferon Alpha-2b14.4

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Progression-free Survival

Progression-free survival measured in months and summarized using the Kaplan-Meier method. Time to objective progression will be measured from the start of treatment until the criteria for progression are met, taking as reference the smallest measurements recorded since the treatment started, including baseline. (NCT01158534)
Timeframe: to progression

Interventionmonths (Median)
Celecoxib and Recombinant Interferon Alpha-2b5.6

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Objective Response Rate Assessed by RECIST Criteria.

The best overall response is the best response recorded from the start of the treatment until disease progression/recurrence (taking as reference for progressive disease the smallest measurements recorded since the treatment started, including baseline). The patient's best response assignment will depend on the achievement of both measurement and confirmation criteria. Objective response will be assessed by RECIST criteria. (NCT01158534)
Timeframe: at week 4 of cycle 2 and every other cycle thereafter

Interventionparticipants (Number)
Complete ResponsePartial ResponseStable DiseaseNo Response
Celecoxib and Recombinant Interferon Alpha-2b0359

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Number of Patients With Statistically Significant Change in Cellular Immune Parameters From Baseline to 2 Months

To evaluate the effect of celecoxib and interferon alpha therapy on cellular immune parameters. Absolute change following two cycles of therapy. (NCT01158534)
Timeframe: at two months from start of treatment

Interventionparticipants (Number)
Celecoxib and Recombinant Interferon Alpha-2b0

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PSA Response

PSA response was defined as a decrease in slope of at least 25%, when log (PSA) is plotted vs. time. (NCT01220973)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Atorvastatin and Celecoxib14

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Level of Pain

Patients will rate their pain for 7 days after surgery using an 11-point visual analog scale, ranging from 0 to 10, in which 0= no pain, 10=worst pain ever. Patients are asked to rate their pain up to four times a day during the post-operative period. Pain scores from each post-operative day each day will be averaged and reported as the pain score for that day. (NCT01323595)
Timeframe: 1 week after surgery

InterventionAnalog pain scale (Mean)
Placebo Treatment6
Celecoxib4

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Number of Participants With Bleeding Complications

We will record whether there are any bleeding complications associated with treatment after surgery. (NCT01323595)
Timeframe: 7 days after surgery

InterventionParticipants (Count of Participants)
Celecoxib0
Sugar Pill0

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Change of WOMAC-Stiffness Subscale at Day 28 From Baseline

"Version 3.1 of the WOMAC knee and hip osteoarthritis index translated in Korean language was used to evaluate the stiffness of the index joint. Two questions were to evaluate Stiffness of the index joint. A higher WOMAC-Stiffness score represents worse symptom severity, with 20 being the worst possible total score (minimum total: 0 point, maximum total: 20 points)." (NCT01341405)
Timeframe: Baseline, Day 28

Interventionunits on a scale (Mean)
CG100649 2mg-3.17
CG100649 4mg-2.87
Celecoxib 200 mg-2.32

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Change of WOMAC-Physical Function Subscale at Day 28 From Baseline

"Version 3.1 of the WOMAC knee and hip osteoarthritis index translated in Korean language was used. The total 17 questions to evaluate Physical Function. A higher score of WOMAC-Physical function subscale represents worse symptom severity, with 170 being the worst possible total score (minimum total: 0 point, maximum total: 170 points)." (NCT01341405)
Timeframe: Baseline, Day 28

Interventionunits on a scale (Mean)
CG100649 2mg-32.44
CG100649 4mg-26.26
Celecoxib 200 mg-28.24

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Change of the WOMAC Pain Subscale at Day 28 From Baseline

Changes in the WOMAC Pain Score from Baseline The primary endpoint of this study was the change in the sum of the WOMAC Pain subscale at Day 28 vs. Baseline (Day 1) using the ITT population). Pain scores were evaluated using the WOMAC Pain subscale, which provided an evaluation of pain during the past 48 hours using a 0-10 numerical rating scale for each of 5 questions (minimum total: 0 point, maximum total: 50 points). A higher WOMAC Pain score represented worse symptom severity. (NCT01341405)
Timeframe: Baseline, Day 28

Interventionunits on a scale (Mean)
CG100649 2mg-14.33
CG100649 4mg-12.47
Celecoxib 200 mg-13.24

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Change of the Sum of WOMAC OA Index at Day 28 From Baseline

The numerical rating scale version of the Western Ontario and McMaster Universities (WOMAC) OA index will be used-i.e., with the patient assessing each question by a 11-point (0-10) numerical rating scale, and the total index score being represented by the sum of the 24 component item scores. A higher WOMAC score represents worse symptom severity, with 240 being the worst possible total score (minimum total: 0 point, maximum total: 240 points). (NCT01341405)
Timeframe: Baseline, Day 28

Interventionunits on a scale (Mean)
CG100649 2mg-49.94
CG100649 4mg-41.61
Celecoxib 200 mg-43.80

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Percentage of Participants With Presence of Joint Swelling and Effusion

Study knees were evaluated at each visit for the presence or absence of swelling and effusion. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventionpercentage of participants (Number)
BaselineVisit 9 (Day 728)
Celecoxib (Celebrex)56.717.7
Chondroitin Sulfate (Condrosan)60.810.3

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WOMAC Pain Subscale

Western Ontario & McMaster Universities Osteoarthritis Index (WOMAC) Pain subscale Score Range: 0 (no pain) - 50 (maximum pain) The study was designed such that the outcome of primary interest is knee pain related to OA. The measure selected to best evaluate this is an improvement in the WOMAC pain subscales. This subscale consists of 5 items which assesses the pain during walking, using stairs, in bed, sitting or lying, and standing.Each item is a 10 cm VAS with 0 and 10 cm representing no pain and extreme pain respectively. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventioncentimeters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)25.5113.6210.69
Chondroitin Sulfate (Condrosan)25.614.7113.51

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Visual Analog Scale (VAS)

"Visual Analogue Scale: 0 No Pain 10 Maximum Pain Huskisson's VAS measures global pain intensity. Patients were asked to quantify their disease status on a 10 cm VAS as follows: Please indicate the severity of knee pain experienced during the last 48 hours by marking a (I) through the line. Left hand marker represents No pain and right hand marker represents The worst pain imaginable." (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventioncentimeters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)5.933.022.45
Chondroitin Sulfate (Condrosan)6.243.433.12

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Synovial Membrane Thickness

"To compare the severity of synovitis score (Thickness of the Synovial Membrane in mm) in Global Knee , at the baseline visit and the follow-up visits in subjects treated either with CHONDROITIN SULPHATE (CONDROSAN) or CELECOXIB.~The severity of synovitis was evaluated through four regions of interest (ROIs) in the images of the axial T1-weighted acquisition complemented with the use of the images of the axial T2-weighted acquisition. The thickness of the synovial membrane was evaluated in the global knee and each of the ROIs and results were expressed in millimetres. The four ROIs were the proximal lateral, distal lateral, proximal medial and distal medial." (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventionmilimeters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)0.961.071.16
Chondroitin Sulfate (Condrosan)0.991.051.19

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Synovial Fluid Volume

To compare the synovial fluid volume of the global knee at the Baseline visit and after 24 months. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventionmililiters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)10.799.499.07
Chondroitin Sulfate (Condrosan)13.8310.3010.97

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Short Form (SF-36) Health Survey

"The SF-36 is composed of 35 items measuring:~8 health concepts (or dimensions), [(Physical Functioning (PF), Role Physical (RP), Bodily Pain (BP), General Health (GH), Vitality (VT), Social Functioning (SF), Role Emotional (RE) and Mental Health (MH)]~and 1 reported health transition item.~The 8 health concepts are summarized in 1 physical (PCS) and 1 mental (MCS) component summary measures. PCS is represented by physical function, role limitations-physical, pain, and general health perception. MCS is represented by vitality, social function, role limitations-emotional, and mental health. Subscale items are summed and scaled from 0-100 to give subscale scores; 0= worst health related quality of life (HRQL), 100=best HRQL. PCS and MCS summary scores are constructed as T-scores (mean =50, standard deviation=10) with no minimum or maximum score; higher scores indicate better health status." (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
InterventionScores on a scales (Median)
Visit 2 (Baseline) Physical Component SummaryVisit 6 (Day 364) Physical Component SummaryVisit 9 (Day 728) Physical Component SummaryVisit 2 (Baseline) Mental Component SummaryVisit 6 (Day 364) Mental Component SummaryVisit 9 (Day 728) Mental Component Summary
Celecoxib (Celebrex)35.741.642.252.754.056.0
Chondroitin Sulfate (Condrosan)35.439.641.851.753.252.7

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Percentage of Participants With the Presence of Extrusion in the Meniscus

The presence of a meniscal extrusion was assessed in each of sub regions. The absence of a severe extrusion in all the sub regions was considered as an absence (score=0) of a severe extrusion in the meniscus. The presence of a severe extrusion in at least one region of the meniscus was sufficient to consider the presence (score=1) of a severe extrusion in the meniscus. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventionpercentage of participants (Number)
Visit 2 (Baseline) Medial meniscusVisit 6 (Day 364) Medial meniscusVisit 9 (Day 728) Medial meniscusVisit 2 (Baseline) Lateral meniscusVisit 6 (Day 364) Lateral meniscusVisit 9 (Day 728) Lateral meniscus
Celecoxib (Celebrex)47.453.660.33.12.93.2
Chondroitin Sulfate (Condrosan)47.453.656.16.27.28.8

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Cartilage Volume Loss of the Global Knee

To compare the cartilage volume loss of the global knee at the Baseline visit and after 12 and 24 months. (NCT01354145)
Timeframe: 12 months (Day 364) and 24 months (Day 728)

,
Interventioncubic milimeters (Mean)
Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)1177011572
Chondroitin Sulfate (Condrosan)1221011877

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WOMAC Stiffness Subscale

Western Ontario & McMaster Universities Osteoarthritis Index, from 0 No Stiffness to 20 Maximum Stiffness WOMAC stiffness subscale was used to measure the stiffness of the knee with pain. Two items are used to assess stiffness grade: after first waking and later in the day.Each item is a 10 cm VAS with 0 and 10 cm representing no difficulty and extreme difficulty respectively. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventioncentimeters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)11.656.605.44
Chondroitin Sulfate (Condrosan)10.766.536.15

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WOMAC Function Subscale

Western Ontario & McMaster Universities Osteoarthritis Index, from 0 No Function to 170 Maximum Function WOMAC functional limitation subscale was used to measure the functionality of the knee with pain. Seventeen items are used to assess functionality of the knee: tair use, rising from sitting, standing, bending, walking, getting in / out of a car, shopping, putting on / taking off socks, rising from bed, lying in bed, getting in / out of bath, sitting, getting on / off toilet, heavy household duties, light household duties. Each item is a 10 cm VAS with 0 and 10 cm representing no difficulty and extreme difficulty respectively. (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventioncentimeters (Mean)
Visit 2 (Baseline)Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)89.551.046.2
Chondroitin Sulfate (Condrosan)88.552.350.0

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Use of Acetaminophen

"Consumption of Acetaminophen: At each post-baseline visit, the investigator had to assess the consumption of acetaminophen, rescue analgesic authorised throughout the study, by reporting the number of caplets dispensed/retrieved since the previous visit.~Daily consumption of acetaminophen was calculated as an average." (NCT01354145)
Timeframe: 3 months (Day 91), 6 momnths (Day 182), 12 months (Day 364), 18 monts (Day 546) and 24 months (Day 728)

InterventionDaily number of caplets taken (Mean)
Chondroitin Sulfate (Condrosan)1.17
Celecoxib (Celebrex)0.94

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Bone Marrow Lesions Score

"To compare the bone marrow lesions (BMLs) score in the global knee and the different sub regions at the baseline visit and the follow-up visits in subjects treated either with CHONDROITIN SULPHATE (CONDROSAN) or CELECOXIB.~The BMLs were assessed in the global knee and the different sub region of the knee (medial trochlea, plateau of the medial femoro-tibial joint, femur of the medial femoro-tibial joint, medial posterior condyle, lateral trochlea, plateau of the lateral femoro-tibial joint, femur of the lateral femoro-tibial joint, lateral posterior femur). The BMLs score was defined as a grade (between 0 and 3) in each knee sub region and summed to derive a global knee score ranging between 0 (absent) and 30 (present). Specifically, each grade was scored as follows:~Grade 0 = Absence of lesion in the sub region~Grade 1 = less than 25% of the surface~Grade 2 = 25-50% of the surface~Grade 3 = more than 50% of the surface" (NCT01354145)
Timeframe: Baseline, 12 months (Day 364) and 24 months (Day 728)

,
Interventionunits on a scale (Mean)
Global Knee - Visit 2 (Baseline)Global Knee - Visit 6 (Day 364)Global Knee - Visit 9 (Day 728)
Celecoxib (Celebrex)2.652.773.37
Chondroitin Sulfate (Condrosan)2.573.163.58

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Cartilage Volume in the Medial Compartment

To compare the cartilage volume loss of the medial compartment at the Baseline visit and after 12 and 24 months. (NCT01354145)
Timeframe: 12 months (Day 364) and 24 months (Day 728)

,
Interventioncubic milimeters (Mean)
Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)55865439
Chondroitin Sulfate (Condrosan)57935672

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Cartilage Volume Loss of the Lateral Compartment

To compare the cartilage volume loss of the lateral compartment (femoral condyle and tibial plateau) at the Baseline visit and after 12 and 24 months of treatment either with CHONDROITIN SULPHATE (CONDROSAN) 1200 mg daily or with CELECOXIB 200 mg daily. (NCT01354145)
Timeframe: 12 months (Day 364) and 24 months (Day 728)

,
Interventioncubic milimeters (Mean)
Visit 6 (Day 364)Visit 9 (Day 728)
Celecoxib (Celebrex)61966143
Chondroitin Sulfate (Condrosan)64086196

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Quality of Life, Social Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Social Function. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise87.3
NSAID80.4

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Quality of Life, Physical Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Performance. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise84.3
NSAID85.2

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Quality of Life, Physical Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Performance (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise30.5
NSAID36.0

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Quality of Life, Physical Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Performance (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise58.1
NSAID55.1

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Quality of Life, Physical Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Performance (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise77.3
NSAID72.5

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Quality of Life, Physical Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Function. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise64.6
NSAID66.5

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Quality of Life, Physical Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Function. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise75.8
NSAID70.3

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Quality of Life, Physical Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Function. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise84.1
NSAID82.6

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Quality of Life, Physical Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Physical Function. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise81.6
NSAID77.2

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Quality of Life, Mental Health.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Mental Health. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise66.4
NSAID67.0

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Quality of Life, Mental Health.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Mental Health. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise71.4
NSAID74.6

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Quality of Life, Mental Health.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Mental Health. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise76.4
NSAID75.6

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Quality of Life, General Health Perceptions.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: General Health Perceptions. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise64.3
NSAID64.7

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Quality of Life, General Health Perceptions.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: General Health Perceptions. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise66.3
NSAID67.1

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Quality of Life, Emotional Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Emotional Performance. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise67.2
NSAID63.4

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Quality of Life, General Health Perceptions.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: General Health Perceptions. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise73.4
NSAID69.3

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Quality of Life, General Health Perceptions.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: General Health Perceptions. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise72.0
NSAID69.2

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Quality of Life, Mental Health.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Mental Health. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise78.5
NSAID76.9

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Quality of Life, Emotional Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Emotional Performance. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise82.5
NSAID84.7

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Quality of Life, Emotional Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Emotional Performance. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise94.1
NSAID93.9

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Quality of Life, Emotional Performance.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Emotional Performance. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise91.2
NSAID82.4

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Quality of Life, Change in Health

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: change in health. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise52.6
NSAID54.5

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Quality of Life, Change in Health

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: change in health. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise60.4
NSAID61.3

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Quality of Life, Change in Health

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: change in health. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise78.0
NSAID70.7

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Quality of Life, Change in Health

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: change in health. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise73.3
NSAID67.0

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Quality of Life, Bodily Pain

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: bodily pain. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise39.5
NSAID39.2

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Quality of Life, Bodily Pain

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: bodily pain. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise57.8
NSAID54.0

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Quality of Life, Bodily Pain

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: bodily pain. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise74.1
NSAID68

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Quality of Life, Bodily Pain

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: bodily pain. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise67.6
NSAID58.7

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PHQ-9 Patient Health Questionnaire (PHQ-9) Depression

Depression was measured with the Patient Health Questionnaire (PHQ-9), which ranged from 0 (no depression) to 27 (severe depression). (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise5.7
NSAID5.1

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Quality of Life, Social Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Social Function. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise88.6
NSAID86

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PHQ-9 Patient Health Questionnaire (PHQ-9) Depression

Depression was measured with the Patient Health Questionnaire (PHQ-9), which ranged from 0 (no depression) to 27 (severe depression). (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise2.3
NSAID3.1

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PHQ-9 Patient Health Questionnaire (PHQ-9) Depression

Depression was measured with the Patient Health Questionnaire (PHQ-9), which ranged from 0 (no depression) to 27 (severe depression). (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise3.0
NSAID3.2

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Visual Analogue Scale of Pain

The best result is 0 and the worst is 100, Pain relief more than 25 mm on the Visual Analogue Scale, assessed 24 weeks after intervention. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise17.8
NSAID17.5

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Oswestry Disability Index

Function was assessed using the Oswestry Disability Index questionnaire Version 2.1a, which ranges from 0 to 100 (greater disability), being worst 100. The Oswestry Disability Index is currently considered by many as the gold standard for measuring degree of disability and estimating quality of life in a person with low back pain. 0% to 20%: Minimal disability, 21%-40%: Moderate Disability, 41%-60%: Severe Disability, 61%-80%: Crippling back pain, 81%-100%: These patients are either bed-bound or have an exaggeration of their symptoms. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise21.9
NSAID26.6

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Oswestry Disability Index

Function was assessed using the Oswestry Disability Index questionnaire Version 2.1a, which ranges from 0 to 100 (greater disability), being worst 100. The Oswestry Disability Index is currently considered by many as the gold standard for measuring degree of disability and estimating quality of life in a person with low back pain. 0% to 20%: Minimal disability, 21%-40%: Moderate Disability, 41%-60%: Severe Disability, 61%-80%: Crippling back pain, 81%-100%: These patients are either bed-bound or have an exaggeration of their symptoms. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise13.8
NSAID17.2

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Oswestry Disability Index

Function was assessed using the Oswestry Disability Index questionnaire Version 2.1a, which ranges from 0 to 100 (greater disability), being worst 100. The Oswestry Disability Index is currently considered by many as the gold standard for measuring degree of disability and estimating quality of life in a person with low back pain. 0% to 20%: Minimal disability, 21%-40%: Moderate Disability, 41%-60%: Severe Disability, 61%-80%: Crippling back pain, 81%-100%: These patients are either bed-bound or have an exaggeration of their symptoms. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise16.6
NSAID19.4

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Missing Workdays

This result shows the average of the number of missed work days. (NCT01374269)
Timeframe: 6 weeks before starting

InterventionDays (Mean)
Excercise1.0
NSAID1.7

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Missing Workdays

This result shows the average of the number of missed work days. (NCT01374269)
Timeframe: 4 weeks

InterventionDays (Mean)
Excercise0.0
NSAID0.3

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Missing Workdays

This result shows the average of the number of missed work days. (NCT01374269)
Timeframe: 24 weeks

InterventionDays (Mean)
Excercise0.2
NSAID0.2

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Missing Workdays

This result shows the average of the number of missed work days. (NCT01374269)
Timeframe: 12 weeks

InterventionDays (Mean)
Excercise0.0
NSAID0.1

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Medical Consultations.

This result shows, the total number of participants received additional medical consultations. (NCT01374269)
Timeframe: 4 weeks

Interventionparticipants (Number)
Excercise4
NSAID6

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Medical Consultations.

This result shows, the total number of participants received additional medical consultations. (NCT01374269)
Timeframe: 24 weeks

Interventionparticipants (Number)
Excercise4
NSAID4

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Medical Consultations.

This result shows, the total number of participants received additional medical consultations. (NCT01374269)
Timeframe: 12 weeks

Interventionparticipants (Number)
Excercise1
NSAID6

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Visual Analogue Scale of Pain

In the Visual Analogue Sacale the best result is 0 and the worst is 100, The primary outcome was pain the mesurement of the Visual Analog Scale (VAS) (0 [no pain] to 100 [maximum pain]) at the beginning. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise47.3
NSAID45.2

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Visual Analogue Scale of Pain

In the VAS the best result is 0 and the worst is 100. The primary outcome was pain improvement of ≥25 mm on the Visual Analog Scale (VAS) (0 [no pain] to 100 [maximum pain]) at 4 weeks. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise28.8
NSAID34.9

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Visual Analogue Scale of Pain

In the VAS the best result is 0 and the worst is 100. The primary outcome was pain improvement of ≥25 mm on the Visual Analog Scale (VAS) (0 [no pain] to 100 [maximum pain]) at 12 weeks. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise21.0
NSAID20.6

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Oswestry Disability Index

Function was assessed using the Oswestry Disability Index questionnaire Version 2.1a, which ranges from 0 to 100 (greater disability), being worst 100. The Oswestry Disability Index is currently considered by many as the gold standard for measuring degree of disability and estimating quality of life in a person with low back pain. 0% to 20%: Minimal disability, 21%-40%: Moderate Disability, 41%-60%: Severe Disability, 61%-80%: Crippling back pain, 81%-100%: These patients are either bed-bound or have an exaggeration of their symptoms. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise28.9
NSAID29.4

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Treatments Associated With Low Back Pain at 6 Months

we are showing in this result, the number of patients who had to receive any additional treatment in either group. The measure is the number of participants who received additional treatment throughout the duration of the study. (NCT01374269)
Timeframe: 6 months

Interventionparticipants (Number)
Excercise3
NSAID14

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Roland-Morris Questionnaire

Improvement in function assessed by the Roland-Morris questionnaire, a widely used health status measure for low back pain. The RMDQ can be used in research or clinical practice. Scoring the RMDQ. The RMDQ is scored by adding up the number of items checked by the patient. The score can therefore vary from 0 to 24. It is not recommended to give patients a 'Yes' / 'No' option. If patients indicate in any way that an item is not applicable to them, the item is scored 'No', i.e. the denominator remains 24. Being worst 24. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise6.9
NSAID7.7

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Roland-Morris Questionnaire

Improvement in function assessed by the Roland-Morris questionnaire, a widely used health status measure for low back pain. The RMDQ can be used in research or clinical practice. Scoring the RMDQ. The RMDQ is scored by adding up the number of items checked by the patient. The score can therefore vary from 0 to 24. It is not recommended to give patients a 'Yes' / 'No' option. If patients indicate in any way that an item is not applicable to them, the item is scored 'No', i.e. the denominator remains 24. Being worst 24. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise4.2
NSAID4.6

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Roland-Morris Questionnaire

Improvement in function assessed by the Roland-Morris questionnaire, a widely used health status measure for low back pain. The RMDQ can be used in research or clinical practice. Scoring the RMDQ. The RMDQ is scored by adding up the number of items checked by the patient. The score can therefore vary from 0 to 24. It is not recommended to give patients a 'Yes' / 'No' option. If patients indicate in any way that an item is not applicable to them, the item is scored 'No', i.e. the denominator remains 24. Being worst 24. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise2.3
NSAID2.5

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Roland-Morris Questionnaire

Improvement in function assessed by the Roland-Morris questionnaire, a widely used health status measure for low back pain. The RMDQ can be used in research or clinical practice. Scoring the RMDQ. The RMDQ is scored by adding up the number of items checked by the patient. The score can therefore vary from 0 to 24. It is not recommended to give patients a 'Yes' / 'No' option. If patients indicate in any way that an item is not applicable to them, the item is scored 'No', i.e. the denominator remains 24. Being worst 24. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise2.6
NSAID3.2

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Relapses of Lumbar Pain

The percentage of patients with relapsed of low back pain was measured. (NCT01374269)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
Excercise5.0
NSAID20.5

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Relapses of Lumbar Pain

The percentage of patients with relapsed of low back pain was measured. (NCT01374269)
Timeframe: 12 weeks

Interventionpercentage of participants (Number)
Excercise7.1
NSAID25

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Quality of Life, Vitality.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Vitality. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise55.5
NSAID55.3

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Quality of Life, Vitality.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Vitality. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise61.3
NSAID64.0

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Quality of Life, Vitality.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Vitality. (NCT01374269)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Excercise70.3
NSAID62.8

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Quality of Life, Vitality.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Vitality. (NCT01374269)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
Excercise67.5
NSAID66.6

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Quality of Life, Social Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Social Function. (NCT01374269)
Timeframe: At the beginning

Interventionunits on a scale (Mean)
Excercise71.3
NSAID65.9

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Quality of Life, Social Function.

Improvement in Quality of life was assessed with the SF-36 questionnaire, which ranges from 0 to 100 being 100 the best quality of life. The Short Form (36) Health Survey is a patient-reported survey of patient health. The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Each scale is directly transformed into a 0-100 scale on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability. This outcome shows the subdomain data: Social Function. (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise80.7
NSAID74.8

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PHQ-9 Patient Health Questionnaire (PHQ-9) Depression

Depression was measured with the Patient Health Questionnaire (PHQ-9), which ranged from 0 (no depression) to 27 (severe depression). (NCT01374269)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Excercise3.9
NSAID3.4

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Health Status According to EuroQoL

"EuroQoL-5D was a standardized instrument for use as a measure of health outcome that provides a simple descriptive profile and a single index value for health status. It was assessed at all of the study visits.~The EQ-5D-3L essentially consists of 2 pages - the EQ-5D descriptive system (page 2) and the EQ visual analogue scale (EQ VAS) (page 3). The EQ-5D-3L descriptive system comprises the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension has 3 levels: no problems, some problems, extreme problems. Total scale range for each dimension reported is 1 to 3.~The EQ VAS records the respondent's self-rated health on a vertical, visual analogue scale where the endpoints are labelled 'Best imaginable health state' and 'Worst imaginable health state'. This information can be used as a quantitative measure of health outcome as judged by the individual respondents.~Total scale range for VAS dimension reported is 0 to 100." (NCT01425853)
Timeframe: 6 months

,
Interventionpoints (Mean)
Mobility BaselineMobility 180 DaysSelf-care BaselineSelf-care 180 daysUsual activities BaselineUsual activities 180 daysPain Discomfort BaselinePain Discomfort 180 daysAnxiety depression baselineAnxiety depression 180 daysVAS BaselineVAS 180 days
Celecoxib1.841.461.441.211.791.422.271.861.601.3452.48870.219
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)1.841.521.391.191.781.422.251.841.701.4354.54569.080

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WOMAC Pain Subscale

Western Ontario & McMaster Universities Osteoarthritis Index (WOMAC) Pain subscale Score Range: 0 (no pain) - 500 (maximum pain) The study was designed such that the outcome of primary interest is knee pain related to OA. The measure selected to best evaluate this is an improvement in the WOMAC pain subscales. This subscale consists of 5 items which assesses the pain during walking, using stairs, in bed, sitting or lying, and standing. (NCT01425853)
Timeframe: 6 months

Interventionunits on a scale (Mean)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)185.79
Celecoxib184.67

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Percentage of Participants With Response as Defined by Outcome Variables for Osteoarthritis Clinical Trials - Osteoarthritis Research Society International (OMERACT-OARSI)

"The OARSI Standing Committee for Clinical Trials Response Criteria Initiative and the OMERACT committee, in concert with the international rheumatology community, has led to the development of a uniform core set of outcome measures for OA. One of the objectives was to propose a set of criteria for measurement based on multiple domains to present the results of changes after treatment in symptomatic parameters as a single variable for clinical trials.~To be considered as responder patients should met one the following criteria:~High improvement in pain or in function ≥ 50% and absolute change ≥ 20 or~Improvement in at least 2 of the 3 following:~Pain ≥ 20% and absolute change ≥ 10~Function ≥ 20% and absolute change ≥ 10~Patient's global assessment ≥ 20% and absolute change ≥ 10" (NCT01425853)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)79.7
Celecoxib79.2

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Number of Participants With at Least One Adverse Events

The safety evaluation was done in the set of randomized patients who took at least one dose of the medication (NCT01425853)
Timeframe: 6 months

Interventionnumber of participants (Number)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)155
Celecoxib151

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Consumption of Rescue Medication

"Use of rescue medication as number of paracetamol tablets 500 mg since the last visit. The tablet count was reconciled with the patient diary.~Total Number of pills per month" (NCT01425853)
Timeframe: 6 months

Interventiondaily tablets consumed/month (Mean)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)31.0
Celecoxib29.0

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Percentage of Presence of Joint Effusion

Study knees were evaluated at each visit for the presence or absence of swelling and/or effusion. (NCT01425853)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)4.1
Celecoxib3.8

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Percentage of Presence of Joint Swelling

Study knees were evaluated at each visit for the presence or absence of swelling and/or effusion. (NCT01425853)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)5.9
Celecoxib4.5

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WOMAC Stiffness Subscale

Western Ontario & McMaster Universities Osteoarthritis Index, from 0 No Stiffness to 200 Maximum Stiffness WOMAC stiffness subscale was used to measure the stiffness of the knee with pain. Two items are used to assess stiffness grade: after first waking and later in the day. (NCT01425853)
Timeframe: 6 months

,
Interventionunits on a scale (Mean)
Baseline180 days
Celecoxib129.4865.78
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)130.1569.06

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WOMAC Function Subscale

Western Ontario & McMaster Universities Osteoarthritis Index, from 0 No Function to 1700 Maximum Function WOMAC functional limitation subscale was used to measure the functionality of the knee with pain. Seventeen items are used to assess functionality of the knee: tair use, rising from sitting, standing, bending, walking, getting in / out of a car, shopping, putting on / taking off socks, rising from bed, lying in bed, getting in / out of bath, sitting, getting on / off toilet, heavy household duties, light household duties. (NCT01425853)
Timeframe: 6 months

,
Interventionunits on a scale (Mean)
Baseline180 days
Celecoxib1111.60595.78
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)1131.40616.96

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Patient's Global Assessment (PGA) and Investigator's Global Assessment (IGA) of Disease Activity

"Patients were asked to quantify their disease status on a VAS scale with range 0 mm (best) and 100 mm (worst) as follows: Considering all the ways your arthritis of the knee affects you, mark (I) on the scale how well you are doing. Left hand marker Very Well, Right hand marked Very Poor." (NCT01425853)
Timeframe: 6 months

,
Interventionunits on a scale (Mean)
PGA Activity BaselinePGA Activity 180 daysIGA Activity BaselineIGA Activity 180 daus
Celecoxib69.4136.8863.2833.40
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)69.1138.3563.235.33

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Patient's and Investigator's Global Assessment of Response to Therapy

"The investigator were asked to evaluated the patient's response to therapy of the index knee by marking a (I) a VAS scale with range 0 mm (best) and 100 mm (worst) as follows: Left hand marker Excellent-Best possible anticipated response, considering the severity and stage of the disease, right hand marker None-no response, absence of drug effect." (NCT01425853)
Timeframe: 6 months

,
Interventionunits on a scale (Mean)
PGA Therapy BaselinePGA Therapy 180 daysIGA Therapy BaselineIGA Therapy 180 days
Celecoxib45.936.0442.2533.83
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)54.5936.8551.434.72

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Number of Adverse Events Defined by Relationship With Treatment

The safety evaluation was done in the set of randomized patients who took at least one dose of the medication (NCT01425853)
Timeframe: 6 months

,
Interventionnumber of events (Number)
Treatment-related AEs: DefinitiveTreatment-related AEs: PossiblyTreatment-related AEs: ProbablyTreatment-related AEs: Non-appraisableTreatment-related AEs: unlikely or unrelated
Celecoxib103812190
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)34325084

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Huskisson's VAS

"Visual Analogue Scale: 0 No Pain 100 Maximum Pain Huskisson's VAS measures global pain intensity. Patients were asked to quantify their disease status on a 100 mm VAS as follows: Please indicate the severity of knee pain experienced during the last 48 hours by marking a (I) through the line. Left hand marker represents No pain and right hand marker represents The worst pain imaginable." (NCT01425853)
Timeframe: 6 months

,
Interventionunits on a scale (Mean)
Baseline180 days
Celecoxib73.4737.64
Chondroitin Sulfate/ Glucosamine Hydrochloride (Droglican)72.7937.86

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Pharmacokinetics: Maximum Concentration (Cmax) of LY3031207

(NCT01449630)
Timeframe: Predose, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48, 96, 144 hours post dose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
5 mg LY3031207185
25 mg LY3031207818
75 mg LY30312072060
225 mg LY30312075610
450 mg LY3031207 Fed7780
450 mg LY3031207 Fasted5670
900 mg LY303120711300

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Pharmacokinetics: Area Under the Concentration-Time Curve (AUC) of LY3031207

AUC from time 0 to last timepoint (AUC0-tlast) with measurable concentration of LY3031207. (NCT01449630)
Timeframe: Predose, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48, 96, 144 hours post dose

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
5 mg LY30312073040
25 mg LY303120713900
75 mg LY303120740000
225 mg LY3031207151000
450 mg LY3031207 Fed171000
450 mg LY3031207 Fasted116000
900 mg LY3031207348000

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Pharmacodynamics: Percent Change From Baseline of Ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation

The effect of LY3031207 on PGE synthesis in whole blood after ex vivo LPS stimulation. (NCT01449630)
Timeframe: Predose, 0.5, 1, 2, 8, 24 and 144 hours post dose.

,,,,,,,,
Interventionpercentage change in PGE (Mean)
0.5 hours (hr)1 hr2 hr8 hr24 hr144 hr
225 mg LY303120712.7-16.8-79.2-79.3-29.5131.1
25 mg LY3031207-15.6-4.8-45.5-40.18.724.3
400 mg Celecoxib-10.4-44.8-68.2-63.1-19.97.6
450 mg LY3031207 Fasted-85.1-92.9-96.4-88.3-54.148.0
450 mg LY3031207 Fed42.7-83.8-104.9-94.3-76.8125.1
5 mg LY3031207-16.2-9.2-34.3-8.589.4178.2
75 mg LY303120733.024.6-47.0-41.360.0153.7
900 mg LY3031207-43.1-93.7-83.3-98.4-88.841.4
Placebo56.165.465.176.9124.8159.1

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Thromboxane A Metabolite (TXAM)

The participant's urine was collected during protocol-defined intervals and the PGE metabolite TXAM was assessed. TXAM results for each interval were then compared to the baseline value. (NCT01449630)
Timeframe: 0 to 2, 2 to 4, 4 to 6, and 6 to 12 hours post dose

,,,,,,,,
Interventionpercentage change in TXAM (Mean)
At 0 - 2 hr intervalAt 2 - 4 hr intervalAt 4 - 6 hr intervalAt 6 - 12 hr interval
225 mg LY3031207-11.30.7-3.88.0
25 mg LY3031207-5.7-15.5-16.5-15.7
400 mg Celecoxib-6.2-25.4-33.3-19.8
450 mg LY3031207 Fasted25.228.316.79.0
450 mg LY3031207 Fed4.440.429.430.9
5 mg LY3031207-9.04.11.36.8
75 mg LY30312070.919.71.220.7
900 mg LY303120711.0106.288.585.8
Placebo-11.5-17.4-18.313.1

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostaglandin E(2) Metabolite (PGEM)

The participant's urine was collected during protocol-defined intervals and the PGE metabolite PGEM was assessed. PGEM results for each interval were then compared to the baseline value. (NCT01449630)
Timeframe: 0 to 2, 2 to 4, 4 to 6, 6 to 12 and 12 to 24 hours post dose

,,,,,,,,
Interventionpercentage change in PGEM (Mean)
0 - 2 hr interval2 - 4 hr interval4 - 6 hr interval6 - 12 hr interval12 - 24 hr interval
225 mg LY3031207-26.6-45.2-44.2-41.9-37.9
25 mg LY303120718.5-2.1-1.5-17.9-32.6
400 mg Celecoxib-14.6-30.7-32.3-36.8-46.5
450 mg LY3031207 Fasted10.729.615.8-13.0-7.3
450 mg LY3031207 Fed17.36.1-9.2-18.8-26.9
5 mg LY303120714.414.5-0.84.93.9
75 mg LY303120711.05.8-22.1-13.5-12.9
900 mg LY3031207-19.8-12.0-24.2-37.5-43.6
Placebo5.811.26.32.90.9

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostacyclin Metabolite (PGIM)

The participant's urine was collected during protocol-defined intervals and the PGE metabolite PGIM was assessed. PGIM results for each interval were then compared to the baseline value. (NCT01449630)
Timeframe: 0 to 2, 2 to 4, 4 to 6, and 6 to 12 hours post dose

,,,,,,,,
Interventionpercentage change in PGIM (Mean)
At 0 - 2 hr intervalAt 2 - 4 hr intervalAt 4 - 6 hr intervalAt 6 - 12 hr interval
225 mg LY303120711.733.172.171.7
25 mg LY303120725.230.519.352.1
400 mg Celecoxib-18.9-44.6-25.6-12.1
450 mg LY3031207 Fasted137.2174.1186.7190.0
450 mg LY3031207 Fed44.6244.7198.3208.5
5 mg LY303120714.134.073.848.0
75 mg LY3031207-3.921.231.063.6
900 mg LY303120737.2122.5264.0201.4
Placebo-17.06.228.357.5

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Total Pain Relief (TOTPAR) Over 0 to 4 Hours. TOTPAR-4.

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight.The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 16 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 4 hours

Interventionunits on a scale*hour (Mean)
Celecoxib2.226
Diclofenac Test (Lower Dose)2.112
Diclofenac Test (Upper Dose)2.530
Placebo1.387

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The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48), ANCOVA Model.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 48 hours

Interventionmm*hour (Mean)
Celecoxib390.468
Diclofenac Test (Lower Dose)392.954
Diclofenac Test (Upper Dose)524.315
Placebo76.887

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TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 96 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 24 hours

Interventionunits on a scale*hour (Mean)
Celecoxib10.670
Diclofenac Test (Lower Dose)10.186
Diclofenac Test (Upper Dose)13.325
Placebo3.566

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TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 192 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 48 hours

Interventionunits on a scale*hour (Mean)
Celecoxib22.972
Diclofenac Test (Lower Dose)21.635
Diclofenac Test (Upper Dose)28.054
Placebo4.925

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TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 32 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 8 hours

Interventionunits on a scale*hour (Mean)
Celecoxib3.840
Diclofenac Test (Lower Dose)3.690
Diclofenac Test (Upper Dose)4.652
Placebo1.943

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VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 24 hours

Interventionmm*hour (Mean)
Celecoxib170.845
Diclofenac Test (Lower Dose)177.101
Diclofenac Test (Upper Dose)230.708
Placebo48.811

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VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 4 hours

Interventionmm*hour (Mean)
Celecoxib25.109
Diclofenac Test (Lower Dose)27.450
Diclofenac Test (Upper Dose)31.568
Placebo14.406

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VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 8 hours

Interventionmm*hour (Mean)
Celecoxib51.675
Diclofenac Test (Lower Dose)56.404
Diclofenac Test (Upper Dose)64.689
Placebo23.151

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The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48)

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01543685)
Timeframe: 0 - 48 hours

Interventionmm*hour (Mean)
Indomethacin 40 mg TID508.2
Indomethacin 40 mg BID329.8
Indomethacin 20 mg TID377.3
Celecoxib 200 mg280.5
Placebo69.4

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Total Pain Relief (TOTPAR) Over 0 to 4 Hours (TOTPAR-4).

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 16 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01543685)
Timeframe: 0 - 4 hours

Interventionunits on a scale*hour (Mean)
Indomethacin 40 mg TID2.5
Indomethacin 40 mg BID2.1
Indomethacin 20 mg TID1.7
Celecoxib 200 mg1.8
Placebo1.2

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VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as a time-weighted sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01543685)
Timeframe: 0 - 24 hours

Interventionmm*hour (Mean)
Indomethacin 40 mg TID226.9
Indomethacin 40 mg BID158.3
Indomethacin 20 mg TID176.9
Celecoxib 200 mg119.4
Placebo28.3

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TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 96 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01543685)
Timeframe: 0 - 24 hours

Interventionunits on a scale*hour (Mean)
Indomethacin 40 mg TID13.4
Indomethacin 40 mg BID8.9
Indomethacin 20 mg TID10.0
Celecoxib 200 mg7.7
Placebo2.6

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TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 192 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01543685)
Timeframe: 0 - 48 hours

Interventionunits on a scale*hour (Mean)
Indomethacin 40 mg TID29.3
Indomethacin 40 mg BID17.8
Indomethacin 20 mg TID19.6
Celecoxib 200 mg16.4
Placebo5.2

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TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 32 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01543685)
Timeframe: 0 - 8 hours

Interventionunits on a scale*hour (Mean)
Indomethacin 40 mg TID4.5
Indomethacin 40 mg BID3.4
Indomethacin 20 mg TID3.4
Celecoxib 200 mg3.0
Placebo1.5

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VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01543685)
Timeframe: 0 - 4 hours

Interventionmm*hour (Mean)
Indomethacin 40 mg TID30.7
Indomethacin 40 mg BID29.8
Indomethacin 20 mg TID17.9
Celecoxib 200 mg20.4
Placebo8.9

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VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01543685)
Timeframe: 0 - 8 hours

Interventionmm*hour (Mean)
Indomethacin 40 mg TID64.1
Indomethacin 40 mg BID55.4
Indomethacin 20 mg TID45.7
Celecoxib 200 mg37.2
Placebo12.0

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Time-Weighted Mean Response in the Participant Global Assessment of Response to Therapy

Participants were asked to rate their global assessment of response to therapy on a Likert scale from 0 to 4, with 0 = excellent, 1 = good, 2 = fair, 3 = poor, 4 = none. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg1.48
Celecoxib 200 mg1.56

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Time-Weighted Mean Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale

The WOMAC osteoarthritis scale consists of 24 items in 3 subscales: pain, stiffness, and physical function. The pain subscale rates participant pain during walking, using stairs, in bed, sitting or lying, and standing using a visual analog scale (VAS) from 0-100mm where 0 is the best possible level of pain and 100 is the highest level of pain. The pain subscale is calculated as the average of the responses to the 5 questions related to pain. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Baseline, Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg-21.40
Celecoxib 200 mg-19.76

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Time-Weighted Mean Change From Baseline in the WOMAC Stiffness Subscale

The WOMAC osteoarthritis scale consists of 24 items in 3 subscales: pain, stiffness, and physical function. The stiffness subscale rates stiffness after first waking and later in the day using a visual analog scale (VAS) from 0-100mm where 0 is the best possible level of stiffness and 100 is the highest level of stiffness. The stiffness subscale is calculated as the average of the responses to the 2 questions related to stiffness. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Baseline, Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg-18.41
Celecoxib 200 mg-17.55

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Time-Weighted Mean Change From Baseline in the WOMAC Physical Function Subscale

The WOMAC osteoarthritis scale consists of 24 items in 3 subscales: pain, stiffness, and physical function. The physical function subscale rates participant pain during stair use, rising from sitting, standing, bending, walking, getting in/out of a car, shopping, putting on/taking off socks, rising from bed, lying in bed, getting in/out of the bath, sitting, getting on/off the toilet, heavy household duties, and light household duties using a visual analog scale (VAS) from 0-100mm where 0 is the best possible level of functioning and 100 is the highest level of functioning. The physical function subscale was calculated as the average of the responses to the 17 questions related to functional status. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Baseline, Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg-17.78
Celecoxib 200 mg-16.46

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Time-Weighted Mean Change From Baseline in the Participant Global Assessment of Disease Status

"The Participant Global Assessmet of Disease was a one item questionnaire that asked participants to answer the following question, Considering all the ways your arthritis affects you, mark (X) on the scale for how well you are doing. The questionnaire employed a 0-100 mm visual analog scale (VAS) to record participant responses, with 0 representing the best possible assessment and 100 representing the worst possible assessment. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average." (NCT01554163)
Timeframe: Baseline, Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg-24.71
Celecoxib 200 mg-23.61

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Time-Weighted Mean Change From Baseline in the Investigator Global Assessment of Disease Status

Study investigators were asked to rate the global assessment of participant disease status on a Likert scale from 0 to 4, with 0 = very well, 1 = good, 2 = fair, 3 = poor and 4 = very poor. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Baseline, Week 2, Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg-1.71
Celecoxib 200 mg-1.62

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Time-Weighted Mean Response on the Investigator Global Assessment of Response to Therapy

Study investigators were asked to rate the global assessment of participant response to therapy on a Likert scale from 0 to 4, with 0 = excellent, 1 = good, 2 = fair, 3 = poor, 4 = none. The calculation of the time-weighted average was done by taking the time between adjacent observations divided by the time from the randomization visit to the last observation in the period of interest, and using it as the weight for computation of the average. (NCT01554163)
Timeframe: Week 6, Week 12

InterventionScore on a Scale (Least Squares Mean)
Etoricoxib 30 mg1.39
Celecoxib 200 mg1.49

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Number of Participants Switching to Another Treatment With the Same Reason for Prescription

Participants who switched to another NSAID or other therapy for the same reason for prescription upon discontinuation of treatment with Arcoxia® or Celebrex® were determined. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
Prescription of a new treatmentNSAIDSAnalgesicsOther (TNF-alpha inhibitors, corticosteroids)
Group Arcoxia®332291
Group Celebrex®292261

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Duration of Prescription for Arcoxia® and Celebrex® at Enrollment

The mean duration of prescription at enrollment for participants treated with Arcoxia® and Celebrex® was determined using the participant's record. (NCT01572675)
Timeframe: Up to 3 months prior to study entry

InterventionDays (Mean)
Group Arcoxia® - Initiation25.5
Group Arcoxia® - Renewal38.1
Group Celebrex® - Initiation23.9
Group Celebrex® - Renewal41.7
Group Arcoxia®31.1
Group Celebrex®34.0

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Number of Participants With Contraindications for Use of Arcoxia®

Participants noted with contraindications for use of Arcoxia® according to the MA during initiation of treatment are described. CHF = congestive heart failure. HA = hepatic impairment. IBD = inflammatory bowel disease. IHD = ischemic heart disease. PAD = peripheral artery disease. (NCT01572675)
Timeframe: At study entry

,,
InterventionParticipants (Number)
At least one contraindication (n=122,100,122)One total contraindication (n=36,34,70)Two total contraindications (n=36,34,70)History of acute rhinitis (n=145,115,260)Creatinine clearance <30 ml/min (n=125,108,233)History of bronchospasm (n=145,117,262)History of urticaria (n=146,116,262)Presence of IBD (n=146,118,264)Presence of CHF (n=146,118,264)Presence of IHD and/or PAD (n=142,118,260)History of allergic reaction (n=145,118,263)History of nasal polyps (n=146,116,262)Blood pressure not controlled (n=146,118,264)History of angioedema (n=145,117,262)Patients with severe HA (n=146,118,264)<16 years of age (n=149,119,268)Pregnancy or lactation (n=92,73,165)
Group Arcoxia®7061935115106231112101
Group Arcoxia® - Initiation36297201952011012100
Group Arcoxia® - Renewal34322150654220100001

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Reasons for Discontinuation of Treatment With Arcoxia® and Celebrex®

The individual reasons for discontinuation of treatment with Arcoxia® or Celebrex® were identified over the course of study through either physician selection from a pre-determined list or verbatim entry by the physician with subsequent re-codification by Sponsor. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
End of prescribed treatmentRecoveryLack of efficacyIntoleranceImproved symptomsSurgical interventionParticipant decisionPhysician decisionDeath unrelated to coxibsOther disease detectedOther - unknown reasonRheumatologist new evaluationMissing data
Group Arcoxia®14016316835211101
Group Celebrex®11823315261211114

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Reasons for Misuse of Arcoxia® and Celebrex®

Proper use of study medication is defined as administration of medication in terms of indication and dosage according to MA. Proper use of Arcoxia® is defined as administration of a starting dose of 30 mg daily, not to exceed 60 mg daily during follow-up, for the treatment of symptoms of osteoarthritis. Proper use of Celebrex® is defined as administration of a starting dose of 200 mg daily, not to exceed 400 mg daily during follow-up, for easing symptoms in the treatment of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. Data to assess proper use were collected through use of a medical questionnaire and patient form. Data pertaining to indication was collected by open-field to allow physicians to precisely indicate the reason for prescription. Recorded indications were then analyzed by two medical experts (an independent expert and a member of the Scientific Community) to assess proper use or misuse. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
Non-MA-Compliant IndicationNon-MA-Compliant Starting DoseNon-MA-Compliant Starting Dose and IndicationNon-MA-Compliant Indication & Dose (Starting &Max)
Group Arcoxia®8362461
Group Celebrex®11419130

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Significant Past Treatments Prior to Initiating Treatment With Arcoxia® or Celebrex®

'Significant' treatments that preceded the use of selective COX-2 inhibitors (Arcoxia® or Celebrex®) were identified using a closed-ended (yes/ no/ do not know) questionnaire. Significant is defined as associated with a chronic disease or having a potential link with participant's current use of a selective COX-2 inhibitors (Arcoxia® or Celebrex®). ARBs = Angiotensin 2 receptor blockers. ACEIs = Angiotensin-converting enzyme inhibitors. SSRIs = Selective serotonin reuptake Inhibitors. PAIs = Platelet aggregation inhibitors. (NCT01572675)
Timeframe: At study entry

,,,,,
InterventionParticipants (Number)
At least one treatment (n=146,118,117,158,264,275)Proton-pump inhibitors (n=146,115,116,156,261,272)Hypolipidemic agents (n=146,116,117,156,262,273)ARBs (n=144,115,116,155,259,271)Diuretics (N=146,117,117,156,263,273)ACEIs (n=145,116,117,157,261,274)SSRIs (n=146,116,117,158,262,275)Anti-diabetic agents (n=146,115,117,158,261,275)Histamine H2 blockers (n=146,117,117,156,263,273)PAIs (n=146,118,117,158,264,275)Oral anticoagulants (n=146,118,117,158,264,275)Alpha-blockers (n=146,116,117,157,262,274)
Group Arcoxia®177101715140333022281352
Group Arcoxia® - Initiation1025839221611151414511
Group Arcoxia® - Renewal75433229242215814841
Group Celebrex®18595696039333325271499
Group Celebrex® - Initiation673024231013867634
Group Celebrex® - Renewal1186545372920251920865

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Total Duration of Treatment With Arcoxia® and Celebrex®

The total duration of treatment (DoT) with Arcoxia® or Celebrex® was determined for populations that achieved end-of study and end-of-protocol or that were categorized as lost to follow-up. Participants enumerated as end-of-study had their treatment discontinued during the protocol-specified one year of follow-up. Participants enumerated as end-of-protocol were ongoing treatment at end of the protocol-specified one year of follow-up. Participants categorized as lost to follow-up had no follow-up visit where a determination of discontinuation from treatment could be made. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionDays (Mean)
DoT - End-of-study participants (n=215,196)DoT - End-of-protocol participants (n=31,56)DoT - Lost to follow-up participants (n=5,4)
Group Arcoxia®85.2472.9122.4
Group Celebrex®117.8595.2142.0

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Type of Arcoxia® and Celebrex® Use

The type of Arcoxia® or Celebrex® use during the study was classified as continuous (without interruption >7 days) or intermittent (with interruption >7 days) by the Investigating Physician at time of treatment discontinuation. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
Missing dataIntermittentContinuous
Group Arcoxia®044171
Group Celebrex®247147

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Type of Arcoxia® and Celebrex® Use According to Duration of Treatment

Use of selective cyclooxygenase-2 (COX-2) inhibitors (Arcoxia® and Celebrex®) as assessed by the Investigating Physician at time of treatment discontinuation was correlated to the overall duration of treatment experienced by the participant (i.e., intermittent or continuous selective COX-2 inhibitor use vs. total participant time on treatment). Type of use was classified as continuous (without interruption >7 days) or intermittent (with interruption >7 days). Four successive treatment intervals were assessed in this endpoint: 1) Up to thirty days of treatment 2) From one to three months of treatment 3) From three months to one year of treatment and 4) More than one year of treatment. (NCT01572675)
Timeframe: Up to 12 months

,,,
InterventionParticipants (Number)
Missing dataIntermittentContinuous
From One to Three Months13873
From Three Months to One Year12252
More Than One Year0711
Up to Thirty Days024182

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Maximum Dosage Prescribed During Treatment With Arcoxia® and Celebrex®

Mean maximum dosage prescribed during follow-up in participants treated with Arcoxia® or Celebrex®. Dosage is expressed as total daily dose. (NCT01572675)
Timeframe: Up to 12 months

Interventionmg/day (Mean)
Group Arcoxia® - Initiation47.1
Group Arcoxia® - Renewal48.4
Group Celebrex® - Initiation228.4
Group Celebrex® - Renewal242.7
Group Arcoxia®47.7
Group Celebrex®236.5

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Number of Participants Treated With Other Agents Prior to Initiation of Arcoxia® and Celebrex®

Other prescribed agents for the same study indication within 3 months preceding the decision to initiate treatment with selective COX-2 inhibitors (Arcoxia® or Celebrex®) were determined using the participant's medical record. NSAIDS = Non-steroidal inflammatory agents. (NCT01572675)
Timeframe: Up to 3 months prior to study entry

,,,,,
InterventionParticipants (Number)
At least one treatment (n=146,118,117,158,264,275)Paracetamol (n=146,118,117,158,264,275)NSAIDS (n=146,118,117,158,264,275)Analgesics (n=146,118,117,158,264,275)Corticosteroids (n=140,107,111,152,247,263)
Group Arcoxia®17916552810
Group Arcoxia® - Initiation93833347
Group Arcoxia® - Renewal86821943
Group Celebrex®16414442819
Group Celebrex® - Initiation62541916
Group Celebrex® - Renewal1029023713

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Mean Dosage of Arcoxia® and Celebrex® During Treatment

The mean dosage of Arcoxia® and Celebrex® during treatment was determined. For participants who stopped treatment after their initial study visit, the maximum dose recorded at their final study visit was considered when calculating their mean dosage during treatment. (NCT01572675)
Timeframe: Up to 12 months

Interventionmg/day (Mean)
Group Arcoxia®44.1
Group Celebrex®221.9

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Number of Participants Demonstrating Proper Use of Arcoxia® and Celebrex®

Proper use of study medication is defined as administration of medication in terms of indication and dosage according to Market Authorization (MA). Proper use of Arcoxia® is defined as administration of a starting dose of 30 mg daily, not to exceed 60 mg daily during follow-up, for the treatment of symptoms of osteoarthritis. Proper use of Celebrex® is defined as administration of a starting dose of 200 mg daily, not to exceed 400 mg daily during follow-up, for easing symptoms in the treatment of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. Data to assess proper use were collected through use of a medical questionnaire and patient form. Data pertaining to indication was collected by open-field to allow physicians to precisely indicate the reason for prescription. Recorded indications were then analyzed by two medical experts (an independent expert and a member of the Scientific Community) to assess proper use or misuse. (NCT01572675)
Timeframe: Up to 12 months

InterventionParticipants (Number)
Group Arcoxia®65
Group Celebrex®118

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Number of Participants Who Discontinued Study Drug Due to an Adverse Event

Discontinuation/withdrawal of study treatment due to an adverse event was performed at the discretion of the investigator or the Sponsor for safety concerns. An adverse event is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure. (NCT01572675)
Timeframe: Up to 12 months

InterventionParticipants (Number)
Group Arcoxia®6
Group Celebrex®5

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Number of Participants Who Experienced at Least One Adverse Event

An adverse event is defined as any unfavorable and unintended sign including an abnormal laboratory finding, symptom or disease associated with the use of a medical treatment or procedure, regardless of whether it is considered related to the medical treatment or procedure. (NCT01572675)
Timeframe: Up to 12 months

InterventionParticipants (Number)
Group Arcoxia®10
Group Celebrex®5

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Blood Pressure at Study Entry in Participants Treated With Arcoxia® and Celebrex®

Participants' BP (SBP/DBP) was assessed at study entry by the Investigating Physician. Definition of controlled BP: SBP <140 mmHg and DBP <90 mmHg. Definition of uncontrolled BP: SBP ≥140 mmHg and/or DBP ≥90 mmHg. (NCT01572675)
Timeframe: At study entry (baseline)

,,,,,
InterventionParticipants (Number)
MIssing data<120/80 mmHg120 mmHg ≤SBP<140 mmHg and/or 80 mmHg ≤DBP<90 mmHg140 mmHg ≤SBP<180 mmHg and/or 90 mmHg≤DBP<100 mmHgSBP≥180 mmHg and/or DBP≥110 mmHg
Group Arcoxia®420185590
Group Arcoxia® - Initiation315105260
Group Arcoxia® - Renewal1580330
Group Celebrex®514214460
Group Celebrex® - Initiation5887210
Group Celebrex® - Renewal06127250

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Co-morbidities in Participants Treated With Arcoxia® and Celebrex®

Associated co-morbidities at study entry (baseline) in participants treated with Arcoxia® or Celebrex® were recorded by the Investigating Physician. CHF/IHD/PAD = Congestive heart failure/Ischemic heart disease/Peripheral artery disease (NCT01572675)
Timeframe: At study entry

,,,,,
InterventionParticipants (Number)
At least one co-morbidityHyperlipidemiaDiabetesHepatic insufficiencyInflammatory bowel diseaseCHF/IHD/PADActive peptic ulceration/ GI bleedingMissing data
Group Arcoxia®99772576317
Group Arcoxia® - Initiation55431442115
Group Arcoxia® - Renewal44341134202
Group Celebrex®94722824904
Group Celebrex® - Initiation3226603304
Group Celebrex® - Renewal62462221600

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Medications Co-Prescribed at Study Entry in Participants Treated With Arcoxia® and Celebrex®

Concomitant medications prescribed to participants treated with Arcoxia® and Celebrex® were collected via the physician prescription note at time of participant's study entry. NSAIDS = Non-steroidal anti-inflammatory agents. (NCT01572675)
Timeframe: At study entry

,,,,,
InterventionParticipants (Number)
Missing dataAt least one treatmentAnalgesicsCardiovascular agentsDigestive system agentsNervous system agentsNSAIDSRheumatologic agentsMetabolic system agentsRespiratory system agentsHormonal agentsHematologic agentsUrinary-genital system agentsDermatological agentsAnti-infectious agentsOther not-classified
Group Arcoxia®3718411870704146383725211188811
Group Arcoxia® - Initiation1595523037172517149814746
Group Arcoxia® - Renewal2289664033242121231613104145
Group Celebrex®2619311390835943524928212218181428
Group Celebrex® - Initiation373383122141523117666425
Group Celebrex® - Renewal231207559614528293821151612141223

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Dosage of Arcoxia® and Celebrex® at Initiation

Dosage at initiation of treatment with Arcoxia® or Celebrex® was identified. MA compliant dosage at initiation corresponds to a (starting) dose of 30 mg daily for Arcoxia® or a (starting) dose of 200 mg daily for Celebrex®. The dose for initiation was calculated by multiplying the number of doses per day with the dose level (total daily dose) as noted in the prescription record. (NCT01572675)
Timeframe: At study entry

,
InterventionParticipants (Number)
30 mg60 mg> 60 mg; <100 mg100 mg>100 mg; < 200 mg200 mg400 mg> 400 mg
Group Arcoxia®151107101000
Group Celebrex®000230219320

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Indications for Which Arcoxia® and Celebrex® Were Prescribed

The reasons (indications) for prescribing of Arcoxia® or Celebrex® were collected in open-field forms by the Investigator; category assignment (i.e, re-codification) of verbatim entries was conducted by a group of medical experts under the guidance approved by the MA. This endpoint gives the number of participants treated per indication. (NCT01572675)
Timeframe: At study entry

,
InterventionParticipants (Number)
Other pain (e.g., spinal pain, joint pain)OsteoarthritisInflammatory rheumatismNeuralgiaNon-joint rheumatismUnclassified arthropathyMissing data
Group Arcoxia®11310513171244
Group Celebrex®11710418241204

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Mean Systolic and Diastolic Blood Pressure (BP) at Study Entry in Participants Treated With Arcoxia® and Celebrex®

Mean systolic blood pressure (SBP) and diastolic blood pressure (DBP) were assessed at study entry by the Investigating Physician. Definition of controlled BP: SBP <140 mmHg and DBP <90 mmHg. Definition of uncontrolled BP: SBP ≥140 mmHg and/or DBP ≥90 mmHg. (NCT01572675)
Timeframe: At study entry (baseline)

,,,,,
InterventionmmHG (Mean)
SBPDBP
Group Arcoxia®129.076.4
Group Arcoxia® - Initiation127.476.0
Group Arcoxia® - Renewal130.976.8
Group Celebrex®128.275.4
Group Celebrex® - Initiation127.976.0
Group Celebrex® - Renewal128.475.1

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Medical History of Participants Treated With Arcoxia® and Celebrex®

Relevant medical history of participants treated with Arcoxia® or Celebrex® was recorded by the Investigating Physician. (NCT01572675)
Timeframe: At study entry

,,,,,
InterventionParticipants (Number)
Arterial hypertension (n=146,118,116,156,264,272)Acute rhinitis (n=145,115,115,157,260,272)Bronchospam (n=145,117,115,158,262,273)Urticaria (n=146,116,115,156,262,271)Peptic ulcer/bleeding (n=146,118,117,158,264,275)Angioedema (n=145,117,114,157,262,271)Nasal polyps (n=146,116,114,158,262,272)
Group Arcoxia®84351510521
Group Arcoxia® - Initiation372095520
Group Arcoxia® - Renewal471565001
Group Celebrex®922284730
Group Celebrex® - Initiation341020310
Group Celebrex® - Renewal581264420

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Mean Body Mass Index (BMI) at Study Entry in Participants Treated With Arcoxia® and Celebrex®

Participants' BMI was assessed at study entry by the Investigating Physician. BMI is calculated as the participant's weight in kilograms (kg) divided by height in meters squared. BMI under 18.5 is commonly considered underweight; within the range (18.5 to 25) as normal weight; within the range (25 to 30) as overweight; and over 30 as obese. (NCT01572675)
Timeframe: At study entry (baseline)

Interventionkg/m^2 (Mean)
Group Arcoxia® - Initiation26.6
Group Arcoxia® - Renewal27.1
Group Celebrex® - Initiation27.3
Group Celebrex® - Renewal27.0
Group Arcoxia®26.8
Group Celebrex®27.1

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Medications Co-Prescribed Over the Course of Follow-up With Arcoxia® and Celebrex®

Concomitant medications prescribed during the course of follow-up to participants treated with Arcoxia® and Celebrex® were extracted from participants' medical records. NSAIDS = Non-steroidal anti-inflammatory agents. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
Missing dataAt least one treatmentAnalgesicsCardiovascular agentsDigestive system agentsNervous system agentsRespiratory system agentsMetabolic system agentsRheumatologic agentsNSAIDSAnti-infectious agentsHormonal agentsDermatological agentsHematologic agentsUrinary-genital system agentsOther
Group Arcoxia®2675584139253228191716121314817
Group Celebrex®386555393632232220211613128817

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Number of Participants Requiring Dose Modification of Arcoxia® and Celebrex®

Participants requiring modifications to their Arcoxia® or Celebrex® dose regimens during their on study treatment course were identified. Dose modifications were defined as an increase, decrease followed by increase, decrease, or increase followed by decrease in the participant's daily dose; all categorizations were exclusive. If the maximum dose at discontinuation of treatment was greater than that at initiation, the participant was considered as having had an increase in dose during treatment. Alternatively, if data obtained from a participant's prescription records showed a successive lowering of dosage, the participant was considered as having had a decrease in dose during treatment. Dosages at baseline were included in the dose modification determination for treatment renewal participants. (NCT01572675)
Timeframe: Up to 12 months

,
InterventionParticipants (Number)
Missing dataDose increaseDose decrease followed by increaseDose decreaseDose increase followed by decrease
Group Arcoxia®142120
Group Celebrex®533053

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Pharmacokinetics: Maximum Concentration (Cmax) of Simvastatin

(NCT01632566)
Timeframe: Predose up to 48 hours post dose at Day -3 and Day 28

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
10 mg Simvastatin Day -31.78
10 mg Simvastatin Day 283.4

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Pharmacokinetics: Time of Maximum Concentration (Tmax) of Simvastatin

(NCT01632566)
Timeframe: Predose up to 48 hours post dose at Day -3 and Day 28

Interventionhours (Median)
10 mg Simvastatin Day -32.00
10 mg Simvastatin Day 281.15

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Pharmacokinetics: Time of Maximum Concentration (Tmax) of LY3031207

Time of maximum concentration (Tmax) of LY3031207 post-repeated once daily doses at Day 28. Day 28 results were not calculated for participants who received 225 mg LY3031207 because the study was terminated prior to participants reaching 28 days of dosing for this treatment arm. (NCT01632566)
Timeframe: Predose up to 48 hours post last dose at Day 28

Interventionhours (Geometric Mean)
25 mg LY30312072.00
75 mg LY3031207 and Simvastatin3.00

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Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY3031207

Area under the concentration versus time curve in a dosing interval (AUC[0-tau]) of LY3031207 post-repeated once daily doses at Day 28. Day 28 results were not calculated for participants who received 225 mg LY3031207 because the study was terminated prior to participants reaching 28 days of dosing for this treatment arm. (NCT01632566)
Timeframe: Predose up to 48 hours post last dose at Day 28

Interventionnanograms*hours/milliliter (hr*ng/mL) (Geometric Mean)
25 mg LY303120712000
75 mg LY3031207 and Simvastatin30400

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Pharmacokinetics: Area Under the Concentration Curve (AUC) of Simvastatin

Area under the concentration versus time curve over the range of all measureable concentrations (AUC[0-tlast]) of simvastatin. (NCT01632566)
Timeframe: Predose up to 48 hours post dose at Day -3 and Day 28

Interventionnanograms*hours/milliliter (hr*ng/mL) (Geometric Mean)
10 mg Simvastatin Day -35.23
10 mg Simvastatin Day 288.97

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Pharmacokinetics: Maximum Concentration (Cmax) of LY3031207

Maximum concentration (Cmax) of LY3031207 post-repeated once daily doses at Day 28. Day 28 results were not calculated for participants who received 225 mg LY3031207 because the study was terminated prior to participants reaching 28 days of dosing for this treatment arm. (NCT01632566)
Timeframe: Predose up to 48 hours post last dose at Day 28

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
25 mg LY30312071120
75 mg LY3031207 and Simvastatin2290

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostacyclin Metabolite (PGIM)

Urinary excretion of PGIM, after correcting for urinary creatinine. PGIM was corrected for urinary creatinine by dividing the picograms per milliliter (pg/mL) of metabolite excreted in urine by the concentration of creatinine [milligrams per milliliter (mg/mL)] in urine. Percent change from baseline of urinary excretion of PGIM=(mg creatinine per pg of metabolite excreted in urine postdose-mg of creatinine per pg of metabolite excreted at baseline)/mg of creatinine per pg of metabolite excreted at baseline*100. (NCT01632579)
Timeframe: Baseline, 0 to 2 hours (h), 2 to 4 h, 4 to 6 h, and 6 to 12 h post-dose

,,,,,,,
Interventionpercent change in PGIM (Median)
Percent Change at 0 to 2 hPercent Change at 2 to 4 hPercent Change at 4 to 6 hPercent Change at 6 to 12 h
0.1 mg LY3023703-34.6-19.6-19.1-29.8
0.5 mg LY302370315.518.6-3.513.6
10 mg LY3023703-1.229.3-0.998.4
2.5 mg LY302370322.49.83.70.6
30 mg LY302370333.151.519.544.1
60 mg LY302370327.774.563.349.9
Celecoxib-32.0-66.0-60.0-45.2
Placebo-6.4-10.9-0.9-6.1

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Thromboxane A Metabolite (TXAM)

Urinary excretion of TXAM, after correcting for urinary creatinine. TXAM was corrected for urinary creatinine by dividing the picograms per milliliter (pg/mL) of metabolite excreted in urine by the concentration of creatinine [milligrams per milliliter (mg/mL)] in urine. Percent change from baseline of urinary excretion of TXAM=(mg creatinine per pg of metabolite excreted in urine postdose-mg of creatinine per pg of metabolite excreted at baseline)/mg of creatinine per pg of metabolite excreted at baseline*100. (NCT01632579)
Timeframe: Baseline, 0 to 2 hours (h), 2 to 4 h, 4 to 6 h, and 6 to 12 h post-dose

,,,,,,,
Interventionpercent change in TXAM (Median)
Percent Change at 0 to 2 hPercent Change at 2 to 4 hPercent Change at 4 to 6 hPercent Change at 6 to 12 h
0.1 mg LY3023703-19.9-11.5-19.8-13.8
0.5 mg LY30237036.511.12.67.7
10 mg LY30237038.721.416.418.0
2.5 mg LY3023703-17.9-7.9-18.8-19.2
30 mg LY30237032.726.3-13.19.8
60 mg LY3023703-10.213.018.519.1
Celecoxib-5.0-17.7-25.7-16.2
Placebo-9.1-12.5-15.0-8.7

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Pharmacodynamics: Percent Change From Baseline of Urinary Excretion of Prostaglandin E(2) Metabolite (PGEM)

Urinary excretion of PGEM, after correcting for urinary creatinine. PGEM was corrected for urinary creatinine by dividing the picograms per milliliter (pg/mL) of metabolite excreted in urine by the concentration of creatinine [milligrams per milliliter (mg/mL)] in urine. Percent change from baseline of urinary excretion of PGEM=(mg creatinine per pg of metabolite excreted in urine postdose-mg of creatinine per pg of metabolite excreted at baseline)/mg of creatinine per pg of metabolite excreted at baseline*100. (NCT01632579)
Timeframe: Baseline, 0 to 2 hours (h), 2 to 4 h, 4 to 6 h, 6 to 12 h, and 12 to 24 hours post-dose

,,,,,,,
Interventionpercent change in PGEM (Median)
Percent Change at 0 to 2 hPercent Change at 2 to 4 hPercent Change at 4 to 6 hPercent Change at 6 to 12 hPercent Change at 12 to 24 h
0.1 mg LY30237037.40.7-0.0-18.5-38.8
0.5 mg LY3023703-4.07.9-25.02.3-18.0
10 mg LY3023703-5.3-21.0-29.1-39.5-28.8
2.5 mg LY30237031.5-0.8-19.0-20.4-19.1
30 mg LY302370317.7-46.6-53.0-37.5-31.2
60 mg LY3023703-6.6-25.1-42.4-48.0-53.0
Celecoxib-7.5-41.5-55.0-49.7-46.2
Placebo4.2-2.8-19.0-18.7-29.7

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Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY3023703

Area under the concentration time curve from the time of dosing to the time of the last observation. (NCT01632579)
Timeframe: Day 1: pre-dose, 0.25, 0.5, 1, 2, 4, 8 and 12 hours, post-dose

Interventionhour*nanograms per milliliter (hr*ng/mL) (Geometric Mean)
0.1 mg LY30237033.19
0.5 mg LY302370354.7
2.5 mg LY3023703245
10 mg LY30237031680
30 mg LY30237039940
60 mg LY302370313800

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Pharmacokinetics: Maximum Concentration (Cmax) of LY3023703

(NCT01632579)
Timeframe: Day 1: pre-dose, 0.25, 0.5, 1, 2, 4, 8 and 12 hours, post-dose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
0.1 mg LY30237031.15
0.5 mg LY30237035.66
2.5 mg LY302370323.5
10 mg LY3023703140
30 mg LY3023703547
60 mg LY3023703756

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Pharmacodynamics: Percent Change From Baseline of ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation

Percent change from baseline of PGE synthesis=(postdose PGE synthesis-baseline PGE synthesis)/baseline PGE synthesis*100, where the unit of measure for PGE synthesis is nanograms per milliliter (ng/ml). (NCT01632579)
Timeframe: Baseline, 0.5 hours (h), 1 h, 2 h, 8 h, 24 h, and 144 h post-dose

Interventionpercent change in PGE (Median)
Percent Change at 0.5 hPercent Change at 1 hPercent Change at 2 hPercent Change at 8 hPercent Change at 144 h
0.1 mg LY3023703102.6106.487.944.2-31.1

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Pharmacodynamics: Percent Change From Baseline of ex Vivo Whole Blood Prostaglandin E (PGE) Synthesis After Lipopolysaccharide (LPS) Stimulation

Percent change from baseline of PGE synthesis=(postdose PGE synthesis-baseline PGE synthesis)/baseline PGE synthesis*100, where the unit of measure for PGE synthesis is nanograms per milliliter (ng/ml). (NCT01632579)
Timeframe: Baseline, 0.5 hours (h), 1 h, 2 h, 8 h, 24 h, and 144 h post-dose

,,,,,,
Interventionpercent change in PGE (Median)
Percent Change at 0.5 hPercent Change at 1 hPercent Change at 2 hPercent Change at 8 hPercent Change at 24 hPercent Change at 144 h
0.5 mg LY3023703-11.6-6.252.190.544.120.5
10 mg LY3023703-12.1-67.6-82.7-56.016.1111.6
2.5 mg LY302370329.3-18.9-59.63.3-7.628.9
30 mg LY3023703-43.5-84.1-102.0-96.5-84.2-61.3
60 mg LY3023703-27.1-82.4-89.1-96.1-80.74.3
Celecoxib-7.1-14.0-42.5-26.7-21.811.6
Placebo-10.125.411.230.0-29.0-36.8

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Change From Baseline in the Maximum Flow Rate (Qmax)

"Efficacy:~Change from Baseline in the maximum flow rate (Qmax) from baseline and 3 months Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
InterventionmL/s (Mean)
Baseline3 monthsChange
Control Group10.011.91.9
Study Group12.212.2-0.09

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Change From Baseline in the Serum Prostate Specific Antigen (PSA) Level

"Efficacy:~Change from Baseline in the serum PSA level from baseline and 3 months Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
Interventionng/mL (Mean)
Baseline3 monthsChange
Control Group15.213.5-1.70
Study Group10.89.42-1.43

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Change From Baseline in the Void Volume (VV)

"Efficacy:~Change from Baseline in the Void Volume (VV) from baseline and 3 months Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
InterventionmL (Mean)
Baseline3 monthsChange
Control Group17523155.7
Study Group259227-32.3

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Change From Baseline in the IPSS Subscore (IPSS Storage) Questionnaires

"Efficacy:~Change from Baseline in the IPSS Storage from baseline and 3 months The IPSS subscore (IPSS Storage) is a 3 symptom questions. The symptom score have 6-point scale ranging from 0 Not at all to 5 Almost always. Each question is assigned points from 0 to 5 indicating increasing severity of the particular symptom.~The total IPSS Storage score can therefore range from 0 to 15 (asymptomatic to very symptomatic).~Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
Interventionunits on a scale (Mean)
Baseline3 monthsChange
Control Group6.064.01-2.05
Study Group5.593.09-2.5

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Change From Baseline in the IPSS Subscore (IPSS Voiding) Questionnaires

"Efficacy:~Change from Baseline in the IPSS Voiding from baseline and 3 months. The IPSS subscore (IPSS Voiding) questionnaires is a 4 symptom questions. The symptom score have 6-point scale ranging from 0 Not at all to 5 Almost always. Each question is assigned points from 0 to 5 indicating increasing severity of the particular symptom.~The total IPSS Voiding score can therefore range from 0 to 20 (asymptomatic to very symptomatic).~Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
Interventionunits on a scale (Mean)
Baseline3 monthsChange
Control Group5.543.45-2.09
Study Group7.553.84-3.71

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Change From Baseline in the International Prostate Symptom Score (IPSS) Questionnaires

"Efficacy:~Change from Baseline in the International Prostate Symptom Score (IPSS) from baseline and 3 months The International Prostate Symptom Score (IPSS) is an 7 symptom questions including 4 voiding questions (IPSS Voiding), 3 storage questions (IPSS Storage) The symptom score have 6-point scale ranging from 0 Not at all to 5 Almost always.~Total IPSS score = IPSS voiding + IPSS Storage Rang = 0 to 35 (asymptomatic to very symptomatic). Mild = 0 to 7; Moderate = 8 to 19; Severe = 20 to 35~Change = Month 3 minus Baseline value" (NCT01678313)
Timeframe: Baseline and 3 months after initial treatment

,
Interventionunits on a scale (Mean)
Baseline3 monthsChange
Control Group12.07.70-4.31
Study Group13.16.45-6.63

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Best Overall Response Rate Among All Patients Who Had RECIST Measurements at Baseline and at Least One Subsequent Occasion

RECIST 1.1 criteria will be used to measure changes in the size of a selected sentinel lesion for each patient. Computed tomographic images will be measured at baseline and at subsequent 9 week intervals. Changes will be measured as percentage of the baseline measure. Results will be reported as the largest negative change. For patients with no negative changes, results will be reported as the smallest positive change. (NCT01729923)
Timeframe: Serial measures at 9 week intervals up to 5 years

Interventionpercentage of baseline lesion size (Mean)
Capecitabine and Celecoxib-17

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Best Overall Response Rate Among All Patients Who Had RECIST Measurements at Baseline and at Least One Subsequent Occasion and Did Not Have Surgery or Radiation Therapy

RECIST 1.1 criteria will be used to measure changes in the size of a selected sentinel lesion for each patient. Computed tomographic images will be measured at baseline and at subsequent 9 week intervals. Changes will be measured as percentage of the baseline measure. Results will be reported as the largest negative change. For patients with no negative changes, results will be reported as the smallest positive change. (NCT01729923)
Timeframe: Serial measures at 9 week intervals up to 5 years

Interventionpercentage of baseline lesion size (Mean)
Capecitabine and Celecoxib11

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Overall Survival

Estimated using the Kaplan-Meier method based on the ITT population starting from the time of induction chemotherapy initiation until death or last reported survival. (NCT01729923)
Timeframe: Until death or last reported survival, up to 5 years

Interventionmonths (Median)
Capecitabine and Celecoxib15

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Rate of CR, Assessed According to CEA and CA 19-9 Measurements and Response Evaluation Criteria in Solid Tumors (RECIST) 1.1

Complete Response (CR): Disappearance of all non-target lesions and normalization of tumor marker level in response to ADAPT therapy. (NCT01729923)
Timeframe: 3 years

InterventionParticipants (Count of Participants)
Capecitabine and Celecoxib1

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Relapse Free Survival in Patients Achieving CR

Relapse-free survival estimated using the Kaplan-Meier method based on the ITT population starting from the time of induction chemotherapy initiation. (NCT01729923)
Timeframe: Up to 5 years

Interventionmonths (Number)
Capecitabine and Celecoxib7

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Change in WOMAC-Pain Subscale

"Western Ontario and McMaster Universities (WOMAC) OA index. Version 3.1 of the WOMAC knee and hip osteoarthritis index translated in Korean language will be used for each site enrolled in the trial.~The numerical rating scale version of the WOMAC-Pain subscale was used, i.e., with the subject assessing each question by a 11-point (0-10) numerical rating scale, and the total pain score being represented by the sum of the 5 component item scores. A higher WOMAC score represented worse symptom severity, with 50 being the worst possible total score." (NCT01765296)
Timeframe: Baseline, Week 6

,,
Interventionunits on a scale (Mean)
BaselineWeek 6Change From Baseline
Celecoxib 200 mg27.721.9-5.8
CG100649 2 mg27.922.7-5.3
Placebo26.824.2-2.5

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Change of the WOMAC-physical Function Subscale at Week 3 and 6 From Pre-dose Baseline

"Western Ontario and McMaster Universities (WOMAC) OA index. Version 3.1 of the WOMAC knee and hip osteoarthritis index translated in Korean language will be used for each site enrolled in the trial.~The 24 questions, which measure with 0-10 point numerical rating scale (NRS) with a maximum of 240 points to evaluate Pain (5 questions), Stiffness (2 questions), and Physical Function (17 questions) in WOMAC 3.1.~Total scores for WOMAC-physical function is from 0 to 170 points. A higher WOMAC score represented worse symptom severity." (NCT01765296)
Timeframe: Baseline, Week 3 and Week 6

,,
Interventionunits on a scale (Least Squares Mean)
Week 3Week 6
Celecoxib 200 mg-10.7-14.9
CG100649 2 mg-13.7-14.3
Placebo-5.7-7.9

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the Change of Numeric Rating Scale

"Numeric Rating Scale is 10 point scale(0~10 score). 0 score: no pain, 10 score: worst possible pain~If there is missing data, LOCF(Last Observation Carried Forward) was applied and analyzed." (NCT01768520)
Timeframe: baseline and 12 weeks

,,
Interventionscore on a scale (Mean)
baseline12 weekschange(12weeks-baseline)
Celebrex Cap.5.544.09-1.54
Entelon Tab. 150mg5.623.57-2.14
Placebo5.444.23-1.50

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the Change of Total Sum of K-WOMAC(Korean The Western Ontario and McMaster Universities Arthritis Index)

"Range of total K-WOMAC score: 0-96 K-WOMAC consists of evaluations of pain, stiffness, physical function. The total K-WOMAC score is the sum of all subscale scores. Higher scores mean a worse outcome.~Range of Subscale K-WOMAC score: pain(0-20), stiffness(0-8), physical function(0~68) Higher scores mean a worse outcome.~If there is missing data, LOCF(Last Observation Carried Forward) was applied and analyzed." (NCT01768520)
Timeframe: baseline and 12 weeks

,,
Interventionscore on a scale (Mean)
baseline12 weekschange(12 weeks-baseline)
Celebrex Cap.54.5733.88-19.26
Entelon Tab. 150mg51.6430.68-19.38
Placebo49.9433.80-16.70

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Percentage of Participants With PGIC for Each Arm Compared at Week 5 (Visit 4) and at Week 10 (Visit 6)

The PGIC is a single-item, self-rated instrument that measures change in the patient's overall status since starting study medication on a scale from 1 (very much improved) to 7 (very much worse), where lower scores indicate greater improvement. This scale was administered at Visit 4 and Visit 6. (NCT01838044)
Timeframe: Week 5 and Week 10

,
Interventionpercentage of participants (Number)
Week 5 - very much improved(n=84, 82)Week 5 - much worse(n=84, 82)Week 5 - much improved(n=84, 82)Week 5 - minimally improved(n=84, 82)Week 5 - no change(n=84, 82)Week 5 - minimally worse(n=84, 82)Week 5 - very much worse(n=84, 82)Week 5 - missing(n=84, 82)Week 10 - very much improved(n=81, 76)Week 10 - much improved(n=81, 76)Week 10 - minimally improved(n=81, 76)Week 10 - no change(n=81, 76)Week 10 - minimally worse(n=81, 76)Week 10 - much worse(n=81, 76)Week 10 - very much worse(n=81, 76)Week 10 - missing(n=81, 76)
Arm A11.944.031.08.34.80.00.00.025.946.921.04.90.01.20.00.0
Arm B12.243.932.99.81.20.00.00.031.651.315.80.01.30.00.00.0

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Change From Baseline in the Weekly Mean Pain Numeric Rating Scale (NRS) Score at Week 5 (ie, Visit 4) Compared Between the Two Study Arms

"The Daily Pain diary consists of an 11-point NRS ranging from 0 (no pain) to 10 (worst possible pain). Participants described their pain during the past 24 hours by choosing the appropriate number between 0 and 10: Select the number that best describes your pain during the past 24 hours from 0 to10 where 0 represents no pain and 10 represents the worst possible pain." (NCT01838044)
Timeframe: Baseline and Week 5

InterventionUnits on a scale (Mean)
Arm A-2.18
Arm B-2.03

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Change in the Weekly Mean Pain NRS Score in Arm B, Compared Between Week 5 (Visit 4) and Week 10 (Visit 6).

"The Daily Pain diary consists of an 11-point NRS ranging from 0 (no pain) to 10 (worst possible pain). Participants described their pain during the past 24 hours by choosing the appropriate number between 0 and 10: Select the number that best describes your pain during the past 24 hours from 0 to10 where 0 represents no pain and 10 represents the worst possible pain." (NCT01838044)
Timeframe: Week 5 and Week 10

InterventionUnits on a scale (Least Squares Mean)
Arm B1.42

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Change From Baseline in Benefit, Satisfaction, and Willingness to Continue Measure Scores Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)

The BSW consists of 3, single-item measures designed to capture the participant's perception of the effect of treatment in terms of the relative benefit, their satisfaction, and their intention or willingness to continue on therapy. The BSW was administered by the investigator or designated site personnel in the local language as a standardized interview during the follow-up visits. The BSW can potentially be self-administered; however, this method of administration has not been tested. Participants completed this questionnaire at Visit 4 and Visit 6. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionPercentage of participants (Number)
Benefit from Treatment - No benefit (Week 5)Benefit from Treatment - Little benefit (Week 5)Benefit from Treatment - Much benefit (Week 5)Satisfaction from Treatment - DVN (Week 5) - YesSatisfaction from Treatment - DVN (Week 5) - NoA Little Satisfied (Week 5)Very Satisfied (Week 5)A Little Dissatisfied (Week 5)Very Dissatisfied (Week 5)Willingness to Continue - DVN (Week 5) - YesWillingness to Continue - DVN (Week 5) - NoA Little Bit Willing (Week 5)Very Willing (Week 5)A Little Unwilling (Week 5)Very Unwilling (Week 5)Benefit from Treatment - No benefit (Week 10)Benefit from Treatment - Little benefit (Week 10)Benefit from Treatment - Much benefit (Week 10)Satisfaction from Treatment - DVN (Week 10) - YesSatisfaction from Treatment - DVN (Week 10) - NoA Little Satisfied (Week 10)Very Satisfied (Week 10)A Little Dissatisfied (Week 10)Very Dissatisfied (Week 10)Willingness to Continue - DVN (Week 10) - YesWillingness to Continue - DVN (Week 10) - NoA Little Bit Willing (Week 10)Very Willing (Week 10)A Little Unwilling (Week 10)Very Unwilling (Week 10)
Arm A10.122.561.878.715.720.258.412.43.494.405.688.8004.514.671.983.17.99.074.25.62.288.82.24.584.302.2
Arm B6.629.753.884.65.526.458.24.41.189.01.14.484.601.13.39.970.380.23.311.069.22.21.181.32.24.476.902.2

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Change From Baseline in Hospital Anxiety and Depression Scale (HADS-A) Anxiety Scores at Week 5 (Visit 4) and Week 10 (Visit 6)

The HADS is a self-administered questionnaire measuring anxiety. Each subscale consists of 7 statements and the participants respond as to how each item applies to them on a scale of 0 to 3 (0 = No anxiety, to 3 = Severe feelings of anxiety). Separate scores are calculated for each subscale and a score (ranging from 0 to 21) is obtained for each subscale. The higher the score the more severe the anxiety. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Mean)
Week 5 (n=84, 82)Week 10 (n=81, 76)
Arm A-2.23-3.09
Arm B-1.91-2.68

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Change From Baseline in Hospital Anxiety and Depression Scale (HADS-D) Depression Scores at Week 5 (Visit 4) and Week 10 (Visit 6)

The HADS is a self-administered questionnaire measuring depression. Each subscale consists of 7 statements and the participants respond as to how each item applies to them on a scale of 0 to 3 (0 = No depression, to 3 = Severe feelings of depression). Separate scores are calculated for each subscale and a score (ranging from 0 to 21) is obtained for each subscale. The higher the score the more severe the depression. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Mean)
Week 5 (n=84, 82)Week 10 (n=81, 76)
Arm A-1.87-2.57
Arm B-1.35-2.01

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Change From Baseline in Medical Outcomes Study (MOS) Sleep Scale - Sleep Disturbance Subscale at Week 5 and Week 10

The MOS-Sleep Scale is a self-administered questionnaire consisting of 12 items that assess key constructs of sleep. Instrument scoring yields 7 subscales (sleep disturbance, snoring, awaken short of breath or with a headache, quantity of sleep, optimal sleep, sleep adequacy, and somnolence) as well as a 9-item overall sleep problems index. With the exception of sleep adequacy, optimal sleep, and quantity, higher scores reflect greater impairment in the MOS-Sleep subscales. Sleep Disturbance: Range=0 to 100; higher scores indicate greater sleep disturbance. Negative changes indicate improvement. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Mean)
Week 5 (n= 84, 82)Week 10 (n= 81, 76)
Arm A-21.3-27.1
Arm B-16.5-22.8

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Change From Baseline in Weekly Mean of Daily Sleep Interference Rating Scale (SIRS) Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)

"The Daily Sleep Interference Rating Scale (SIRS) consists of an 11-point NRS ranging from 0 (pain does not interfere with sleep) to 10 (pain completely interferes with sleep [unable to sleep due to pain]). Participants described how pain had interfered with their sleep during the past 24 hours: Select the number that best describes how your pain has interfered with your sleep during the past 24 hours on a scale from 0 to 10 where 0 represents 'does not interfere with sleep' and 10 represents 'completely interferes' which means you are unable to sleep due to pain." (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Least Squares Mean)
Week 5(n= 85, 79)Week 10(n=81, 75)
Arm A-2.46-3.69
Arm B-2.12-3.38

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Patient Global Impression of Change (PGIC) Compared Between Arms at Week 5 (Visit 4) and at Week 10 (Visit 6)

The PGIC is a single-item, self-rated instrument that measures change in the patient's overall status since starting study medication on a scale from 1 (very much improved) to 7 (very much worse), where lower scores indicate greater improvement. This scale was administered at Visit 4 and Visit 6. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Mean)
Week 5 (n=84, 82)Week 10 (n=81, 76)
Arm A2.692.31
Arm B2.642.11

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Percentage of Days in Mild, Moderate and Severe Pain at Period 1 and Period 2

Period 1 indicates from Visit 2 (baseline) to Visit 4 (Week 5). Period 2 indicates from Visit 4 (Week 5) to Visit 6 (Week 10). A rating of 0 is considered no pain; 1-3 is considered mild pain; 4-6, moderate pain; and 7-10, severe pain. (NCT01838044)
Timeframe: Period 1 and Period 2

,
Intervention% of days (Mean)
Period 1 (n=88, 90) (Mild)Period 2 (n=84, 81) (Mild)Period 1 (n=88, 90) (Moderate)Period 2 (n=84, 81) (Moderate)Period 1 (n=88, 90) (Severe)Period 2 (n=84, 81) (Severe)
Arm A19.133.540.233.238.826.5
Arm B15.325.037.644.244.821.8

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Percentage of Participants With >= 30% Reduction From Baseline in the Weekly Mean Pain NRS Score at Week 5 and Week 10

"The Daily Pain diary consists of an 11-point NRS ranging from 0 (no pain) to 10 (worst possible pain). Participants described their pain during the past 24 hours by choosing the appropriate number between 0 and 10: Select the number that best describes your pain during the past 24 hours from 0 to10 where 0 represents no pain and 10 represents the worst possible pain." (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionPercentage of participants (Number)
Yes (Week 5)No (Week 5)Yes (Week 10)No (Week 10)
Arm A51.148.963.631.8
Arm B35.664.458.931.1

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Change From Baseline in Brief Pain Inventory Short Form (BPI sf) - Pain Severity Index Score at Week 5 and Week 10

BPI-sf is a self-administered questionnaire developed to assess the severity of pain and the impact of pain on daily functions during the past 24 hours. The Pain severity domain: The BPI severity domain includes pain at its 'worst,' 'least,' 'average,' and 'now' (current pain) on 0-10 NRS scales and takes the mean of these 4 items. Scores range from 0 (no pain) to 10 (pain as bad as you can imagine), therefore higher scores indicate greater pain severity. (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionUnits on a scale (Mean)
Week 5 (n=84, 82)Week 10 (n=81, 76)
Arm A-1.75-2.83
Arm B-1.68-2.99

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Percentage of Participants With >= 50% Reduction From Baseline in the Weekly Mean Pain NRS Score at Week 5 and Week 10

"The Daily Pain diary consists of an 11-point NRS ranging from 0 (no pain) to 10 (worst possible pain). Participants described their pain during the past 24 hours by choosing the appropriate number between 0 and 10: Select the number that best describes your pain during the past 24 hours from 0 to10 where 0 represents no pain and 10 represents the worst possible pain." (NCT01838044)
Timeframe: Week 5 and Week 10

,
InterventionPercentage of participants (Number)
Yes (Week 5)No (Week 5)Yes (Week 10)No (Week 10)
Arm A25.075.042.053.4
Arm B20.080.037.852.2

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Change From Baseline in the Weekly Mean Pain NRS Score at Week 10 (Visit 6) Compared Between the Two Study Arms

"The Daily Pain diary consists of an 11-point NRS ranging from 0 (no pain) to 10 (worst possible pain). Participants described their pain during the past 24 hours by choosing the appropriate number between 0 and 10: Select the number that best describes your pain during the past 24 hours from 0 to10 where 0 represents no pain and 10 represents the worst possible pain." (NCT01838044)
Timeframe: Baseline and Week 10

InterventionUnits on a scale (Least Squares Mean)
Arm A-3.21
Arm B-3.45

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve [AUC(0-24)] of LY3023703

(NCT01849055)
Timeframe: Post-First Dose on Days 1-28 (Time Frame: Day 1: -0.5, 1, 2, 4, 8, 12, 24 hours; Days 5, 12, 20: -0.5 hours; Day 28: -0.5, 1, 2, 4, 8, 12, 24 hours.)

,,,
Interventionhours•nanogram/milliliter (hr•ng/mL) (Geometric Mean)
Single Oral Dose (Day 1)Multiple Oral Doses (Day 28)
15 mg LY302370323002880
2.5 mg LY3023703332300
30 mg LY302370352908520
7.5 mg LY302370311401340

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Change From Baseline to Day 27 in Blood Pressure (BP)

The Day 27 change from Day -1 was analyzed by using analysis of covariance (ANCOVA) with treatment as a fixed effect and baseline Day -1 as a covariate. The treatment mean, difference to placebo, and difference to celecoxib were output with corresponding 90% confidence intervals. (NCT01849055)
Timeframe: Baseline, Day 27

,,,,,
Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Systolic Blood Pressure (SBP)Diastolic Blood Pressure (DBP)
15 mg LY3023703-2.99-0.68
2.5 mg LY3023703-2.67-0.11
30 mg LY3023703-2.98-1.22
400 mg Celecoxib-5.29-2.24
7.5 mg LY3023703-2.54-0.83
Placebo-1.450.28

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Pharmacokinetics: Maximum Concentration (Cmax) of LY3023703

(NCT01849055)
Timeframe: Post first dose on Day 1 through Day 28 (Time Frame: Day 1: -0.5, 1, 2, 4, 8, 12, 24 hours; Days 5, 12, 20: -0.5 hours; Day 28: -0.5, 1, 2, 4, 8, 12, 24 hours.)

,,,
Interventionng/mL (Geometric Mean)
Single Oral Dose (Day 1)Multiple Oral Doses (Day 28)
15 mg LY3023703228243
2.5 mg LY302370342.641.9
30 mg LY3023703556711
7.5 mg LY3023703126151

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Pharmacokinetics: Time of Maximum Concentration (Tmax) of LY3023703

(NCT01849055)
Timeframe: Post first dose on Day 1 through Day 28 (Time Frame: Day 1: -0.5, 1, 2, 4, 8, 12, 24 hours; Days 5, 12, 20: -0.5 hours; Day 28: -0.5, 1, 2, 4, 8, 12, 24 hours.)

,,,
InterventionHours (Median)
Single Oral Dose (Day 1)Multiple Oral Doses (Day 28)
15 mg LY30237034.004.00
2.5 mg LY30237032.012.00
30 mg LY30237034.004.00
7.5 mg LY30237033.002.00

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Part A: Weighted Mean Change From Baseline in Pain Intensity Over the First 8 Hours Post-Dose Using VAS

Pain intensity was rated by the participant on a 100-mm VAS: 0 mm (no pain) and 100 mm (worst pain imaginable). The participant marked the line at the point that corresponded with his or her perception of pain. Weighted mean change from baseline was calculated as: [the area under the change in pain intensity versus time curve] / 8 hours (h). The baseline pain intensity was the pain assessment prior to dosing of study medication (0 h). Least Squares (LS) mean were calculated using a Bayesian analysis of covariance analysis (ANCOVA) adjusted for treatment as a fixed effect and baseline pain VAS as a continuous covariate. The measure of dispersion reported is 95% Credible Interval (CrI) not Confidence Interval (CI). A negative direction indicates a pain reduction from baseline. (NCT01872910)
Timeframe: 0 to 8 h post-dose

Interventionmm (Least Squares Mean)
Part A - LY3023703-3.8
Part A - Celecoxib-47.4
Part A - Placebo-12.7

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Time to First Use of Rescue Medication

"Time to first use of rescue medication is defined as the time from study drug administration to the measured first use of rescue medication in hours. Participants were censored at 24 h post-dose if no rescue medication was administered.~Pre-Part B used 3 participants in order for the study site to develop proficiency in the dialysate placement, collection, and maintenance techniques. There were no planned efficacy analysis for Pre-Part B per protocol." (NCT01872910)
Timeframe: Study drug administration to first use of rescue medication (0 to 24 h post-dose)

Interventionh (Median)
Part A - LY30237031.8
Part A - CelecoxibNA
Part A - Placebo2.9
Part B - LY30237031.9
Part B - Placebo1.8

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Part A: Patient Global Impression of Improvement (PGI-I) Scale Score

PGI-I is a participant-rated instrument that measures the improvement of the participants symptoms on a 7-point scale: 1 (very much improved), 4 (no change), and 7 (very much worse). LS mean was calculated using Mixed Effect Model Repeated Measures (MMRM) adjusted for treatment, time, the interaction of treatment and time and baseline pain VAS and fixed effects. (NCT01872910)
Timeframe: 2, 4, 8, 12 and 24 h post-dose

,,
Interventionunits on a scale (Least Squares Mean)
2 h4 h8 h12 h24 h
Part A - Celecoxib1.951.921.962.031.74
Part A - LY30237032.912.172.291.911.29
Part A - Placebo3.122.451.941.781.34

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Summed Pain Intensity Difference (SPID) Over the First 24 Hours Post-Dose as Measured by a 4-point Categorical Scale

"The summed (time-weighted) pain intensity difference to baseline (SPID) at 4, 6, 8, 12, and 24 h post-dosing, as measured by a participant-rated 4-point categorical scale of 0 (no pain) to 3 (severe pain) and was calculated as: the area under the change in pain intensity versus time curve. Total scores range: -24 (best) to 8 (worst) for SPID 0 to 8 h. Score ranges for SPID(0-4h), SPID(0-6), SPID(0-12) and SPID(0-24) are -12 to 4, -18 to 6, -36 to 12 and -72 to 24 respectively. Participants were required to have moderate (score=2) or severe (score=3) pain at baseline in order to be eligible for randomization.LS mean were calculated using ANCOVA and was adjusted for treatment as a fixed effect and baseline pain intensity as a continuous covariate. The measure of dispersion reported is 95% CrI not CI. A negative direction indicated a pain reduction from baseline.~There were no planned efficacy analysis for Pre-Part B per protocol." (NCT01872910)
Timeframe: 0 to 4, 0 to 6, 0 to 8, 0 to 12, and 0 to 24 h post-dose

,,,,
Interventionunits on a scale (Least Squares Mean)
0 to 4 h0 to 6 h0 to 8 h0 to 12 h0 to 24 h
Part A - Celecoxib-4.1-6.9-9.4-13.7-27.1
Part A - LY3023703-0.6-1.0-1.3-2.1-5.2
Part A - Placebo-1.2-2.1-3.2-5.5-13.0
Part B - LY30237030.00.20.30.72.4
Part B - Placebo0.30.20.1-0.2-1.7

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Total Pain Relief (TOPAR) Score at 4, 6, 8, 12 and 24 Hours Post-Dose

"TOPAR was calculated as the area under the pain relief versus time curve of the participant reported pain relief scores from the 5-point pain relief scale of 0 (no pain relief) to 4 (complete pain relief). LS mean were calculated using ANCOVA adjusted for treatment as a fixed effect. The measure of dispersion reported is CrI not CI. A negative direction indicated a pain relief from baseline.~Pre-Part B used 3 participants in order for the study site to develop proficiency in the dialysate placement, collection, and maintenance techniques. There were no planned efficacy analysis for Pre-Part B per protocol." (NCT01872910)
Timeframe: 0 to 4, 0 to 6, 0 to 8, 0 to 12, and 0 to 24 h post-dose

,,,,
Interventionpain relief * h (Least Squares Mean)
0 to 4 h0 to 6 h0 to 8 h0 to 12 h0 to 24 h
Part A - Celecoxib8.113.418.428.057.3
Part A - LY30237032.23.85.28.317.9
Part A - Placebo3.66.39.215.134.2
Part B - LY30237031.11.82.33.15.4
Part B - Placebo1.12.03.15.212.4

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Part A: Time to Onset of Meaningful Pain Relief

Time to onset of meaningful pain relief is defined as the time from study drug administration to the measured onset of meaningful pain relief in hours as reported by the participant. Participants who received rescue mediation prior to meaningful pain relief were censored at the time the rescue medication was received. (NCT01872910)
Timeframe: Study drug administration to meaningful pain relief (0 to 24 h post-dose)

Interventionh (Median)
Part A - LY30237033.8
Part A - Celecoxib1.2
Part A - Placebo2.2

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Weighted Mean Change From Baseline in Pain Intensity Over the First 24 Hours Post-Dose as Measured by VAS

"Pain intensity was rated by the participant on a 100-mm VAS: 0 mm (no pain) and 100 mm (worst pain imaginable). The participant marked the line at the point that corresponded with his or her perception of post oral surgery pain. Weighted mean change from baseline was calculated as: [area under the change in pain intensity versus time curve] / [time period that is (i.e.) 24 h for 0 to 24 h endpoint]. The baseline pain intensity was the pain assessment prior to dosing of study medication. LS mean were calculated using ANCOVA adjusted for treatment, time and interaction of treatment as a fixed effect and baseline pain VAS as a continuous covariate. The measure of dispersion reported is the 95% CrI not CI. A negative direction indicated a pain reduction from baseline.~Pre-Part B used 3 participants in order for the study site to develop proficiency in the dialysate placement, collection, and maintenance techniques. There were no planned efficacy analysis for Pre-Part B per protocol." (NCT01872910)
Timeframe: Part A and B: 0 to 4, 0 to 6, 0 to 12, and 0 to 24 h post-dose and Part B 0 to 8 h post-dose

,,,,
Interventionmm (Least Squares Mean)
0 to 4 h0 to 6 h0 to 8 h0 to 12 h0 to 24 h
Part A - Celecoxib-40.5-46.1NA-47.5-47.9
Part A - LY3023703-3.2-3.6NA-4.0-5.2
Part A - Placebo-8.5-10.9NA-14.7-17.7
Part B - LY30237031.01.72.11.03.9
Part B - Placebo-0.6-1.8-2.3-0.6-4.0

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Part A: Time to Onset of First Perceptible Pain Relief

Time to onset of the first perceptible pain relief is defined as the time from study drug administration to the measured onset of first perceptible pain relief in hours as reported by the participant. Participants who received rescue mediation prior to first perceptible pain relief were censored at the time the rescue medication was received. (NCT01872910)
Timeframe: Study drug administration to first perceptible pain relief (0 to 24 h post-dose)

Interventionh (Median)
Part A - LY30237030.9
Part A - Celecoxib0.7
Part A - Placebo1.0

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Self Paced Walking Test (SPWT)

Our primary aim also included a performance-based outcome measure, which was the distance walked during the SPWT. The analysis was a comparison of between-group changes in SPWT between baseline and 8 weeks. The Self-Paced Walking Test (SPWT) is a validated objective measure of a patient's walking capacity, which is performed on a level walking surface. The patient is instructed to walk at their own pace and to stop when the symptoms are troublesome enough that s/he needs to sit down to rest. The total time and total distance walked are measured by the research assistant. Our unit of measure was the total distance walked, expressed in meters. (NCT01943435)
Timeframe: Primary end-point was 8 weeks ( 2 weeks after 6 week intervention is completed).

Interventionmeters (Mean)
Medical Care130.5
Group Exercise219.2
Manual Therapy and Exercise267.8

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Sense Wear Armband

Our secondary aim was to measure the change in physical activity between baseline and 8 weeks using the Sense Wear armband (SWA). The outcome measure was the average number of minutes spent daily performing physical activities >1.5 metabolic equivalents (METs).The SWA is a small device that collects information from multiple sensors: a triaxial accelerometer, heat flux, skin temperature, and galvanic signal. The information is integrated and processed by software using proprietary algorithms utilizing subjects' demographic characteristics (gender, age, height, and weight) to provide minute-by-minute estimates of physical activity. The SWA has shown good reliability and validity. The research participants in our study will wear the SWA for a week before and after they complete the treatment interventions. (NCT01943435)
Timeframe: Primary End-Point was 8 weeks ( 2 weeks after completion of 6-week intervention).

Interventionminutes per day (Mean)
Medical Care-23.1
Group Exercise4.3
Manual Therapy and Exercise-6.0

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Swiss Spinal Stenosis (SSS) Questionnaire Score

Our primary aim included a primary outcome measure of self-reported pain/function, which was the change in SSS total score between baseline and 8 weeks. The Swiss Spinal Stenosis Questionnaire (SSS) is a validated 12-item condition-specific instrument for patients with lumbar spinal stenosis. It provides a patient self-report measure of pain and physical function. Higher scores represent worse symptoms and less physical function. The 12-item SSS total score range is 12-55. For our analysis, we compared the change in the 12-item Total score from baseline to 8 weeks. (NCT01943435)
Timeframe: Primary End-Point was 8 weeks ( 2 weeks after completion of 6-week intervention).

Interventionunits on a scale (Mean)
Medical Care-2.0
Group Exercise-1.7
Manual Therapy and Exercise-4.1

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Pharmacokinetics (PK): Area Under the Concentration Curve Versus Time Curve From Zero to Infinity (AUC 0-∞) of Single Dose LY3127760

(NCT01968070)
Timeframe: Day 1: -1, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, 36, 48, 96, and 144 Hours

Interventionnanograms•hour/milliliter (ng•hr/mL) (Geometric Mean)
Part 1: 20 mg LY3127760NA
Part 1: 60 mg LY31277603010
Part 1: 200 mg LY312776017200
Part 1: 600 mg LY312776040000
Part 1: 600 mg LY3127760 (Fasted)47400
Part 1: 900 mg LY312776071900

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PK: Maximum Observed Concentration (Cmax) of Single Dose LY3127760

(NCT01968070)
Timeframe: Day 1: -1, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, 36, 48, 96, and 144 Hours

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Part 1: 20 mg LY3127760264
Part 1: 60 mg LY3127760890
Part 1: 200 mg LY31277603880
Part 1: 600 mg LY312776010300
Part 1: 600 mg LY3127760 (Fasted)18900
Part 1: 900 mg LY312776021600

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PK: Area Under the Concentration Versus Time Curve During One Dosing Interval [AUC-tau (τ)] of Multiple Doses LY3127760

AUC-tau (τ) where τ is 24-hours for the 20 mg, 60 mg, and 200 mg cohorts, and 12-hours for the 300 mg cohort. (NCT01968070)
Timeframe: Day 28: -1, 0.25, 0.5, 1, 2, 4, 8, 12, 16, and 24 Hours

Interventionng•hr/ml (Geometric Mean)
Part 2: 20 mg LY31277601020
Part 2: 60 mg LY31277604350
Part 2: 200 mg LY312776011300
Part 2: 300 mg LY312776019700

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PK: Cmax of Multiple Doses LY3127760

(NCT01968070)
Timeframe: Post last dose on Day 28: 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, 72, and 168 Hours

Interventionng/mL (Geometric Mean)
Part 2: 20 mg LY3127760301
Part 2: 60 mg LY31277601210
Part 2: 200 mg LY31277603650
Part 2: 300 mg LY31277606170

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PK: Time of Maximum Observed Concentration (Tmax) of Single Dose LY3127760

(NCT01968070)
Timeframe: Day 1: -1, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, 36, 48, 96, and 144 Hours

InterventionHour (Median)
Part 1: 20 mg LY31277602.00
Part 1: 60 mg LY31277602.00
Part 1: 200 mg LY31277602.00
Part 1: 600 mg LY31277602.00
Part 1: 600 mg LY3127760 (Fasted)1.00
Part 1: 900 mg LY31277601.50

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PK: Tmax of Multiple Doses LY3127760

(NCT01968070)
Timeframe: Post-last dose on Day 28: 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, 72, and 168 Hours

Interventionhour (Median)
Part 2: 20 mg LY31277602.00
Part 2: 60 mg LY31277601.65
Part 2: 200 mg LY31277602.00
Part 2: 300 mg LY31277602.00

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Weighted Needle (Pain) Threshold (WNT) in the Secondary Flare Area of Capsaicin-irritated Skin

"Weighted needle (pain) threshold (WNT) in the secondary flare area of capsaicin-irritated skin. The weighted needle (pain) threshold (WNT) will be determined (with regard to investigation of mechanical hyperalgesia in the secondary hyperalgesia zone around the primary capsaicin application zone) by fixed weight steps - contact made by rounded needle tip to skin (ranging from 1 mN to 512 mN)." (NCT02037165)
Timeframe: up to 24 hours(h): -1:20h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionmillinewton (mN) (Mean)
at -1:20hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
150 mg Pregabalin (Prega)347.12301.48280.38254.70265.51255.45266.83273.42330.26340.76
200 mg BI 1026706369.98285.78262.20225.48222.66235.15228.09234.30274.92277.38
50 mg BI 1026706366.65295.65285.35287.94265.58265.77270.27281.21313.77312.85
Placebo348.72312.88290.28269.70274.30268.38261.50292.30331.76323.38

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Overall Peak-to-Peak(PtP) N2/P2-component Amplitude of Laser (Somatosensory/Radiant Heat) Evoked Potentials (LEP) in Ultraviolet B (UVB) -Irradiated Skin

"Overall Peak-to-Peak (PtP) N2/P2-component amplitude of Laser (somatosensory/radiant heat) evoked potentials (LEP) in UVB-irradiated skin.~Treated set (TS)" (NCT02037165)
Timeframe: up to 24 hours (h): -2:05h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
InterventionMicrovolts (µv) (Mean)
at -2:05hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
200 mg BI 102670628.9324.8826.7729.0329.0231.4430.7929.0434.5032.98
200 mg Celecoxib (Cele)26.3526.6027.6024.8725.0523.9724.1026.7733.0630.03
50 mg BI 102670626.0828.0027.1128.7830.9331.4030.1028.1232.5132.83
Placebo29.2227.8425.5726.7429.4830.5431.7432.1634.4834.43

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"Electronic Visual Analogue Scale (100mm VAS Post Laser Pain Scales) - Measured in the Capsaicin-irritated Skin Type."

"Electronic Visual Analogue Scale (100mm VAS Post Laser Pain scales) - measured in the capsaicin-irritated skin type, where 0mm = 'no pain' and 100mm = 'severe pain'." (NCT02037165)
Timeframe: up to 24 hours(h): -1:20h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionunits on a scale (Mean)
at -1:20hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
150 mg Pregabalin (Prega)22.6031.2832.8032.1637.1640.9243.9241.5636.3237.80
200 mg BI 102670620.3627.9233.7636.9244.5248.4047.5647.0039.4838.60
50 mg BI 102670616.7925.9630.0832.7938.7941.7944.2947.2134.2936.83
Placebo18.6430.6435.4839.5246.4447.4849.1650.4838.5239.92

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"Electronic Visual Analogue Scale (VAS) (100mm VAS Post Laser Pain Scales) - Measured in the UVB-irradiated Skin Type"

"Electronic Visual Analogue Scale (100mm VAS Post Laser Pain scales) - measured in the UVB-irradiated skin type, where 0mm = 'no pain' and 100mm = 'severe pain'." (NCT02037165)
Timeframe: up to 24 hours(h): -2:05h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionunits on a scale (Mean)
at -2:05hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
200 mg BI 102670630.1632.2437.1646.8855.5262.0465.4866.6057.7661.13
200 mg Celecoxib (Cele)35.0838.0038.2844.0052.7256.6856.5256.4859.2861.96
50 mg BI 102670628.4232.4636.6742.9253.2556.3363.7165.4657.1361.96
Placebo30.4039.2441.4850.5656.4062.1666.6069.2461.6865.00

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Overall Peak-to-Peak (PtP) N2/P2-component Amplitude of (LEP) in Capsaicin-irritated Skin

Overall Peak-to-Peak (PtP) N2/P2-component amplitude of (LEP) in capsaicin-irritated skin. (NCT02037165)
Timeframe: up to 24 hours(h): -1:20h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionµv (Mean)
at -1:20hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
150 mg Pregabalin (Prega)22.4425.2024.8024.8324.4622.7623.0023.3023.1522.59
200 mg BI 102670619.5725.3523.1124.9826.1325.2625.3124.0623.5323.91
50 mg BI 102670618.5325.0023.6723.9425.6826.7425.8124.1424.4622.94
Placebo21.1727.2127.9627.9727.6927.5326.2525.7726.7524.83

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"Single Peripheral N2-component Amplitudes - Measured in UVB-irradiated Skin Type"

"Single peripheral N2-component amplitudes - measured in UVB-irradiated skin type." (NCT02037165)
Timeframe: up to 24 hours(h): -2:05h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionµv (Mean)
at -2:05hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
200 mg BI 102670614.2512.7013.4515.0614.5816.9516.9315.3018.9318.58
200 mg Celecoxib (Cele)13.4513.6214.2912.2212.6111.8712.0714.0416.9916.67
50 mg BI 102670612.7813.7714.4214.9016.8516.9216.8715.5117.1217.74
Placebo14.6214.4812.5414.4016.0816.5217.2017.4618.7119.01

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"Single Central P2-component Amplitudes - Measured in Capsaicin-irritated Skin Type"

"Single central P2-component amplitudes - measured in capsaicin-irritated skin type." (NCT02037165)
Timeframe: up to 24 hours(h): -1:20h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionµv (Mean)
at -1:20hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
150 mg Pregabalin (Prega)11.4513.0312.7712.6511.9411.9011.5111.2711.3811.24
200 mg BI 102670610.3013.1811.6112.6212.7412.6312.4711.7812.0012.21
50 mg BI 10267068.8812.2712.2412.0912.9713.2012.7911.8711.6211.24
Placebo10.7513.8314.2514.2014.2514.0113.3213.4113.1611.65

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"Single Peripheral N2-component Amplitudes - Measured in Capsaicin-irritated Skin Type"

"Single peripheral N2-component amplitudes - measured in capsaicin-irritated skin type." (NCT02037165)
Timeframe: up to 24 hours(h): -1:20h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionµv (Mean)
at -1:20hat 0:30hat 1:00hat 2:00hat 3:00hat 4:00hat 5:00hat 6:00hat 22:00hat 24:00h
150 mg Pregabalin (Prega)10.9912.1712.0312.1812.5110.8611.4912.0311.7711.35
200 mg BI 10267069.2712.1711.5012.3613.3912.6312.8412.2711.5311.70
50 mg BI 10267069.6512.7311.4311.8512.7113.5413.0112.2712.8411.71
Placebo10.4213.9513.7013.7713.4413.5212.9312.3613.5913.18

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"Single Central P2-component Amplitudes - Measured in UVB-irradiated Skin Type"

"Single central P2-component amplitudes - measured in UVB-irradiated skin type." (NCT02037165)
Timeframe: up to 24 hours(h): -2:05h, 0:30h, 1:00h, 2:00h, 3:00h, 4:00h, 5:00h, 6:00h, 22:00h, 24:00h (relative to study drug administration [h:min])

,,,
Interventionµv (Mean)
UVB, at -2:05hUVB, at 0:30hUVB, at 1:00hUVB, at 2:00hUVB, at 3:00hUVB, at 4:00hUVB, at 5:00hUVB, at 6:00hUVB, at 22:00hUVB, at 24:00h
200 mg BI 102670614.6812.1813.3213.9714.4414.4913.8713.7415.5714.40
200 mg Celecoxib (Cele)12.9012.9813.3112.6512.4412.1012.0312.7316.0713.36
50 mg BI 102670613.3114.2312.6913.8814.0814.4913.2312.6115.4015.09
Placebo14.5914.0613.0312.3413.4014.0114.5414.7115.7715.43

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Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0)

Here is the number of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT02054104)
Timeframe: Date treatment consent signed to final collection of AE data, approximately 9 months and 12 days for cohort 1 and 8 months and 22 days for cohort 2.

InterventionParticipants (Count of Participants)
Cohort 1/Vaccine Plus Chemotherapy8
Cohort 2/Vaccine Alone6

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Fold Change From Baseline of Intensity of Programmed Cell Death Protein 1(PD-1) Expression on Tregs

The Mann=Whitney U test was used to compare the fold change of intensity of PD-1 expression on Tregs between the two groups. A decrease in the fold change is consistent with a better outcome. The difference, or the relative difference, in the values at the two time points were obtained and tested to determine if the difference is equal to zero. If a paired t-test is able to be used, with at least 20 evaluable participants, there is 81% power to detect a change equal to ¾ of a standard deviation of the change at the two-sided 0.025 significance level. This was done in order to allow for a conservative adjustment due to determining the significance of the change in the percent of Tregs on two arms. (NCT02054104)
Timeframe: one month after first 6 vaccinations

Interventionfold change (Mean)
Cohort 1/Vaccine Plus Chemotherapy0.84
Cohort 2/Vaccine Alone0.91

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Fold Change From Baseline of Percent Tregs

The Mann-Whitney U test was used to compare the fold change of percent Tregs between the two groups. A decrease in the fold change is consistent with a better outcome. The difference, or the relative difference, in the values at the two time points were obtained and tested to determine if the difference is equal to zero. If a paired t-test is able to be used, with at least 20 evaluable participants, there is 81% power to detect a change equal to ¾ of a standard deviation of the change at the two-sided 0.025 significance level. This was done in order to allow for a conservative adjustment due to determining the significance of the change in the percent of Tregs on two arms. (NCT02054104)
Timeframe: one month after first 6 vaccinations

Interventionfold change (Mean)
Cohort 1/Vaccine Plus Chemotherapy0.87
Cohort 2/Vaccine Alone0.73

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Number of Participants With an Immunologic Responses

Immunologic responses are defined as an appearance of new serologic reactivity, or increase in existing antibody response to cancer-testis on the X chromosome (CT-X) antigen. Antigens such as New York esophageal squamous cell carcinoma-1 (NY-ESO1) and melanoma antigen gene (MAGE) family members assessed by enzyme-linked immunosorbent assay (ELISA) one month after the 6th vaccine. (NCT02054104)
Timeframe: one month after the 6th vaccine

InterventionParticipants (Count of Participants)
Cohort 1/Vaccine Plus Chemotherapy4
Cohort 2/Vaccine Alone4

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SPID0-8h

Time-weighted sum of pain intensity difference (PID) from 0 to 8 hours post drug administration (SPID0-8h). SPID0-8h: possible range (-400; 800). The greater SPID0-8 the greater the reduction of pain intensity over the first 8 hours post drug administration. (NCT02084511)
Timeframe: up to 8 hours post drug administration

Interventionunits on scale (Least Squares Mean)
BI 50 mg PfOS-50.14
BI 200 mg PfOS-24.06
Placebo-77.54
Celecoxib 200 mg124.47

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Time to First Dose of Rescue Medication

"The time to first dose of rescue medication was defined by the difference in time of the study drug intake and the time of first rescue medication use within the first 10 h after study drug administration.~Kaplan-Meier estimates over time for each treatment and time to event endpoint 'Time to first dose of rescue medication' were presented descriptively.~Subjects without intake of rescue medication within the first 10 hours after study drug administration were censored at 10 hours." (NCT02084511)
Timeframe: up to 10 hours post drug administration

Interventionhours (Median)
BI 50 mg PfOS1.57
BI 200 mg PfOS1.53
Placebo1.52
Celecoxib 200 mgNA

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Time to Meaningful Pain Relief

"Time to meaningful pain relief was captured by a stopwatch started by the trial staff immediately after administration of study medication and stopped by the subject as soon as a meaningful pain relief was felt by the subject. If a subject did not have any meaningful pain relief up to 10 h, the time was censored at 10 h.~Kaplan-Meier estimates over time for each treatment and time to event endpoint 'Time to meaningful pain relief' were presented descriptively." (NCT02084511)
Timeframe: up to 10 hours post drug administration

Interventionhours (Median)
BI 50 mg PfOS5.00
BI 200 mg PfOS2.67
PlaceboNA
Celecoxib 200 mg1.93

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TOTPAR0-8h

Time-weighted total pain relief (PAR) from 0 to 8 hours (TOTPAR0-8h). (TOTPAR0-8h)TOTPAR0-8h: possible range (0;32). The greater TOTPAR0-8h the more pain relief was experienced over the first 8 hours post drug administration. (NCT02084511)
Timeframe: up to 8 hours post drug administration

Interventionunits on scale (Least Squares Mean)
BI 50 mg PfOS3.85
BI 200 mg PfOS3.14
Placebo2.16
Celecoxib 200 mg10.12

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SPID0-2h

Time-weighted sum of PID from 0 to 2 hours (SPID0-2h). SPID0-2h: possible range (-100; 200). The greater SPID0-2 the greater the reduction of pain intensity over the first 2 hours post drug administration. (NCT02084511)
Timeframe: up to 2 hours post drug administration

Interventionunits on scale (Least Squares Mean)
BI 50 mg PfOS-8.08
BI 200 mg PfOS6.57
Placebo-14.01
Celecoxib 200 mg5.20

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Overall Survival (OS)

The length of time from the start of treatment that diagnosed patients are still alive. (NCT02151448)
Timeframe: Up to 5 years

Interventionmonths (Median)
α DC1 Vaccine + Chemokine Modulatory Regimen52

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Time to Progression (TTP)

The length of time from the start of treatment until disease progression, per RECIST 1.1 considering only patients whose deaths were from cancer. Disease progression per RECIST 1.1 Progressive Disease (PD): At least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (Note: the appearance of one or more new lesions is also considered progression). (NCT02151448)
Timeframe: Up to18 months

Interventionmonths (Median)
α DC1 Vaccine + Chemokine Modulatory Regimen15.9

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CXCL10 (Interferon Gamma-induced Protein 10) Levels

Chemokine CXCL10 (Interferon gamma-induced protein 10) concentration levels measures in peripheral blood as a biomarker of anti-tumor activity. Increased levels can be predictive of good prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + Chemokine Modulatory Regimen1221.516335.0137.6

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CXCL11 (C-X-C Motif Chemokine 11) Levels

CXCL11 (C-X-C motif chemokine 11) protein concentration levels measures in peripheral blood. Increased levels can be predictive of good prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + Chemokine Modulatory Regimen359.412893.2208.9

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Interleukin 10 (IL-10) Levels

Interleukin 10 (IL-10) (human cytokine synthesis inhibitory factor (CSIF)) concentration levels measures in peripheral blood. Increased levels of IL-10 is associated with advanced disease and poor prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/ml (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + Chemokine Modulatory Regimen1.27.97.5

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Interleukin-8 (IL-8) Cytokine Levels

Interleukin-8 (IL-8) cytokine concentration levels measures in peripheral blood. Increased levels of IL-8 is associated with associated with advanced disease and poor prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + 1 Cycle of Chemokine Modulatory Regimen9.516.928.6

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Interleukin 6 (IL-6) Cytokine Levels

Interleukin 6 (IL-6) concentration levels measures in peripheral blood. Increased levels of IL-6 is associated with associated with advanced disease and poor prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + 1 Cycle of Chemokine Modulatory Regimen15.232.811.1

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Stromal Derived Factor 1 Alpha (SDF-1A/CXCL-12) Chemokine Levels

Levels of stromal derived factor 1 alpha (SDF-1A/CXCL-12) chemokine in peripheral blood. Higher levels of SDF-1A/CXCL-12 is associated with good prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + 1 Cycle of Chemokine Modulatory Regimen1267.32160.3510.0

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Progression-free Survival (PFS)

The length of time during and after the treatment that patients remain alive with disease that does not progress. Per RECIST 1.1, Progressive Disease (PD): At least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (Note: the appearance of one or more new lesions is also considered progression). (NCT02151448)
Timeframe: Up to 5 years

Interventionmonths (Median)
colon cancerappendiceal cancerMesothelioma
α DC1 Vaccine + Chemokine Modulatory Regimen1916NA

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Tumor Necrosis Factor (TFNα) Cytokine Levels

Tumor necrosis factor (TFNα) cytokine concentration levels measures in peripheral blood. Higher TFNα levels is associated with good prognosis. (NCT02151448)
Timeframe: Prior to vaccine administration (Week 1), prior to vaccine booster (Week 4) and after vaccine booster (Week 8)

Interventionpg/mL (Mean)
Prior to vaccine administration (Week 1)Prior to vaccine booster (Week 4)After vaccine booster (Week 8)
α DC1 Vaccine + 1 Cycle of Chemokine Modulatory Regimen10.831.017.2

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Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Diastolic Blood Pressure (DBPday)

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-7.5
Amlodipine+Placebo-5.53
Placebo+Celecoxib-1.5
Placebo+Placebo-0.32

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Frequency of Adverse Events (Number of Participants Affected/Number of Participants at Risk)

Including any untoward medical occurrence in a participant administered study drug, which do not necessarily have a causal relationship with the study drug [i.e., any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of the study drug, whether or not related to the study drug]. (NCT02172040)
Timeframe: 1 month

InterventionParticipants (Count of Participants)
Amlodipine+Celecoxib27
Amlodipine+Placebo28
Placebo+Celecoxib14
Placebo+Placebo10

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Mean Change in Average 24-hour Ambulatory Diastolic Blood Pressure (DBP24h)

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-7.1
Amlodipine+Placebo-4.8
Placebo+Celecoxib-0.5
Placebo+Placebo0.22

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Mean Change in Average 24-hour Ambulatory Systolic Blood Pressure (SBP24h)

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-10.3
Amlodipine+Placebo-8.02
Placebo+Celecoxib-0.5
Placebo+Placebo-1.19

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Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday) - Primary Endpoint

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-10.6
Amlodipine+Placebo-8.83
Placebo+Celecoxib-0.5
Placebo+Placebo-2.11

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Mean Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday) - Secondary Endpoint

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-10.6
Amlodipine+Placebo-8.83
Placebo+Celecoxib-0.5
Placebo+Placebo-2.11

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Mean Change in Average Night-time (01:00 to 06:00) Ambulatory Systolic Blood Pressure (SBPnight)

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-10.5
Amlodipine+Placebo-6.35
Placebo+Celecoxib-1.7
Placebo+Placebo-1.42

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Mean Log-transformed Amlodipine Plasma Concentration

(NCT02172040)
Timeframe: 24 hours post-dose on Day 14

Interventionlog(pg/mL) (Mean)
Amlodipine+Celecoxib9.634
Amlodipine+Placebo10.025

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Mean Log-transformed Celecoxib Plasma Concentration

(NCT02172040)
Timeframe: 24 hours post-dose on Day 14

Interventionlog(ng/mL) (Mean)
Amlodipine+Celecoxib4.785
Placebo+Celecoxib4.636

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Mean Non-transformed Amlodipine Plasma Concentration

(NCT02172040)
Timeframe: 24 hours post-dose on Day 14

Interventionpg/mL (Mean)
Amlodipine+Celecoxib15,800.83
Amlodipine+Placebo23,453

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Mean Non-transformed Celecoxib Plasma Concentration

(NCT02172040)
Timeframe: 24 hours post-dose on Day 14

Interventionng/mL (Mean)
Amlodipine+Celecoxib139.708
Placebo+Celecoxib138.667

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Mean Change in Average Night-time (01:00 to 06:00) Ambulatory Diastolic Blood Pressure (DBPnight)

(NCT02172040)
Timeframe: Baseline and 2 weeks

InterventionmmHg (Mean)
Amlodipine+Celecoxib-7.0
Amlodipine+Placebo-3.23
Placebo+Celecoxib0.3
Placebo+Placebo0.01

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Change From Baseline to 8 Weeks in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale

The 24-question WOMAC Osteoarthritis Index assesses osteoarthritis (OA) symptoms using pain (5 questions), stiffness (2 questions) and physical function (17 questions) subscales. The WOMAC pain subscale was calculated for each participant at each time point for analysis as the mean score (range 0-100 millimeter [mm] VAS; 0=very good and 100=very poor) of all 5 questions related to pain. Bayesian posterior adjusted mean was calculated using a Bayesian Normal Dynamic Linear Model (NDLM) dose response model with baseline and pooled investigator site included as baseline covariates. (NCT02192190)
Timeframe: Baseline, 8 Weeks

Interventionmm (Least Squares Mean)
Placebo-19.2
Celecoxib-31.3
LY2951742 5 mg + Placebo-16.4
LY2951742 50 mg + Placebo-24.2
LY2951742 120 mg + Placebo-21.8
LY2951742 300 mg + Placebo-17.7

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Change From Baseline to 8 Weeks in the WOMAC Physical Function Subscale

The 24-question WOMAC Osteoarthritis Index assesses osteoarthritis symptoms using pain (5 questions), stiffness (2 questions) and physical function (17 questions) subscales. The WOMAC Osteoarthritis Index version 3.1 was administered according to the study schedule. The WOMAC physical function subscale was calculated for each participant at each time point for analysis as the mean score (range 0-100 mm VAS; 0=very good and 100=very poor) of all 17 questions related to physical function. Least Square Mean (LSM) was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates. (NCT02192190)
Timeframe: Baseline, 8 Weeks

Interventionmm (Least Squares Mean)
Placebo-16.5
Celecoxib-30.6
LY2951742 5 mg + Placebo-15.4
LY2951742 50 mg + Placebo-23.5
LY2951742 120 mg + Placebo-19.5
LY2951742 300 mg + Placebo-18.4

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Change From Baseline to 8 Weeks in the WOMAC Stiffness Subscale

The 24-question WOMAC Osteoarthritis Index assesses osteoarthritis symptoms using pain (5 questions), stiffness (2 questions) and physical function (17 questions) subscales. The WOMAC stiffness subscale will be calculated for each participant at each time point for analysis as the mean score (range 0-100 mm VAS; 0=very good and 100=very poor) of 2 questions related to stiffness. LSM mean was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates. LSM mean was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates. (NCT02192190)
Timeframe: Baseline, 8 Weeks

Interventionmm (Least Squares Mean)
Placebo-18.5
Celecoxib-31.4
LY2951742 5 mg + Placebo-15.1
LY2951742 50 mg + Placebo-23.7
LY2951742 120 mg + Placebo-21.3
LY2951742 300 mg + Placebo-17.3

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Change From Baseline to 8 Weeks in the WOMAC Total Score

The 24-question WOMAC Osteoarthritis Index assesses osteoarthritis symptoms using pain (5 questions), stiffness (2 questions) and physical function (17 questions) subscales.The WOMAC total score was calculated for each participant at each time point for analysis as the mean score (range 0-100 mm VAS; 0=very good and 100=very poor) of 24 questions. LSM mean was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates. LSM mean was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates. (NCT02192190)
Timeframe: Baseline, 8 Weeks

Interventionmm (Least Squares Mean)
Placebo-17.0
Celecoxib-31.1
LY2951742 5 mg + Placebo-15.6
LY2951742 50 mg + Placebo-23.7
LY2951742 120 mg + Placebo-20.0
LY2951742 300 mg + Placebo-18.4

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Change in Baseline to 8 Weeks in Patient's Global Assessment of Osteoarthritis

"The PGA is a patient-rated instrument that measures their assessment of overall OA symptoms. It is based on the participant's response to the question Considering all the ways your osteoarthritis affects you, how are you doing today? using a 100 mm VAS (0=very good and 100=very poor). LSM mean was calculated using a mixed-effects model repeated measures (MMRM) approach with treatment, visit and the interaction of treatment and visit were fitted as fixed effects in the model and baseline and pooled investigator site as baseline covariates." (NCT02192190)
Timeframe: Baseline, 8 Weeks

Interventionmm (Least Squares Mean)
Placebo-22.5
Celecoxib-36.7
LY2951742 5 mg + Placebo-18.5
LY2951742 50 mg + Placebo-19.4
LY2951742 120 mg + Placebo-21.2
LY2951742 300 mg + Placebo-20.4

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Number of Participants With a Response Rate Measured by the Outcome Measures for Rheumatology Committee and Osteoarthritis Research Society International Standing Committee for Clinical Trials Response Criteria Initiative (OMERACT-OARSI)

The responders according to OMERACT-OARSI criteria: participants with at least 50 % improvement in pain or in function scores, along with absolute improvement of 20 mm, were considered responders. Alternatively, participants were considered responders if they showed at least 20% improvement and absolute improvement of 10 mm in at least two of the following scores: pain, function and Patients Global Assessment (PGA) scores. (NCT02192190)
Timeframe: 8 Weeks

Interventionparticipants (Number)
Placebo21
Celecoxib14
LY2951742 5 mg + Placebo7
LY2951742 50 mg + Placebo15
LY2951742 120 mg + Placebo10
LY2951742 300 mg + Placebo10

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Length of Hospital Stay

Participants will be followed for the duration of hospital stay, an expected average of 2-7 days. (NCT02351934)
Timeframe: Up to 7 days

Interventionhours (Median)
Furosemide + Enhanced Recovery After Surgery (ERAS)99.6
Enhanced Recovery After Surgery (ERAS)80.6

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Number of Participants Readmitted to Mayo Clinic Within 30-days

(NCT02351934)
Timeframe: Within 30 days of release from hospital

InterventionParticipants (Count of Participants)
Furosemide + Enhanced Recovery After Surgery (ERAS)13
Enhanced Recovery After Surgery (ERAS)10

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Number of Participants Requiring Nasogastric Tube Placement

(NCT02351934)
Timeframe: Up to 7 days

InterventionParticipants (Count of Participants)
Furosemide + Enhanced Recovery After Surgery (ERAS)6
Enhanced Recovery After Surgery (ERAS)1

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Time to Stool Output

(NCT02351934)
Timeframe: Up to 4 days

Interventionhours (Median)
Furosemide + Enhanced Recovery After Surgery (ERAS)48.8
Enhanced Recovery After Surgery (ERAS)45.4

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Number of Participants With Acute Kidney Injury

Acute kidney injury (AKI) refers to an abrupt decrease in kidney function, resulting in the retention of urea and other nitrogenous waste products and in the dysregulation of extracellular volume and electrolytes. The term AKI has largely replaced acute renal failure (ARF), reflecting the recognition that smaller decrements in kidney function that do not result in overt organ failure are of substantial clinical relevance and are associated with increased morbidity and mortality. The AKI experienced by these patients was not considered an adverse event. (NCT02351934)
Timeframe: Up to 7 days

InterventionParticipants (Count of Participants)
Furosemide + Enhanced Recovery After Surgery (ERAS)2
Enhanced Recovery After Surgery (ERAS)2

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Number of Participants With Hypokalemia

Hypokalemia is generally defined as a serum potassium level of less than 3.5 mmol/L. (NCT02351934)
Timeframe: Up to 7 days

InterventionParticipants (Count of Participants)
Furosemide + Enhanced Recovery After Surgery (ERAS)2
Enhanced Recovery After Surgery (ERAS)3

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Montgomery Asberg Depression Rating Scale (MADRS)

"This depression rating scale will be used to determine clinical outcome for depressed participants.~Scores range from 0-60. The higher the score, the worse the outcome (see below)~Normal: 0-6 Mild Depression: 7-19 Moderate Depression: 20-34 Severe Depression: 35+ Very Severe Depression: 60" (NCT02389465)
Timeframe: Week 6

InterventionTotal Score (Sum of Points) (Mean)
Healthy Control1.27
Placebo19.14
Escitalopram14.04
Escitalopram + Celecoxib12.93

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IL-6 Levels

IL6 levels were measured in participants by blood draw 6 weeks after the first dose was given. (NCT02389465)
Timeframe: up to week 6

Interventionpg/mL (Mean)
Healthy Control5.25
Placebo18.24
Escitalopram3.69
Escitalopram + Celecoxib6.84

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IL10 Levels

IL10 levels were measured in participants by blood draw 6 weeks after the first dose was given (NCT02389465)
Timeframe: up to 6 weeks

Interventionpg/mL (Mean)
Healthy Control4.21
Placebo64.9
Escitalopram12.24
Escitalopram + Celecoxib18.56

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Quantification of Plasma Lipids in the Whole Blood: 15-Hydroxyeicosatetraenoic Acid (15-HETE)

15-HETE in blood taken from celecoxib-treated subjects and stimulated ex vivo with LPS was compared to similarly treated blood from placebo group. Plasma 15-HETE was normalized to sample volume (ng/ml) and expressed as a percentage of subject's pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents 15-HETE concentration in ng/ml. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib49
Placebo81.65

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Quantification of Plasma Lipids in the Whole Blood: Prostaglandin E2 (PGE2)

PGE2 in blood taken from celecoxib-treated subjects and stimulated ex vivo with LPS was compared to similarly treated blood from placebo group. Plasma PGE2 was normalized to sample volume (ng/ml) and expressed as a percentage of subject's pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents PGE2 concentration in ng/ml. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib49.9
Placebo110

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Quantification of Plasma Lipids in the Whole Blood: Prostaglandin F2a (PGF2a)

PGF2a in blood taken from celecoxib-treated subjects and stimulated ex vivo with LPS was compared to similarly treated blood from placebo group. Plasma PGF2a was normalized to sample volume (ng/ml) and expressed as a percentage of subject's pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents PGF2a concentration in ng/ml. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib45.48
Placebo97.2

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Quantification of Plasma Lipids in the Whole Blood: Thromboxane B2 (TxB2)

TxB2 in blood taken from celecoxib-treated subjects and stimulated ex vivo with LPS was compared to similarly treated blood from placebo group. Plasma TxB2 was normalized to sample volume (ng/ml) and expressed as a percentage of subject's pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents TxB2 concentration in ng/ml. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib52.2
Placebo83.4

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Urinary Lipid Metabolites: PGE2 Metabolite (PGE-M)

Effect of celecoxib on systemic PGE2 was assessed by comparing urine PGE-M in celecoxib vs placebo-treated groups. Urine data are reported as a percentage of the volunteer's own pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents metabolite concentration in ng/mg creatinine. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib79.15
Placebo106

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Celecoxib Plasma Concentration

Celecoxib plasma concentration will be measured in drug-treated and placebo groups by UPLC-MS/MS, and will be expressed as amount of the drug per volume of plasma (ng/ml). At Tmax of 3 hours after a single oral dose of celecoxib of 200 mg, drug plasma concentration should correspond to the maximum plasma concentration or Cmax. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionng/ml (Mean)
Celecoxib352.6
Placebo0

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Urinary Lipid Metabolites: PGI2 Metabolite (PGI-M)

Effect of celecoxib on systemic PGI2 was assessed by comparing urine PGI-M in celecoxib vs placebo-treated groups. Urine data are reported as a percentage of the volunteer's own pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents metabolite concentration in ng/mg creatinine. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib41.47
Placebo78.6

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Urinary Lipid Metabolites: TxB2 Metabolite (Tx-M)

Effect of celecoxib on systemic TxB2 was assessed by comparing urine Tx-M in celecoxib vs placebo-treated groups. Urine data are reported as a percentage of the volunteer's own pre-dose control using the formula: percentage of pre-dose control = (Cpost-dose/Cpre-dose) × 100%, where C represents metabolite concentration in ng/mg creatinine. (NCT02413203)
Timeframe: A single visit of around 4 hours

Interventionpercentage of pre-dose control (Mean)
Celecoxib79
Placebo77.9

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Overall Survival

First local recurrence and first distant recurrence will be recorded on separate parts of the CRF. In the event of local progression, all patients must be followed up for distant recurrence, second malignancy and survival. Similarly in the case of second malignancy, the appropriate CRF should be completed and patients should REACT Protocol, Version 39, dated 01.11.2016 Page 34 of 48 continue to be followed for disease progression and where possible the relation of any subsequent disease progression and/or death due to the primary or second cancer should be established. (NCT02429427)
Timeframe: Date of randomisation until the date of death from any cause or censored at the date the patient was last seen alive, this will be assessed at 2 and 5 years

,
InterventionPercentage of participants (Number)
2 Year5 Year
Celecoxib9790
Placebo9691

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Disease Free Survival (DFS) Benefit of Two Years Adjuvant Therapy With the COX-2 Inhibitor Celecoxib Compared With Placebo in Primary Breast Cancer Patients.

From time of randomisation to the date of first event; with events contributing to the analysis defined as loco-regional and distant breast cancer recurrence, new primary breast cancer (ipsilateral or contralateral) and death without disease relapse (intercurrent death) (NCT02429427)
Timeframe: Patients will be followed up to 10 years. DFS will be calculated from date of randomization until the date of first documented DFS event, this will be assessed at 2 and 5 years

,
InterventionPercentage of participants (Number)
2 Year DFS rate5 Year DFS rate
Celecoxib9184
Placebo9083

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Number of Participants With Incidence of Second Primary Breast Cancers

Any malignant contralateral breast disease will be included and recorded as a second primary (NCT02429427)
Timeframe: From randomisation until a second primary breast cancer is diagnosed. Patients will be followed up to 10 years.

InterventionParticipants (Count of Participants)
Celecoxib19
Placebo12

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Cardiovascular Mortality

Number of deaths recorded as having cardiovascular involvement are reported by treatment group. (NCT02429427)
Timeframe: Patients are followed up to 10 years, any deaths within this timeframe with cardiovascular involvement reported are included in the analysis.

InterventionParticipants (Count of Participants)
Celecoxib6
Placebo5

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St. George's Respiratory Questionnaire

"St. George's Respiratory Questionnaire is a commonly used questionnaire to assess the respiratory function of an individual.~The minimum and maximyum socres on this Questionnaire are: 0 and 100. A higher score shows more limitations, so a lower score is better in terms of respiratory function.~There are no subscales. Below we are providing mean scores for all 9 participants in this trial." (NCT02484664)
Timeframe: 1 year

Interventionscore on a scale (Least Squares Mean)
Celecoxib20.2

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Number of Participants With Adverse Events as a Measure of Safety and Tolerability

Number of Participants with Adverse Events as a Measure of Safety and Tolerability in LAM patients (NCT02484664)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Celecoxib11

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FEV1

Forced expiratory volume in 1 second (NCT02484664)
Timeframe: 1 year

Interventionml (Least Squares Mean)
Celecoxib2583

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Angiomyolipoma Size Measured Volumetrically on MRI

We are reporting the number of participants in this trial who had angiomyolipoma either at the beginning or end of the study. (NCT02484664)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Celecoxib3

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VEGF-D Serum Levels

VEGF-D serum levels (NCT02484664)
Timeframe: 6 months

Interventionpg/mL (Median)
Celecoxib656

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COX-2 Activity in Vivo

COX-2 activity was measured in vivo by quantifying the urinary metabolite of prostaglandin I2 before, and 1, 2, 4, 8, and 12 h after treatment, normalized to urinary creatinine and expressed as AUC over the 12 hour dosing interval. (NCT02502006)
Timeframe: 12 hours

Interventionng*h/mg creatinine (Mean)
Celecoxib1.610
Naproxen1.253
Placebo2.413

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Diastolic Blood Pressure

Blood pressure was measured over 12 hours using an automatic ambulatory blood pressure monitor. (NCT02502006)
Timeframe: 12 hours

Interventionmm Hg (Mean)
Celecoxib74.8
Naproxen76.6
Placebo89.7

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Mean Arterial Pressure

Blood pressure was measured over 12 hours using an automatic ambulatory blood pressure monitor. (NCT02502006)
Timeframe: 12 hours

Interventionmm Hg (Mean)
Celecoxib90.4
Naproxen92.9
Placebo89.7

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Systolic Blood Pressure

Blood pressure was measured over 12 hours using an automatic ambulatory blood pressure monitor. (NCT02502006)
Timeframe: 12 hours

Interventionmm Hg (Mean)
Celecoxib123.0
Naproxen127.1
Placebo124.1

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COX-1 Activity in Vivo

COX-1 activity was measured in vivo by quantifying the urinary metabolite of thromboxane A2 before, and 1, 2, 4, 8, and 12 h after treatment, normalized to urinary creatinine and expressed as AUC over the 12 hour dosing interval. (NCT02502006)
Timeframe: 12 hours

Interventionng*h/mg creatinine (Mean)
Celecoxib8.018
Naproxen2.907
Placebo9.509

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COX-1 Activity ex Vivo

COX-1 activity was measured ex vivo using a whole blood assay. Thromboxane A2 serum concentrations were quantified before, and 0.5, 1, 2, 4, 8, and 12 h after treatment and expressed as AUC over the 12 hour dosing interval. (NCT02502006)
Timeframe: 12 hours

Interventionng*h/ml (Mean)
Celecoxib2869
Naproxen115.7
Placebo3135

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COX-2 Activity ex Vivo

COX-2 activity was assessed ex vivo using a whole blood assay. Prostaglandin E2 concentrations in LPS-treated plasma were quantified before, and 0.5, 1, 2, 4, 8, and 12 h after treatment and expressed as AUC over the 12 hour dosing interval. (NCT02502006)
Timeframe: 12 hours

Interventionng*h/ml (Mean)
Celecoxib87.86
Naproxen54.71
Placebo154.1

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Assessment of Joint Swelling, Effusion or Both

Assessment of Joint Swelling, joint Effusion or Both (NCT02688400)
Timeframe: Day 182 or early termination

,
Interventionparticipants (Number)
Joint SwellingJoint EffusionJoint Swelling and Effusion
Celecoxib483723
Diacerein473719

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OARSI Responders

Osteoarthritis Research Society International (OARSI) Responders (NCT02688400)
Timeframe: Day 182 or early termination

InterventionParticipants (Count of Participants)
Diacerein99
Celecoxib97

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Change From Baseline in WOMAC A Pain Subscale

Relative mean change from baseline in WOMAC Pain subscore (NCT02688400)
Timeframe: baseline and 728 days

Interventionpercentage of change in WOMAC Pain score (Mean)
Diacerein-26.2
Celecoxib-37.1

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Change From Baseline in Patient's Global Assessment of Disease Activity

Change from baseline in global assessment of disease activity was assessed using a VAS scale (0-10cm; 10=worse) (NCT02688400)
Timeframe: Day 182 or early termination

,
Interventionscore (Mean)
Patient's Global AssessmentInvestigator's Global Assessment
Celecoxib-1.97-2.65
Diacerein-1.81-2.02

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Change From Baseline in WOMAC OA Scores

"Absolute Changes from Baseline in Western Ontario and McMaster Universities Arthritis Index (WOMAC) after 182 days of treatment.~WOMAC scale: 0 - 240 cm; 240 = worse - Intention-To-Treat (N=370) Pain subscale: 0-50cm; 50 = worse; Stifness subscale: 0-20cm; 20 = worse; Function subscale: 0-170cm; 170 = worse Absolute changes in WOMAC scores: <0 = improvement; 0 = stable; >0 = worsening" (NCT02688400)
Timeframe: Day 182 or early termination

,
Interventionscore (Mean)
Total ScorePain ScoreStiffness ScorePhysical Function Score
Celecoxib-42.9-9.60-3.99-29.3
Diacerein-41.0-10.03-3.56-27.2

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Global Assessment of Response to Therapy

Between group comparison in Patient's and Investigator's Global Assessment of Response to Therapy using a 0-10 cm disease activity VAS scale: 0 cm = very well; 10 cm = very poorly (NCT02688400)
Timeframe: Day 182 or early termination

,
Interventionscore on a scale (Mean)
Patient's Global AssessementInvestigator's Global Assessment
Celecoxib3.613.35
Diacerein3.893.85

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Quality of Life SF-36

Absolute Changes from Baseline in Physical Component Summary (PCS) and Mental Component Summary (MCS) scores from the Quality of Life questionnaire SF-36. Scale range for each component (PCS and MCS): minimum = 0, maximum = 100, with higher scores indicating better quality of life. Absolute changes in each component (PCS and MCS): >0 = improvement; 0 = stable; <0 = worsening. (NCT02688400)
Timeframe: Day 182 or early termination

,
Interventionscore on a scale (Mean)
Physical Component SummaryMental Component Summary
Celecoxib4.57-0.14
Diacerein2.461.56

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Change From Baseline in Visual Analogue Scale Pain (VAS-Huskisson's)

Relative change from baseline in Visual Analogue Scale pain (VAS-Huskisson's) (NCT02688400)
Timeframe: baseline and 728 days

InterventionPercentage of change in VAS score (Mean)
Diacerein-31.4
Celecoxib-37.6

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Change From Baseline in Synovitis (Synovial Membrane Thickness) Using MRI

Absolute Change from baseline in synovitis (synovial membrane thickness) in the global knee using MRI (NCT02688400)
Timeframe: baseline and 728 days

Interventionmm (Mean)
Diacerein0.24
Celecoxib0.27

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Change From Baseline in Global Stiffness Using WOMAC Subscale

Relative Change from baseline in global stiffness using WOMAC subscale (NCT02688400)
Timeframe: baseline and 728 days

Interventionpercentage of change in WOMACStifness sc (Mean)
Diacerein-24.3
Celecoxib-38.1

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Change Form Baseline in WOMAC A Pain Subscale

"Change form baseline in Western Ontario and McMaster Universities Arthritis Index (WOMAC) A pain subscale after 182 days of treatment.~WOMAC A pain subscale: 0 - 50 cm; 50 = worse" (NCT02688400)
Timeframe: baseline and 182 days

Interventioncm (Mean)
Diacerein-11.14
Celecoxib-11.82

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Consumption of Acetaminophen

Overall Daily number of tablets taken during the 6 month study (NCT02688400)
Timeframe: Day 182 or early termination

Interventiontablets (Mean)
Diacerein1.06
Celecoxib0.91

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Cartilage Volume Loss From Baseline in the Medial Compartment Using MRI

Relative cartilage volume loss from baseline in the medial compartment of the knee using MRI (NCT02688400)
Timeframe: baseline and 728 days

Interventionpercentage of volume loss (Mean)
Diacerein-4.8
Celecoxib-6.0

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Cartilage Volume Loss From Baseline in the Lateral Compartment Using MRI

Relative cartilage volume loss from baseline in the lateral compartment of the knne using MRI (NCT02688400)
Timeframe: baseline and 728 days

Interventionpercentage of volume loss (Mean)
Diacerein-4.4
Celecoxib-4.1

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Absolute Changes From Baseline in Pain Visual Analogue Scale

Absolute Changes from Baseline in Pain Visual Analogue Scale (VAS): 0-10 cm; 10 = worse (NCT02688400)
Timeframe: Day 182 or early termination

Interventionscore (Mean)
Diacerein-2.34
Celecoxib-2.46

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Narcotic Use at 2 Weeks Postop

Assessment of the amount of narcotic use postoperatively at 2 weeks. will use opioid equivalence table to convert all narcotic use to oxycodone equivalents (NCT02703259)
Timeframe: 2 weeks

Interventionmorphine milligram equivalents (Mean)
Gabapentin167.2
Control187.3

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Narcotic Use at 24 Hours Postop

Assessment of the amount of narcotic use postoperatively at 24 hours. will use opioid equivalence table to convert all narcotic use to oxycodone equivalents (NCT02703259)
Timeframe: 24 hours

Interventionmorphine milligram equivalents (Mean)
Gabapentin158.8
Control175.0

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Subjective Pain at 2 Weeks Postop

"Assessment of the subject pain score postoperatively at 2 weeks. will use a numeric analog scale from 0-10.~The pain scale ranging from 0-10 with 0 representing No Pain and 10 representing the Worst Pain Possible" (NCT02703259)
Timeframe: 2 weeks

Interventionscore on a scale (Mean)
Gabapentin1.3
Control1.4

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Subjective Pain at 24 Hours Postoperative

Pain score assesses patient subjective pain via patient reported numeric analogue scale, range 0-10 with 0 being no pain and 10 being severe pain. (NCT02703259)
Timeframe: 24 hours

Interventionscore on a scale (Mean)
Gabapentin3.4
Control3.4

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Number of Patient With Gabapentin Adverse Effects at 2 Weeks Postoperatively

Will assess for known symptoms of gabapentin postoperatively at 2 weeks. We will survey subjects regarding their experience of the following symptoms: dizziness/drowsiness, fatigue, loss of balance, blurry vision, tremulousness, swelling, nausea, vomiting, diarrhea, and allergic reaction (NCT02703259)
Timeframe: 2 weeks

,
InterventionParticipants (Count of Participants)
DizzinessBlurred visionSomnolenceDifficulty walkingTremulousnessNauseaVomiting
Control83215271
Gabapentin1241854120

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Number of Patient With Gabapentin Adverse Effects at 24 Hours Postoperatively

Will assess for known symptoms of gabapentin postoperatively at 24 hours. We will survey subjects regarding their experience of the following symptoms: dizziness/drowsiness, fatigue, loss of balance, blurry vision, tremulousness, swelling, nausea, vomiting, diarrhea, and allergic reaction (NCT02703259)
Timeframe: 24 hours

,
InterventionParticipants (Count of Participants)
DizzinessBlurred VisionSomnolenceDifficulty walkingTremulousnessNauseaVomiting
Control84231162515
Gabapentin177201311249

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Number of Days of Rescue Medication Use During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64: Observed Data

In case of inadequate pain relief, acetaminophen/paracetamol tablets up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Number of days the participants used the rescue medication during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64

,,
Interventiondays (Mean)
Week 2Week 4Week 8Week 12Week 16Week 24Week 32Week 40Week 48Week 56Week 64
Celecoxib0.80.70.70.70.51.00.70.50.60.41.0
Tanezumab 10 mg0.80.60.40.40.40.40.30.50.40.40.6
Tanezumab 5 mg0.90.80.60.40.51.10.70.50.80.71.1

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Number of Participants Who Took Rescue Medication During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56: Last Observation Carried Forward (LOCF)

In case of inadequate pain relief, acetaminophen/paracetamol caplets, tablets, or capsules up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Number of participants with any use of rescue medication during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56

,,
InterventionParticipants (Count of Participants)
Week 2Week 4Week 8Week 12Week 16Week 24Week 32Week 40Week 48Week 56
Celecoxib33282729263234273032
Tanezumab 10 mg24241916212627302828
Tanezumab 5 mg37302817153227242829

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Number of Participants Who Took Rescue Medication During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64: Observed Data

In case of inadequate pain relief, acetaminophen/paracetamol tablets up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Number of participants with any use of rescue medication during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, 56 and 64

,,
InterventionParticipants (Count of Participants)
Week 2Week 4Week 8Week 12Week 16Week 24Week 32Week 40Week 48Week 56Week 64
Celecoxib3327252721141258914
Tanezumab 10 mg2423191418109109913
Tanezumab 5 mg3630281714211411151623

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Number of Participants With Abnormal Physical Examination Findings

Physical examination included assessment of general appearance, skin, head, neck, eyes, ears, nose, throat, abdomen, lungs, heart, thyroid, and extremities. Investigator judged abnormality in physical examinations. Only those rows have been reported which had at least 1 participant with abnormality data in any of the reporting arms. (NCT02725411)
Timeframe: At Screening

,,
InterventionParticipants (Count of Participants)
SkinNeckEyesEarNoseExtremitiesHeart
Celecoxib3012111
Tanezumab 10 mg0111013
Tanezumab 5 mg1210002

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Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent were events between first dose of study drug and up to 24 weeks after last dose of study drug (up to Week 80) that were absent before treatment or that worsened relative to pretreatment state. AEs included both serious and non-serious AEs. (NCT02725411)
Timeframe: Baseline (Day 1) up to 24 weeks after last dose of study drug (up to Week 80)

,,
InterventionParticipants (Count of Participants)
Participants with AEsParticipants with SAEs
Celecoxib674
Tanezumab 10 mg6311
Tanezumab 5 mg708

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Observation Time-Adjusted Event Rate for an Individual Adjudicated Joint Safety Outcome/Event

Individual adjudicated joint safety outcomes/event: rapidly progressive OA (type-1,type-2), primary osteonecrosis, pathological fracture and subchondral insufficiency fracture. Observation time was defined as the start day of first SC study medication until either the (i) date of completion of or withdrawal from study, if a participant did not have the event, or (ii) date of the event (earliest event within each participant in the case of multiple events). Event rate for any individual adjudicated joint safety outcome/event = the number of events per 1000 participant-years at risk. (NCT02725411)
Timeframe: Baseline (Day 1) up to Week 80

,,
Interventionevents per 1000 participant-years (Number)
Rapidly Progressive OA Type 1Rapidly Progressive OA Type 2Primary OsteonecrosisPathological FractureSubchondral Insufficiency Fracture
Celecoxib00000
Tanezumab 10 mg010.40010.5
Tanezumab 5 mg8.90000

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Percentage of Participants Achieving Change of >=2 Points From Baseline in Patient's Global Assessment (PGA) of Low Back Pain at Weeks 16, 24, 40 and 56

"PGA of low back pain assessed by asking question to participants: Considering all ways your low back pain affects you, how are you doing today? They responded on 5 point Likert scale ranging from 1 to 5, using IRT, where 1= very good (asymptomatic and no limitation of normal activities); 2= good (mild symptoms and no limitation of normal activities); 3= fair (moderate symptoms and limitation of some normal activities); 4= poor (severe symptoms and inability to carry out most normal activities); 5= very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher scores indicated worsening of condition. Percentage of participants with positive change of at least 2 points from baseline in PGA of low back pain were reported." (NCT02725411)
Timeframe: Baseline, Weeks 16, 24, 40 and 56

,,
Interventionpercentage of participants (Number)
Week 16Week 24Week 40Week 56
Celecoxib16.39.89.810.9
Tanezumab 10 mg12.915.111.811.8
Tanezumab 5 mg17.418.523.918.5

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Percentage of Participants With >=30 Percent (%), >=50%, >=70% and >=90% Reduction From Baseline in Weekly Average Low Back Pain Intensity (LBPI) Score at Weeks 16, 24, 40 and 56

Average LBPI was assessed on an 11-point numeric rating scale (NRS). Participants described their average LBPI during the past 24 hours (at each specified/scheduled time point) on a scale ranging from 0 (no pain) to 10 (worst possible pain), where higher scores indicated worse pain. Percentage of participants with reduction in average LBPI of at least (>=) 30%, 50%, 70% and 90% at Weeks 16, 24, 40, and 56 compared to baseline are reported here. Participants (%) might have been counted more than once under various rows. (NCT02725411)
Timeframe: Baseline, Weeks 16, 24, 40 and 56

,,
Interventionpercentage of participants (Number)
Week 16: At least 30% reductionWeek 16: At least 50% reductionWeek 16: At least 70% reductionWeek 16: At least 90% reductionWeek 24: At least 30% reductionWeek 24: At least 50% reductionWeek 24: At least 70% reductionWeek 24: At least 90% reductionWeek 40: At least 30% reductionWeek 40: At least 50% reductionWeek 40: At least 70% reductionWeek 40: At least 90% reductionWeek 56: At least 30% reductionWeek 56: At least 50% reductionWeek 56: At least 70% reductionWeek 56: At least 90% reduction
Celecoxib58.732.68.72.253.338.010.91.148.935.917.4051.141.317.41.1
Tanezumab 10 mg57.035.517.24.351.643.021.54.348.440.924.75.447.338.725.84.3
Tanezumab 5 mg71.751.119.63.365.250.025.06.566.353.334.87.663.053.335.99.8

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Percentage of Participants With Chronic Low Back Pain Responders Index at Weeks 16, 24, 40 and 56

Chronic low back pain responder index analysis is a composite endpoint of average low back pain intensity (aLBPI) score, PGA of low back pain, and RMDQ total score. aLBPI: evaluate average pain during the past 24 hours, range 0 (no pain) to 10 (worst possible pain), higher scores = higher worse pain. PGA of low back pain: evaluated participants' well-being due to low back pain on day of assessment, range 1 (very good) to 5 (very poor), higher scores = worse condition. RMDQ total score: assessed ability to perform daily activities, range 0 (no disability) to 24 (maximum disability), higher scores = more disability. Participants were successful responders if they had: >=30 percent reduction in aLBPI from baseline to particular week; decrease of >=30 percent in PGA of low back pain from baseline to particular week and no worsening (increase) in RMDQ total score from baseline to particular week. (NCT02725411)
Timeframe: Weeks 16, 24, 40 and 56

,,
Interventionpercentage of participants (Number)
Week 16Week 24Week 40Week 56
Celecoxib50.042.441.342.4
Tanezumab 10 mg48.445.243.039.8
Tanezumab 5 mg54.353.356.551.1

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Percentage of Participants With Cumulative Percent Change From Baseline in Average Low Back Pain Intensity (LBPI) Score at Weeks 16, 24 and 56

Average LBPI was assessed on an 11-point numeric rating scale (NRS). Participants described their average LBPI during the past 24 hours (at each specified/scheduled time point) on a scale ranging from 0 (no pain) to 10 (worst possible pain), where higher scores indicated worse pain. Percentage of participants with cumulative reduction (as percent change) (greater than [>] 0%; >= 10, 20, 30, 40, 50, 60, 70, 80, 90 and equals to [=] 100%) in average LBPI from baseline to weeks 16, 24 and 56 were reported. Participants (%) might have been counted more than once under various rows. (NCT02725411)
Timeframe: Baseline, Weeks 16, 24 and 56

,,
Interventionpercentage of participants (Number)
Week 16: >0%Week 16: >=10%Week 16: >=20%Week 16: >=30%Week 16: >=40%Week 16: >=50%Week 16: >=60%Week 16: >=70%Week 16: >=80%Week 16: >=90%Week 16: =100%Week 24: >0%Week 24: >=10%Week 24: >=20%Week 24: >=30%Week 24: >=40%Week 24: >=50%Week 24: >=60%Week 24: >=70%Week 24: >=80%Week 24: >=90%Week 24: =100%Week 56: >=0%Week 56: >=10%Week 56: >=20%Week 56: >=30%Week 56: >=40%Week 56: >=50%Week 56: >=60%Week 56: >=70%Week 56: >=80%Week 56: >=90%Week 56: =100%
Celecoxib81.578.366.358.745.732.616.38.76.52.22.259.857.655.453.346.738.020.710.94.31.1052.251.151.151.144.641.332.617.410.91.11.1
Tanezumab 10 mg81.777.467.757.046.235.525.817.214.04.34.360.257.055.951.648.443.035.521.516.14.33.251.650.550.547.343.038.733.325.814.04.32.2
Tanezumab 5 mg89.185.976.171.759.851.133.719.613.03.33.372.870.769.665.257.650.038.025.017.46.52.268.568.564.163.059.853.341.335.923.99.84.3

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Percentage of Participants With Individual Adjudicated Joint Safety Outcome/Event

Percentage of participants with individual joint safety adjudication outcomes: rapidly progressive osteoarthritis (OA) type-1 only, rapidly progressive OA type-2 only, primary osteonecrosis, pathological fracture and subchondral insufficiency fracture is reported. Rapidly progressive (RP) OA type 1 events were those that the adjudication committee considered to have significant loss of joint space width >= 2 millimeter within approximately 1 year without gross structural failure. RP OA type 2 events were those considered to have destruction of bone including limited or total collapse of at least 1 subchondral surface that is not normally present in conventional end-stage osteoarthritis. Subchondral insufficiency fractures are a type of stress fractures which occur below the cartilage on the weight bearing surface of a bone. (NCT02725411)
Timeframe: Baseline up to Week 80

,,
Interventionpercentage of participants (Number)
Rapidly Progressive OA type 1Rapidly Progressive OA type 2Primary OsteonecrosisPathological FractureSubchondral Insufficiency Fracture
Celecoxib00000
Tanezumab 10 mg01001
Tanezumab 5 mg10000

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Time to Discontinuation Due to Lack of Efficacy

Time to discontinuation (in days) due to lack of efficacy was defined as the time interval from the date of first study drug administration up to the date of discontinuation of participant from treatment due to lack of efficacy. Results reported below are contributed only by participants who discontinued due to lack of efficacy. (NCT02725411)
Timeframe: Baseline up to Week 56

,,
Interventiondays (Number)
Minimum1st Percentile2nd Percentile5th PercentileMaximum
Celecoxib141141141NA141
Tanezumab 10 mg151529NA113
Tanezumab 5 mg111111NANA111

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Treatment Satisfaction Questionnaire for Medication Version II (TSQM v II) Scores at Weeks 16 and 56

TSQM v.II: participant rated 11 items questionnaire. Items 1, 2, 7 to 11 were scored as: 1= extremely dissatisfied, 2= very dissatisfied, 3= dissatisfied, 4= somewhat satisfied, 5= satisfied, 6= very satisfied, 7= extremely satisfied. Items 4 to 6 were scored as: 1= extremely dissatisfied, 2= very dissatisfied, 3= somewhat dissatisfied, 4= slightly dissatisfied, 5= not at all dissatisfied. Item 3 was scored as: 0= No, 1= Yes. Four parameters with respect to study medication were evaluated: Effectiveness = ([Item 1+Item 2] - 2 )/12 *100; Side effects = ([Item 4 + Item 5 + Item 6] - 3)/12 *100, if one item is missing then: ([Sum of two completed items]-2]/8 *100; Convenience = ([Item 7 + Item 8 + Item 9] - 3)/18 *100, if one item is missing then: ([Sum of two completed items]-2)/12 *100; Global satisfaction = ([Item 10+Item 11] - 2 ]/12 *100. Each of the 4 parameters had a scale of 0 (no satisfaction) to 100 (best level of satisfaction), higher score = greater satisfaction. (NCT02725411)
Timeframe: Weeks 16 and 56

Interventionunits on a scale (Mean)
Week 16: EffectivenessWeek 16: Side EffectsWeek 16: ConvenienceWeek 16: Global SatisfactionWeek 56: EffectivenessWeek 56: ConvenienceWeek 56: Global Satisfaction
Tanezumab 5 mg61.4156.9464.7963.4171.3069.9372.22

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Treatment Satisfaction Questionnaire for Medication Version II (TSQM v II) Scores at Weeks 16 and 56

TSQM v.II: participant rated 11 items questionnaire. Items 1, 2, 7 to 11 were scored as: 1= extremely dissatisfied, 2= very dissatisfied, 3= dissatisfied, 4= somewhat satisfied, 5= satisfied, 6= very satisfied, 7= extremely satisfied. Items 4 to 6 were scored as: 1= extremely dissatisfied, 2= very dissatisfied, 3= somewhat dissatisfied, 4= slightly dissatisfied, 5= not at all dissatisfied. Item 3 was scored as: 0= No, 1= Yes. Four parameters with respect to study medication were evaluated: Effectiveness = ([Item 1+Item 2] - 2 )/12 *100; Side effects = ([Item 4 + Item 5 + Item 6] - 3)/12 *100, if one item is missing then: ([Sum of two completed items]-2]/8 *100; Convenience = ([Item 7 + Item 8 + Item 9] - 3)/18 *100, if one item is missing then: ([Sum of two completed items]-2)/12 *100; Global satisfaction = ([Item 10+Item 11] - 2 ]/12 *100. Each of the 4 parameters had a scale of 0 (no satisfaction) to 100 (best level of satisfaction), higher score = greater satisfaction. (NCT02725411)
Timeframe: Weeks 16 and 56

,
Interventionunits on a scale (Mean)
Week 16: EffectivenessWeek 16: Side EffectsWeek 16: ConvenienceWeek 16: Global SatisfactionWeek 56: EffectivenessWeek 56: Side EffectsWeek 56: ConvenienceWeek 56: Global Satisfaction
Celecoxib58.0568.7564.3961.9367.0579.1768.6067.44
Tanezumab 10 mg61.4880.5666.8562.3171.3283.3368.8672.29

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Health Care Resource Utilization (HCRU): Number of Participants Who Used Any Aids/Devices for Doing Things

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Number of participants who used any aids/devices for doing things were evaluated. Aids included walking aid, wheelchair, device or utensil for dress/bathe/eat and any other aids/devices. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

InterventionParticipants (Count of Participants)
Baseline: Walking aid use71912452Baseline: Walking aid use71912453Baseline: Walking aid use71912451Baseline: Wheelchair use71912453Baseline: Wheelchair use71912452Baseline: Wheelchair use71912451Baseline: Device/Utensil to Dress Bathe Eat71912453Baseline: Device/Utensil to Dress Bathe Eat71912452Baseline: Device/Utensil to Dress Bathe Eat71912451Baseline: Other Aids or Devices71912452Baseline: Other Aids or Devices71912453Baseline: Other Aids or Devices71912451Week 64: Walking aid use71912452Week 64: Walking aid use71912453Week 64: Walking aid use71912451Week 64: Wheelchair use71912452Week 64: Wheelchair use71912451Week 64: Wheelchair use71912453Week 64: Device/Utensil to Dress Bathe Eat71912452Week 64: Device/Utensil to Dress Bathe Eat71912451Week 64: Device/Utensil to Dress Bathe Eat71912453Week 64: Other aids or devices71912453Week 64: Other aids or devices71912451Week 64: Other aids or devices71912452Week 80: Walking aid use71912453Week 80: Walking aid use71912451Week 80: Walking aid use71912452Week 80: Wheelchair use71912451Week 80: Wheelchair use71912452Week 80: Wheelchair use71912453Week 80: Device/Utensil to Dress Bathe Eat71912452Week 80: Device/Utensil to Dress Bathe Eat71912453Week 80: Device/Utensil to Dress Bathe Eat71912451Week 80: Other Aids Or Devices71912452Week 80: Other Aids Or Devices71912453Week 80: Other Aids Or Devices71912451
AlwaysNeverRarelySometimesOften
Tanezumab 10 mg91
Celecoxib90
Tanezumab 5 mg92
Celecoxib92
Tanezumab 10 mg93
Celecoxib91
Tanezumab 5 mg90
Tanezumab 10 mg87
Tanezumab 10 mg2
Celecoxib3
Tanezumab 5 mg88
Tanezumab 10 mg86
Celecoxib85
Tanezumab 5 mg1
Tanezumab 5 mg2
Tanezumab 5 mg91
Tanezumab 10 mg88
Tanezumab 5 mg0
Celecoxib0
Celecoxib86
Tanezumab 10 mg85
Celecoxib80
Celecoxib2
Tanezumab 5 mg61
Tanezumab 10 mg41
Tanezumab 5 mg62
Tanezumab 10 mg42
Celecoxib43
Celecoxib42
Tanezumab 10 mg1
Celecoxib1
Tanezumab 10 mg0

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Number of Participants Responding to Patient Reported Treatment Impact Assessment-Modified (mPRTI) at Weeks 16 and 56 for Preference of Study Drug Versus Prior Treatment

The mPRTI was a self-administered questionnaire containing 4 items to assess participant satisfaction, previous treatment, preference and willingness to continue using the study medication. To assess preference to continue using study drug versus previous treatment, participants responded using IRT on 5 point Likert scale from 1-5, where, 1= yes, I definitely prefer drug that I am receiving now, 2= I have a slight preference for drug that I am receiving now, 3= I have no preference either way, 4= I have a slight preference for my previous treatment, 5= No, I definitely prefer my previous treatment. Higher scores indicate lesser preference to use study drug. (NCT02725411)
Timeframe: Weeks 16 and 56

InterventionParticipants (Count of Participants)
Week 1671912452Week 1671912453Week 1671912451Week 5671912451Week 5671912452Week 5671912453
No preference either waySlight preference for my previous treatmentYes, definitely prefer the study drugSlight preference for the study drugNo, definitely prefer my previous treatment
Tanezumab 5 mg38
Tanezumab 10 mg33
Celecoxib31
Tanezumab 5 mg25
Tanezumab 10 mg26
Celecoxib30
Tanezumab 5 mg22
Tanezumab 10 mg28
Celecoxib23
Tanezumab 5 mg6
Tanezumab 10 mg2
Celecoxib3
Tanezumab 5 mg1
Tanezumab 10 mg1
Celecoxib1
Tanezumab 5 mg33
Tanezumab 10 mg21
Celecoxib19
Tanezumab 5 mg15
Tanezumab 10 mg14
Celecoxib16
Tanezumab 5 mg13
Tanezumab 10 mg7
Celecoxib8
Tanezumab 5 mg0
Tanezumab 5 mg2
Tanezumab 10 mg0
Celecoxib0

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Number of Participants Responding to Patient Reported Treatment Impact Assessment-Modified (mPRTI) at Weeks 16 and 56 for Willingness to Use Study Drug Again

The mPRTI was a self-administered questionnaire containing 4 items to assess participant satisfaction, previous treatment, preference and willingness to continue using the study medication. To assess participants willingness to use study drug again, participants responded using IRT on 5 point Likert scale ranged from 1-5, where, 1= yes, I would definitely want to use the same drug again, 2= I might want to use the same drug again, 3= I am not sure, 4= I might not want to use the same drug again, 5= no, I definitely would not want to use the same drug again. Higher scores indicated lesser willingness to use the study drug. (NCT02725411)
Timeframe: Weeks 16 and 56

InterventionParticipants (Count of Participants)
Week 1671912452Week 1671912451Week 1671912453Week 5671912451Week 5671912452Week 5671912453
Might not want to use the same drug againYes, definitely want to use the same drug againMight want to use the same drug againI am not sureNo,definitely wouldn't want to use same drug again
Tanezumab 5 mg41
Tanezumab 10 mg37
Celecoxib40
Tanezumab 5 mg28
Tanezumab 10 mg27
Celecoxib25
Tanezumab 5 mg18
Tanezumab 10 mg25
Tanezumab 5 mg3
Tanezumab 10 mg1
Tanezumab 5 mg2
Tanezumab 5 mg34
Tanezumab 10 mg19
Celecoxib21
Tanezumab 5 mg12
Tanezumab 10 mg13
Celecoxib15
Tanezumab 5 mg16
Tanezumab 10 mg10
Celecoxib6
Tanezumab 5 mg0
Celecoxib1
Tanezumab 5 mg1
Tanezumab 10 mg0
Celecoxib0

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 48

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 48

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.09
Tanezumab 10 mg-0.01
Celecoxib0.04

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Number of Days of Rescue Medication Use During Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56: LOCF

In case of inadequate pain relief, acetaminophen/paracetamol caplets, tablets, or capsules up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Number of days the participants used the rescue medication during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56

,,
Interventiondays (Mean)
Week 2Week 4Week 8Week 12Week 16Week 24Week 32Week 40Week 48Week 56
Celecoxib0.80.80.80.80.71.61.51.41.51.4
Tanezumab 10 mg0.80.60.40.50.61.21.21.31.21.3
Tanezumab 5 mg1.00.80.60.40.51.51.31.21.31.3

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Change From Baseline in Average Low Back Pain Intensity (LBPI) at Week 64: Observed Data

Average LBPI was assessed on an 11-point NRS. Participants described their average LBPI during the past 24 hours (at each specified/scheduled time-point) on a scale ranging from 0 (no pain) to 10 (worst possible pain), where higher scores indicated worse pain. (NCT02725411)
Timeframe: Baseline, Week 64

Interventionunits on a scale (Mean)
Tanezumab 5 mg-3.60
Tanezumab 10 mg-3.96
Celecoxib-3.46

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 16

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 16

Interventionunits on a scale (Mean)
Tanezumab 5 mg-0.02
Tanezumab 10 mg0.05
Celecoxib0.01

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 24

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Tanezumab 5 mg-0.02
Tanezumab 10 mg0.09
Celecoxib0.28

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 32

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 32

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.00
Tanezumab 10 mg-0.01
Celecoxib0.04

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 4

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 4

Interventionunits on a scale (Mean)
Tanezumab 5 mg-0.08
Tanezumab 10 mg-0.02
Celecoxib0.11

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 40

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 40

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.14
Tanezumab 10 mg0.04
Celecoxib0.04

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 56

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 56

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.09
Tanezumab 10 mg-0.02
Celecoxib0.04

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 64

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 64

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.18
Tanezumab 10 mg0.01
Celecoxib0.04

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 8

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 8

Interventionunits on a scale (Mean)
Tanezumab 5 mg-0.04
Tanezumab 10 mg0.15
Celecoxib0.13

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 80

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 80

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.03
Tanezumab 10 mg0.00
Celecoxib0.17

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Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Score at Week 64: Observed Data

The RMDQ is a self-administered, widely used health status measure index of how well participants with low back pain (LBP) are able to function with regard to daily activities. It measures pain and function, using 24 items describing limitations to everyday life that can be caused by LBP. Participants were asked to check/select only those items out of 24 items, which described them at each specified time point. The total number of items checked in questionnaire was equal to RMDQ total score, overall possible score ranging from 0 (no disability) to 24 (maximum disability), where higher scores indicated greater/more disability. (NCT02725411)
Timeframe: Baseline, Week 64

Interventionunits on a scale (Mean)
Tanezumab 5 mg-4.55
Tanezumab 10 mg-5.72
Celecoxib-5.02

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Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Early Termination Follow-up Visit 1

"SAS: participant rated 12 items questionnaire for males; 11 items questionnaire for females. SAS measures autonomic symptoms of neuropathy and their impact on participants' well-being, during past 6 months. Each item was related to a symptom/health problem. At scheduled time points, participants answered Yes or No for each of symptoms/health problems experienced during past 6 months. If participant answered Yes for a symptom, then impact of that symptom was rated on 5 point scale (1 [least sever impact] to 5 [most severe impact]); higher scores = more severe impact of symptoms. Total impact score = sum of impact of all symptoms; range for males =0 (no impact) to 60 (extreme impact); females =0 (no impact) to 55 (extreme impact); higher scores = more severe impact of symptoms on participants' well-being. Participants discontinuing from study treatment before Week 56, had early termination follow-up visit 1 at 8 weeks after last dose of tanezumab or placebo matched to tanezumab." (NCT02725411)
Timeframe: Screening, Early Termination Follow-up Visit 1 (at 8 weeks after last dose of tanezumab or placebo matched to tanezumab)

Interventionunits on a scale (Mean)
Tanezumab 5 mg2.50
Tanezumab 10 mg0.82
Celecoxib2.15

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Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Week 56

"SAS is a participant rated 12 items questionnaire for males and 11 items questionnaire for females. SAS measures autonomic symptoms of neuropathy and their impact on participants' well-being, during the past 6 months. Each item was related to a symptom/health problem. At scheduled time points, participants were asked to answer Yes or No for each of symptoms/health problems experienced during past 6 months. If a participant answered Yes for a symptom, then impact of that symptom was rated on a 5 point scale, ranged from 1 (least sever impact) to 5 (most severe impact), where higher scores signified more severe impact of symptoms. The total symptom impact score was calculated as the sum of impact of all symptoms. Overall possible range for the total symptom impact score was 0 (no impact) to 60 (extreme impact) for males and 0 (no impact) to 55 (extreme impact) for females, higher scores indicated more severe impact of symptoms on participants' well-being." (NCT02725411)
Timeframe: Screening, Week 56

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.89
Tanezumab 10 mg0.86
Celecoxib0.35

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Change From Screening in Mean Total Symptom Impact Scores as Per Survey of Autonomic Symptoms (SAS) at Early Termination Follow-up Visit 3

"SAS: participant rated 12 items questionnaire for males; 11 items questionnaire for females. SAS measures autonomic symptoms of neuropathy and their impact on participants' well-being, during past 6 months. Each item was related to a symptom/health problem. At scheduled time points, participants answered Yes or No for each of symptoms/health problems experienced during past 6 months. If participant answered Yes for a symptom, then impact of that symptom was rated on 5 point scale (1 [least sever impact] to 5 [most severe impact]); higher scores = more severe impact of symptoms. Total impact score = sum of impact of all symptoms; range for males =0 (no impact) to 60 (extreme impact); females =0 (no impact) to 55 (extreme impact); higher scores = more severe impact of symptoms on participants' well-being. Participants discontinuing from study treatment before Week 56, had early termination follow-up visit 3 at 24 weeks after last dose of tanezumab or placebo matched to tanezumab." (NCT02725411)
Timeframe: Screening, Early Termination Follow-up Visit 3 (at 24 weeks after last dose of tanezumab or placebo matched to tanezumab)

Interventionunits on a scale (Mean)
Tanezumab 5 mg1.89
Tanezumab 10 mg1.60
Celecoxib0.88

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Change From Screening in Mean Total Symptom Impact Scores as Per Survey of Autonomic Symptoms (SAS) at Week 80

"SAS is a participant rated 12 items questionnaire for males and 11 items questionnaire for females. SAS measures autonomic symptoms of neuropathy and their impact on participants' well-being, during the past 6 months. Each item was related to a symptom/health problem. At scheduled time points, participants were asked to answer Yes or No for each of symptoms/health problems experienced during past 6 months. If a participant answered Yes for a symptom, then impact of that symptom was rated on a 5 point scale, ranged from 1 (least sever impact) to 5 (most severe impact), where higher scores signified more severe impact of symptoms. The total symptom impact score was calculated as the sum of impact of all symptoms. Overall possible range for the total symptom impact score was 0 (no impact) to 60 (extreme impact) for males and 0 (no impact) to 55 (extreme impact) for females, higher scores indicated more severe impact of symptoms on participants' well-being." (NCT02725411)
Timeframe: Screening, Week 80

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.69
Tanezumab 10 mg1.26
Celecoxib0.72

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Largest Change From Baseline in Neuropathy Impairment Score (NIS) to Any Post-baseline Visit

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. Largest change from baseline here means worst post- baseline change value (among all change from baseline values). (NCT02725411)
Timeframe: Baseline to any post-baseline visit (until Week 80)

Interventionunits on a scale (Mean)
Tanezumab 5 mg0.33
Tanezumab 10 mg0.37
Celecoxib0.78

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Number of Participants Who Discontinued Due to Lack of Efficacy

Number of participants who discontinued from study treatment due to lack of efficacy have been reported here. (NCT02725411)
Timeframe: Baseline up to Week 56

InterventionParticipants (Count of Participants)
Tanezumab 5 mg1
Tanezumab 10 mg4
Celecoxib1

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Number of Participants With Anti Tanezumab Antibodies From Baseline up to Week 80

Human serum samples were analyzed for the presence or absence of anti-tanezumab antibodies by using a validated analytical method. Number of participants with presence of anti-tanezumab antibodies are reported. (NCT02725411)
Timeframe: Baseline up to Week 80

InterventionParticipants (Count of Participants)
Tanezumab 5 mg21
Tanezumab 10 mg41
Celecoxib62

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Number of Participants With Clinically Significant Electrocardiogram (ECG) Assessments

Electrocardiogram assessment included PR, QRS, QT, QT interval corrected using Fridericia's formula (QTcF), QT interval corrected using Bazett's formula (QTcB), RR intervals, and heart rate. Investigator judged clinical significance of electrocardiogram assessment. (NCT02725411)
Timeframe: Baseline up to Week 16

InterventionParticipants (Count of Participants)
Tanezumab 5 mg2
Tanezumab 10 mg0
Celecoxib2

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Number of Participants With Clinically Significant Laboratory Test Abnormalities

Abnormality criteria included: hemoglobin (HGB); hematocrit; erythrocytes < 0.8*lower limit of normal (LLN); erythrocyte mean corpuscular volume/HGB/ HGB concentration, erythrocytes distribution width <0.9*LLN, >1.1*upper limit of normal (ULN); platelets <0.5*LLN,>1.75* ULN; white blood cell count<0.6*LLN, >1.5*ULN; lymphocytes, leukocytes, neutrophils <0.8*LLN, >1.2*ULN; basophils, eosinophils, monocytes >1.2*ULN; total bilirubin>1.5*ULN; aspartate aminotransferase (AT), alanine AT, gamma glutamyl transferase, lactate dehydrogenase, alkaline phosphatase >3.0*ULN; total protein; albumin<0.8*LLN, >1.2*ULN; blood urea nitrogen, creatinine, cholesterol, triglycerides >1.3*ULN; urate >1.2*ULN; sodium <0.95*LLN,>1.05*ULN; potassium, chloride, calcium, magnesium, bicarbonate <0.9*LLN, >1.1*ULN; phosphate <0.8*LLN, >1.2*ULN; glucose <0.6*LLN, >1.5*ULN; HGB A1C >1.3*ULN; creatine kinase >2.0*ULN; nitrite >=1. Investigator judged clinical significance of laboratory test abnormalities. (NCT02725411)
Timeframe: Baseline up to Week 80

InterventionParticipants (Count of Participants)
Tanezumab 5 mg1
Tanezumab 10 mg0
Celecoxib1

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Number of Participants With Clinically Significant Vital Signs Abnormalities

Vital signs included systolic blood pressure, diastolic blood pressure and pulse rate. Investigator judged clinical significance of vital signs' abnormalities. (NCT02725411)
Timeframe: Baseline up to Week 80

InterventionParticipants (Count of Participants)
Tanezumab 5 mg4
Tanezumab 10 mg2
Celecoxib5

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Number of Participants With Confirmed Orthostatic Hypotension From Baseline up to Week 80

Orthostatic hypotension was defined as postural change (supine to standing) that met the following criteria: for systolic blood pressure (BP) less than or equal to (<=) 150 millimeter of mercury (mmHg) (mean supine): reduction in systolic BP >=20 mmHg or reduction in diastolic BP >=10 mmHg at the 1 and/or 3 minute standing BP measurements. For systolic BP greater than (>) 150 mmHg (mean supine): reduction in systolic BP >=30 mmHg or reduction in diastolic BP >=15 mmHg at the 1 and/or 3 minute standing BP measurements. If the 1 minute or 3 minute standing BP in a sequence met the orthostatic hypotension criteria, then that sequence was considered positive. If 2 of 2 or 2 of 3 sequences were positive, then orthostatic hypotension was considered confirmed. (NCT02725411)
Timeframe: Baseline up to Week 80

InterventionParticipants (Count of Participants)
Tanezumab 5 mg0
Tanezumab 10 mg2
Celecoxib0

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Observation Time-Adjusted Event Rate for Total Joint Replacement (TJR) Event

Observation time was defined as the start day of first SC study medication until either the (i) date of completion of or withdrawal from study, if a participant had no TJR, or (ii) date of TJR (earliest TJR within each participant in the case of multiple TJRs). Event rate = number of events per 1000 participant-years at risk. (NCT02725411)
Timeframe: Baseline (Day 1) up to Week 80

Interventionevents per 1000 participant-years (Number)
Tanezumab 5 mg0
Tanezumab 10 mg10.4
Celecoxib0

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Percentage of Participants With At Least 1 Total Joint Replacement

Percentage of participants with at least 1 total knee, total hip or total shoulder joint replacement were reported. (NCT02725411)
Timeframe: Baseline (Day 1) up to Week 80

Interventionpercentage of participants (Number)
Tanezumab 5 mg0
Tanezumab 10 mg1
Celecoxib0

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Amount of Rescue Medication Used in Weeks 2, 4, 8, 12, and 16: LOCF

In case of inadequate pain relief, acetaminophen/paracetamol caplets, tablets, or capsules up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Amount of rescue medication used during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12 and 16

,,
Interventionmilligrams (Mean)
Week 2Week 4Week 8Week 12Week 16
Celecoxib809821855742652
Tanezumab 10 mg701543661631584
Tanezumab 5 mg1042885813648693

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Amount of Rescue Medication Used in Weeks 2, 4, 8, 12, and 16: Observed Data

In case of inadequate pain relief, acetaminophen/paracetamol tablets up to 3000 mg per day up to 3 days in a week could be taken as rescue medication between Day 1 to Week 64. Amount of rescue medication used during each specified/scheduled study week were summarized. (NCT02725411)
Timeframe: Weeks 2, 4, 8, 12 and 16

,,
Interventionmilligrams (Mean)
Week 2Week 4Week 8Week 12Week 16
Celecoxib809812776657642
Tanezumab 10 mg701440559477292
Tanezumab 5 mg1029885813655680

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Change From Baseline in Average Low Back Pain Intensity (LBPI) at Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48, and 56: Multiple Imputation

Average LBPI was assessed on an 11-point numeric rating scale (NRS). Participants described their average LBPI during the past 24 hours (at each specified/scheduled time-point) on a scale ranging from 0 (no pain) to 10 (worst possible pain), where higher scores indicated worse pain. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48 and 56

,,
Interventionunits on a scale (Least Squares Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 16Change at Week 24Change at Week 32Change at Week 40Change at Week 48Change at Week 56
Celecoxib-0.46-0.56-1.07-1.85-2.28-2.11-2.08-2.06-2.09-2.13
Tanezumab 10 mg-0.69-1.05-1.64-2.46-2.51-2.41-2.34-2.32-2.31-2.22
Tanezumab 5 mg-0.47-0.83-1.24-2.19-2.91-2.88-2.95-3.00-3.07-2.98

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Average Pain at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. BPI-sf scores for average pain: participants were asked to rate their pain by circling any 1 number from 0 (no pain) to 10 (pain as bad as you can imagine) that best describes their pain on average in the last 24 hours; higher scores indicated worse pain. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.50-1.01-1.16-2.57-3.92-4.16-4.30-3.70
Tanezumab 10 mg-0.78-1.28-1.87-3.07-4.66-4.50-4.42-3.72
Tanezumab 5 mg-0.68-1.12-1.49-3.07-4.10-4.38-4.43-3.53

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference Index at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. Pain interference index was calculated as the mean of the 7 BPI-sf pain interference items: pain interference with general activity; mood; walking ability; normal work (outside home and housework); relations with other people; sleep and enjoyment of life. Each of the 7 items had score range from 0 (does not interfere) to 10 (completely interferes), higher scores indicated more interference in daily activities due to pain. Overall score range for pain interference index was 0 (no interference) to 10 (complete interference), higher score = higher interference. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.78-1.16-1.51-2.62-3.52-3.69-3.54-3.17
Tanezumab 10 mg-0.87-1.32-1.84-2.70-3.74-3.48-3.79-3.29
Tanezumab 5 mg-0.98-1.43-1.75-2.98-3.76-3.88-3.86-3.31

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With General Activity at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. BPI-sf scores for pain interference with general activity: participants were asked to circle from any 1 number from 0 (no interference) to 10 (complete interference) that described how, during the past 24 hours, pain has interfered with their general activity; higher scores indicated higher interference. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.67-1.26-1.77-2.92-4.06-4.23-4.19-3.63
Tanezumab 10 mg-1.05-1.54-2.04-3.04-4.62-4.36-4.65-3.88
Tanezumab 5 mg-1.10-1.68-2.04-3.29-4.30-4.59-4.49-3.89

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Normal Work at Weeks 2, 4, 8, 16, 24, 40, 56 and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. BPI-sf scores for pain interference with normal work: participants were asked to circle from any 1 number from 0 (does not interfere) to 10 (completely interferes) that described how, during the past 24 hours, pain has interfered with their normal work; higher scores indicated higher interference. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.96-1.30-1.69-2.93-4.02-4.16-4.14-3.77
Tanezumab 10 mg-1.17-1.39-2.11-3.04-4.26-3.86-4.16-3.53
Tanezumab 5 mg-1.04-1.49-1.93-3.35-4.44-4.52-4.49-3.84

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Sleep at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. BPI-sf scores for pain interference with sleep: participants were asked to circle from any 1 number from 0 (does not interfere) to 10 (completely interferes) that described how, during the past 24 hours, pain has interfered with their sleep; higher scores indicated higher interference. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.59-0.85-1.29-2.30-3.19-3.41-3.19-2.79
Tanezumab 10 mg-0.77-1.37-1.96-2.75-3.46-3.25-3.65-3.35
Tanezumab 5 mg-1.02-1.28-1.80-2.97-3.62-3.73-3.78-3.26

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Pain Interference With Walking Ability at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified/scheduled time points. BPI-sf scores for pain interference with walking ability: participants were asked to circle from any 1 number from 0 (does not interfere) to 10 (completely interferes) that described how, during the past 24 hours, pain has interfered with their walking ability; higher scores indicated higher interference. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.73-1.12-1.37-2.52-3.44-3.64-3.56-3.16
Tanezumab 10 mg-1.06-1.23-1.91-2.60-3.76-3.36-3.58-3.09
Tanezumab 5 mg-0.89-1.37-1.59-2.89-3.81-3.78-3.76-3.18

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Change From Baseline in Brief Pain Inventory-short Form (BPI-sf) Scores for Worst Pain at Weeks 2, 4, 8, 16, 24, 40, 56, and 64

BPI-sf is a self-administered questionnaire to assess the severity of pain and pain interference on daily functions during 24 hours prior to evaluation at specified time points. BPI-sf scores for worst pain: participants were asked to rate their pain by circling any 1 number from 0 (no pain) to 10 (pain as bad as you can imagine) that best describes their pain at its worst in the last 24 hours; higher scores indicated worse pain. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 40, 56 and 64

,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 40Change at Week 56Change at Week 64
Celecoxib-0.61-0.95-1.28-2.67-4.13-4.39-4.47-3.91
Tanezumab 10 mg-0.81-1.22-1.89-2.92-4.78-4.64-4.70-3.51
Tanezumab 5 mg-0.82-1.25-1.65-3.26-4.27-4.70-4.76-3.71

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Change From Baseline in in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Impairment While Working Due to Chronic Low Back Pain at Weeks 16, 56 and 64

WPAI: LBP is a participant rated questionnaire that measures the effect of participant's chronic low back pain (CLBP) on general health and symptom severity on work productivity and regular activities. Percentage of impairment while working due to CLBP was recorded on a score range of 0 (no impairment) to 100 (extreme impairment), higher scores indicated greater impairment while working and lesser productivity. (NCT02725411)
Timeframe: Baseline, Weeks 16, 56 and 64

,,
Interventionpercentage of impairment (Mean)
BaselineChange at Week 16Change at Week 56Change at Week 64
Celecoxib56.4-28.3-27.1-30.8
Tanezumab 10 mg53.7-24.7-36.6-33.9
Tanezumab 5 mg55.4-31.6-38.7-31.9

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Change From Baseline in Neuropathy Impairment Score (NIS) at Week 2

NIS is a standardized instrument used to evaluate signs of peripheral neuropathy in participants. NIS is the sum of scores of 37 items, from both the left and right side of following 4 domains: cranial nerves (5 items), muscle weakness (19 items), reflexes (5 items) and sensation (8 items). Each of 24 items related to cranial nerves and muscle weakness, scored from 0 (normal) to 4 (paralysis); higher scores indicated higher abnormality/impairment. Each of 13 items related to reflexes and sensation, scored as 0 (normal), 1 (decreased) and 2 (absent); higher scores indicated lesser reflexes and sensation. For NIS possible overall score (combined of both left and right sides of each domain), ranged from 0 (no impairment) to 244 (maximum impairment), higher scores indicated increased/more neuropathic deficits. (NCT02725411)
Timeframe: Baseline, Week 2

,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2
Celecoxib0.870.11
Tanezumab 10 mg1.01-0.01
Tanezumab 5 mg0.84-0.04

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Change From Baseline in Roland-Morris Disability Questionnaire (RMDQ) Total Scores at Weeks 2, 4, 8, 16, 24, 32, 40, 48, and 56: Multiple Imputation

The RMDQ is a self-administered, widely used health status measure index of how well participants with low back pain (LBP) are able to function with regard to daily activities. It measures pain and function, using 24 items describing limitations to everyday life that can be caused by LBP. Participants were asked to check/select only those items out of 24 items, which described them at each specified time point. The total number of items checked in questionnaire was equal to RMDQ total score, overall possible score ranging from 0 (no disability) to 24 (maximum disability), where higher scores indicated greater/more disability. (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 32, 40, 48 and 56

,,
Interventionunits on a scale (Least Squares Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 32Change at Week 40Change at Week 48Change at Week 56
Celecoxib-1.23-1.89-2.68-3.84-3.16-3.02-2.90-3.19-2.94
Tanezumab 10 mg-2.09-2.35-3.23-4.38-3.32-3.11-2.95-2.96-2.91
Tanezumab 5 mg-2.09-2.41-2.74-3.85-3.58-3.62-3.98-3.99-3.95

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Change From Baseline in the Patient's Global Assessment (PGA) of Low Back Pain at Weeks 2, 4, 8, 16, 24, 32, 40, 48, 56 and 64

"PGA of low back pain was assessed by asking a question to participants: Considering all the ways your low back pain affects you, how are you doing today? Participants responded on a 5 point Likert scale ranging from 1 to 5, using interactive response technology (IRT), where 1= very good (asymptomatic and no limitation of normal activities); 2= good (mild symptoms and no limitation of normal activities); 3= fair (moderate symptoms and limitation of some normal activities); 4= poor (severe symptoms and inability to carry out most normal activities); and 5= very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher scores indicated worsening of condition." (NCT02725411)
Timeframe: Baseline, Weeks 2, 4, 8, 16, 24, 32, 40, 48, 56 and 64

,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2Change at Week 4Change at Week 8Change at Week 16Change at Week 24Change at Week 32Change at Week 40Change at Week 48Change at Week 56Change at Week 64
Celecoxib3.13-0.28-0.37-0.44-0.81-0.96-0.91-1.02-1.02-1.07-0.86
Tanezumab 10 mg3.14-0.40-0.46-0.66-0.82-1.22-1.13-1.09-1.11-1.14-0.84
Tanezumab 5 mg3.24-0.43-0.48-0.62-0.92-1.10-1.14-1.29-1.21-1.13-0.94

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Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Activity Impairment Due to Chronic Low Back Pain at Weeks 16, 56 and 64

WPAI: LBP is a participant rated questionnaire that measures the effect of participant's chronic low back pain (CLBP) on general health and symptom severity on work productivity and regular activities. Percentage of daily activity impairment due to CLBP was recorded on a score range of 0 (no impairment) to 100 (extreme impairment), higher scores indicated greater daily activity impairment and lesser productivity. (NCT02725411)
Timeframe: Baseline, Weeks 16, 56 and 64

,,
Interventionpercentage of impairment (Mean)
BaselineChange at Week 16Change at Week 56Change at Week 64
Celecoxib54.7-25.4-32.6-33.0
Tanezumab 10 mg53.7-25.0-35.1-34.4
Tanezumab 5 mg57.8-30.1-42.1-37.3

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Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Overall Work Impairment Due to Chronic Low Back Pain at Weeks 16, 56 and 64

WPAI: LBP is a participant rated questionnaire that measures the effect of participant's chronic low back pain (CLBP) on general health and symptom severity on work productivity and regular activities. Percentage of overall work impairment due to CLBP was recorded on a score range of 0 (no impairment) to 100 (extreme impairment), higher scores indicated greater overall work impairment and lesser productivity. (NCT02725411)
Timeframe: Baseline, Weeks 16, 56 and 64

,,
Interventionpercentage of impairment (Mean)
BaselineChange at Week 16Change at Week 56Change at Week 64
Celecoxib57.2-27.8-27.7-27.9
Tanezumab 10 mg56.0-26.8-38.3-33.7
Tanezumab 5 mg56.0-31.8-39.2-32.1

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Change From Baseline in Work Productivity and Activity Impairment Questionnaire: Low Back Pain (WPAI:LBP)- Percent Work Time Missed Due to Chronic Low Back Pain at Weeks 16, 56 and 64

WPAI:LBP is a participant rated questionnaire that measures the effect of participant's chronic low back pain (CLBP) on general health and symptom severity on work productivity and regular activities. Percentage of work time missed by participants due to CLBP was recorded on a score range of 0 (no impact on work time) to 100 (extreme impact on work time), higher scores indicated greater work time missed and lesser productivity. (NCT02725411)
Timeframe: Baseline, Weeks 16, 56 and 64

,,
Interventionpercentage of work time missed (Mean)
BaselineChange at Week 16Change at Week 56Change at Week 64
Celecoxib5.8-1.9-1.33.1
Tanezumab 10 mg5.7-4.8-2.3-0.6
Tanezumab 5 mg5.0-0.8-2.4-1.6

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Change From Screening in Mean Total Symptom Impact Score as Per Survey of Autonomic Symptoms (SAS) at Week 24

"SAS is a participant rated 12 items questionnaire for males and 11 items questionnaire for females. SAS measures autonomic symptoms of neuropathy and their impact on participants' well-being, during the past 6 months. Each item was related to a symptom/health problem. At scheduled time points, participants were asked to answer Yes or No for each of symptoms/health problems experienced during past 6 months. If a participant answered Yes for a symptom, then impact of that symptom was rated on a 5 point scale, ranged from 1 (least sever impact) to 5 (most severe impact), where higher scores signified more severe impact of symptoms. The total symptom impact score was calculated as the sum of impact of all symptoms. Overall possible range for the total symptom impact score was 0 (no impact) to 60 (extreme impact) for males and 0 (no impact) to 55 (extreme impact) for females, higher scores indicated more severe impact of symptoms on participants' well-being." (NCT02725411)
Timeframe: Screening (up to 37 days before Day 1), Week 24

,,
Interventionunits on a scale (Mean)
ScreeningChange at Week 24
Celecoxib1.100.04
Tanezumab 10 mg0.860.93
Tanezumab 5 mg0.760.79

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European Quality of Life-5 Dimension-5 Levels (EQ-5D-5L): Dimensions Scores at Baseline, Weeks 16 and 56

EQ-5D-5L is a standardized participant completed questionnaire that measures health-related quality of life and translates that score into an index value or utility score. EQ-5D-5L consists of two components: a health state profile and an optional visual analogue scale (VAS). EQ-5D health state profile is comprised of 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension has 5 levels: 1= no problems, 2= slight problems, 3= moderate problems, 4= severe problems, and 5= extreme problems. Higher scores indicated greater levels of problems across each of the five dimensions. (NCT02725411)
Timeframe: Baseline, Weeks 16 and 56

,,
Interventionunits on a scale (Mean)
Baseline: MobilityBaseline: Self-careBaseline: Usual activitiesBaseline: Pain/DiscomfortBaseline: Anxiety/DepressionWeek 16: MobilityWeek 16: Self-careWeek 16: Usual activitiesWeek 16: Pain/DiscomfortWeek 16: Anxiety/DepressionWeek 56: MobilityWeek 56: Self-careWeek 56: Usual activitiesWeek 56: Pain/DiscomfortWeek 56: Anxiety/Depression
Celecoxib2.31.62.32.91.61.51.21.62.11.21.41.01.31.81.1
Tanezumab 10 mg2.21.62.42.91.81.51.11.52.01.21.31.11.31.71.1
Tanezumab 5 mg2.31.82.42.91.81.61.21.62.01.21.31.01.31.71.1

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European Quality of Life-5 Dimension-5 Levels (EQ-5D-5L): Overall Health Utility Score/ Index Value

"EQ-5D health state profile has 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension has 5 levels: 1= no problems, 2= slight problems, 3= moderate problems, 4= severe problems, and 5= extreme problems. Responses from each of the 5 domains were used to calculate overall health state/a single utility index value. Example: if a participant responded no problems for each 5 dimensions, then health state was coded as 11111 with a predefined single index value to it. Every health state (coded as combination of responses on each of 5 dimensions) had a unique predefined utility index value assigned to it, by EuroQol. Japan value sets (with all possible health states) was used in the study, overall health utility score ranged from -0.111 (minimum score) to 1 (maximum score). Higher (positive) scores = better health state." (NCT02725411)
Timeframe: Baseline, Weeks 16 and 56

,,
Interventionunits on a scale (Mean)
BaselineWeek 16Week 56
Celecoxib0.630.760.82
Tanezumab 10 mg0.620.770.83
Tanezumab 5 mg0.610.760.83

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Health Care Resource Utilization (HCRU): Duration Since Quitting Job Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Domain evaluated was duration (in years) at each specified time point since quitting job due to low back pain. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

,
Interventionyears (Median)
BaselineWeek 64
Celecoxib2.50.2
Tanezumab 10 mg1.60.7

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Health Care Resource Utilization (HCRU): Duration Since Quitting Job Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Domain evaluated was duration (in years) at each specified time point since quitting job due to low back pain. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

Interventionyears (Median)
BaselineWeek 64Week 80
Tanezumab 5 mg1.53.30.1

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Health Care Resource Utilization (HCRU): Number of Nights Stayed in the Hospital Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Number of nights stayed in the hospital due to low back pain were evaluated. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

Interventionnights (Median)
Week 64
Tanezumab 5 mg1.0

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Health Care Resource Utilization (HCRU): Number of Nights Stayed in the Hospital Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Number of nights stayed in the hospital due to low back pain were evaluated. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

,
Interventionnights (Median)
BaselineWeek 64
Celecoxib2.02.0
Tanezumab 10 mg24.01.0

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Health Care Resource Utilization (HCRU): Number of Participants Hospitalized Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months for baseline, weeks 64 and 80, via IRT. Domain evaluated was number of participants who were hospitalized due to low back pain. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

,,
InterventionParticipants (Count of Participants)
BaselineWeek 64Week 80
Celecoxib110
Tanezumab 10 mg110
Tanezumab 5 mg010

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Health Care Resource Utilization (HCRU): Number of Participants Visited to the Emergency Room Due to Low Back Pain

Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Number of participants who visited the emergency room due to low back pain were evaluated. (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

,,
InterventionParticipants (Count of Participants)
BaselineWeek 64Week 80
Celecoxib020
Tanezumab 10 mg000
Tanezumab 5 mg000

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Health Care Resource Utilization (HCRU): Number of Participants Who Quit Job Due to Low Back Pain

"Low back pain HCRU assessed utilization of healthcare resources during the last 3 months (last 3 months before Baseline [Day 1] visit, weeks 64 and 80 visit, via IRT). Number of participants who answered as Yes for quitting job due to low back pain, were evaluated." (NCT02725411)
Timeframe: Baseline, Weeks 64 and 80

,,
InterventionParticipants (Count of Participants)
BaselineWeek 64Week 80
Celecoxib510
Tanezumab 10 mg220
Tanezumab 5 mg311

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Knee Society Functional Score

"The Knee Society Functional score was developed by the Knee Society as a method of evaluating how well a patient can use their joint. Knee function was evaluated in two categories: walking, and stair usage. Points range from 0-100. 0 = extreme problems, 100 = no problems.~In each category, points range from 0-50, where 0 = extreme problems to 50 = no problems. Total scores are 0-100 with lower scores indicating extreme knee function problems and higher scores indicating no knee function problems." (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
Interventionscore on a 0-100 scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone64.777.3
MUA With Dexamethasone and Celecoxib64.274.2

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Knee Injury and Osteoarthritis Outcome Score (KOOS): Pain Score

The KOOS is a commonly used questionnaire which focuses on how patients are affected by osteoarthritis symptoms in five areas: knee pain, stiffness, daily activity, sport and recreation, and quality of life. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
InterventionScore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone68.984.1
MUA With Dexamethasone and Celecoxib62.779.8

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Knee Injury and Osteoarthritis Outcome Score (KOOS): Activities of Daily Living (ADL) Score

The KOOS is a commonly used questionnaire which focuses on how patients are affected by osteoarthritis symptoms in five areas: knee pain, stiffness, daily activity, sport and recreation, and quality of life. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after MUA, 1 year after MUA

,
Interventionscore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone74.181.0
MUA With Dexamethasone and Celecoxib70.376.6

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Knee Injury and Osteoarthritis Outcome Score (KOOS) for Joint Replacement (JR)

KOOS JR is a questionnaire designed to measure outcomes for patients with knee replacements. Questions focus on knee stiffness, pain, and function for daily activities. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
Interventionscore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone64.972.5
MUA With Dexamethasone and Celecoxib62.769.0

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Short Form Survey 12-item Version 2 (SF-12v2): Physical Health

The SF-12v2 questionnaire uses questions selected from the longer SF-36 Health Survey to measure patient wellness and quality of life. Responses were scored using the SF12v2 New England Medical Center (NEMC) scoring algorithm which converts the raw score from the questionnaire into a t-score. The algorithm is calibrated so that an average healthy person would have a t-score of 50 points with a standard deviation of 10. Higher scores indicate better physical health. (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone38.744.8
MUA With Dexamethasone and Celecoxib37.043.3

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Short Form Survey 12-item Version 2 (SF-12v2): Mental Health

The SF-12v2 questionnaire uses questions selected from the longer SF-36 Health Survey to measure patient wellness and quality of life. Responses were scored using the SF12v2 New England Medical Center (NEMC) scoring algorithm which converts the raw score from the questionnaire into a t-score. The algorithm is calibrated so that an average healthy person would have a t-score of 50 points with a standard deviation of 10. Higher scores indicate better mental health. (NCT02739035)
Timeframe: 6 weeks after MUA, 1 Year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone51.754.4
MUA With Dexamethasone and Celecoxib53.754.3

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PROMIS-29 Outcome Form: Social Activities

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For social activities, higher scores indicate a better ability to participate in social roles and activities.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, and 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone49.262.3
MUA With Dexamethasone and Celecoxib51.556.1

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PROMIS-29 Outcome Form: Sleep Disturbance

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For sleep disturbance, lower scores indicate less sleep disturbance.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, and 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone54.748.3
MUA With Dexamethasone and Celecoxib57.448.0

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PROMIS-29 Outcome Form: Physical Function

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For physical function, higher scores indicate better function.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone41.052.2
MUA With Dexamethasone and Celecoxib42.545.2

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Knee Range of Motion After Manipulation Under Anesthesia

Knee range of motion after manipulation will be measured in degrees as the total arc of motion from maximum passive flexion to maximum passive extension. (NCT02739035)
Timeframe: 1 year from the date of the manipulation

InterventionDegrees (Mean)
MUA Alone107.7
MUA With Dexamethasone and Celecoxib107.6

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Knee Injury and Osteoarthritis Outcome Score (KOOS): Sport and Recreation Score

The KOOS is a commonly used questionnaire which focuses on how patients are affected by osteoarthritis symptoms in five areas: knee pain, stiffness, daily activity, sport and recreation, and quality of life. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after MUA, 1 year after MUA

,
Interventionscore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone48.561.0
MUA With Dexamethasone and Celecoxib52.862.2

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PROMIS-29 Outcome Form: Pain Interference

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For pain interference, higher scores indicate more frequent interference in activities due to pain.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone56.147.4
MUA With Dexamethasone and Celecoxib58.256.7

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PROMIS-29 Outcome Form: Fatigue

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For fatigue, lower scores indicate less fatigue.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, and 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone46.639.3
MUA With Dexamethasone and Celecoxib48.241.5

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PROMIS-29 Outcome Form: Anxiety

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For anxiety, lower scores indicate less anxiety.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, and 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone48.343.6
MUA With Dexamethasone and Celecoxib48.945.5

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PROMIS-29 Outcome Form: Depression

"The PROMIS-29 outcome form measures physical and mental health outcomes for patients. Patients responded to 29 questions in seven categories: physical function, pain interference, depressive symptoms, anxiety, ability to participate in social activities, and sleep disturbance. Scores were scaled so that an average healthy person would score 50 points. A higher score represents more of what is being measured. For depression, lower scores indicate fewer depressive symptoms.~Patient questionnaire responses are scored using the PROMIS-29 scoring algorithm. Scores are scaled to a mean of 50 for a healthy reference population with a standard deviation of 10." (NCT02739035)
Timeframe: 6 weeks after MUA, and 1 year after MUA

,
Interventiont-score (Mean)
6 weeks after MUA1 year after MUA
MUA Alone46.641.0
MUA With Dexamethasone and Celecoxib48.746.8

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Knee Society Knee Score

"The Knee Society Knee Score is method of joint evaluation developed by the Knee Society to measure the condition of a patient's knee. Knee condition was evaluated in three categories: pain, range of motion, and stability. Points range from 0-100. 0 = extreme problems, 100 = no problems.~Up to 50 points for pain, 25 points for range of motion, and 25 points for stability. Deductions occur for Extension lag, flexion contracture, malalignment, and pain at rest." (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
InterventionScore on a 0-100 scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone65.174.2
MUA With Dexamethasone and Celecoxib66.868.6

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Knee Range of Motion After Manipulation Under Anesthesia

Knee range of motion after manipulation will be measured in degrees as the total arc of motion from maximum passive flexion to maximum passive extension. (NCT02739035)
Timeframe: 6 weeks after manipulation

InterventionDegrees (Mean)
MUA Alone98.7
MUA With Dexamethasone and Celecoxib101.2

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Knee Injury and Osteoarthritis Outcomes Score (KOOS): Quality of Life

The KOOS is a commonly used questionnaire which focuses on how patients are affected by osteoarthritis symptoms in five areas: knee pain, stiffness, daily activity, sport and recreation, and quality of life. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after MUA, 1 year after MUA

,
Interventionscore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone49.283.0
MUA With Dexamethasone and Celecoxib50.067.1

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Knee Injury and Osteoarthritis Outcome Score (KOOS): Symptom Score

The KOOS is a commonly used questionnaire which focuses on how patients are affected by osteoarthritis symptoms in five areas: knee pain, stiffness, daily activity, sport and recreation, and quality of life. Results are scored 0-100. 0 = extreme problems, 100 = no problems. (NCT02739035)
Timeframe: 6 weeks after the MUA, and 1 year after the MUA

,
InterventionScore on a scale (Mean)
6 weeks after MUA1 year after MUA
MUA Alone64.282.5
MUA With Dexamethasone and Celecoxib58.075.7

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Visual Analog Score for Pain (VAS) in the Immediate Post Operative Period

The pain VAS is a uni dimensional measure of pain intensity. It is a continuous scale comprised of a 0-10 pain rating. A score of 0 indicates no pain while a score of 10 would indicate extreme pain. (NCT02779166)
Timeframe: Pre operative on day of surgery, immediately following OR close, 1 hr post operatively, 2 hrs post operatively

,
Interventionscore on a scale (Mean)
Pre-Operative VAS ScoreImmediate Post Op VAS Score1 hr Post Op VAS Score2 hr Post Op VAS Score
Intervention2.114.414.634.11
Placebo2.335.025.364.92

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Time to Discharge Following Surgery

Total time to discharge from OR close following surgery, measured in minutes (NCT02779166)
Timeframe: time from OR to discharge, up to a maximum of 6 hours postoperatively

Interventionminutes (Mean)
Intervention152.9
Placebo172.9

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Total Narcotic Consumption in the Post Anesthesia Care Unit (PACU)

Monitored consumption of narcotic medications following surgery, measured in morphine equivalents (NCT02779166)
Timeframe: duration of PACU stay,immediate post op period up to a maximum of 4 hours postoperatively

Interventionmorphine milligram equivalents (Mean)
Intervention15.326
Placebo15.419

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Eyelid Retraction as Measured in Millimeters (Right Eye)

A clinical measure of the most common manifestation of thyroid eye disease--change in eyelid retraction as measured in millimeters at each visit over the duration of the study. (NCT02845336)
Timeframe: At baseline, 1, 3 and 6 months

Interventionmillimeters (Number)
Baseline1 month3 months6 months
Celecoxib0.50.50.50.5

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Number of Participants With Ocular Misalignment

Presence or absence of ocular misalignment measured in prism diopters. (NCT02845336)
Timeframe: At 1 month

InterventionParticipants (Count of Participants)
PresentAbsent
Celecoxib01

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Number of Participants With Ocular Misalignment

Presence or absence of ocular misalignment measured in prism diopters. (NCT02845336)
Timeframe: At 3 months

InterventionParticipants (Count of Participants)
PresentAbsent
Celecoxib01

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Number of Participants With Ocular Misalignment

Presence or absence of ocular misalignment measured in prism diopters. (NCT02845336)
Timeframe: At 6 months

InterventionParticipants (Count of Participants)
PresentAbsent
Celecoxib01

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Number of Participants With Ocular Misalignment

Presence or absence of ocular misalignment measured in prism diopters. (NCT02845336)
Timeframe: At baseline

InterventionParticipants (Count of Participants)
PresentAbsent
Celecoxib01

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Eyelid Retraction as Measured in Millimeters (Left Eye)

A clinical measure of the most common manifestation of thyroid eye disease--change in eyelid retraction as measured in millimeters at each visit over the duration of the study. (NCT02845336)
Timeframe: At baseline, 1, 3 and 6 months

Interventionmillimeters (Number)
Baseline1 month3 months6 months
Celecoxib2222

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Proptosis as Measured in Millimeters With an Exophthalmometer (Left Eye)

A clinical measure of how prominent the eyes are and any change in this measure over the duration of the study, as measured in millimeters with an exophthalmometer. (NCT02845336)
Timeframe: At baseline, 1, 3 and 6 months

Interventionmillimeters (Number)
Baseline1 month3 months6 months
Celecoxib21.521.521.521.5

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Proptosis as Measured in Millimeters With an Exophthalmometer (Right Eye)

A clinical measure of how prominent the eyes are and any change in this measure over the duration of the study, as measured in millimeters with an exophthalmometer. (NCT02845336)
Timeframe: At baseline, 1, 3 and 6 months

Interventionmillimeters (Number)
Baseline1 month3 months6 months
Celecoxib20.520.520.520.5

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Thyroid Eye Disease Clinical Activity Score

A clinical score based on examination findings at each clinic visit. Clinical Activity Scores ranged from 0 to 10; 0 = Normal 1-3 = Mild 4-6 = Moderate 7-10 = Severe (NCT02845336)
Timeframe: At baseline, 1, 3 and 6 months

InterventionParticipants (Count of Participants)
Baseline724993991 month724993993 months724993996 months72499399
NormalModerateSevereMild
Celecoxib1
Celecoxib0

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Difference in Amount of Rescue Pain Medication Consumed

The total amount of rescue pain medication consumed in the 2-week postop period will be compared between the two treatment groups. (NCT02934191)
Timeframe: 2 weeks post-operative

Interventionmg/kg (Mean)
Acetaminophen/Oxycodone + Celecoxib1.03
Acetaminophen/Oxycodone + Placebo1.40

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Difference in Number of Days Requiring Rescue Pain Medication

The number of days on narcotic pain medication following surgery will be compared between the two treatment groups (NCT02934191)
Timeframe: 2 weeks post-operative

InterventionDays (Mean)
Acetaminophen/Oxycodone + Celecoxib5.00
Acetaminophen/Oxycodone + Placebo5.75

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Log-transformed Plasma Concentration of Amlodipine

A venous blood sample was collected 24 hours ± 1 hour after the last dose of study drugs (i.e., on Day 14). The blood sample was processed to plasma and the concentration of amlodipine measured using a validated LC-MS/MS method. The concentrations were logarithmically transformed and used for the comparison between the amlodipine+celecoxib and amlodipine+placebo arms to evaluate the effect of celecoxib on the mean log-transformed plasma concentrations of amlodipine. (NCT02979197)
Timeframe: 24 hours post-dose on Day 14

Interventionng/mL (Mean)
Amlodipine+Celecoxib2.7
Amlodipine+Placebo2.8

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Non-transformed Plasma Concentration of Amlodipine

A venous blood sample was collected 24 hours ± 1 hour after the last dose of study drugs (i.e., on Day 14). The blood sample was processed to plasma and the concentration of amlodipine measured using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The resulting concentrations, without logarithmic transformation, were used for the comparison between the amlodipine+celecoxib and amlodipine+placebo arms to evaluate the effect of celecoxib on the mean non-transformed plasma concentrations of amlodipine. (NCT02979197)
Timeframe: 24 hours post-dose on Day 14

Interventionng/mL (Mean)
Amlodipine+Celecoxib15.9
Amlodipine+Placebo18.3

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Occurrence of Treatment Emergent Adverse Events

Treatment emergent adverse events (TEAEs) included any untoward medical occurrence that initiated or worsened after the first dose of study drugs and within 14 days of the last dose of study drugs. (NCT02979197)
Timeframe: 1 month

InterventionParticipants (Count of Participants)
Amlodipine+Celecoxib35
Amlodipine+Placebo32
Placebo+Placebo6

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Change in Average 24-hour Ambulatory Diastolic Blood Pressure (DBP24h)

An ABPM fitted to upper arm was used for continuous recording of blood pressure over three 25-hour periods: Days -1 to 0 (Baseline), Days 6 to 7, & Days 13 to 14. The ABPM recorded blood pressure every 20 minutes between 09:00 and 21:59 and every 30 minutes between 22:00 and 08:59. DBP24h was calculated by averaging all of the diastolic blood pressure measurements between the protocol-defined first & last study measurements of the period; measurements during the first hour (white-coat window) were not included. Change in DBP24h was calculated by subtracting the Baseline value from the end of study value (Day 13 to Day 14 period). If the Day 13 to Day 14 value was not available, the Day 6 to Day 7 value was used (LOCF method). A negative value for change in DBP24h indicates a decrease in diastolic blood pressure and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 days

InterventionmmHg (Mean)
Amlodipine+Celecoxib-4.4
Amlodipine+Placebo-3.8

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Change in Average 24-hour Ambulatory Systolic Blood Pressure (SBP24h)

An ABPM fitted to upper arm was used for continuous recording of blood pressure over three 25-hour periods: Days -1 to 0 (Baseline), Days 6 to 7, & Days 13 to 14. The ABPM recorded blood pressure every 20 minutes between 09:00 and 21:59 and every 30 minutes between 22:00 and 08:59. SBP24h was calculated by averaging all of the systolic blood pressure measurements between the protocol-defined first & last study measurements of the period; measurements during the first hour (white-coat window) were not included. Change in SBP24h was calculated by subtracting the Baseline value from the end of study value (Day 13 to Day 14 period). If the Day 13 to Day 14 value was not available, the Day 6 to Day 7 value was used (LOCF method). A negative value for change in SBP24h indicates a decrease in systolic blood pressure and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 days

InterventionmmHg (Mean)
Amlodipine+Celecoxib-8.2
Amlodipine+Placebo-8.5

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Change in Average Daytime (9:00 to 21:00) Ambulatory Systolic Blood Pressure (SBPday)

An ambulatory blood pressure monitor (ABPM) fitted to upper arm was used for continuous recording of blood pressure over three 25-hour periods: Days -1 to 0 (Baseline), Days 6 to 7, & Days 13 to 14. The ABPM recorded blood pressure every 20 minutes between 09:00 and 21:59 and every 30 minutes between 22:00 and 08:59. SBPday was calculated by averaging all of the systolic blood pressure measurements between the protocol-defined first & last study measurements of the period that fell between 9:00 and 21:00; measurements during the first hour (white-coat window) were not included. Change in SBPday was calculated by subtracting the Baseline value from the end of study value (Day 13 to Day 14 period). If the Day 13 to Day 14 value was not available, the Day 6 to Day 7 value was used [last observation carried forward (LOCF) method]. A negative value for change in SBPday indicates a decrease in systolic blood pressure and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 days

InterventionmmHg (Mean)
Amlodipine+Celecoxib-8.0
Amlodipine+Placebo-9.8

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Change in Body Weight

Body weight was measured at the Initial Screening Visit (Day -10 to -14), at Baseline (Day 0), and at Days 7 and 14. The measurements were made using a calibrated scale with the subject wearing underwear and a light gown. Change in body weight was calculated by subtracting the Baseline value from the end of treatment value (recorded on Day 14). If the Day 14 value was not available, the Day 7 value was used (LOCF method). A negative value for change in body weight indicates a decrease in body weight and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 days

Interventionkg (Mean)
Amlodipine+Celecoxib0.3
Amlodipine+Placebo-0.3
Placebo+Placebo-1.5

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Change in Creatinine Clearance

Subjects had blood collected for the measurement of creatinine at the Initial Screening Visit (Day -10 to -14), at Baseline (Day 0), and at Days 7 and 14. Estimated creatinine clearance was calculated using Cockcroft-Gault equation: (140 - age) X body weight (kg)/72 X serum creatinine concentration (mg/dL); multiplied by 0.85 for women. Change in creatinine clearance was calculated by subtracting the Baseline value from the end of treatment value (recorded on Day 14). If the Day 14 value was not available, the Day 7 value was used (LOCF method). A negative value for change in creatinine clearance indicates a decrease in creatinine clearance and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 days

InterventionmL/min (Mean)
Amlodipine+Celecoxib4.9
Amlodipine+Placebo3.4

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Change in Serum Creatinine

Subjects had blood collected for the measurement of creatinine at the Initial Screening Visit (Day -10 to -14), at Baseline (Day 0), and at Days 7 and 14. Change in serum creatinine was calculated by subtracting the Baseline value from the end of treatment value (recorded on Day 14). A negative value for change in serum creatinine indicates a decrease in creatinine and a positive value indicates an increase. (NCT02979197)
Timeframe: Baseline and 14 Days

Interventionμmol/L (Mean)
Amlodipine+Celecoxib-2.8
Amlodipine+Placebo-2.4
Placebo+Placebo-1.9

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Subject-Rated Treatment Satisfaction at 24 Hours Postdose - PPMQ-R (DB1 and DB2)

Patient Perception of Migraine Questionnaire-Revised had 30 questions assessing subject's satisfaction with migraine medication, including 3 global items & 4 subscales (i.e., efficacy, function, ease of use, tolerability). A 5-point scale (1-Not At All to 5-Extremely) was used for tolerability subscale questions; a 7-point scale (1-Very Satisfied to 7-Very Dissatisfied) was used for all other subscales and global items. Total score was average of efficacy/function/ease of use subscale scores. Each subscale & total scores were transformed to range from 0-100, with higher scores indicating better satisfaction or tolerability. Total raw score/global items were not transformed. The total raw score could range from 17 (min) to 119 (max), with lower scores indicating better satisfaction. Change from baseline scores at 24-hour-postdose for each subscale score, global item score, total score, & total raw score were summarized by treatment group below. (NCT03006276)
Timeframe: 24 hours postdose

,,,
Interventionunits on a scale (Mean)
Total ScoreTotal Raw ScoreEfficacyFunctionEase of UseTolerabilityMedication Effectiveness (Global Item)Side Effects (Global Item)Overall Satisfaction (Global Item)
DFN-15 DB14.367-1.2542.2927.9312.8768.450.22.60.1
DFN-15 DB23.940-1.4483.6048.1690.0476.720.2-0.30.0
Placebo DB1-0.6570.835-4.196-0.0202.2475.990.7-0.30.5
Placebo DB23.544-0.7440.3856.2394.0099.010.2-0.70.1

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Headache Pain Freedom Among BMI Category (DB1 and DB2)

The percentage of subjects who were pain-free at 2 and 4 hours postdose whose BMI was <30 kg/m2 vs. subjects whose BMI was ≥30 kg/m2 during each DB treatment period were summarized by treatment group and time point. (NCT03006276)
Timeframe: 2 to 4 hours postdose

,,,
Interventionpercentage of subjects (Number)
2 hours postdose (BMI<30)4 hours postdose (BMI <30)2 hours postdose (BMI>=30)4 hours postdose (BMI>=30)
DFN-15 DB131.555.940.356.9
DFN-15 DB241.967.850.456.2
Placebo DB122.141.721.147.8
Placebo DB226.850.037.350.0

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Absence of Screening MBS at Time Points Postdose (DB1 and DB2)

The percentage of subjects with their Screening MBS (most bothersome symptoms) among nausea, photophobia, and phonophobia (from eDiary data collection) absent at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2 period), 4, and 24 hours postdose during each DB treatment period were summarized by treatment group and time point. (NCT03006276)
Timeframe: 15 minutes to 24 hours postdose

,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB16.317.328.539.649.157.867.482.5
DFN-15 DB28.922.936.844.753.463.478.089.6
Placebo DB110.617.422.525.038.744.861.386.0
Placebo DB28.015.827.535.842.650.060.783.7

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Headache Pain Freedom Postdose (DB1 and DB2)

The percentage of subjects who were pain-free at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2), and 4, and 24 hours postdose during each DB treatment period were summarized by treatment group. (NCT03006276)
Timeframe: 15 minutes to 24 hours postdose

,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB20.96.812.723.236.146.261.982.9
Placebo DB21.46.411.715.825.231.150.075.1

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Headache Pain Relief Postdose (DB1 and DB2)

Headache pain relief during postdose in DB1 was defined as a reduction from moderate or severe pain at predose reduced to mild or none postdose, and for DB2 as moderate or severe pain at predose reduced to mild or none postdose, or mild pain at predose reduced to none postdose. Outcome measure shows percentage of subjects experiencing headache pain relief by time point. (NCT03006276)
Timeframe: 15 minutes to 24 hours postdose

,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB113.432.246.556.870.074.579.692.4
DFN-15 DB211.731.647.756.166.474.482.293.8
Placebo DB116.628.940.245.155.260.575.292.5
Placebo DB210.927.537.143.853.360.775.089.0

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Use of Rescue Medication Postdose (DB1 and DB2)

The percentage of subjects who used rescue mediation after 2 hours (2 to 24 hours) postdose compared between DFN-15 and placebo in each DB period. (NCT03006276)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB130.1
DFN-15 DB115.8
Placebo DB218.4
DFN-15 DB216.7

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Subject-Rated Treatment Satisfaction Postdose (DB1 and DB2)

"Subject-rated treatment overall satisfaction was based on a 7-point scale at 2 and 4 hours postdose during each DB treatment period. The difference between the subject-rated study drug treatment satisfaction score at 2 and 4 hours postdose and the baseline PPMQ-R (Patient Perception of Migraine Questionnaire) response for the same question were summarized by treatment group (global satisfaction item at baseline asked about the subject's usual migraine treatment). The possible values of the subject treatment satisfaction scale were: 1=very satisfied, 2=satisfied, 3=somewhat satisfied, 4=neither satisfied nor dissatisfied, 5=somewhat dissatisfied, 6=dissatisfied, 7=very dissatisfied.~A decrease in values indicates improvement from baseline." (NCT03006276)
Timeframe: 2 to 4 hours postdose

,,,
Interventionunits on a scale (Mean)
2 hours postdose4 hours postdose
DFN-15 DB13.33.2
DFN-15 DB23.12.9
Placebo DB13.93.7
Placebo DB23.63.5

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Freedom From Nausea, Photophobia, and Phonophobia Postdose (DB1 and DB2)

The percentage of subjects who were free from nausea, photophobia, and phonophobia at 15, 30, and 45 minutes and 1, 1.5, 2, 4, and 24 hours postdose during each DB treatment period were summarized by symptom, treatment group, and time point. (NCT03006276)
Timeframe: 15 minutes through 24 hours

,,,,,,,,,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DB1 DFN-15 (Nausea)15.732.945.356.863.567.675.090.6
DB1 DFN-15 (Phonophobia)10.524.635.845.050.861.171.585.1
DB1 DFN-15 (Photophobia)9.620.130.638.947.458.369.985.7
DB1 Placebo (Nausea)16.833.643.849.358.562.275.591.4
DB1 Placebo (Phonophobia)15.726.026.738.347.254.572.989.7
DB1 Placebo (Photophobia)8.813.020.226.536.044.461.285.2
DB2 DFN-15 (Nausea)13.731.444.351.967.369.285.093.5
DB2 DFN-15 (Phonophobia)10.327.438.644.056.367.776.290.5
DB2 DFN-15 (Photophobia)8.021.936.243.752.564.078.191.6
DB2 Placebo (Nausea)14.526.941.852.560.266.974.287.1
DB2 Placebo (Phonophobia)8.515.625.834.243.248.759.081.5
DB2 Placebo (Photophobia)7.514.422.127.935.445.962.884.6

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Change in Functional Disability Score Postdose (DB1 and DB2)

"The values of the functional disability scale were: 0=no disability, able to function normally; 1=performance of daily activities mildly impaired, can still do everything but with difficulty; 2=performance of daily activities moderately impaired, unable to do some things; 3=performance of daily activities severely impaired, cannot do all or most things, bed rest may be necessary.~A decrease in values indicates improvement from baseline." (NCT03006276)
Timeframe: 2 to 24 hours postdose

,,,
Interventionunits on a scale (Mean)
2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB1-0.9-1.3-1.7
DFN-15 DB2-0.9-1.2-1.5
Placebo DB1-0.7-1.1-1.8
Placebo DB2-0.6-1.0-1.5

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Headache Pain Freedom Postdose (DB1 and DB2)

The percentage of subjects who were pain-free at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2), and 4, and 24 hours postdose during each DB treatment period were summarized by treatment group. (NCT03006276)
Timeframe: 15 minutes to 24 hours postdose

,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose4 hours postdose24 hours postdose
DFN-15 DB10.43.011.117.927.156.477.3
Placebo DB11.33.68.612.817.444.477.2

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Time to Headache Pain Freedom Postdose (DB1 and DB2)

(NCT03006276)
Timeframe: 2 hours postdose

Interventionminutes (Mean)
Placebo DB166.6
DFN-15 DB168.5
Placebo DB268.8
DFN-15 DB280.8

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Headache Pain Freedom Among Subjects With Cutaneous Allodynia (DB1 and DB2)

The percentage of subjects who were pain-free at 2 and 4 hours postdose during each DB treatment period among those subjects reporting cutaneous allodynia before dosing were summarized by treatment group and time point. (NCT03006276)
Timeframe: 2 to 4 hours postdose

,,,
Interventionpercentage of subjects (Number)
2 hours postdose4 hours postdose
DFN-15 DB138.056.0
DFN-15 DB254.356.5
Placebo DB119.245.3
Placebo DB231.040.5

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Sustained Headache Pain Relief Postdose (DB1 and DB2)

Sustained headache pain relief was defined as pain relief at 2 hours postdose with no use of rescue medication and no worsening of headache pain within 2 to 24 hours postdose. This outcome measure shows the percentage of subjects who reported pain relief at 2 hours postdose with no use of rescue medication or worsening of headache pain through 24 hours postdose. (NCT03006276)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB143.4
DFN-15 DB155.1
Placebo DB249.7
DFN-15 DB260.2

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Sustained Headache Pain Freedom Postdose (DB1 and DB2)

Sustained headache pain freedom was defined as pain-free at 2 hours postdose, with no use of rescue medication and no recurrence of headache pain within 2 to 24 hours postdose. This outcome measure shows percentage of subjects who were pain-free at 2 hours postdose without the use of rescue medication or recurrence of headache pain through 24 hours postdose. (NCT03006276)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB117.0
DFN-15 DB126.8
Placebo DB226.5
DFN-15 DB239.8

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Percentage of Subjects Who Are Pain-free at 2 Hours Postdose (DB1)

Percentage of subjects who were pain-free 2 hours postdose compared between DFN-15 and placebo in the DB1 period (defined as a reduction from predose moderate [Grade 2] or severe [Grade 3] pain to none [Grade 0]) during DB1. (NCT03006276)
Timeframe: 2 hours post dose

Interventionpercentage of subjects (Number)
Placebo LOCF21.7
DFN-15 LOCF35.6
Placebo OC22.1
DFN-15 OC35.8

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Percentage of Subjects Who Are Free From Their MBS at 2 Hours Postdose (DB1)

Percentage of subjects who are free from their most bothersome symptom (MBS) among nausea, photophobia, and phonophobia at 2 hours postdose during DB1. (NCT03006276)
Timeframe: 2 hours post dose

Interventionpercentage of subjects (Number)
Placebo LOCF44.8
DFN-15 LOCF57.8
Placebo OC45.4
DFN-15 OC58.3

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Headache Pain Recurrence Postdose (DB1 and DB2)

Headache pain recurrence was defined as pain-free at 2 hours postdose with pain reported as mild, moderate, or severe at 24 hours postdose. This outcome measure shows percentage of subjects who reported pain-free status and 2 hours postdose but subsequently reported recurrent pain at 24 hours postdose. (NCT03006276)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB114.0
DFN-15 DB19.2
Placebo DB26.6
DFN-15 DB26.4

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Time to Headache Pain Relief Postdose (DB1 and DB2)

(NCT03006276)
Timeframe: 2 hours postdose

Interventionminutes (Mean)
Placebo DB159.5
DFN-15 DB168.9
Placebo DB255.3
DFN-15 DB262.1

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Percentage of Subjects Who Are Pain-free at 2 Hours Postdose (First Treated Double-blind Treatment Period)

The primary efficacy end point (for first treated DB1 attack only) were the percentage of subjects who were pain-free 2 hours postdose compared between DFN-15 and placebo (defined as a reduction from predose moderate [Grade 2] or severe [Grade 3] pain to none [Grade 0] (NCT03009019)
Timeframe: 2 hours postdose

Interventionpercentage of subjects (Number)
DFN-15 Placebo (LOCF)25.8
DFN-15 Active (LOCF)32.9
DFN-15 Placebo (OC)24.6
DFN-15 Active (OC)32.4

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Sustained Headache Pain Freedom Postdose (DB1 and DB2)

The percentage of subjects who had sustained pain freedom at 2 to 24 hours postdose compared between DFN-15 and placebo in each DB period. Sustained pain freedom at 2 to 24 hours postdose is defined as pain-free at 2 hours postdose, with no use of rescue medication, and no recurrence of headache pain within 2 to 24 hours postdose (NCT03009019)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB118.9
DFN-15 DB127.6
Placebo DB220.0
DFN-15 DB229.1

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Sustained Headache Pain Relief Postdose (DB1 and DB2)

The percentage of the population of subjects who reported headache pain relief between 2 and 24 hours postdose. (NCT03009019)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB139.8
DFN-15 DB155.1
Placebo DB244.3
DFN-15 DB256.6

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Time to Headache Pain Freedom Postdose (DB1 and DB2)

The time to headache pain freedom was defined as the time in minutes from when a subject took study drug until the time pain freedom was indicated by the subject in the eDiary within 2 hours postdose. (NCT03009019)
Timeframe: 2 hours postdose

Interventiontime (minutes) (Median)
Placebo DB1NA
DFN-15 DB1NA
Placebo DB2NA
DFN-15 DB2NA

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Time to Headache Pain Relief Postdose (DB1 and DB2)

The time to headache pain relief was defined as the time in minutes from when a subject took study drug until the time pain relief was indicated by the subject in the eDiary within 2 hours postdose. (NCT03009019)
Timeframe: 2 hours postdose

Interventiontime (hours) (Mean)
Placebo DB1NA
DFN-15 DB1NA
Placebo DB2NA
DFN-15 DB2NA

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Use of Rescue Medication Postdose (DB1 and DB2)

The percentage of subjects who used rescue medication after 2 hours (2 to 24 hours) postdose compared between DFN-15 and placebo in each DB period (NCT03009019)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB128.5
DFN-15 DB118.8
Placebo DB222.9
DFN-15 DB218.4

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The Number of Subjects With TEAEs After Study Drug Compared Between DFN-15 and Placebo

"For DB1: TEAE that started or worsening of a pre-existing condition on or after the first dose of study drug (DFN-15 or placebo) in to taking DB2 study drug, whichever occurs first.~For DB2: TEAE that started or worsened on or after the first dose of study drug in DB2 up to 5 days after the date of the last dose of study drug in DB2." (NCT03009019)
Timeframe: Per protocol, the maximum dosing timeframe for DB2 was 10 weeks; therefore, the maximum AE collection window was 11 weeks total.

InterventionParticipants (Count of Participants)
Placebo DB128
DFN-15 DB131
Placebo DB226
DFN-15 DB221

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Headache Pain Freedom Postdose (DB1 and DB2)

The percentage of subjects who were pain-free at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2 period), 4, and 24 hours postdose compared between DFN-15 and placebo (NCT03009019)
Timeframe: 15 minutes to 24 hours postdose

,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB22.88.611.918.727.136.759.185.3
Placebo DB20.51.77.311.920.724.346.774.7

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Headache Pain Recurrence Postdose (DB1 and DB2)

The percentage of subjects who had pain recurrence between 2 to 24 hours (i.e., pain-free at 2 hours postdose, with pain [mild, moderate, or severe] reported at 24 hours postdose) compared between DFN-15 and placebo (NCT03009019)
Timeframe: 2 to 24 hours postdose

Interventionpercentage of subjects (Number)
Placebo DB110.1
DFN-15 DB17.6
Placebo DB26.9
DFN-15 DB24.5

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Subject-Rated Treatment Satisfaction Postdose (DB1 and DB2)

"Subject-rated treatment overall satisfaction was based on a 7-point scale at 2 and 4 hours postdose during each DB treatment period. The difference between the subject-rated study drug treatment satisfaction score at 2 and 4 hours postdose and the baseline PPMQ-R (Patient Perception of Migraine Questionnaire) response for the same question were summarized by treatment group (global satisfaction item at baseline asked about the subject's usual migraine treatment). The possible values of the subject treatment satisfaction scale were: 1=very satisfied, 2=satisfied, 3=somewhat satisfied, 4=neither satisfied nor dissatisfied, 5=somewhat dissatisfied, 6=dissatisfied, 7=very dissatisfied.~A decrease in values indicates improvement from baseline." (NCT03009019)
Timeframe: 2 and 4 hours postdose

,,,
Interventionunits on a scale (Mean)
Difference at 2 hoursDifference at 4 hours
DFN-15 DB1-0.1-0.1
DFN-15 DB2-0.1-0.1
Placebo DB10.70.7
Placebo DB20.30.4

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Percentage of Subjects Who Are Free From Their MBS at 2 Hours Postdose

Percentage of subjects who are free from their Most Bothersome Symptom (MBS) among nausea, photophobia, and phonophobia (first double-blind treatment period) (NCT03009019)
Timeframe: 2 hours postdose

Interventionpercentage of subjects (Number)
DFN-15 Placebo (LOCF)45.0
DFN-15 Active (LOCF)58.9
DFN-15 Placebo (OC)44.4
DFN-15 Active (OC)58.5

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Subject-Rated Treatment Satisfaction at 24 Hours Postdose - PPMQ-R (DB1 and DB2)

Patient Perception of Migraine Questionnaire-Revised had 30 questions assessing subject's satisfaction with migraine medication, including 3 global items & 4 subscales (i.e., efficacy, function, ease of use, tolerability). A 5-point scale (1-Not At All to 5-Extremely) was used for tolerability subscale questions; a 7-point scale (1-Very Satisfied to 7-Very Dissatisfied) was used for all other subscales and global items. Total score was average of efficacy/function/ease of use subscale scores. Each subscale & total scores were transformed to range from 0-100, with higher scores indicating better satisfaction or tolerability. Total raw score/global items were not transformed. The total raw score could range from 17 (min) to 119 (max), with lower scores indicating better satisfaction. Change from baseline scores at 24-hour-postdose for each subscale score, global item score, total score, & total raw score were summarized by treatment group below. (NCT03009019)
Timeframe: 24 hours postdose

,,,
Interventionunits on a scale (Mean)
Total ScoreTotal Raw ScoreEfficacyFunctionEase of UseTolerabilityMedication effectiveness (Global Item)Side Effects (Global Item)Overall Satisfaction (Global Item)
DFN-15 DB15.112-1.4983.0168.5543.7666.980.1-0.40.1
DFN-15 DB26.691-2.3126.04410.7083.3607.62-0.1-0.5-0.1
Placebo DB1-4.8662.463-9.591-3.812-1.1976.090.9-0.50.8
Placebo DB20.4910.426-3.2612.5592.1745.870.6-0.20.5

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Headache Pain Relief Postdose (DB1 and DB2)

Headache pain relief was defined for DB1 as a reduction from moderate or severe pain before dosing to mild or none postdose, and for DB2 as moderate or severe pain before dosing reduced to mild or none postdose, or mild pain before dosing reduced to none postdose. Data are reported by percentage reporting headache pain relief over time postdose. (NCT03009019)
Timeframe: 15 minutes to 24 hours postdose

,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB112.625.340.049.658.868.682.994.3
DFN-15 DB215.028.040.052.862.769.684.795.1
Placebo DB112.622.435.039.849.656.973.892.7
Placebo DB27.923.035.341.951.958.674.688.2

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Headache Pain Freedom Postdose (DB1 and DB2)

The percentage of subjects who were pain-free at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2 period), 4, and 24 hours postdose compared between DFN-15 and placebo (NCT03009019)
Timeframe: 15 minutes to 24 hours postdose

,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose4 hours postdose24 hours postdose
DFN-15 DB11.23.79.518.024.749.179.4
Placebo DB12.95.59.712.619.840.271.9

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Headache Pain Freedom Among Subjects With Cutaneous Allodynia (DB1 and DB2)

The percentage of subjects who were pain-free at 2 and 4 hours postdose compared between DFN-15 and placebo, among those reporting cutaneous allodynia predose (NCT03009019)
Timeframe: 2 and 4 hours postdose

,,,
Interventionpercentage of subjects (Number)
2 hours postdose4 hours postdose
DFN-15 DB126.239.3
DFN-15 DB239.554.5
Placebo DB126.237.9
Placebo DB225.543.1

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Headache Pain Freedom Among BMI Category (DB1 and DB2)

The percentage of subjects who were pain-free at 2 and 4 hours postdose whose BMI was < 30 kg/m2 vs. subjects whose BMI was ≥ 30 kg/m2, and whose BMI was < 25 kg/m2 vs. subjects whose BMI was ≥ 25 kg/m2 (NCT03009019)
Timeframe: 2 and 4 hours postdose

,,,
Interventionpercentage of subjects (Number)
2 hours postdose (BMI<30)4 hours postdose (BMI<30)2 hours postdose (BMI>=30)4 hours postdose (BMI>=30)
DFN-15 DB125.643.641.956.0
DFN-15 DB234.355.040.064.7
Placebo DB122.938.129.342.7
Placebo DB222.144.326.549.2

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Freedom From Nausea, Photophobia, and Phonophobia Postdose (DB1 and DB2)

The percentage of subjects who were free from nausea, photophobia, and phonophobia at 15, 30, and 45 minutes and 1, 1.5, 2, 4, and 24 hours postdose compared between DFN-15 and placebo (NCT03009019)
Timeframe: 15 minutes to 24 hours postdose

,,,,,,,,,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB1 Nausea14.332.444.455.958.866.783.089.6
DFN-15 DB1 Phonophobia15.524.533.939.552.059.268.588.9
DFN-15 DB1 Photophobia9.015.925.232.046.358.070.586.5
DFN-15 DB2 Nausea16.227.244.056.962.972.984.093.3
DFN-15 DB2 Phonophobia13.225.936.948.155.661.375.889.2
DFN-15 DB2 Photophobia10.421.230.237.248.253.773.790.4
Placebo DB1 Nausea20.335.340.345.853.560.474.089.1
Placebo DB1 Phonophobia11.116.829.432.540.947.065.282.5
Placebo DB1 Photophobia6.214.722.825.935.642.957.583.9
Placebo DB2 Nausea10.427.540.455.158.968.573.190.8
Placebo DB2 Phonophobia8.719.529.238.252.453.969.587.6
Placebo DB2 Photophobia3.315.025.330.842.250.361.085.7

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Change in Functional Disability Score Postdose (DB1 and DB2)

"Change in functional disability score at 2, 4, and 24 hours postdose compared between DFN-15 and placebo. The values of the functional disability scale were: 0=no disability, able to function normally; 1=performance of daily activities mildly impaired, can still do everything but with difficulty; 2=performance of daily activities moderately impaired, unable to do some things; 3=performance of daily activities severely impaired, cannot do all or most things, bed rest may be necessary.~A decrease in values indicates improvement from baseline." (NCT03009019)
Timeframe: 2 to 24 hours postdose

,,,
Interventionunits on a scale (Mean)
2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB1-0.9-1.2-1.7
DFN-15 DB2-0.9-1.2-1.7
Placebo DB1-0.7-1.0-1.7
Placebo DB2-0.6-0.9-1.5

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Absence of Screening MBS at Time Points Postdose (DB1 and DB2)

The percentage of subjects with their Screening MBS (Most Bothersome Symptom) absent at 15, 30, and 45 minutes and 1, 1.5, 2 (DB2 period), 4, and 24 hours postdose compared between DFN-15 and placebo. (NCT03009019)
Timeframe: 15 minutes to 24 hours postdose

,,,
Interventionpercentage of subjects (Number)
15 minutes postdose30 minutes postdose45 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose4 hours postdose24 hours postdose
DFN-15 DB110.418.229.136.048.858.970.186.4
DFN-15 DB29.621.531.142.051.856.975.691.0
Placebo DB18.317.024.027.638.145.061.483.8
Placebo DB25.816.428.132.344.751.361.586.7

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Interference as Measured by the Brief Pain Inventory (BPI) at 1 Year

"The participant is asked circle the one number that describes how much, during the past week pain has interfered with general activity, mood, walking ability, normal work (includes both work outside the home and housework), relations with other people, sleep, and enjoyment of life.~0=does not interference and 10 = completely interferes. The higher number indicates more interference from pain.~The scores for each subsection will be averaged." (NCT03084536)
Timeframe: At 1 year

Interventionscore on a scale (Median)
Preoperative PECS Blocks0
Placebo PECS Blocks0

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Worst Pain as Measured by the Brief Pain Inventory (BPI) at 1 Year

"The participant is asked to rate their pain by circling the one number that best describes their pain at its worst in the past week.~0=no pain and 10 = pain as bad as they can imagine. The higher number indicates worse pain." (NCT03084536)
Timeframe: At 1 year

Interventionscore on a scale (Median)
Preoperative PECS Blocks0
Placebo PECS Blocks0

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Change in Quality of Life as Measured by the Veterans RAND12 Questionnaire Physical Health Summary Measure

"The 12 items in the questionnaire correspond to eight principal physical and mental health domains including general health perceptions; physical functioning; role limitations due to physical and emotional problems; bodily pain; energy-fatigue, social functioning and mental health. The 12 items are summarized into two scores, a Physical Health Summary Measure (PCS) and a Mental Health Summary Measure (MCS).~The higher the score the better quality of life.~Scores are standardized to a mean of 50 with a range of -0.809-70.71." (NCT03084536)
Timeframe: At baseline and 1 year post-surgery

Interventionscore on a scale (Median)
Preoperative PECS Blocks-3.1
Placebo PECS Blocks-0.8

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Average Pain as Measured by the Brief Pain Inventory (BPI) at 1 Year

"The participant is asked to rate their pain by circling the one number that best describes their pain on the average.~0=no pain and 10 = pain as bad as they can imagine. The higher number indicates worse pain." (NCT03084536)
Timeframe: At 1 year

Interventionscore on a scale (Median)
Preoperative PECS Blocks0
Placebo PECS Blocks0

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Change in Quality of Life as Measured by the Veterans RAND12 Questionnaire Mental Health Summary Measure

"The 12 items in the questionnaire correspond to eight principal physical and mental health domains including general health perceptions; physical functioning; role limitations due to physical and emotional problems; bodily pain; energy-fatigue, social functioning and mental health. The 12 items are summarized into two scores, a Physical Health Summary Measure (PCS) and a Mental Health Summary Measure (MCS).~The higher the score the better quality of life.~Scores are standardized to a mean of 50 with a range of -1.465-77.09." (NCT03084536)
Timeframe: At baseline and 1 year post-surgery

Interventionscore on a scale (Median)
Preoperative PECS Blocks0
Placebo PECS Blocks1.9

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Sum of Pain Intensity Differences (SPID)

"The primary efficacy variable was the Pain Intensity (PI) measured by the Numerical Pain Rating Scale (NPRS); a scale from zero to 10 on which subjects circled a single number to indicate current pain level, with zero representing No Pain and 10 representing Worst Possible Pain. The primary analysis endpoint was the Sum of Pain Intensity Differences (SPID) from 0 to 48 hours. Pain Intensity Differences (PID) was the difference between current PI at assessment minus baseline PI (prior to the first dose). Baseline PI ranged from 5 to 9. SPID was calculated as a time-weighted Sum of PID scores over 48 hours. Negative differences correspond to an amelioration of pain, while positive differences correspond to recrudescence of pain. The total scale ranged from -480 (best) to +480 (worst). A higher negative value of SPID indicates greater pain relief." (NCT03108482)
Timeframe: Assessments was recorded from time 0 to 48 hours.

Interventionunits on a scale (Least Squares Mean)
Co-crystal E-58425 (Tramadol/Celecoxib)-139.12
Tramadol (Ultram®)-109.08
Celecoxib (Celebrex®)-103.69
Placebo-74.55

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered a study drug which may or may not have a causal relationship with the study drug. TEAE was defined as an AE with an onset that occurs after receiving study drug. A serious adverse event (SAE) was defined as any untoward medical occurrence that resulted in any of the following outcomes: death, life-threatening, required initial or prolonged in-patient hospitalization, persistent or significant disability/incapacity, congenital anomaly/birth defect, or considered as medically important event. Any TEAE included participants with both serious and non-serious TEAEs. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo186
NSAIDs406
Fasinumab 1 mg403

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Serum Concentrations of Functional Fasinumab

(NCT03304379)
Timeframe: At Weeks 0, 4, 8, 16, 24 and 44

InterventionMilligrams per Liter (mg/L) (Mean)
Week 0Week 4Week 8Week 16Week 24Week 44
Fasinumab 1 mg0.0001550.04690.06440.07380.07130.000349

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Number of Participants With At-least One Positive Anti-Drug Antibody (ADA) Development

Immunogenicity was characterized by ADA responses & titers. Responses categories: Pre-existing immunoreactivity - ADA positive response at baseline with all post first dose negative results or positive response at baseline with all post first dose ADA responses < 9-fold over baseline titer levels; Treatment-boosted response - positive response in the assay post first dose, >= 9-fold over baseline titer levels, when baseline results are positive; Treatment-emergent response - ADA positive response post first dose when baseline results = negative or missing. (NCT03304379)
Timeframe: Baseline up to Week 44

,,
InterventionParticipants (Count of Participants)
Pre-Existing ImmunoreactivityTreated-Boosted ResponseTreatment-Emergent Response
Fasinumab 1 mg1504
NSAIDs901
Placebo1003

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Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

Physical function referred to participant's ability to move around and perform usual activities of daily living. The WOMAC physical function subscale was a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index joint (knee or hip) during past 48 hours. It was calculated as mean of the scores from 17 individual questions scored on a NRS of 0 (minimum difficulty) to 10 (maximum difficulty), where higher scores indicated maximum difficulty. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.65-2.62
Placebo-2.02-1.80

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Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

Physical function referred to participant's ability to move around and perform usual activities of daily living. The WOMAC physical function subscale was a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index joint (knee or hip) during past 48 hours. It was calculated as mean of the scores from 17 individual questions scored on a NRS of 0 (minimum difficulty) to 10 (maximum difficulty), where higher scores indicated maximum difficulty. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.65-2.62
NSAIDs-2.33-2.26

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Change From Baseline in WOMAC Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index joint (knee or hip) in the past 48 hours. It is calculated as the mean of the scores from the 5 individual questions scored on a NRS of 0 (no pain) to 10 (higher pain), where higher scores indicated higher pain. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.84-2.78
NSAIDs-2.60-2.48

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Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

WOMAC pain subscale was a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index joint (knee or hip) in past 48 hours. It was calculated as the mean of the scores from the 5 individual questions scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (higher pain), where higher scores indicated higher pain. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.84-2.78
Placebo-2.21-2.01

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Number of Participants With Sympathetic Nervous System (SNS) Dysfunction Events

Potential events of SNS dysfunction were monitored throughout the study through physical examination, AE reporting, assessment of orthostatic hypotension, and the Survey of Autonomic Symptoms. Sympathetic nervous system dysfunction was diagnosed after consultation with an appropriate specialist, such as a neurologist and/or cardiologist. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo0
NSAIDs0
Fasinumab 1 mg0

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Number of Participants With Joint Replacement (JR) Surgery Reported at End of Study (EOS) (Week 72)

An EOS phone contact was conducted at Week 72 following the last dose of study drug (Week 24) to evaluate the number of participants who had undergone or were scheduled for JR surgery. (NCT03304379)
Timeframe: At Week 72

InterventionParticipants (Count of Participants)
Placebo11
NSAIDs29
Fasinumab 1 mg21

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Number of Participants With At-least One Peripheral Sensory Adverse Events (AEs)

Any participants with a peripheral sensory event that persisted for 2 months was referred for a neurology or other specialty consultation and reported as an Adverse Events of Special Interest (AESI). (NCT03304379)
Timeframe: Baseline up to Week 44

InterventionParticipants (Count of Participants)
Placebo8
NSAIDs24
Fasinumab 1 mg31

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Number of Participants With Adjudicated Arthropathy (AA) Events

AA was a composite term that encompasses the following conditions: Rapidly progressive Osteoarthritis (OA) type 1 and 2, Subchondral insufficiency fractures, and Primary Osteonecrosis confirmed by an arthropathy adjudication committee. AAs were also evaluated to determine if they met Destructive Arthropathy criteria. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo5
NSAIDs9
Fasinumab 1 mg34

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Number of Participants With AA Events Meeting Destructive Arthropathy (DA) Criteria

DA is a unique clinical form of rapidly destructive arthropathy over and above that seen in the normal progression of OA. DA criteria can be associated with Rapidly Progressive OA type 2, Subchondral Insufficiency fracture, and Primary Osteonecrosis confirmed by an arthropathy adjudication committee. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo0
NSAIDs0
Fasinumab 1 mg2

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Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 44

Number of participants who underwent a JR surgery from baseline up to follow-up period (Week 44) were reported. (NCT03304379)
Timeframe: Baseline up to Week 44

InterventionParticipants (Count of Participants)
Placebo6
NSAIDs13
Fasinumab 1 mg10

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Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 24

Number of participants who underwent a JR surgery from baseline up to Week 24 were reported. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionParticipants (Count of Participants)
Placebo2
NSAIDs7
Fasinumab 1 mg3

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Change From Baseline in Weekly Average Walking Index Joint Pain Score up to Week 24 by Using the Numeric Rating Scale (NRS) Pain Scale

Participants reported weekly average walking index joint pain based on NRS. The NRS was nationally recognized numeric scale from 0 to 10, where 0 would demonstrate no pain, 1 to 3 would demonstrate mild pain, 4 to 6 would be moderate pain, 7 to 9 would be severe pain and 10 would be the worst pain possible. Higher score indicated greater pain. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
Pooled Placebo-1.85
NSAIDs-2.13
Fasinumab 1 mg-2.51

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Change From Baseline in PGA Score up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

The PGA was a patient-rated assessment of current disease state on a 5-point Likert scale where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (Severe symptoms and inability to carry out most normal activities) and, 5 =very poor (Very severe symptoms which were intolerable and inability to carry out all normal activities). Higher score indicated severe condition. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
NSAIDs-0.75
Fasinumab 1 mg-0.81

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Change From Baseline in Patient Global Assessment (PGA) Score up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

The PGA was a patient-rated assessment of current disease state on a 5-point Likert scale where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (Severe symptoms and inability to carry out most normal activities) and, 5 =very poor (Very severe symptoms which were intolerable and inability to carry out all normal activities). Higher score indicated severe condition. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
Placebo-0.66
Fasinumab 1 mg-0.81

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Percentage of Participants With Greater Than or Equal to (≥) 30 Percent (%) Reduction From Baseline up to Week 24 in WOMAC Pain Subscale Score in Participants Treated With Fasinumab Compared to Placebo

WOMAC pain subscale was a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index knee during past 48 hours. It was calculated as mean of the scores from 5 individual questions scored on a NRS of 0 (minimum pain) to 10 (maximum pain), where higher scores indicate more pain. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionPercentage of Participants (Number)
Placebo48.7
Fasinumab 1 mg59.8

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Average Inpatient Hydromorphone Use

Average inpatient hydromorphone use measured in milligrams (NCT03331315)
Timeframe: 48 hrs following surgery

InterventionMilligrams (Mean)
Ketorolac0.7
Celecoxib0.8

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Average Inpatient Ondansetron Use

Average inpatient ondansetron use measured in milligrams (NCT03331315)
Timeframe: 48 hrs following surgery

InterventionMilligrams (Mean)
Ketorolac1.5
Celecoxib1.3

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Average Inpatient Postoperative Pain Score

Pain measured using the Visual Analog Scale, no pain (0-0.4 cm), mild pain(0.5-4.4 cm), moderate pain (4.5-7.4 cm), and severe pain (7.5-10.0 cm). Subscale scoring was not used in analysis but provided as reference for patient and nursing staff. (NCT03331315)
Timeframe: 48 hrs following surgery

Interventionunits on a scale (Mean)
Ketorolac2.7
Celecoxib2.4

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Days of Oral Narcotic Use After Discharge

Measured using postoperative questionnaire (NCT03331315)
Timeframe: 2 weeks after discharge

InterventionDays (Mean)
Ketorolac5.7
Celecoxib3.8

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Total Hospital Stay

Total hospital stay from time fo admission to time of discharge measured in hours (NCT03331315)
Timeframe: Following surgery

InterventionHours (Mean)
Ketorolac11.6
Celecoxib11.9

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Return to Activities of Daily Living

Average number of days required for complete return to independent activities of daily living (NCT03331315)
Timeframe: 2 weeks after discharge

InterventionDays (Mean)
Ketorolac2.4
Celecoxib2.2

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Number of Participants With Perioperative Complications

Perioperative Complications measured intraoperatively and postoperatively by type (NCT03331315)
Timeframe: During and after surgery

InterventionPatients (Number)
Ketorolac5
Celecoxib6

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Number of Oral Narcotic Pills Used After Discharge

Number of oral narcotic pills used after discharge until 2 week postoperative visit. (NCT03331315)
Timeframe: 2 weeks after discharge

InterventionPills (Mean)
Ketorolac8.1
Celecoxib6.0

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Objective Response Rate (ORR) Assessed by Response Evaluation Criteria in Solid Tumors Version (RECIST) 1.1

Will be treated as binary data and summarized using frequencies and relative frequencies; with the ORR estimated using a 90% confidence interval obtained using Jeffrey's prior method. (NCT03403634)
Timeframe: Up to 12 months

InterventionParticipants (Count of Participants)
Treatment (Celecoxib, Interferon Alfa-2b, Rintatolimod)0

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Change in Tumor-infiltrating Lymphocytes (TILs) in the Colorectal Cancer Lesions

"The TILs will be summarized by time-point (pre-/post-treatment) using the mean, median, standard deviation; and graphically using dot-plots.~The TIL of interest is CD8a expression, which is reported as the mean fold change from pre-treatment (i.e. post treatment / pre treatment)." (NCT03403634)
Timeframe: Baseline up to 12 months

Interventionfold change (Mean)
Treatment (Celecoxib, Interferon Alfa-2b, Rintatolimod)7.25

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Overall Survival

Will be treated as bivariate time-to-event data and will be summarized using standard Kaplan-Meier methods. (NCT03403634)
Timeframe: From the start of treatment until death due to any cause or last follow-up, assessed up to 12 months

InterventionMonths (Median)
Treatment (Celecoxib, Interferon Alfa-2b, Rintatolimod)10.5

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Progression Free Survival

Will be treated as bivariate time-to-event data and will be summarized using standard Kaplan-Meier methods. (NCT03403634)
Timeframe: From the start of treatment until disease progression (defined by RECIST 1.1) or last-follow-up, assessed up to 12 months

InterventionMonths (Median)
Treatment (Celecoxib, Interferon Alfa-2b, Rintatolimod)1.5

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Pharmacy Costs

The costs of the pain medications given during the specified time period. (NCT03472469)
Timeframe: until discharge from hospital or 30 days post admission (whichever is sooner)

Interventiondollars (Median)
Original MMPR - Descending Dose Arm507
MAST MMPR - Escalating Dose Arm397

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Pain as Assessed by Score on the Numeric Rating Scale (NRS)

An average will be calculated of the daily numeric rating scale (NRS) for pain (0=no pain, 10=worst pain). This assessment is used in verbal participants. (NCT03472469)
Timeframe: until discharge from hospital or 30 days post admission (whichever is sooner)

Interventionunits on a scale (Median)
Original MMPR - Descending Dose Arm3.3
MAST MMPR - Escalating Dose Arm3.3

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Pain as Assessed by Score on the Behavioral Pain Scale (BPS)

An average will be calculated of the daily score on the Behavioral Pain Scale (BPS). BPS score ranges from 3-12, with higher scores indicating worse pain. This assessment is used in non-verbal participants. (NCT03472469)
Timeframe: until discharge from hospital or 30 days post admission (whichever is sooner)

Interventionscore on a scale (Median)
Original MMPR - Descending Dose Arm2.5
MAST MMPR - Escalating Dose Arm2.3

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Overall Costs

the costs associated with the overall hospitalization or the first 30 days (whichever is sooner) related to post trauma care and complications incurred. (NCT03472469)
Timeframe: until discharge from hospital or 30 days post admission (whichever is sooner)

Interventiondollars (Median)
Original MMPR - Descending Dose Arm20093
MAST MMPR - Escalating Dose Arm19561

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Opioid Use Per Day

Opioid use per day is calculated by tallying the dose equivalency of all opioids received and dividing by the number of days hospitalized. Morphine milligram equivalents (MME) per day are reported. (NCT03472469)
Timeframe: until discharge from hospital or 30 days post admission (whichever is sooner)

InterventionMME per day (Median)
Original MMPR - Descending Dose Arm48
MAST MMPR - Escalating Dose Arm34

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Number of Ventilator Days

"The number of days the patient on a ventilator post injury or up to 30 days (whichever is sooner). Zero-inflated models are presented as estimated marginal means (95% Credible Interval). The data reported as mean actually refers to marginal mean, and the data reported as 95% Confidence Interval actually refers to a 95% Credible Interval." (NCT03472469)
Timeframe: 30 days

Interventionventilator days (Mean)
Original MMPR - Descending Dose Arm0.08
MAST MMPR - Escalating Dose Arm0.06

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Number of Participants Discharged From the Hospital With an Opioid Prescription

(NCT03472469)
Timeframe: Up to 30 days

InterventionParticipants (Count of Participants)
Original MMPR - Descending Dose Arm527
MAST MMPR - Escalating Dose Arm476

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Number of Intensive Care Unti (ICU) Days

"The number of days the patient was in the ICU post injury or up to 30 days (whichever is sooner). Zero-inflated models are presented as estimated marginal means (95% Credible Interval). The data reported as mean actually refers to marginal mean, and the data reported as 95% Confidence Interval actually refers to a 95% Credible Interval." (NCT03472469)
Timeframe: 30 days

InterventionICU days (Mean)
Original MMPR - Descending Dose Arm0.21
MAST MMPR - Escalating Dose Arm0.21

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Number of Hospital Days

"The number of days the patient was hospitalized post injury or up to 30 days (whichever is sooner). Zero-inflated models are presented as estimated marginal means (95% Credible Interval). The data reported as mean actually refers to marginal mean, and the data reported as 95% Confidence Interval actually refers to a 95% Credible Interval." (NCT03472469)
Timeframe: 30 days

Interventionhospital days (Mean)
Original MMPR - Descending Dose Arm4.97
MAST MMPR - Escalating Dose Arm5.12

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Change of Pain Score

Change of pain score by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-2
NSAIDs x 6 Weeks-2

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Change of Bath Ankylosing Spondylitis Function Index (BASFI)

Change of BASFI by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-0.8
NSAIDs x 6 Weeks-1.2

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Change of Bath Ankylosing Spondylitis Disease Activity Index (BASDAI)

Change of BASDAI by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-1.7
NSAIDs x 6 Weeks-2.09

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Change of ASAS Endorsed Disease Activity Score (ASDAS)

Change of ASDAS by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-0.37
NSAIDs x 6 Weeks-0.84

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Nausea

rate of nausea (NCT03540030)
Timeframe: 2 Weeks

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention1340
Observational5232

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Pain Satisfaction

Satisfaction with overall pain using Numeric Pain Rating (NRS) scale. yes, no. No being better than yes. (NCT03540030)
Timeframe: 2 Months

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention2924
Observational2352

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Pain Satisfaction

Satisfaction with overall pain using Numeric Pain Rating (NRS) scale. yes, no. No being better than yes. (NCT03540030)
Timeframe: 2 Weeks

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention3410
Observational2712

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Veterans RAND 12 Item Health Survey (VR-12©) Physical Health Subscore, and Mental Health Subscore

quality of life using VR-12 subscores. Physical Health (PCS) subscore and Mental Health (MCS) subscore, not summed. Range reported in weighted units. Physical Health subscore: 1 point increase in PCS is associated with 6% lower total health care expenditures, 5% lower pharmacy expenditures, 9% lower rate of hospital inpatient visits, 4% lower rate of medical provider visits, 5% lower rate of hospital outpatient visits. Mental Health sub score a 1 point increase in MCS is associated with 7% lower total health care expenditures, 4% lower pharmacy expenditures, 15% lower rate of hospital inpatient visits, and 4% lower rate of medical provider visits. Both PCS/MCS are score 0-100 with 100 indicating the highest level of health. (NCT03540030)
Timeframe: 2 Months

,
Interventionscore on a scale (Median)
PCSMCS
Non-Opioid Intervention40.360.8
Observational38.458.7

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Veterans RAND 12 Item Health Survey (VR-12©) Physical Health Subscore, and Mental Health Subscore

quality of life using VR-12 subscores. Physical Health (PCS) subscore and Mental Health (MCS) subscore, not summed. Range reported in weighted units. Physical Health subscore: 1 point increase in PCS is associated with 6% lower total health care expenditures, 5% lower pharmacy expenditures, 9% lower rate of hospital inpatient visits, 4% lower rate of medical provider visits, 5% lower rate of hospital outpatient visits. Mental Health sub score a 1 point increase in MCS is associated with 7% lower total health care expenditures, 4% lower pharmacy expenditures, 15% lower rate of hospital inpatient visits, and 4% lower rate of medical provider visits. Both PCS/MCS are score 0-100 with 100 indicating the highest level of health. (NCT03540030)
Timeframe: 2 Weeks

,
Interventionscore on a scale (Median)
PCSMCS
Non-Opioid Intervention35.059.1
Observational36.756.3

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Constipation

rate of constipation (NCT03540030)
Timeframe: 2 Weeks

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention13220
Observational1992

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Morphine Use

Morphine milli-equivalents In-hospital post-operative. Continuous scale of MME, no defined better/worse. Measured as number and dose of medications taken. For example, if the patient received an opioid, the drug and dose was recorded and converted to MME. A time frame of when to assess opioid use in-hospital post-operative was not used but was a continuous monitor for rescue opioid from in-hospital post-operative through discharge. (NCT03540030)
Timeframe: In-hospital Stay

InterventionMorphine milli-equivalents (Median)
Observational45.0
Non-Opioid Intervention19.0

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Post Op Pain

Pain at patient discharge or 24-hours, whichever comes first - measured on a 0 (no pain) -10 (worst possible pain) numeric rating scale (NRS). A score of 0(no pain) is preferable to 10(worst possible pain) (NCT03540030)
Timeframe: 24 hours

Interventionscore on a scale (Median)
Observational3.0
Non-Opioid Intervention2.0

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Simple Shoulder Test

Simple Shoulder Test (SST) activity score. Range 0-12. 0 = worse activity score. (NCT03540030)
Timeframe: 2 Months

Interventionscore on a scale (Median)
Observational6
Non-Opioid Intervention6

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Simple Shoulder Test

Simple Shoulder Test (SST) activity score. Range 0-12. 0 = worse activity score. (NCT03540030)
Timeframe: 2 Weeks

Interventionscore on a scale (Median)
Observational2.0
Non-Opioid Intervention2.0

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Nausea

rate of nausea (NCT03540030)
Timeframe: 2 Months

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention1300
Observational0282

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Additional Post Op Pain

post-operative pain: measured on a 0 (no pain) -10 (worst) numeric rating scale (NRS) at 6hrs, 12hrs, 2 weeks, and 2 months. A score of 0(no pain) is preferable to 10(worst possible pain) (NCT03540030)
Timeframe: 6hrs, 12hrs, 2weeks, 2 months

,
Interventionscore on a scale (Median)
6 Hrs12 hrs2 weeks2 months
Non-Opioid Intervention0.000.820
Observational241.30.7

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Constipation

rate of constipation (NCT03540030)
Timeframe: 2 Months

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention4274
Observational7212

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Falls

rate of falls (NCT03540030)
Timeframe: 2 Months

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention4274
Observational4242

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Falls

rate of falls (NCT03540030)
Timeframe: 2 Weeks

,
InterventionParticipants (Count of Participants)
YesNoUnknown
Non-Opioid Intervention5300
Observational1272

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ASES

American Shoulder and Elbow Surgeons (ASES) Shoulder Score for pain and function. Range 0-100. Low score = worse shoulder condition. Function, disability, and pain subscores (all ranges 0-50), and are summed for total ASES score. (NCT03540030)
Timeframe: 2 Weeks

Interventionunits on a scale (Median)
Observational54.3
Non-Opioid Intervention54.2

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Summed Pain Intensity Difference Over the First Six Hours

"The primary endpoint is the Summed Pain Intensity Difference over the first 6 hours (SPID6) after dosing compared between DFN-15 and placebo. Pain intensity (P) will be measured at timepoints of 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, 5 and 6, hours after baseline ,using 11-point Pain Intensity Numerical Rating Scale (NPRS). Zero (0) equals no pain and Ten (10) equals worst pain imaginable.~SPID6 is created by summing the time weighted pain intensity differences (PID) scores using the area under the PID curve methodology. All SPID calculations will be performed using the standard trapezoidal rule SPIDx =∑_(i=0)^x▒((〖PID〗_i+〖PID〗_(i+1))/2) * (T_(i+1)- T_i ) Where: PID_i = P_i - PBL (Pain score at time i and Pain score at Baseline), and (T_i+1 - T_i) is the Time difference in minutes between time i and time i+1.~Therefore, SPID6 values may theoretically range between a maximum score of 0 ( no improvement) and a minimum score of -3525 (best improvement)" (NCT03554772)
Timeframe: 6 hours post dose

Interventionunits on a scale (Mean)
Placebo-420.2
DFN-15 (Celecoxib Oral Solution) 62.5 mg-1101.0
DFN-15 (Celecoxib Oral Solution) 125 mg-1771.7
DFN-15 (Celecoxib Oral Solution) 250 mg-1463.5

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Change From Baseline in Brief Arthritis Stiffness Scale (BASS) Score at Day 4

Brief Arthritis Stiffness Scale (BASS) is a patient-reported outcome (PRO) instrument measuring of the severity of osteoarthritis-related stiffness in the target knee joint. The BASS score ranges from 0 to 40 and a higher score indicates worse stiffness. (NCT03570554)
Timeframe: Day 4

InterventionScores on a scale (Least Squares Mean)
Naproxen-5.2
Acetaminophen ER-5.3
Celecoxib-4.8
Placebo-1.3

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Absolute Brief Arthritis Stiffness Scale (BASS) Score at Each Time Point

Brief Arthritis Stiffness Scale (BASS) is a patient-reported outcome (PRO) instrument measuring of the severity of osteoarthritis-related stiffness in the target knee joint. The BASS score ranges from 0 to 40 and a higher score indicates worse stiffness. (NCT03570554)
Timeframe: 4 days

,,,
InterventionScores on a scale (Least Squares Mean)
Day 1Day 2Day 3Day 4
Acetaminophen ER23.319.718.418.0
Celecoxib24.620.618.918.5
Naproxen23.020.818.418.1
Placebo22.623.222.422.0

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Sum of Change in Brief Arthritis Stiffness Scale (BASS) Scores Over the 4-day Treatment Period

Brief Arthritis Stiffness Scale (BASS) is a patient-reported outcome (PRO) instrument measuring of the severity of osteoarthritis-related stiffness in the target knee joint. The BASS score ranges from 0 to 40 and a higher score indicates worse stiffness. This endpoint was calculated by summing the changes from baseline (CFB) in BASS scores at Days 2, 3, and 4 of the treatment periods. (NCT03570554)
Timeframe: 4 days

InterventionScores on a scale (Least Squares Mean)
Naproxen-12.6
Acetaminophen ER-13.6
Celecoxib-11.7
Placebo-2.3

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Pain Intensity Scores at 24 Hours at Rest Using Numerical Rating Scale (NRS)

Numeric Rating Scale (NRS) of pain intensity from 0-10 where 0 is no pain and 10 is the worst pain imaginable at 24 hours (NCT03885596)
Timeframe: 24 hours

Interventionunits on a scale (Mean)
CA-008 Cohort 10.6
CA-008 Cohort 21.7
CA-008 Cohort 35.1
Exparel6.0

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Pain Intensity Scores at 48 Hours at Rest Using Numerical Rating Scale (NRS)

Numeric Rating Scale (NRS) of pain intensity from 0-10 where 0 is no pain and 10 is the worst pain imaginable at 48 hours (NCT03885596)
Timeframe: 48 hours

Interventionscore on a scale (Mean)
CA-008 Cohort 11.3
CA-008 Cohort 20.6
CA-008 Cohort 32.7
Exparel4.8

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Area Under the Curve (AUC) of Numerical Rating Scale (NRS) Scores (at Rest) Over 72h

Area Under the Curve of pain intensity scores (using a Numeric Rating Scale of pain intensity from 0-10 where 0 is no pain and 10 is the worst pain imaginable) over 72 hours (NCT03885596)
Timeframe: 0-72 hours

Interventionscore on a scale*hour (Mean)
CA-008 Cohort 172.30
CA-008 Cohort 266.24
CA-008 Cohort 3203.76
Exparel306.58

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Opioid Consumption

Summary of opioid consumption in oral morphine equivalents (NCT03885596)
Timeframe: 0-72 hours

Interventionmg morphine equivalents (Mean)
CA-008 (Vocacapsaicin) Cohort 110.83
CA-008 (Vocacapsaicin) Cohort 23.33
CA-008 (Vocacapsaicin) Cohort 338.33
Exparel80.83

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Pain Intensity Scores at 72 Hours at Rest Using Numerical Rating Scale (NRS)

Numeric Rating Scale (NRS) of pain intensity from 0-10 where 0 is no pain and 10 is the worst pain imaginable at 72 hours (NCT03885596)
Timeframe: 72 hours

Interventionscore on a scale (Mean)
CA-008 Cohort 11.2
CA-008 Cohort 20.3
CA-008 Cohort 32.0
Exparel4.6

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Change of Pain Intensity After 5, 24 and 38 Days of Treatment

Pain intensity was measured using 0-10 point Numeric Rating Scale (NRS). NRS is 11-step scale for assessment of pain intensity at the moment of patient's examination ranging from 0 (no pain) to 10 (worst pain imaginable). Pain intensity was measured at baseline, at 5, 24 and 38 days after the start of treatment.Changes of pain intensity from baseline to Day 5, from baseline to Day 24 and from baseline to Day 38 after the start of treatment were calculated separately. (NCT03892707)
Timeframe: Baseline; Visit 2 (5 days after the start of treatment), Visit 4 (24 days after the start of treatment); Visit 5 (38 days after the start of treatment)

,
Interventionunits on a scale (Mean)
Change of pain intensity from baseline to Day 5 after the start of treatmentChange of pain intensity from baseline to Day 24 after the start of treatmentChange of pain intensity from baseline to Day 38 after the start of treatment
NSAIDs Group-3.1-6.1-6.3
NSAIDs+Milgamma+Milgamma Compositum Group-2.4-5.3-6.0

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Patient Satisfaction With Treatment

Patient satisfaction with treatment was evaluated using a 5-point verbal rating scale (1= very dissatisfied, 2= dissatisfied, 3= neutral, 4= satisfied, 5= very satisfied) after 5, 10, 38 days and 3 months (94 days) since the start of treatment. (NCT03892707)
Timeframe: Visit 2 (5 days after the start of treatment); Visit 3 (10 days after the start of treatment); Visit 5 (38 days after the start of treatment) and Visit 9 (94 days after the start of treatment)

,
Interventionunits on a scale (Mean)
Visit 2 (5 days after the start of treatment)Visit 3 (10 days after the start of treatment)Visit 5 (38 days after the start of treatment)Visit 9 (94 days after the start of treatment)
NSAIDs Group3.84.24.54.6
NSAIDs+Milgamma+Milgamma Compositum Group3.84.14.54.7

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Percentage of Patients With 30% Low Back Pain Relief After 5, 10, 24 and 38 Days of Treatment.

Pain intensity was measured using 0-10 point Numeric Rating Scale (NRS). NRS is 11-step scale for assessment of pain intensity at the moment of patient's examination ranging from 0 (no pain) to 10 (worst pain imaginable). Relief in pain intensity was defined as 100%*(pain intensity at baseline - pain intensity at Visit 2, 3, 4 or 5)/ pain intensity at baseline. Percentage of patients showing at least 30% low back pain relief at Visit 2 (5 days after the start of treatment), at Visit 3 (10 days after the start of treatment), at Visit 4 (24 days after the start of treatment) and at Visit 5 (38 days after the start of treatment) were calculated separately. (NCT03892707)
Timeframe: Visit 2 (5 days after the start of treatment); Visit 3 (10 days after the start of treatment); Visit 4 (24 days after the start of treatment) and Visit 5 (38 days after the start of treatment)

,
InterventionParticipants (Count of Participants)
Number and percentage of patients with 30% pain relief at Day 5 after the start of treatmentNumber and percentage of patients with 30% pain relief at Day 10 after the start of treatmentNumber and percentage of patients with 30% pain relief at Day 24 after the start of treatmentNumber and percentage of patients with 30% pain relief at Day 38 after the start of treatment
NSAIDs Group194235241244
NSAIDs+Milgamma+Milgamma Compositum Group140214240241

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Percentage of Patients With at Least One Pain Flare-up Resulting in Consultancy With Physician, Resulting in Disruption of Daily Activity, and Resulting in NSAIDs Intake

"Episode of pain flare-up was defined as presence of at least 1 day with low back pain following a period without pain lasting at least 4 weeks. Therefore pain flare-ups were registered no earlier than 4 weeks after the start of treatment, i.e. starting from Visit 5 (38 days after the start of treatment). The occurrence of pain flare-up was determined by the investigator.~Percentages of patients with at least one pain flare-up resulting in consultancy with physician or professional management, resulting in disruption of daily activity, and resulting in NSAIDs intake were analyzed separately." (NCT03892707)
Timeframe: From Visit 5 (38 days after the start of treatment) to Visit 9 (End of Study Visit, 94 days after the start of treatment)

,
InterventionParticipants (Count of Participants)
Patients with at least one pain flare-up resulting in consultancy with physicianPatients with at least one pain flare-up resulting in disruption of daily activityPatients with at least one pain flare-up resulting in NSAIDs intake
NSAIDs Group42019
NSAIDs+Milgamma+Milgamma Compositum Group448

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Prescribed and Actual Number of Milgamma® Injections

Prescribed number of Milgamma® injections was reported at Baseline visit. Actual number of injections was calculated by counting the number of injections administered and reported starting from Visit 2. If the treatment was interrupted, the days patient did not receive Milgamma® injections were not contribute to the total number of injections. (NCT03892707)
Timeframe: From Baseline to Visit 9 (End of Study Visit, 94 days after the start of treatment)/ Early Discontinuation Visit

Interventionnumber of injections (Mean)
Prescribed exposure of Milgamma® injectionsActual exposure of Milgamma® injections
NSAIDs+Milgamma+Milgamma Compositum Group9.39.3

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Prescribed and Actual Number of Treatment Days With Milgamma® Compositum

Prescribed number of treatment days with Milgamma® compositum intake was reported at Baseline visit. Actual number of treatment days was calculated by summing up all the individual periods of treatment with Milgamma® compositum (in days) reported starting from Visit 2. If the treatment was interrupted, the days patient did not receive Milgamma® compositum were not contribute to the total number of treatment days with Milgamma® compositum intake. (NCT03892707)
Timeframe: From Baseline to Visit 9 (End of Study Visit, 94 days after the start of treatment)/ Early Discontinuation Visit

InterventionDays of treatment (Mean)
Prescribed exposure of Milgamma® compositumActual exposure of Milgamma® compositum
NSAIDs+Milgamma+Milgamma Compositum Group30.129.9

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Change of Pain Intensity After 10 Days of Treatment

Pain intensity was measured using 0-10 point Numeric Rating Scale (NRS). NRS is 11-step scale for assessment of pain intensity at the moment of patient's examination ranging from 0 (no pain) to 10 (worst pain imaginable). Pain intensity was measured at baseline and at 10 days after the start of treatment. (NCT03892707)
Timeframe: Baseline; Visit 3 (10 days after the start of treatment)

Interventionunits on a scale (Mean)
NSAIDs Group-5.1
NSAIDs+Milgamma+Milgamma Compositum Group-4.0

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Change of Pain Intensity Over Time

Pain intensity was measured using 0-10 point Numeric Rating Scale (NRS). NRS is 11-step scale for assessment of pain intensity at the moment of patient's examination ranging from 0 (no pain) to 10 (worst pain imaginable). Pain intensity was measured at baseline, at 5, 10, 24 and 38 days after the start of treatment. A mixed model repeated measures was used to analyze change from baseline in pain intensity over time from Baseline to Visit 5 (38 days after the start of treatment) in each group. The model included a random effect for subject and fixed effect terms for treatment, visit, treatment-by-visit interaction, baseline pain intensity. An unstructured covariance structure was used to model the within-subject errors. P-value was calculated for the difference between treatment groups. (NCT03892707)
Timeframe: From Baseline to Visit 5 (38 days after the start of treatment)

Interventionunits on a scale (Least Squares Mean)
NSAIDs Group-5.1
NSAIDs+Milgamma+Milgamma Compositum Group-4.4

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Number of Treatment Days With NSAIDs

Number of treatment days with NSAIDs was calculated using the data collected on the NSAIDs intake during the study irrespective of the specific drug used. Duration of each intake period was determined as Stop date - Start date +1 and, finally, all individual duration values were summed up. In case medication intake was ongoing at the End of Study Visit, stop date was imputed by the date of study completion. (NCT03892707)
Timeframe: From Baseline to Visit 9 (End of Study Visit, 94 days after the start of treatment)/ Early Discontinuation Visit

InterventionDays of treatment (Mean)
NSAIDs Group9.6
NSAIDs+Milgamma+Milgamma Compositum Group10.6

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Percentage of Patients With at Least One Pain Flare-up During the Study

Episode of pain flare-up was defined as presence of at least 1 day with low back pain following a period without pain lasting at least 4 weeks. Therefore pain flare-ups were registered no earlier than 4 weeks after the start of treatment, i.e. starting from Visit 5 (38 days after the start of treatment). The occurrence of pain flare-up was determined by the investigator. (NCT03892707)
Timeframe: From Visit 5 (38 days after the start of treatment) to Visit 9 (End of Study Visit, 94 days after the start of treatment)

InterventionParticipants (Count of Participants)
NSAIDs Group35
NSAIDs+Milgamma+Milgamma Compositum Group10

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Number of Participants by Degree of Synovial Lymphocytic Inflammation

Inflammatory cells including lymphocytes, mast cells, neutrophils, and eosinophils were scored by presence and degree (None present, Slight/Mild, Moderate, Marked/Band). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
None presentSlight/MildModerateMarked/Band
Fasinumab3532
Non-steroidal Anti-inflammatory Drug (NSAID)2210
Placebo0020

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Number of Participants by Degree of Bony Changes

Microscopic articular features including degree of bony changes were evaluated and scored (Normal, Sclerosis [Lamellar/Mixed], Subarticular Fracture/Collapse). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
NormalSclerosis (Lamellar/Mixed)Subarticular Fracture/Collapse
Fasinumab175
Non-steroidal Anti-inflammatory Drug (NSAID)122
Placebo110

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Number of Participants by Degree of Cartilage Loss

Microscopic articular features including degree of cartilage were evaluated and scored (Superficial Fibrillation, Deep fissuring, Loss to Tide Mark, Loss to Exposed Bone). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
Superficial FibrillationDeep fissuringLoss to Tide MarkLoss to Exposed Bone
Fasinumab2029
Non-steroidal Anti-inflammatory Drug (NSAID)1013
Placebo0101

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Median Time to First Ambulation Postsurgery.

(NCT03974932)
Timeframe: 72 hours

InterventionHours (Median)
Cohort 1 and Cohort 2 (Pooled)20.66
Cohort 3: Group A23.20
Cohort 3: Group B26.72
Cohort 420.58

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Median Time to First Opioid Rescue Medication.

(NCT03974932)
Timeframe: Through 72 hours

InterventionHours (Median)
Cohort 1 and Cohort 2 (Pooled)6.12
Cohort 3: Group A5.63
Cohort 3: Group B9.96
Cohort 412.76

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Percentage of Subjects Unable to Participate in Each Rehabilitation Session Because of Pain.

(NCT03974932)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Cohort 1 and Cohort 2 (Pooled)23
Cohort 3: Group A1
Cohort 3: Group B2
Cohort 43

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Percentage of Subjects Who Are Opioid-free

(NCT03974932)
Timeframe: 72 Hours to Day 11

Interventionparticipants (Number)
Cohort 1 and Cohort 2 (Pooled)25
Cohort 3: Group A4
Cohort 3: Group B3
Cohort 410

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Percentage of Subjects Who Are Opioid-free Through 72 Hours Who Remain Opioid-free Through Day 11.

(NCT03974932)
Timeframe: 72 hours through Day 11

InterventionParticipants (Count of Participants)
Cohort 1 and Cohort 2 (Pooled)9
Cohort 3: Group A1
Cohort 3: Group B0
Cohort 45

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Percentage of Subjects Who do Not Receive an Opioid Prescription at Discharge.

(NCT03974932)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Cohort 1 and Cohort 2 (Pooled)41
Cohort 3: Group A8
Cohort 3: Group B12
Cohort 413

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Percentage of Subjects Who do Not Receive an Opioid Prescription Between Discharge and the Day 11 Visit.

(NCT03974932)
Timeframe: 72 hours through Day 11

InterventionParticipants (Count of Participants)
Cohort 1 and Cohort 2 (Pooled)44
Cohort 3: Group A8
Cohort 3: Group B8
Cohort 417

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1) Pain Control Based on Patient Global Assessment (PGA)."-NCT03974932">

"Percentage of Subjects Achieving a Score of Good or Better (>1) Pain Control Based on Patient Global Assessment (PGA)."

Patient's Global Assessment (PGA) of pain control is a 4-point scale in which subjects rate how well their pain has been controlled (0 = Poor; 1 = Fair; 2 = Good; 3 = Excellent). (NCT03974932)
Timeframe: 24 hours, 48 hours, 72 hours, Day 11

,,,
InterventionParticipants (Count of Participants)
24 Hours48 Hours72 HoursDay 11
Cohort 1 and Cohort 2 (Pooled)60616650
Cohort 3: Group A10111211
Cohort 3: Group B14141511
Cohort 416161815

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Maximum Concentration (Cmax)

(NCT03974932)
Timeframe: 72 hours

,,,
Interventionng/mL (Mean)
BupivacaineMeloxicam
Cohort 1 and Cohort 2 (Pooled)566238
Cohort 3: Group A534247
Cohort 3: Group B742251
Cohort 4851385

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Mean AUC of the NRS of Pain Intensity at Rest (NRS-R).

"Pain intensity scores are assessed using an 11-point Numeric Rating Scale (NRS) (0-10) where 0 represents no pain and 10 represents worst pain. NRS scores are measured at rest." (NCT03974932)
Timeframe: 72 hours

Interventionpain intensity score*hr (Mean)
Cohort 1 and Cohort 2 (Pooled)309.89
Cohort 3: Group A355.20
Cohort 3: Group B311.00
Cohort 4245.00

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Mean Area Under the Curve (AUC) of the Visual Analogue Scale (VAS).

"The Visual Analog Scale (VAS) consists of a straight 10-cm line that represents pain ranging from no pain to pain as bad as it could be. Subjects were asked to mark their current pain level on the line." (NCT03974932)
Timeframe: 12 through 48 hours

Interventionpain intensity score*hr (Mean)
Cohort 1 and Cohort 2 (Pooled)155.57
Cohort 3: Group A185.27
Cohort 3: Group B161.36
Cohort 4126.59

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Time of Occurrence of Maximum Concentration (Tmax)

(NCT03974932)
Timeframe: 72 hours

,,,
Interventionhours (Median)
BupivacaineMeloxicam
Cohort 1 and Cohort 2 (Pooled)21.0547.13
Cohort 3: Group A20.5458.58
Cohort 3: Group B20.1437.17
Cohort 422.4848.58

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Percentage of Subjects Who Are Discharged Home vs to a Skilled Nursing Facility.

Number Analyzed represents Subjects who were discharged home. (NCT03974932)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Cohort 1 and Cohort 2 (Pooled)61
Cohort 3: Group A10
Cohort 3: Group B16
Cohort 420

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Mean Overall Benefit of Analgesia Score (OBAS).

Subjects were questioned about their overall benefit of analgesia. Overall benefit of analgesia score (OBAS) assesses current pain at rest, vomiting, itching, sweating, freezing, dizziness, and overall satisfaction with postoperative pain during the previous 24 hours. To calculate the OBAS score, each of the subscale scores (0=minimum; 4=maximum) are summed for a combined OBAS score. Possible scores could range from 0 to 28 with a lower score indicating greater benefit. (NCT03974932)
Timeframe: 24 hours, 48 hours, 72 hours, Day 11

,,,
InterventionScores on a scale (Mean)
24 Hours48 Hours72 HoursDay 11
Cohort 1 and Cohort 2 (Pooled)6.55.75.15.0
Cohort 3: Group A7.44.94.15.2
Cohort 3: Group B7.65.94.94.9
Cohort 45.95.34.84.9

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Mean Total TSQM-9 Score

The Treatment Satisfaction Questionnaire for Medication (TSQM-9) contains 9 items assessing Effectiveness, Convenience, and Global Satisfaction domains. Responses to items are rated on a 5-point or 7-point rating scale. Scores for each domain are computed by adding the TSQM items in each domain and then transforming the values in to a composite score ranging from 0 to 100, with higher scores representing higher satisfaction. (NCT03974932)
Timeframe: 72 hours through Day 11

,,,
InterventionScores on a scale (Mean)
Global Satisfaction Domain - 72 HoursEffectiveness Doman - 72 HoursConvenience Domain - 72 HoursGlobal Satisfaction Domain - Day 11Effectiveness Doman - Day 11Convenience Domain - Day 11
Cohort 1 and Cohort 2 (Pooled)86.986.490.178.076.390.1
Cohort 3: Group A77.080.284.574.569.486.9
Cohort 3: Group B89.384.093.172.869.480.9
Cohort 486.881.986.982.967.090.6

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Percentage of Subjects Who First Achieve an MPADSS Score ≥9.

Subjects were assessed for readiness for discharge using the Modified Post-Anesthesia Discharge Scoring System (MPADSS) that assesses 5 clinical variables: vital signs, ambulation, nausea/vomiting, pain, and surgical bleeding, each on a 3-point scale of 0, 1, or 2 with 0 being the worst score and 2 being the best score. Subjects with an MPADSS score of 9 or 10 were considered ready for discharge. (NCT03974932)
Timeframe: 2 hours, 4 hours, 6 hours, 8 hours, 12 hours, 24, hours, 36 hours, 48 hours, 60 hours, 72 hours

,,,
InterventionParticipants (Count of Participants)
Through 2 HoursThrough 4 HoursThrough 6 HoursThrough 8 HoursThrough 12 HoursThrough 24 HoursThrough 36 HoursThrough 48 HoursThrough 60 HoursThrough 72 Hours
Cohort 1 and Cohort 2 (Pooled)15162129384552575759
Cohort 3: Group A23667812121213
Cohort 3: Group B225891113131515
Cohort 4037881518191919

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Percentage of Subjects With Severe Pain.

Severe Pain defined as a VAS score ≥7.5 cm. (NCT03974932)
Timeframe: 24 hours, 48 hours, 72 hours

,,,
InterventionParticipants (Count of Participants)
24 Hours48 Hours72 Hours
Cohort 1 and Cohort 2 (Pooled)262923
Cohort 3: Group A455
Cohort 3: Group B555
Cohort 4667

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Mean Total Postoperative Opioid Consumption (in IV Morphine Milligram Equivalents [MME]).

(NCT03974932)
Timeframe: 72 hours

InterventionMME, morphine milligram equivalency (Mean)
Cohort 1 and Cohort 2 (Pooled)26.40
Cohort 3: Group A31.50
Cohort 3: Group B23.40
Cohort 417.62

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Mean AUC of VAS Scores.

"The Visual Analog Scale (VAS) consists of a straight 10-cm line that represents pain ranging from no pain to pain as bad as it could be. Subjects were asked to mark their current pain level on the line." (NCT03974932)
Timeframe: 72 hours

Interventionpain intensity score*hr (Mean)
Cohort 1 and Cohort 2 (Pooled)277.03
Cohort 3: Group A319.81
Cohort 3: Group B276.87
Cohort 4216.18

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Recurrence-free Survival (RFS)

RFS is defined as local/regional invasive recurrence, invasive ipsilateral breast tumor recurrence, distant recurrence, inoperable (meaning no surgery because of progression), and/or death from breast cancer (per standard of care according to physician discretion) or any cause. RFS will be calculated from the time of treatment to event. The median RFS was estimated using standard Kaplan-Meier methods (where NR = not reached). (NCT04081389)
Timeframe: At 3 years

Interventionmonths (Median)
Arm 1: Interferon Alpha-2b at DL 112.0
Arm 2: Interferon Alpha-2b at DL 2NA
Arm 3: Interferon Alpha-2b at DL 311.4
Arm 4: Interferon Alpha-2b at DL 411.5

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Overall Survival (OS)

OS is defined by death from breast cancer, non-breast cancer, unknown, or any other cause and will be calculated from the time of study entry to event. The median OS is estimated using standard Kaplan-Meier methods (where NR = not reached). (NCT04081389)
Timeframe: At 3 years

Interventionmonths (Median)
Arm 1: Interferon Alpha-2b at DL 121.7
Arm 2: Interferon Alpha-2b at DL 2NA
Arm 3: Interferon Alpha-2b at DL 3NA
Arm 4: Interferon Alpha-2b at DL 4NA

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Number of Patients With Dose Limiting Toxicities

"Safety and toxicity will be assessed using the CTEP NCI Common Terminology Criteria for Adverse Events (CTCAE Version 5.0). The resulting dose limiting toxicity (DLT) information is used to identify the appropriate dose level of CKM and paclitaxel for future clinical exploration.~The following events will be considered a DLT:~The event occurs within 3 weeks following 1st dose of combination CKM + paclitaxel therapy and subsequent enrollment for dose-escalation will only proceed after the 3-week period has been completed.~The toxicity has been determined by the investigator to be possibly, probably or definitely related to celecoxib, rintatolimod, interferon-α2b or paclitaxel.~Any death not clearly due to th" (NCT04081389)
Timeframe: Within 21 days of treatment adminstration

InterventionParticipants (Count of Participants)
Arm 1: Interferon Alpha-2b at DL 10
Arm 2: Interferon Alpha-2b at DL 20
Arm 3: Interferon Alpha-2b at DL 30
Arm 4: Interferon Alpha-2b at DL 40

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Number of Patients With Pathological Complete Response (pCR)

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI, where Complete Response (CR) corresponds to the disappearance of all target lesions. (NCT04081389)
Timeframe: Up to 4 week post-treatment (with a range of 7 to 11 weeks).

InterventionParticipants (Count of Participants)
Arm 1: Interferon Alpha-2b at DL 10
Arm 2: Interferon Alpha-2b at DL 21
Arm 3: Interferon Alpha-2b at DL 32
Arm 4: Interferon Alpha-2b at DL 42

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Estimated Blood Loss

milliliters (mL) (NCT04429022)
Timeframe: 0-300 minutes

Interventionmilliliters (Mean)
Prospective Cohort63.50
Historical Control58.46

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Length of Stay in Hours

Length of stay in hours (NCT04429022)
Timeframe: 0- 240 hours

Interventionhours (Mean)
Prospective Cohort12.05
Historical Control35.82

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Number of Patients With Return to the Clinic, Emergency Department Due to Post Operative Pain Within a 2 Week Period

Number of patients with return to the clinic, emergency department due to post operative pain within a 2 week period (NCT04429022)
Timeframe: 0-14 days

InterventionParticipants (Count of Participants)
Prospective Cohort1
Historical Control3

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Operative Time

minutes (NCT04429022)
Timeframe: 0-300 minutes

Interventionminutes (Mean)
Prospective Cohort128.80
Historical Control139.69

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Pain Scores

Subjective, Score 0-10 with 0 being no pain and 10 being severe pain (NCT04429022)
Timeframe: 0-3 hours after surgery

Interventionscore on a scale (Mean)
Prospective Cohort3.82
Historical Control5.13

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Pain Scores

Subjective, Score 0-10 with 0 being no pain and 10 being severe pain (NCT04429022)
Timeframe: 3-24 hours after surgery

Interventionscore on a scale (Mean)
Prospective Cohort1.75
Historical Control5.43

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Total Opioid Pain Medications Required 0-3h Post op in Morphine Milligram Equivalents (MME)

Total opioid pain medications required 0-3h post op in morphine milligram equivalents (MME) (NCT04429022)
Timeframe: 0-3 hours after surgery

Interventionmorphine milligram equivalents (MME) (Mean)
Prospective Cohort2.00
Historical Control5.32

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Total Opioid Pain Medications Required Through 3-24h Post op in MME

Total opioid pain medications required through 3-24h post op in MME (NCT04429022)
Timeframe: 3-24 hours after surgery

Interventionmorphine milligram equivalents (MME) (Mean)
Prospective Cohort.20
Historical Control12.27

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Cmax Of Molybdenum With Coadministration Of Celecoxib

Blood samples were collected for PK analysis of total molybdenum (as a measure of ALXN1840) and plasma ultrafiltrate (PUF) molybdenum. Cmax is reported as ng/mL. (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionng/mL (Mean)
Total MolybdenumPUF Molybdenum
Treatment B373.482.44

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AUCinf Of Molybdenum With Coadministration Of Celecoxib

Blood samples were collected for PK analysis of total molybdenum (as a measure of ALXN1840) and PUF molybdenum. AUCinf is reported as h•ng/mL. (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionh•ng/mL (Mean)
Total MolybdenumPUF Molybdenum
Treatment B209102305

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AUCt Of Molybdenum With Coadministration Of Celecoxib

Blood samples were collected for PK analysis of total molybdenum (as a measure of ALXN1840) and PUF molybdenum. AUCt is reported as h•ng/mL. (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionh•ng/mL (Mean)
Total MolybdenumPUF Molybdenum
Treatment B192401796

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Area Under The Plasma Concentration Versus Time Curve From Time 0 To Infinity (AUCinf) Of Celecoxib With And Without The Coadministration Of ALXN1840

Blood samples were collected for pharmacokinetic (PK) analysis of celecoxib. Area Under The Plasma Concentration Versus Time Curve From Time 0 To Infinity (AUCinf) is reported as h•ng/mL. (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionh•ng/mL (Mean)
Treatment A6743
Treatment B6869

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Area Under The Plasma Concentration Versus Time Curve From Time 0 To The Last Quantifiable Concentration (AUCt) Of Celecoxib With And Without The Coadministration Of ALXN1840

Blood samples were collected for pharmacokinetic (PK) analysis of celecoxib. Area Under The Plasma Concentration Versus Time Curve From Time 0 To The Last Quantifiable Concentration (AUCt) is reported as hours•ng/mL (h•ng/mL). (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionh•ng/mL (Mean)
Treatment A6406
Treatment B6482

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Maximum Observed Plasma Concentration (Cmax) Of Celecoxib With And Without The Coadministration Of ALXN1840

Blood samples were collected for pharmacokinetics (PK) analysis of celecoxib. Cmax is reported as nanograms (ng)/milliliter (mL). (NCT04526197)
Timeframe: Baseline, up to 336 hours post-dose

Interventionng/mL (Mean)
Treatment A637.1
Treatment B567.4

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
ethylene dichloride
ethylene dichloride: RN given refers to 1,2-isomer; structure given in first source. 1,2-dichloroethane : A member of the class of chloroethanes substituted by two chloro groups at positions 1 and 2.		2.0510chloroethaneshepatotoxic agent;
mutagen;
non-polar solvent
2,3-dihydroxybenzoic acid
2,3-dihydroxybenzoic acid: RN given refers to parent cpd. dihydroxybenzoic acid : Any member of the class of hydroxybenzoic acids carrying two phenolic hydroxy groups on the benzene ring and its derivatives.. 2,3-dihydroxybenzoic acid : A dihydroxybenzoic acid that is benzoic acid substituted by hydroxy groups at positions 2 and 3. It occurs naturally in Phyllanthus acidus and in the aquatic fern Salvinia molesta.		2.0110dihydroxybenzoic acidhuman xenobiotic metabolite;
plant metabolite
phosphoserine
Phosphoserine: The phosphoric acid ester of serine.		2.4320non-proteinogenic alpha-amino acid;
O-phosphoamino acid;
serine derivative		human metabolite
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		14.174114amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
aminolevulinic acid
Aminolevulinic Acid: A compound produced from succinyl-CoA and GLYCINE as an intermediate in heme synthesis. It is used as a PHOTOCHEMOTHERAPY for actinic KERATOSIS.. 5-aminolevulinic acid : The simplest delta-amino acid in which the hydrogens at the gamma position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp.		8.85304-oxo monocarboxylic acid;
amino acid zwitterion;
delta-amino acid		antineoplastic agent;
dermatologic drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
ethylene glycol
Ethylene Glycol: A colorless, odorless, viscous dihydroxy alcohol. It has a sweet taste, but is poisonous if ingested. Ethylene glycol is the most important glycol commercially available and is manufactured on a large scale in the United States. It is used as an antifreeze and coolant, in hydraulic fluids, and in the manufacture of low-freezing dynamites and resins.. ethanediol : Any diol that is ethane or substituted ethane carrying two hydroxy groups.. ethylene glycol : A 1,2-glycol compound produced via reaction of ethylene oxide with water.		2.4720ethanediol;
glycol		metabolite;
mouse metabolite;
solvent;
toxin
acetic acid
Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed). acetic acid : A simple monocarboxylic acid containing two carbons.		8.76100monocarboxylic acidantimicrobial food preservative;
Daphnia magna metabolite;
food acidity regulator;
protic solvent
acetamide
acetimidic acid : A carboximidic acid that is acetic acid in which the carbonyl oxygen is replaced by an imino group.		2.0510acetamides;
carboximidic acid;
monocarboxylic acid amide;
N-acylammonia
acetone
methyl ketone : A ketone of formula RC(=O)CH3 (R =/= H).		2.4520ketone body;
methyl ketone;
propanones;
volatile organic compound		EC 3.5.1.4 (amidase) inhibitor;
human metabolite;
polar aprotic solvent
adenine
[no description available]		2.76306-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
adipic acid
adipic acid : An alpha,omega-dicarboxylic acid that is the 1,4-dicarboxy derivative of butane.		7.2110alpha,omega-dicarboxylic acid;
dicarboxylic fatty acid		food acidity regulator;
human xenobiotic metabolite
agmatine
Agmatine: Decarboxylated arginine, isolated from several plant and animal sources, e.g., pollen, ergot, herring sperm, octopus muscle.		2.0410guanidines;
primary amino compound		Escherichia coli metabolite;
mouse metabolite
allantoin
[no description available]		2.0510imidazolidine-2,4-dione;
ureas		Escherichia coli metabolite;
human metabolite;
Saccharomyces cerevisiae metabolite;
vulnerary
curdlan
D-hexose : A hexose that has D-configuration at position 5.		2.4110hexose
ammonium hydroxide
azane : Saturated acyclic nitrogen hydrides having the general formula NnHn+2.		2.0310azane;
gas molecular entity;
mononuclear parent hydride		EC 3.5.1.4 (amidase) inhibitor;
metabolite;
mouse metabolite;
neurotoxin;
NMR chemical shift reference compound;
nucleophilic reagent;
refrigerant
quinacrine
Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.		2.0510acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
benzoic acid
Benzoic Acid: A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.. benzoic acid : A compound comprising a benzene ring core carrying a carboxylic acid substituent.. aromatic carboxylic acid : Any carboxylic acid in which the carboxy group is directly bonded to an aromatic ring.		2.8330benzoic acidsalgal metabolite;
antimicrobial food preservative;
drug allergen;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
human xenobiotic metabolite;
plant metabolite
betaine
glycine betaine : The amino acid betaine derived from glycine.		3.5920amino-acid betaine;
glycine derivative		fundamental metabolite
bromide
Bromides: Salts of hydrobromic acid, HBr, with the bromine atom in the 1- oxidation state. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)		2.4110halide anion;
monoatomic bromine
hydrobromic acid
Hydrobromic Acid: Hydrobromic acid (HBr). A solution of hydrogen bromide gas in water.. hydrobromide : Salts formally resulting from the reaction of hydrobromic acid with an organic base.. hydrogen bromide : A diatomic molecule containing covalently bonded hydrogen and bromine atoms.		2.4920gas molecular entity;
hydrogen halide;
mononuclear parent hydride		mouse metabolite
1-butanol
1-Butanol: A four carbon linear hydrocarbon that has a hydroxy group at position 1.. butan-1-ol : A primary alcohol that is butane in which a hydrogen of one of the methyl groups is substituted by a hydroxy group. It it produced in small amounts in humans by the gut microbes.		2.0510alkyl alcohol;
primary alcohol;
short-chain primary fatty alcohol		human metabolite;
mouse metabolite;
protic solvent
carbamates
[no description available]		3.0140amino-acid anion
carbon monoxide
Carbon Monoxide: Carbon monoxide (CO). A poisonous colorless, odorless, tasteless gas. It combines with hemoglobin to form carboxyhemoglobin, which has no oxygen carrying capacity. The resultant oxygen deprivation causes headache, dizziness, decreased pulse and respiratory rates, unconsciousness, and death. (From Merck Index, 11th ed). carbon monoxide : A one-carbon compound in which the carbon is joined only to a single oxygen. It is a colourless, odourless, tasteless, toxic gas.		2.1310carbon oxide;
gas molecular entity;
one-carbon compound		biomarker;
EC 1.9.3.1 (cytochrome c oxidase) inhibitor;
human metabolite;
ligand;
metabolite;
mitochondrial respiratory-chain inhibitor;
mouse metabolite;
neurotoxin;
neurotransmitter;
P450 inhibitor;
probe;
signalling molecule;
vasodilator agent
carnitine
[no description available]		11.1862amino-acid betainehuman metabolite;
mouse metabolite
methane
Methane: The simplest saturated hydrocarbon. It is a colorless, flammable gas, slightly soluble in water. It is one of the chief constituents of natural gas and is formed in the decomposition of organic matter. (Grant & Hackh's Chemical Dictionary, 5th ed). methane : A one-carbon compound in which the carbon is attached by single bonds to four hydrogen atoms. It is a colourless, odourless, non-toxic but flammable gas (b.p. -161degreeC).		2.7930alkane;
gas molecular entity;
mononuclear parent hydride;
one-carbon compound		bacterial metabolite;
fossil fuel;
greenhouse gas
choline
[no description available]		2.0410cholinesallergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter;
nutrient;
plant metabolite;
Saccharomyces cerevisiae metabolite
citric acid, anhydrous
Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms.		2.0510tricarboxylic acidantimicrobial agent;
chelator;
food acidity regulator;
fundamental metabolite
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		2.7530halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
hydrochloric acid
Hydrochloric Acid: A strong corrosive acid that is commonly used as a laboratory reagent. It is formed by dissolving hydrogen chloride in water. GASTRIC ACID is the hydrochloric acid component of GASTRIC JUICE.. hydrogen chloride : A mononuclear parent hydride consisting of covalently bonded hydrogen and chlorine atoms.		2.9740chlorine molecular entity;
gas molecular entity;
hydrogen halide;
mononuclear parent hydride		mouse metabolite
coumarin
2H-chromen-2-one: coumarin derivative		2.0710coumarinsfluorescent dye;
human metabolite;
plant metabolite
salicylic acid
Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL).		7.7330monohydroxybenzoic acidalgal metabolite;
antifungal agent;
antiinfective agent;
EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor;
keratolytic drug;
plant hormone;
plant metabolite
gallic acid
gallate : A trihydroxybenzoate that is the conjugate base of gallic acid.		7.3110trihydroxybenzoic acidantineoplastic agent;
antioxidant;
apoptosis inducer;
astringent;
cyclooxygenase 2 inhibitor;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
geroprotector;
human xenobiotic metabolite;
plant metabolite
hydrogen sulfide
Hydrogen Sulfide: A flammable, poisonous gas with a characteristic odor of rotten eggs. It is used in the manufacture of chemicals, in metallurgy, and as an analytical reagent. (From Merck Index, 11th ed). hydrogen sulfide : A sulfur hydride consisting of a single sulfur atom bonded to two hydrogen atoms. A highly poisonous, flammable gas with a characteristic odour of rotten eggs, it is often produced by bacterial decomposition of organic matter in the absence of oxygen.. thiol : An organosulfur compound in which a thiol group, -SH, is attached to a carbon atom of any aliphatic or aromatic moiety.		340gas molecular entity;
hydracid;
mononuclear parent hydride;
sulfur hydride		Escherichia coli metabolite;
genotoxin;
metabolite;
signalling molecule;
toxin;
vasodilator agent
4-aminophenol
4-aminophenol: RN given refers to parent cpd. 4-aminophenol : An amino phenol (one of the three possible isomers) which has the single amino substituent located para to the phenolic -OH group.		2.0510aminophenolallergen;
metabolite
bupropion
Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.		9.5470aromatic ketone;
monochlorobenzenes;
secondary amino compound		antidepressant;
environmental contaminant;
xenobiotic
methylmalonic acid
Methylmalonic Acid: A malonic acid derivative which is a vital intermediate in the metabolism of fat and protein. Abnormalities in methylmalonic acid metabolism lead to methylmalonic aciduria. This metabolic disease is attributed to a block in the enzymatic conversion of methylmalonyl CoA to succinyl CoA.. methylmalonic acid : A dicarboxylic acid that is malonic acid in which one of the methylene hydrogens is substituted by a methyl group.		2.0710C4-dicarboxylic acidhuman metabolite
n(g),n(g')-dimethyl-l-arginine
N,N-dimethylarginine: asymmetric dimethylarginine; do not confuse with N,N'-dimethylarginine		2.5720alpha-amino acid
malic acid
malic acid : A 2-hydroxydicarboxylic acid that is succinic acid in which one of the hydrogens attached to a carbon is replaced by a hydroxy group.. 2-hydroxydicarboxylic acid : Any dicarboxylic acid carrying a hydroxy group on the carbon atom at position alpha to the carboxy group.		2.15102-hydroxydicarboxylic acid;
C4-dicarboxylic acid		food acidity regulator;
fundamental metabolite
cyanic acid
[no description available]		2.4920one-carbon compound;
pseudohalogen oxoacid
aminocaproic acid
Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator.		3.8630amino acid zwitterion;
epsilon-amino acid;
omega-amino fatty acid		antifibrinolytic drug;
hematologic agent;
metabolite
creatine
[no description available]		5.2231glycine derivative;
guanidines;
zwitterion		geroprotector;
human metabolite;
mouse metabolite;
neuroprotective agent;
nutraceutical
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		9.562302-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
dimethyl sulfoxide
Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.		2.9640sulfoxide;
volatile organic compound		alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		4.41200aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
hexachlorocyclohexane
Lindane: An organochlorine insecticide made up of greater than 99% gamma-Hexachlorocyclohexane. It has been used as a pediculicide and scabicide, and shown to cause cancer.. beta-hexachlorocyclohexane : The beta-isomer of hexachlorocyclohexane.		2.0510chlorocyclohexane
glycine
[no description available]		3.3160alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
glycerol
Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.		2.520alditol;
triol		algal metabolite;
detergent;
Escherichia coli metabolite;
geroprotector;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
solvent
glycolic acid
glycolic acid: RN given refers to parent cpd. glycolic acid : A 2-hydroxy monocarboxylic acid that is acetic acid where the methyl group has been hydroxylated.		7.41102-hydroxy monocarboxylic acid;
primary alcohol		keratolytic drug;
metabolite
carbonic acid
Carbonic Acid: Carbonic acid (H2C03). The hypothetical acid of carbon dioxide and water. It exists only in the form of its salts (carbonates), acid salts (hydrogen carbonates), amines (carbamic acid), and acid chlorides (carbonyl chloride). (From Grant & Hackh's Chemical Dictionary, 5th ed)		2.4920carbon oxoacid;
chalcocarbonic acid		mouse metabolite
hydrogen cyanide
Hydrogen Cyanide: Hydrogen cyanide (HCN); A toxic liquid or colorless gas. It is found in the smoke of various tobacco products and released by combustion of nitrogen-containing organic materials.. hydrogen cyanide : A one-carbon compound consisting of a methine group triple bonded to a nitrogen atom		2.4920hydracid;
one-carbon compound		Escherichia coli metabolite;
human metabolite;
poison
hydrogen carbonate
Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.. hydrogencarbonate : The carbon oxoanion resulting from the removal of a proton from carbonic acid.		210carbon oxoanioncofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
dalteparin
Dalteparin: A low-molecular-weight fragment of heparin, prepared by nitrous acid depolymerization of porcine mucosal heparin. The mean molecular weight is 4000-6000 daltons. It is used therapeutically as an antithrombotic agent. (From Merck Index, 11th ed)		2.4220
histamine
[no description available]		3.2860aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
thiocyanic acid
thiocyanic acid : A hydracid that is cyanic acid in which the oxygen is replaced by a sulfur atom.		2.4920hydracid;
one-carbon compound;
organosulfur compound		Escherichia coli metabolite
hydrogen
Hydrogen: The first chemical element in the periodic table with atomic symbol H, and atomic number 1. Protium (atomic weight 1) is by far the most common hydrogen isotope. Hydrogen also exists as the stable isotope DEUTERIUM (atomic weight 2) and the radioactive isotope TRITIUM (atomic weight 3). Hydrogen forms into a diatomic molecule at room temperature and appears as a highly flammable colorless and odorless gas.. dihydrogen : An elemental molecule consisting of two hydrogens joined by a single bond.		3.2350elemental hydrogen;
elemental molecule;
gas molecular entity		antioxidant;
electron donor;
food packaging gas;
fuel;
human metabolite
hydroquinone
[no description available]		2.0510benzenediol;
hydroquinones		antioxidant;
carcinogenic agent;
cofactor;
Escherichia coli metabolite;
human xenobiotic metabolite;
mouse metabolite;
skin lightening agent
indole
[no description available]		2.3110indole;
polycyclic heteroarene		Escherichia coli metabolite
indoleacetic acid
indoleacetic acid: RN given refers to unlabeled parent cpd; structure in Merck Index, 9th ed, #4841. auxin : Any of a group of compounds, both naturally occurring and synthetic, that induce cell elongation in plant stems (from Greek alphaupsilonxialphanuomega, "to grow").. indole-3-acetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens has been replaced by a 1H-indol-3-yl group.		3.2710indole-3-acetic acids;
monocarboxylic acid		auxin;
human metabolite;
mouse metabolite;
plant hormone;
plant metabolite
dihydroxyphenylalanine
Dihydroxyphenylalanine: A beta-hydroxylated derivative of phenylalanine. The D-form of dihydroxyphenylalanine has less physiologic activity than the L-form and is commonly used experimentally to determine whether the pharmacological effects of LEVODOPA are stereospecific.. dopa : A hydroxyphenylalanine carrying hydroxy substituents at positions 3 and 4 of the benzene ring.		2.1710hydroxyphenylalanine;
non-proteinogenic alpha-amino acid;
tyrosine derivative		human metabolite
kynurenine
Kynurenine: A metabolite of the essential amino acid tryptophan metabolized via the tryptophan-kynurenine pathway.. kynurenine : A ketone that is alanine in which one of the methyl hydrogens is substituted by a 2-aminobenzoyl group.		4.8621aromatic ketone;
non-proteinogenic alpha-amino acid;
substituted aniline		human metabolite
thioctic acid
Thioctic Acid: An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.		3.4111dithiolanes;
heterocyclic fatty acid;
thia fatty acid		fundamental metabolite;
geroprotector
inositol
Inositol: An isomer of glucose that has traditionally been considered to be a B vitamin although it has an uncertain status as a vitamin and a deficiency syndrome has not been identified in man. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1379) Inositol phospholipids are important in signal transduction.. inositol : Any cyclohexane-1,2,3,4,5,6-hexol.. 1D-chiro-inositol : Belonging to the inositol family of compounds, D-chiro-inositol (DCI) is an isomer of glucose. It is an important secondary messenger in insulin signal transduction.. muco-inositol : An inositol that is cyclohexane-1,2,3,4,5,6-hexol having a (1R,2R,3r,4R,5S,6r)-configuration.		2.4620cyclitol;
hexol
melatonin
[no description available]		3.4670acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
croton oil
[no description available]		2.4420N-acyl-hexosamine
nickel
Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.. nickel ion : A nickel atom having a net electric charge.. nickel atom : Chemical element (nickel group element atom) with atomic number 28.		2.4520metal allergen;
nickel group element atom		epitope;
micronutrient
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		3.4870pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		3.8630pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
nitrates
Nitrates: Inorganic or organic salts and esters of nitric acid. These compounds contain the NO3- radical.		3.6590monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species
nitric acid
Nitric Acid: Nitric acid (HNO3). A colorless liquid that is used in the manufacture of inorganic and organic nitrates and nitro compounds for fertilizers, dye intermediates, explosives, and many different organic chemicals. Continued exposure to vapor may cause chronic bronchitis; chemical pneumonitis may occur. (From Merck Index, 11th ed). nitric acid : A nitrogen oxoacid of formula HNO3 in which the nitrogen atom is bonded to a hydroxy group and by equivalent bonds to the remaining two oxygen atoms.		2.0610nitrogen oxoacidprotic solvent;
reagent
nitrites
Nitrites: Salts of nitrous acid or compounds containing the group NO2-. The inorganic nitrites of the type MNO2 (where M=metal) are all insoluble, except the alkali nitrites. The organic nitrites may be isomeric, but not identical with the corresponding nitro compounds. (Grant & Hackh's Chemical Dictionary, 5th ed)		3.470monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species		human metabolite
hydroxide ion
[no description available]		2.1110oxygen hydridemouse metabolite
orotic acid
Orotic Acid: An intermediate product in PYRIMIDINE synthesis which plays a role in chemical conversions between DIHYDROFOLATE and TETRAHYDROFOLATE.. orotic acid : A pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6.		2.0510pyrimidinemonocarboxylic acidEscherichia coli metabolite;
metabolite;
mouse metabolite
4-aminobenzoic acid
4-Aminobenzoic Acid: An aminobenzoic acid isomer that combines with pteridine and GLUTAMIC ACID to form FOLIC ACID. The fact that 4-aminobenzoic acid absorbs light throughout the UVB range has also resulted in its use as an ingredient in SUNSCREENS.. 4-ammoniobenzoate : A zwitterion obtained by transfer of a proton from the carboxy to the amino group of 4-aminobenzoic acid.. 4-aminobenzoic acid : An aminobenzoic acid in which the amino group is para to the carboxy group.		2.5420aminobenzoic acid;
aromatic amino-acid zwitterion		allergen;
Escherichia coli metabolite;
plant metabolite
4-nitrophenol
4-nitrophenol: RN given refers to parent cpd. mononitrophenol : A nitrophenol that is phenol carrying a single nitro substituent at unspecified position.. 4-nitrophenol : A member of the class of 4-nitrophenols that is phenol in which the hydrogen that is para to the hydroxy group has been replaced by a nitro group.		2.15104-nitrophenolshuman xenobiotic metabolite;
mouse metabolite
palmitic acid
Palmitic Acid: A common saturated fatty acid found in fats and waxes including olive oil, palm oil, and body lipids.. hexadecanoic acid : A straight-chain, sixteen-carbon, saturated long-chain fatty acid.		2.0810long-chain fatty acid;
straight-chain saturated fatty acid		algal metabolite;
Daphnia magna metabolite;
EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor;
plant metabolite
phenol
[no description available]		2.7430phenolsantiseptic drug;
disinfectant;
human xenobiotic metabolite;
mouse metabolite
phenylacetic acid
phenylacetic acid : A monocarboxylic acid that is toluene in which one of the hydrogens of the methyl group has been replaced by a carboxy group.		2.0510benzenes;
monocarboxylic acid;
phenylacetic acids		allergen;
Aspergillus metabolite;
auxin;
EC 6.4.1.1 (pyruvate carboxylase) inhibitor;
Escherichia coli metabolite;
human metabolite;
plant growth retardant;
plant metabolite;
Saccharomyces cerevisiae metabolite;
toxin
phosphorylcholine
Phosphorylcholine: Calcium and magnesium salts used therapeutically in hepatobiliary dysfunction.. phosphocholine : The phosphate of choline; and the parent compound of the phosphocholine family.		2.4920phosphocholinesallergen;
epitope;
hapten;
human metabolite;
mouse metabolite
picolinic acid
picolinic acid: iron-chelating agent that inhibits DNA synthesis; may interfere with iron-dependent production of stable free organic radical which is essential for ribonucleotide reductase formation of deoxyribonucleotides; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7206. picolinic acid : A pyridinemonocarboxylic acid in which the carboxy group is located at position 2. It is an intermediate in the metabolism of tryptophan.		2.110pyridinemonocarboxylic acidhuman metabolite;
MALDI matrix material
propylene glycol
Propylene Glycol: A clear, colorless, viscous organic solvent and diluent used in pharmaceutical preparations.. propane-1,2-diol : The simplest member of the class of propane-1,2-diols, consisting of propane in which a hydrogen at position 1 and a hydrogen at position 2 are substituted by hydroxy groups. A colourless, viscous, hygroscopic, low-melting (-59degreeC) and high-boiling (188degreeC) liquid with low toxicity, it is used as a solvent, emulsifying agent, and antifreeze.		2.5320glycol;
propane-1,2-diols		allergen;
human xenobiotic metabolite;
mouse metabolite;
protic solvent
propionic acid
propionic acid : A short-chain saturated fatty acid comprising ethane attached to the carbon of a carboxy group.		2.0410saturated fatty acid;
short-chain fatty acid		antifungal drug
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		4.0940monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
pyrazole
1H-pyrazole : The 1H-tautomer of pyrazole.		3.2450pyrazole
pyridine
azine : An organonitrogen compound of general structure RCH=N-N=CHR or RR'C=N-N=CRR'.		2.0410azaarene;
mancude organic heteromonocyclic parent;
monocyclic heteroarene;
pyridines		environmental contaminant;
NMR chemical shift reference compound
pyridoxal phosphate
Pyridoxal Phosphate: This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).. pyridoxal 5'-phosphate : The monophosphate ester obtained by condensation of phosphoric acid with the primary hydroxy group of pyridoxal.		4.7821methylpyridines;
monohydroxypyridine;
pyridinecarbaldehyde;
vitamin B6 phosphate		coenzyme;
cofactor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
pyridoxine
4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms).		5.1750hydroxymethylpyridine;
methylpyridines;
monohydroxypyridine;
vitamin B6		cofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
quinolinic acid
Quinolinic Acid: A metabolite of tryptophan with a possible role in neurodegenerative disorders. Elevated CSF levels of quinolinic acid are correlated with the severity of neuropsychological deficits in patients who have AIDS.. pyridinedicarboxylic acid : Any member of the class of pyridines carrying two carboxy groups.. quinolinic acid : A pyridinedicarboxylic acid that is pyridine substituted by carboxy groups at positions 2 and 3. It is a metabolite of tryptophan.		2.4820pyridinedicarboxylic acidEscherichia coli metabolite;
human metabolite;
mouse metabolite;
NMDA receptor agonist
sulfurous acid
[no description available]		2.4920sulfur oxoacid
succinic acid
Succinic Acid: A water-soluble, colorless crystal with an acid taste that is used as a chemical intermediate, in medicine, the manufacture of lacquers, and to make perfume esters. It is also used in foods as a sequestrant, buffer, and a neutralizing agent. (Hawley's Condensed Chemical Dictionary, 12th ed, p1099; McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed, p1851). succinic acid : An alpha,omega-dicarboxylic acid resulting from the formal oxidation of each of the terminal methyl groups of butane to the corresponding carboxy group. It is an intermediate metabolite in the citric acid cycle.		2.4820alpha,omega-dicarboxylic acid;
C4-dicarboxylic acid		anti-ulcer drug;
fundamental metabolite;
micronutrient;
nutraceutical;
radiation protective agent
sulfuric acid
sulfuric acid : A sulfur oxoacid that consists of two oxo and two hydroxy groups joined covalently to a central sulfur atom.		2.4920sulfur oxoacidcatalyst
taurine
[no description available]		2.0810amino sulfonic acid;
zwitterion		antioxidant;
Escherichia coli metabolite;
glycine receptor agonist;
human metabolite;
mouse metabolite;
nutrient;
radical scavenger;
Saccharomyces cerevisiae metabolite
thiamine
thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively.		3.8630primary alcohol;
vitamin B1		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
toluene
methylbenzene : Any alkylbenzene that is benzene substituted with one or more methyl groups.		2.0510methylbenzene;
toluenes;
volatile organic compound		cholinergic antagonist;
fuel additive;
neurotoxin;
non-polar solvent
uracil
2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder		10.4653pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		2.4620uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		3.4370isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
catechin
[no description available]		2.0510hydroxyflavan
normetanephrine
Normetanephrine: A methylated metabolite of norepinephrine that is excreted in the urine and found in certain tissues. It is a marker for tumors.		2.0410catecholamine
menthol
Menthol: A monoterpene cyclohexanol produced from mint oils.		2.0510p-menthane monoterpenoid;
secondary alcohol		volatile oil component
5,7-Dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromen-3-yl 3,4,5-trihydroxybenzoate
[no description available]		3.3110catechin
1,2-dimethylhydrazine
1,2-Dimethylhydrazine: A DNA alkylating agent that has been shown to be a potent carcinogen and is widely used to induce colon tumors in experimental animals.. 1,2-dimethylhydrazine : A member of the class of hydrazines that is hydrazine in which one of the hydrogens attached to each nitrogen is replaced by a methyl group. A powerful DNA alkylating agent and carcinogen, it is used to induce colon cancer in laboratory rats and mice.		9.03130hydrazinesalkylating agent;
carcinogenic agent
1-(1-naphthyl)piperazine
1-(1-naphthyl)piperazine: serotonin agonist; structure given in first source		3.1210N-arylpiperazine
pk 11195
PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine		3.8621aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes		antineoplastic agent
1-(3-chlorophenyl)piperazine
1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.		2.0810monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
1-anilino-8-naphthalenesulfonate
1-anilino-8-naphthalenesulfonate: RN given refers to parent cpd. 8-anilinonaphthalene-1-sulfonic acid : A naphthalenesulfonic acid that is naphthalene-1-sulfonic acid substituted by a phenylamino group at position 8.		2.0510aminonaphthalene;
naphthalenesulfonic acid		fluorescent probe
pd 173074
[no description available]		2.0810aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist
n-(3-(aminomethyl)benzyl)acetamidine
N-(3-(aminomethyl)benzyl)acetamidine: structure in first source. N-[3-(aminomethyl)benzyl]acetamidine : An aralkylamine that is Nbenzylacetamidine substituted at position 3 on the benzene ring by an aminomethyl group. An inhibitor of nitric oxide synthase.		2.4120aralkylamine;
carboxamidine;
primary amino compound		angiogenesis inhibitor;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
geroprotector
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one: structure given in first source; inhibits guanylyl cyclase. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one : A member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group.		2.0310oxadiazoloquinoxalineEC 4.6.1.2 (guanylate cyclase) inhibitor
hoe 33342
BXI-72: structure in first source		2.4620bibenzimidazole;
N-methylpiperazine		fluorochrome
2,4,6-tribromophenol
[no description available]		2.0110bromophenolenvironmental contaminant;
fungicide;
marine metabolite
2,4-dinitrophenol
2,4-Dinitrophenol: A toxic dye, chemically related to trinitrophenol (picric acid), used in biochemical studies of oxidative processes where it uncouples oxidative phosphorylation. It is also used as a metabolic stimulant. (Stedman, 26th ed). dinitrophenol : Members of the class of nitrophenol carrying two nitro substituents.. 2,4-dinitrophenol : A dinitrophenol having the nitro groups at the 2- and 4-positions.		2.0510dinitrophenolallergen;
antiseptic drug;
bacterial xenobiotic metabolite;
geroprotector;
oxidative phosphorylation inhibitor
2-aminoethoxydiphenyl borate
2-aminoethoxydiphenyl borate: is a novel membrane-penetrable modulator and transient receptor potential channel blocker; structure in first source; do not confuse with 2-APB cpd. 2-aminoethoxydiphenylborane : An organoboron compound that is diphenylborane in which the borane hydrogen is replaced by a 2-aminoethoxy group.		3.6920organoboron compound;
primary amino compound		calcium channel blocker;
IP3 receptor antagonist;
potassium channel opener
zopolrestat
zopolrestat: structure given in first source		3.3110
chlorocresol
chlorocresol: injections for relief of intractable pain; RN given refers to parent cpd. 4-chloro-m-cresol : A hydroxytoluene that is 3-methylphenol which is substituted by a chlorine at position 4. A ryanodine receptor agonist.		3.3510hydroxytoluene;
monochlorobenzenes		antimicrobial agent;
disinfectant;
ryanodine receptor agonist
4-nonylphenol
4-nonylphenol: structure in first source; see also record for nonylphenol. 4-nonylphenol : A member of the class of phenols that is phenol which is para-substituted with a nonyl group.		3.3510phenolsenvironmental contaminant
phenytoin
[no description available]		7.38131imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
7-nitroindazole
7-nitroindazole: an inhibitor of nitric oxide synthase; exhibits anti-nociceptive activity without increasing blood pressure		2.4620
tacrine
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.		5.0870acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor
aa 861
2,3,5-trimethyl-6-(12-hydroxy-5,10-dodecadiynyl)-1,4-benzoquinone: structure given in first source. docebenone : A member of the class of benzoquinones that is p-benzoquinone in which the hydrogens are substituted by three methyl groups and a 12-hydroxydodeca-5,10-diyn-1-yl group.		3.15501,4-benzoquinones;
acetylenic compound;
primary alcohol		EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor
abt 702
[no description available]		2.0810bipyridines
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		4.1140aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
acemetacin
acemetacin : A carboxylic ester that is the carboxymethyl ester of indometacin. A non-steroidal anti-inflammatory drug, it is used in the treatment of rheumatoid arthritis, osteoarthritis, and low back pain, as well as for postoperative pain and inflammation. Its activity is due to both acemetacin and its major metabolite, indometacin.		8.8221carboxylic ester;
indol-3-yl carboxylic acid;
monocarboxylic acid;
monochlorobenzenes;
N-acylindole		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		17.7111948acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		8.61600monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
acetohexamide
Acetohexamide: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.. acetohexamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is replaced by a p-acetylphenylsulfonyl group, while a hydrogen attached to the other nitrogen is replaced by a cyclohexyl group.		2.4620acetophenones;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		3.8730acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
acridone
acridone : A member of the class of acridines that is 9,10-dihydroacridine substituted by an oxo group at position 9.		2.0810acridines;
cyclic ketone
ag-1296
6,7-dimethoxy-3-phenylquinoxaline: ATP-competitive inhibitor of receptor kinase		2.0310quinoxaline derivative
alaproclate
alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer		3.2310alpha-amino acid ester
albendazole
[no description available]		4.0940aryl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
albuterol
Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).		4.0840phenols;
phenylethanolamines;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
environmental contaminant;
xenobiotic
alendronate
alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.		3.57201,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
alfuzosin
alfuzosin: structure given in first source		3.5920monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
alosetron
alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.		3.5520imidazoles;
pyridoindole		antiemetic;
gastrointestinal drug;
serotonergic antagonist
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.6820organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		2.0810secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
altretamine
Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.		3.5920triamino-1,3,5-triazine
am 251
AM 251: an analog of SR141716A; structure given in first source. AM-251 : A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor.		3.0140amidopiperidine;
carbohydrazide;
dichlorobenzene;
organoiodine compound;
pyrazoles		antidepressant;
antineoplastic agent;
apoptosis inducer;
CB1 receptor antagonist
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		4.7750adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
ambenonium
ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens.		3.2310quaternary ammonium ionEC 3.1.1.8 (cholinesterase) inhibitor
ambroxol
Ambroxol: A metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride.		2.0510aromatic amine
amfenac
amfenac: RN given refers to parent cpd; structure. amfenac : An oxo monocarboxylic acid that is benzophenone in which one of the phenyl groups is substituted by an amino group and a carboxymethyl group at position 2 and 3, respectively. The corresponding carboxamide, nepafenac, is a prodrug of amfenac and is used for the treatment of pain and inflammation following cataract surgery.		2.4620amino acid;
benzophenones;
oxo monocarboxylic acid;
primary amino compound;
substituted aniline		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
diatrizoic acid
Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.		3.6120acetamides;
benzoic acids;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
amifostine anhydrous
Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy.		3.2310diamine;
organic thiophosphate		antioxidant;
prodrug;
radiation protective agent
aminoglutethimide
Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.		2.9740dicarboximide;
piperidones;
substituted aniline		adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
pimagedine
pimagedine: diamine oxidase & nitric oxide synthase inhibitor; an advanced glycosylation end product inhibitor; used in the treatment of diabetic complications; structure. aminoguanidine : A one-carbon compound whose unique structure renders it capable of acting as a derivative of hydrazine, guanidine or formamide.		2.9640guanidines;
one-carbon compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
EC 1.4.3.4 (monoamine oxidase) inhibitor
p-aminohippuric acid
p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow.		4.7750N-acylglycineDaphnia magna metabolite
ampyrone
Ampyrone: A metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.		2.110primary amino compound;
pyrazolone		antipyretic;
antirheumatic drug;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
marine xenobiotic metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
theophylline
[no description available]		4.4260dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		4.57701-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
dan 2163
[no description available]		6.0932aromatic amide;
aromatic amine;
benzamides;
pyrrolidines;
sulfone		environmental contaminant;
second generation antipsychotic;
xenobiotic
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		6.6791carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amlexanox
amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position.		2.0810monocarboxylic acid;
pyridochromene		anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		6.17150dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
amobarbital
Amobarbital: A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565). amobarbital : A member of the class of barbiturates that is pyrimidine-2,4,6(1H,3H,5H)-trione substituted by a 3-methylbutyl and an ethyl group at position 5. Amobarbital has been shown to exhibit sedative and hypnotic properties.		2.0510barbiturates
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		2.0610aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		4.140dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.9740acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
anastrozole
[no description available]		5.0770nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
anethole trithione
Anethole Trithione: Choleretic used to allay dry mouth and constipation due to tranquilizers.		2.0510methoxybenzenes
anthralin
Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9.		2.4720anthracenesantipsoriatic
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		4.5551pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
n'-(3-aminopropyl)homospermidine
[no description available]		1.9910
acetovanillone
apocynin : An aromatic ketone that is 1-phenylethanone substituted by a hydroxy group at position 4 and a methoxy group at position 3.		2.0810acetophenones;
aromatic ketone;
methyl ketone		antirheumatic drug;
EC 1.6.3.1. [NAD(P)H oxidase (H2O2-forming)] inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug;
plant metabolite
arcaine
arcaine: RN given refers to parent cpd; structure. 1,4-diguanidinobutane : A guanidine derivative consisting of butane having guanidino groups at the 1- and 4-positions.		2.0410guanidines
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		18.8722237benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		3.1650benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		11.0481ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
atrazine
[no description available]		7.1710chloro-1,3,5-triazine;
diamino-1,3,5-triazine		environmental contaminant;
herbicide;
xenobiotic
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		4.2650aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
baclofen
[no description available]		4.0840amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
barbital
5,5-diethylbarbituric acid : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by two ethyl groups. Formerly used as a hypnotic (sleeping aid).		2.0510barbituratesdrug allergen
bendazac
bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts.		3.5920indazoles;
monocarboxylic acid		non-steroidal anti-inflammatory drug;
radical scavenger
bendroflumethiazide
Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group.		3.2310benzothiadiazine;
sulfonamide		antihypertensive agent;
diuretic
benzbromarone
Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.		4.55701-benzofurans;
aromatic ketone		uricosuric drug
benzo(a)pyrene
Benzo(a)pyrene: A potent mutagen and carcinogen. It is a public health concern because of its possible effects on industrial workers, as an environmental pollutant, an as a component of tobacco smoke.. benzo[a]pyrene : An ortho- and peri-fused polycyclic arene consisting of five fused benzene rings.		7.4720ortho- and peri-fused polycyclic arenecarcinogenic agent;
mouse metabolite
benzocaine
Benzocaine: A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.. dextran sulfate sodium : An organic sodium salt of dextran sulfate. It induces colitis in mice.. benzocaine : A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.		2.0810benzoate ester;
substituted aniline		allergen;
antipruritic drug;
sensitiser;
topical anaesthetic
benzyl benzoate
benzyl benzoate: structure; acarosan, a moist powder composed of wetted cellulose and benzyl benzoate, is used on carpets as an acaricide. benzyl benzoate : A benzoate ester obtained by the formal condensation of benzoic acid with benzyl alcohol. It has been isolated from the plant species of the genus Polyalthia.		2.0810benzoate ester;
benzyl ester		acaricide;
plant metabolite;
scabicide
berberine
[no description available]		2.0710alkaloid antibiotic;
berberine alkaloid;
botanical anti-fungal agent;
organic heteropentacyclic compound		antilipemic drug;
antineoplastic agent;
antioxidant;
EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor;
EC 1.21.3.3 (reticuline oxidase) inhibitor;
EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
hypoglycemic agent;
metabolite;
potassium channel blocker
betahistine
Betahistine: A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.. betahistine : An aminoalkylpyridine that is pyridine substituted by a 2-(methylamino)ethyl group at position 2. It acts as a histamine agonist and a vasodilator, and is thought to improve the microcirculation of the labyrinth, resulting in reduced endolymphatic pressure. It is used (generally as the hydrochloride or mesylate salt) to reduce the symptoms of vertigo, tinnitus, and hearing loss associated with Meniere's disease.		2.0510aminoalkylpyridine;
secondary amino compound		H1-receptor agonist;
vasodilator agent
betaxolol
[no description available]		3.2310propanolamineantihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bethanechol
Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention.		3.2310carbamate ester;
quaternary ammonium ion		muscarinic agonist
2,5-di-tert-butylhydroquinone
2,5-di-tert-butylbenzene-1,4-diol : A member of the class of hydroquinones that is benzene-1,4-diol substituted by tert-butyl groups at position 2 and 5.		3.3510hydroquinones
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		4.4260(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
bay h 4502
bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1.		2.4720biphenyls;
imidazoles
biperiden
Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease.		3.2310piperidines;
tertiary alcohol;
tertiary amino compound		antidote to sarin poisoning;
antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist;
parasympatholytic
bisacodyl
Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)		3.6120diarylmethane
bisbenzimidazole
Bisbenzimidazole: A benzimidazole antifilarial agent; it is fluorescent when it binds to certain nucleotides in DNA, thus providing a tool for the study of DNA replication; it also interferes with mitosis.		2.0410bibenzimidazole;
N-methylpiperazine		anthelminthic drug;
fluorochrome
bisoprolol
Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.		3.5920secondary alcohol;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bithionol
Bithionol: Halogenated anti-infective agent that is used against trematode and cestode infestations.. bithionol : An aryl sulfide that is diphenyl sulfide in which each phenyl group is substituted at position 2 by hydroxy and at positions 3 and 5 by chlorine. A fungicide and anthelmintic, it was used in various topical drug products for the treatment of liver flukes, but withdrawn after being shown to be a potent photosensitizer with the potential to cause serious skin disorders.		2.0510aryl sulfide;
bridged diphenyl antifungal drug;
bridged diphenyl fungicide;
dichlorobenzene;
organochlorine pesticide;
polyphenol		antifungal agrochemical;
antiplatyhelmintic drug
bromhexine
Bromhexine: A mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p744). bromhexine : A substituted aniline that is 2,4-dibromoaniline which is substituted at position 6 by a [cyclohexyl(methyl)amino]methyl group. It is used (as the monohydrochloride salt) as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum).		2.0810organobromine compound;
substituted aniline;
tertiary amino compound		mucolytic
bromopride
bromopride: RN given refers to parent cpd; structure		2.0810benzamides
bromisovalum
Bromisovalum: A sedative and mild hypnotic with potentially toxic effects.. bromisoval : A racemate comprising equimolar amounts of (R)- and (S)-bromisoval. It was previously used for its hypnotic and sedative properties but the use of bromides is now deprecated due to the possibility of the toxic accumulation of bromine in the body.. 2-bromo-N-carbamoyl-3-methylbutanamide : An N-acylurea that is urea in which one of the hydrogens is replaced by a 2-bromo-3-methybutanoyl group.		2.0510N-acylurea;
organobromine compound
bronopol
[no description available]		2.0810nitro compound
brotizolam
brotizolam: structure		2.0510organic molecular entity
bumetanide
[no description available]		4.7850amino acid;
benzoic acids;
sulfonamide		diuretic;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
bupivacaine
Bupivacaine: A widely used local anesthetic agent.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline.. bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic.		8.34117aromatic amide;
piperidinecarboxamide;
tertiary amino compound
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		4.4260azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
busulfan
[no description available]		4.2750methanesulfonate esteralkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent
secbutabarbital
secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital		3.2310barbiturates
butalbital
butalbital: management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol; RN given refers to parent cpd. butalbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by an allyl group and an isobutyl group. Frequently combined with other medicines, such as aspirin, paracetamol and codeine, it is used for treatment of pain and headache.		2.0510barbituratesanalgesic;
sedative
caffeine
[no description available]		11.34111purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		5.95130aromatic ether;
nitrile;
polyether;
tertiary amino compound
candesartan cilexetil
candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects		2.4620biphenyls
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		9.460benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		4.96110dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carbinoxamine
carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease.		3.2310monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist
carisoprodol
Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.		3.8630carbamate estermuscle relaxant
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.7630N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
carprofen
carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.		2.7930carbazoles;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
photosensitizing agent
carvedilol
[no description available]		4.3150carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.1710hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
cefuroxime
Cefuroxime: Broad-spectrum cephalosporin antibiotic resistant to beta-lactamase. It has been proposed for infections with gram-negative and gram-positive organisms, GONORRHEA, and HAEMOPHILUS.. cefuroxime : A 3-(carbamoyloxymethyl)cephalosporin compound having a 7-(2Z)-2-(furan-2-yl)-2-(methoxyimino)acetamido side chain.		2.0710carbamate ester;
cephalosporin
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		5.2560ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
cgp 37157
CGP 37157: benzothiazepine derivative of clonazepam; inhibits the in vitro activity of mitochondrial sodium-calcium exchange		3.3510benzothiazepine
chelerythrine
chelerythrine : A benzophenanthridine alkaloid isolated from the root of Zanthoxylum simulans, Chelidonium majus L., and other Papaveraceae.		3.930benzophenanthridine alkaloid;
organic cation		antibacterial agent;
antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor
chloral hydrate
[no description available]		2.0510aldehyde hydrate;
ethanediol;
organochlorine compound		general anaesthetic;
mouse metabolite;
sedative;
xenobiotic
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		4.0940aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chlorcyclizine
chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness		3.2310diarylmethane
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		3.8730benzodiazepine
chlormezanone
Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.		3.59201,3-thiazine;
lactam;
monochlorobenzenes;
sulfone		antipsychotic agent;
anxiolytic drug;
muscle relaxant
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		4.87100aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
chlorothiazide
Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension.		3.6620benzothiadiazineantihypertensive agent;
diuretic
chloroxylenol
chloroxylenol: topical antiseptic; RN given refers to parent cpd; structure. 4-chloro-3,5-dimethylphenol : A member of the class of phenols that is 3,5-xylenol which is substituted at position 4 by chlorine. It is bactericidal against most Gram-positive bacteria but less effective against Staphylococci and Gram-negative bacteria, and often inactive against Pseudomonas species. It is ineffective against bacterial spores.		2.0510monochlorobenzenes;
phenols		antiseptic drug;
disinfectant;
molluscicide
chlorphenesin carbamate
[no description available]		2.0810carbamate ester;
monochlorobenzenes;
secondary alcohol		muscle relaxant
chlorpheniramine
Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.		3.8730monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		5.46110organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
chlorpropamide
Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.		4.0940monochlorobenzenes;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
chlorthalidone
Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.		3.6120isoindoles;
monochlorobenzenes;
sulfonamide
chlorzoxazone
Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.		4.55701,3-benzoxazoles;
heteroaryl hydroxy compound;
organochlorine compound		muscle relaxant;
sedative
cifenline
[no description available]		2.0810diarylmethane
ciclopirox
[no description available]		2.4720cyclic hydroxamic acid;
hydroxypyridone antifungal drug;
pyridone		antibacterial agent;
antiseborrheic
ciglitazone
ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.		2.9540aromatic ether;
thiazolidinone		antineoplastic agent;
insulin-sensitizing drug
cilostazol
[no description available]		8.9230lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		7.65142aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
cinoxacin
Cinoxacin: Synthetic antimicrobial related to OXOLINIC ACID and NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.. cinoxacin : A member of the class of cinnolines that is 6,7-methylenedioxycinnolin-4(1H)-one bearing an ethyl group at position 1 and a carboxylic acid group at position 3. An analogue of oxolinic acid, it has similar antibacterial actions. It was formerly used for the treatment of urinary tract infections.		2.0510cinnolines;
oxacycle;
oxo carboxylic acid		antibacterial drug;
antiinfective agent
ciprofibrate
[no description available]		2.9740cyclopropanes;
monocarboxylic acid;
organochlorine compound		antilipemic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		7.15101aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
cisapride
Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.		4.5151benzamides
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		8.941142-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
clenbuterol
Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.. clenbuterol : A substituted aniline that is 2,6-dichloroaniline in which the hydrogen at position 4 has been replaced by a 2-(tert-butylamino)-1-hydroxyethyl group.		2.0310amino alcohol;
dichlorobenzene;
ethanolamines;
primary arylamine;
secondary amino compound;
substituted aniline		beta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
clioquinol
Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease.		2.4720monohydroxyquinoline;
organochlorine compound;
organoiodine compound		antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antiprotozoal drug;
chelator;
copper chelator
clobazam
Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.		2.47201,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		2.7630monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		4.4160aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clomiphene
[no description available]		4.0940tertiary amineestrogen antagonist;
estrogen receptor modulator
clomipramine
Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.		4.2750dibenzoazepineanticoronaviral agent;
antidepressant;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
serotonergic antagonist;
serotonergic drug;
serotonin uptake inhibitor
clonazepam
Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.		3.23101,4-benzodiazepinone;
monochlorobenzenes		anticonvulsant;
anxiolytic drug;
GABA modulator
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		5.7861clonidine;
imidazoline
4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide
[no description available]		2.0810sulfonamide
chlorazepate
clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.		3.23101,4-benzodiazepinoneanticonvulsant;
anxiolytic drug;
GABA modulator;
prodrug
clotiazepam
clotiazepam: was heading 1975-94 (see under AZEPINES 1978-90; was Y 6047 see under AZEPINES 1975-77); Y 6047 was see CLOTIAZEPAM 1978-94; use AZEPINES to search CLOTIAZEPAM 1975-94; thienodiazepine derivative with actions similar to those of benzodiazepines		2.0510organic molecular entity
clotrimazole
[no description available]		5.2890conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
cromolyn
cromoglycic acid : A dicarboxylic acid that is the bis-chromone derivative of glycerol. It is effective as a mast cell stabilizer.		2.0510chromones;
dicarboxylic acid		anti-asthmatic drug;
calcium channel blocker
cyclandelate
Cyclandelate: A direct-acting SMOOTH MUSCLE relaxant used to dilate BLOOD VESSELS.. cyclandelate : The ester obtained by formal condensation of mandelic acid and 3,3,5-tricyclohexanol. It is a direct-acting smooth muscle relaxant used to dilate blood vessels.		2.0510carboxylic ester;
secondary alcohol		vasodilator agent
cyclobenzaprine
cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm.		3.6120carbotricyclic compoundantidepressant;
muscle relaxant;
tranquilizing drug
cyclofenil
Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE.		3.2310organic molecular entity
cyproheptadine
Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.		4.9140piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
cystamine
[no description available]		2.0110organic disulfide;
primary amino compound		EC 2.3.2.13 (protein-glutamine gamma-glutamyltransferase) inhibitor
danthron
danthron: structure. chrysazin : A dihydroxyanthraquinone that is anthracene-9,10-dione substituted by hydroxy groups at positions 1 and 8.		2.0510dihydroxyanthraquinoneapoptosis inducer;
plant metabolite
dapi
DAPI: RN given refers to parent cpd.		2.0110indolesfluorochrome
dapsone
[no description available]		4.2550substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug
deferoxamine
Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator.		3.5920acyclic desferrioxaminebacterial metabolite;
ferroptosis inhibitor;
iron chelator;
siderophore
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		5.1880dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		8.8930primary amine
eflornithine
Eflornithine: An inhibitor of ORNITHINE DECARBOXYLASE, the rate limiting enzyme of the polyamine biosynthetic pathway.. eflornithine : A fluoroamino acid that is ornithine substituted by a difluoromethyl group at position 2.		7.76111alpha-amino acid;
fluoroamino acid		trypanocidal drug
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		4.43601,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		4.0840benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		19.5925759amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
ddt
1,1-bis(p-chlorophenyl)-2,2,2-trichloroethane: structure in first source		2.0510benzenoid aromatic compound;
chlorophenylethane;
monochlorobenzenes;
organochlorine insecticide		bridged diphenyl acaricide;
carcinogenic agent;
endocrine disruptor;
persistent organic pollutant
dichlorphenamide
Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma.		6.24420dichlorobenzene;
sulfonamide		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
ophthalmology drug
dicyclomine
Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.		3.2310carboxylic ester;
tertiary amine		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
diethylcarbamazine
Diethylcarbamazine: An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa.		2.0510N-carbamoylpiperazine;
N-methylpiperazine
pentetic acid
Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium.		3.2310pentacarboxylic acidcopper chelator
diflunisal
Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position.		4.0840monohydroxybenzoic acid;
organofluorine compound		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
3,3'-diindolylmethane
3,3'-diindolylmethane: anti-inflammatory from edible cruciferous vegetables; a cytochrome P-450 antagonist		2.0410indolesantineoplastic agent;
P450 inhibitor
dimercaprol
Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury.		3.5920dithiol;
primary alcohol		chelator
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		3.5920ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
dipyridamole
Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.		4.4260piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol		adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
disopyramide
Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.		4.9360monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
disulfiram
[no description available]		9.6980organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		12.52122branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		2.0810benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
donepezil
Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.		9.7690aromatic ether;
indanones;
piperidines;
racemate		EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
doxapram
Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.		3.2310morpholines;
pyrrolidin-2-ones		central nervous system stimulant
doxazosin
Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.		10.861aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines		alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
doxepin
Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.		3.8730dibenzooxepine;
tertiary amino compound		antidepressant
doxylamine
Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM.		3.2310pyridines;
tertiary amine		anti-allergic agent;
antiemetic;
antitussive;
cholinergic antagonist;
H1-receptor antagonist;
histamine antagonist;
sedative
droperidol
Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.		4.0740aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
dup 697
DuP 697: structure given in first source		4.6680thiophenes
dyphylline
Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs.		3.2310oxopurine;
propane-1,2-diols		bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
muscle relaxant;
vasodilator agent
ebastine
[no description available]		2.0810organic molecular entity
ebselen
ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.		2.0410benzoselenazoleanti-inflammatory drug;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 3.5.4.1 (cytosine deaminase) inhibitor;
EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor;
enzyme mimic;
ferroptosis inhibitor;
genotoxin;
hepatoprotective agent;
neuroprotective agent;
radical scavenger
econazole
Econazole: An imidazole derivative that is commonly used as a topical antifungal agent.. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.. 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group.		2.0510dichlorobenzene;
ether;
imidazoles;
monochlorobenzenes
edrophonium
Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.		3.2310phenols;
quaternary ammonium ion		antidote;
diagnostic agent;
EC 3.1.1.8 (cholinesterase) inhibitor
emodin
Emodin: Purgative anthraquinone found in several plants, especially RHAMNUS PURSHIANA. It was formerly used as a laxative, but is now used mainly as a tool in toxicity studies.. emodin : A trihydroxyanthraquinone that is 9,10-anthraquinone which is substituted by hydroxy groups at positions 1, 3, and 8 and by a methyl group at position 6. It is present in the roots and barks of numerous plants (particularly rhubarb and buckthorn), moulds, and lichens. It is an active ingredient of various Chinese herbs.		7.0110trihydroxyanthraquinoneantineoplastic agent;
laxative;
plant metabolite;
tyrosine kinase inhibitor
enflurane
Enflurane: An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate.. enflurane : An ether in which the oxygen atom is connected to 2-chloro-1,1,2-trifluoroethyl and difluoromethyl groups.		2.0510ether;
organochlorine compound;
organofluorine compound		anaesthetic
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.47201,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
eperisone
eperisone : A racemate that is an equimolar mixture of (R)- and (S)-eperisone. It is used (as the hydrochloride salt) as a muscle relaxant for the symptomatic treatment of muscle spasm and spasticity.. 1-(4-ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one : An aromatic ketone that is N-propylpiperidine in which a hydrogen at positon 2 of the propyl group is replaced by a p-ethylbenzoyl group.		7.0344aromatic ketone;
piperidines
epinastine
epinastine: RN given refers parent cpd. epinastine : A benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine.		2.0810benzazepine;
guanidines		anti-allergic agent;
H1-receptor antagonist;
histamine antagonist;
ophthalmology drug
erythrosine
Fluoresceins: A family of spiro(isobenzofuran-1(3H),9'-(9H)xanthen)-3-one derivatives. These are used as dyes, as indicators for various metals, and as fluorescent labels in immunoassays.		2.0310
estazolam
Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.		3.5920triazoles;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA modulator
etanidazole
Etanidazole: A nitroimidazole that sensitizes hypoxic tumor cells that are normally resistant to radiation therapy.. etanidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitro-1H-imidazol-1-yl)acetic acid with the amino group of ethanolamine. Used as a radiosensitising agent for hypoxic tumour cells.		210C-nitro compound;
imidazoles;
monocarboxylic acid amide		alkylating agent;
antineoplastic agent;
prodrug;
radiosensitizing agent
ethacrynic acid
Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor.		3.8730aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid		EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic
ethosuximide
Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures.		3.8730dicarboximide;
pyrrolidinone		anticonvulsant;
geroprotector;
T-type calcium channel blocker
ethotoin
ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective.		3.2310imidazolidine-2,4-dioneanticonvulsant
ethoxyresorufin
ethoxyresorufin: structure		210phenoxazine
ethoxzolamide
Ethoxzolamide: A carbonic anhydrase inhibitor used as diuretic and in glaucoma. It may cause hypokalemia.. ethoxzolamide : A sulfonamide that is 1,3-benzothiazole-2-sulfonamide which is substituted by an ethoxy group at position 6. A carbonic anhydrase inhibitor, it has been used in the treatment of glaucoma, and as a diuretic.		5.19440aromatic ether;
benzothiazoles;
sulfonamide		antiglaucoma drug;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
eicosapentaenoic acid ethyl ester
[no description available]		2.0510
etidronate
Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces.		4.22201,1-bis(phosphonic acid)antineoplastic agent;
bone density conservation agent;
chelator
etodolac
Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active.		8.28221monocarboxylic acid;
organic heterotricyclic compound		antipyretic;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
brl 42810
[no description available]		4.11402-aminopurines;
acetate ester		antiviral drug;
prodrug
carbonyl cyanide p-trifluoromethoxyphenylhydrazone
Carbonyl Cyanide p-Trifluoromethoxyphenylhydrazone: A proton ionophore that is commonly used as an uncoupling agent in biochemical studies.. carbonyl cyanide p-trifluoromethoxyphenylhydrazone : A hydrazone that is hydrazonomalononitrile in which one of the hydrazine hydrogens is substituted by a p-trifluoromethoxyphenyl group.		2.0510aromatic ether;
hydrazone;
nitrile;
organofluorine compound		ATP synthase inhibitor;
geroprotector;
ionophore
felbamate
Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy.		3.8630carbamate esteranticonvulsant;
neuroprotective agent
4-biphenylylacetic acid
biphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis.		2.0810biphenyls;
monocarboxylic acid		non-steroidal anti-inflammatory drug
felodipine
Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.		4.7790dichlorobenzene;
dihydropyridine;
ethyl ester;
methyl ester		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
fenbufen
fenbufen: structure; RN given refers to parent cpd		2.05104-oxo monocarboxylic acid;
biphenyls		non-steroidal anti-inflammatory drug
fendiline
Fendiline: Coronary vasodilator; inhibits calcium function in muscle cells in excitation-contraction coupling; proposed as antiarrhythmic and antianginal agents.		2.4620diarylmethane
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		7.72181aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
fenoldopam
Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.		3.2310benzazepinealpha-adrenergic agonist;
antihypertensive agent;
dopamine agonist;
dopaminergic antagonist;
vasodilator agent
fenoprofen
Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding.		4.4530monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fentanyl
Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.		12.252112anilide;
monocarboxylic acid amide;
piperidines		adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		4.7750piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
fipexide
fipexide: regulates dopaminergic systems at macromolecular level		3.5920benzodioxoles
flavoxate
Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol.		3.2310carboxylic ester;
flavones;
piperidines;
tertiary amino compound		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		3.8730aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		2.0810difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		9.6780conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		4.0940aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
flufenamic acid
Flufenamic Acid: An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16). flufenamic acid : An aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent. An analgesic and anti-inflammatory, it is used in rheumatic disorders.		3.0140aromatic amino acid;
organofluorine compound		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fluphenazine
[no description available]		4.4130N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		4.0940ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
flunitrazepam
Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia.		2.05101,4-benzodiazepinone;
C-nitro compound;
monofluorobenzenes		anxiolytic drug;
GABAA receptor agonist;
sedative
fluorescite
fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer.		3.8730benzoic acids;
cyclic ketone;
hydroxy monocarboxylic acid;
organic heterotricyclic compound;
phenols;
xanthene dye		fluorescent dye;
radioopaque medium
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		15.626728nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		8.06151(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
flurazepam
Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia.		3.23101,4-benzodiazepinone;
monofluorobenzenes;
organochlorine compound;
tertiary amino compound		anticonvulsant;
anxiolytic drug;
GABAA receptor agonist;
sedative
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		10.97190fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fp 83
FP 83: structure given in first source		2.1710organic molecular entity
fluspirilene
Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.		2.0510diarylmethane
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		4.87100(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
fomepizole
Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4.		3.5920pyrazolesantidote;
EC 1.1.1.1 (alcohol dehydrogenase) inhibitor;
protective agent
foscarnet
Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		3.5920carboxylic acid;
one-carbon compound;
phosphonic acids		antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
furafylline
[no description available]		2.0710oxopurine
furegrelate
furegrelate: structure given in UD 35:175:d		210benzofurans
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		7.8172chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
gabapentin
Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.		14.224212gamma-amino acidanticonvulsant;
calcium channel blocker;
environmental contaminant;
xenobiotic
gemfibrozil
[no description available]		4.4260aromatic etherantilipemic drug
gentamicin
Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.		2.7220
2,5-dihydroxybenzoic acid
2,5-dihydroxybenzoic acid: RN given refers to parent cpd; a oxidative product of saligenin. 2,5-dihydroxybenzoic acid : A dihydroxybenzoic acid having the two hydroxy groups at the 2- and 5-positions.		2.0110dihydroxybenzoic acidEC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
fungal metabolite;
human metabolite;
MALDI matrix material;
mouse metabolite
glafenine
Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market.		3.8630aminoquinoline;
carboxylic ester;
glycol;
organochlorine compound;
secondary amino compound		inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gliclazide
Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.		2.9740N-sulfonylureahypoglycemic agent;
insulin secretagogue;
radical scavenger
glimepiride
glimepiride: structure given in first source		4.0840sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		9.4460aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glutethimide
Glutethimide: A hypnotic and sedative. Its use has been largely superseded by other drugs.		2.4620piperidines
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		10.36100monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester
[no description available]		3.2310benzenes
go 6976
[no description available]		2.0310indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor
gossypol
Gossypol: A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer.		2.9940
granisetron
[no description available]		3.6120aromatic amide;
indazoles
guaiazulene
guaiazulene: structure		2.0510sesquiterpene
guaifenesin
Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations.		9.0540methoxybenzenes
guanethidine
Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.		3.5620azocanes;
guanidines		adrenergic antagonist;
antihypertensive agent;
sympatholytic agent
guanfacine
Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.		3.6120acetamides
guanidine
Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines.		3.6120carboxamidine;
guanidines;
one-carbon compound
gyki 52466
GYKI 52466: an AMPA (non-NMDA) receptor antagonist; structure given in first source		2.0310benzodiazepine
fasudil
fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.		2.4720isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		4.5570aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
halothane
[no description available]		2.0510haloalkane;
organobromine compound;
organochlorine compound;
organofluorine compound		inhalation anaesthetic
hexachlorophene
Hexachlorophene: A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797). hexachlorophene : An organochlorine compound that is diphenylmethane in which each of the phenyl groups is substituted by chlorines at positions 2, 3, and 5, and by a hydroxy group at position 6. An antiseptic that is effective against Gram-positive organisms, it is used in soaps and creams for the treatment of various skin disorders. It is also used in agriculture as an acaricide and fungicide, but is not approved for such use within the European Union.		2.4620bridged diphenyl fungicide;
polyphenol;
trichlorobenzene		acaricide;
antibacterial agent;
antifungal agrochemical;
antiseptic drug
miltefosine
miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.		2.0510phosphocholines;
phospholipid		anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor
hexestrol
[no description available]		2.0510stilbenoid
hexetidine
Hexetidine: A bactericidal and fungicidal antiseptic. It is used as a 0.1% mouthwash for local infections and oral hygiene. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797)		2.0510organic heteromonocyclic compound;
organonitrogen heterocyclic compound
hexobarbital
Hexobarbital: A barbiturate that is effective as a hypnotic and sedative.. hexobarbital : A member of the class of barbiturates taht is barbituric acid substituted at N-1 by methyl and at C-5 by methyl and cyclohex-1-enyl groups.		2.0510barbiturates
hycanthone
Hycanthone: Potentially toxic, but effective antischistosomal agent, it is a metabolite of LUCANTHONE.. hycanthone : A thioxanthen-9-one compound having a hydroxymethyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. It was formerly used (particularly as the monomethanesulfonic acid salt) as a schistosomicide for individual or mass treatement of infection with Schistosoma haematobium and S. mansoni, but due to its toxicity and concern about possible carcinogenicity, it has been replaced by other drugs such as praziquantel.		2.0510thioxanthenesmutagen;
schistosomicide drug
hydralazine
Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent.		4.140azaarene;
hydrazines;
ortho-fused heteroarene;
phthalazines		antihypertensive agent;
vasodilator agent
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		5.96310benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroflumethiazide
Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide.		3.6120benzothiadiazine;
thiazide		antihypertensive agent;
diuretic
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		5.0750aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
hydroxyurea
[no description available]		9.27223one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		3.5920hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
hypericin
[no description available]		2.4320
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		18.9321247monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
phenelzine
Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.		3.8630primary amine
lidocaine
Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.		11.9781benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
alverine
alverine : A tertiary amine having one ethyl and two 3-phenylprop-1-yl groups attached to the nitrogen. An antispasmodic that acts directly on intestinal and uterine smooth muscle, it is used (particularly as the citrate salt) in the treatment of irritable bowel syndrome.		2.0510tertiary amineantispasmodic drug
idebenone
[no description available]		2.05101,4-benzoquinones;
primary alcohol		antioxidant;
ferroptosis inhibitor
ifosfamide
[no description available]		7.4981ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		4.7890dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
amrinone
Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.		4.0940bipyridinesEC 3.1.4.* (phosphoric diester hydrolase) inhibitor
indapamide
Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.		4.140indoles;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic
indirubin-3'-monoxime
indirubin-3'-monoxime: has antiangiogenic activity. indirubin-3'-monoxime : A member of the class of biindoles that is indirubin in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime.		2.0810
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		17.230119aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
indoprofen
Indoprofen: A drug that has analgesic and anti-inflammatory properties. Following reports of adverse reactions including reports of carcinogenicity in animal studies it was withdrawn from the market worldwide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p21). indoprofen : A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-(1-oxo-1,3-dihydroisoindol-2-yl)phenyl group. Initially used as an anti-inflammatory and analgesic, it was withdrawn from the market due to causing severe gastrointestinal bleeding. It has been subsequently found to increase production of the survival motor neuron protein.		2.0110gamma-lactam;
isoindoles;
monocarboxylic acid		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
iohexol
Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position.		2.4720benzenedicarboxamide;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
iodipamide
Iodipamide: A water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.. adipiodone : An organoiodine compound that is 3-amino-2,4,6-triiodobenzoic acid in which one of the amino hydrogens is substituted by a 6-(3-carboxy-2,4,6-triiodoanilino)-6-oxohexanoyl group. It is a water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.		2.0510benzoic acids;
organoiodine compound;
secondary carboxamide		radioopaque medium
ioversol
[no description available]		3.2310amidobenzoic acid
iproniazid
[no description available]		4.0940carbohydrazide;
pyridines
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		5.0570azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
isocarboxazid
Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311)		3.5920benzenes
isoflurane
Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.		2.7230organofluorine compoundinhalation anaesthetic
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		5.1980carbohydrazideantitubercular agent;
drug allergen
2-propanol
2-Propanol: An isomer of 1-PROPANOL. It is a colorless liquid having disinfectant properties. It is used in the manufacture of acetone and its derivatives and as a solvent. Topically, it is used as an antiseptic.. propan-2-ol : A secondary alcohol that is propane in which one of the hydrogens attached to the central carbon is substituted by a hydroxy group.		2.0510secondary alcohol;
secondary fatty alcohol		protic solvent
propyphenazone
propyphenazone: structure. propyphenazone : A pyrazolone derivative that is antipyrine substituted at C-4 by an isopropyl group.		3.8421pyrazolonenon-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		4.0840catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
isoxsuprine
Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.		3.5920alkylbenzene
isradipine
Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.		4.2750benzoxadiazole;
dihydropyridine;
isopropyl ester;
methyl ester
itraconazole
[no description available]		4.4360piperazines
ketamine
Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.		7.2461cyclohexanones;
monochlorobenzenes;
secondary amino compound		analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
ketanserin
Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.		2.7730aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		4.87100dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketoprofen
Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.		11.23247benzophenones;
oxo monocarboxylic acid		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketorolac
Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.		12.84259amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate		analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
ketotifen
Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.		7.5220cyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound		anti-asthmatic drug;
H1-receptor antagonist
khellin
Khellin: A vasodilator that also has bronchodilatory action. It has been employed in the treatment of angina pectoris, in the treatment of asthma, and in conjunction with ultraviolet light A, has been tried in the treatment of vitiligo. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1024). khellin : A furanochrome in which the basic tricyclic skeleton is substituted at positions 4 and 9 with methoxy groups and at position 7 with a methyl group. A major constituent of the plant Ammi visnaga it is a herbal folk medicine used for various illnesses, its main effect being as a vasodilator.		2.5320furanochromone;
organic heterotricyclic compound;
oxacycle		anti-asthmatic agent;
bronchodilator agent;
cardiovascular drug;
vasodilator agent
kojic acid
[no description available]		4.19204-pyranones;
enol;
primary alcohol		Aspergillus metabolite;
EC 1.10.3.1 (catechol oxidase) inhibitor;
EC 1.10.3.2 (laccase) inhibitor;
EC 1.13.11.24 (quercetin 2,3-dioxygenase) inhibitor;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 1.4.3.3 (D-amino-acid oxidase) inhibitor;
NF-kappaB inhibitor;
skin lightening agent
kynurenic acid
Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool.. kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4.		3.5720monohydroxyquinoline;
quinolinemonocarboxylic acid		G-protein-coupled receptor agonist;
human metabolite;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist;
Saccharomyces cerevisiae metabolite
3-phenyllactic acid
3-phenyllactic acid: alpha-hydroxy analog of phenylalanine; RN given refers to cpd without isomeric designation. 3-phenyllactic acid : A 2-hydroxy monocarboxylic acid that is lactic acid in which one of the methyl hydrogens is substituted by a phenyl group.		2.15102-hydroxy monocarboxylic acidhuman metabolite
labetalol
Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5.		3.8630benzamides;
benzenes;
phenols;
primary carboxamide;
salicylamides;
secondary alcohol;
secondary amino compound
lamotrigine
[no description available]		4.1401,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		9.1134benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
beta-lapachone
beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.		2.4420benzochromenone;
orthoquinones		anti-inflammatory agent;
antineoplastic agent;
plant metabolite
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		11.39110(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
letrozole
[no description available]		12.5893nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
lg 100268
LG 100268: a retinoid X receptor (RXR) selective compound; structure given in first source		2.0810
lofepramine
Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.		2.4720aromatic ketone;
dibenzoazepine;
monochlorobenzenes;
tertiary amino compound		antidepressant
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		3.2310fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
lomustine
[no description available]		9.4360N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
loperamide
Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		4.9260monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol		anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		4.9260benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
lorazepam
Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.		8.0643benzodiazepine
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		9.2750biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
loxapine
Loxapine: An antipsychotic agent used in SCHIZOPHRENIA.		3.6120dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
loxoprofen
loxoprofen: RN given refers to parent cpd without isomeric designation; structure in first source. loxoprofen : A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration.		8.992410cyclopentanones;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		3.75100chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
mafenide
Mafenide: A sulfonamide that inhibits the enzyme CARBONIC ANHYDRASE and is used as a topical anti-bacterial agent, especially in burn therapy.		4.99360aromatic amine
malathion
Malathion: A wide spectrum aliphatic organophosphate insecticide widely used for both domestic and commercial agricultural purposes.. malathion : A racemate comprising equimolar amounts of (R) and (S)-malathion. It is a broad spectrum organophosphate proinsecticide used to control a wide range of pests including Coleoptera, Diptera, fruit flies, mosquitos and spider mites.. diethyl 2-[(dimethoxyphosphorothioyl)thio]succinate : A diester that is diethyl succinate in which position 2 is substituted by a (dimethoxyphosphorothioyl)thio group.		2.0510diester;
ethyl ester;
organic thiophosphate
diisopropyl 1,3-dithiol-2-ylidenemalonate
diisopropyl 1,3-dithiol-2-ylidenemalonate: structure in first source		2.0510isopropyl ester
manidipine
[no description available]		2.0510diarylmethane
maprotiline
Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.		4.0840anthracenes
mazindol
Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.		2.0510organic molecular entity
edaravone
[no description available]		2.4110pyrazoloneantioxidant;
radical scavenger
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		4.2750aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
mecamylamine
Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.		3.2310primary aliphatic amine
mechlorethamine
nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.		3.2310nitrogen mustard;
organochlorine compound		alkylating agent
meclizine
Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.		3.8630diarylmethane
meclofenamic acid(1-)
meclofenamic acid(1-) : A monocarboxylic acid anion resulting from the removal of the proton from the carboxy group of meclofenamic acid. The major species at pH 7.3.		2.1510monocarboxylic acid anion
meclofenamic acid
Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.		3.8530aminobenzoic acid;
organochlorine compound;
secondary amino compound		analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
meclofenamate sodium anhydrous
[no description available]		4.3350organic sodium salt
meclofenoxate
Meclofenoxate: An ester of DIMETHYLAMINOETHANOL and para-chlorophenoxyacetic acid.		2.0510monocarboxylic acid
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		11.2191aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
memantine
[no description available]		9.0740adamantanes;
primary aliphatic amine		antidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
vitamin k 3
Vitamin K 3: A synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.		2.46201,4-naphthoquinones;
vitamin K		angiogenesis inhibitor;
antineoplastic agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
human urinary metabolite;
nutraceutical
mepenzolate
mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure		3.2310diarylmethane
meperidine
Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.		6.0442ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
mephenytoin
Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism.		3.8730imidazolidine-2,4-dioneanticonvulsant
mepivacaine
Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic.		3.5920piperidinecarboxamidedrug allergen;
local anaesthetic
meprobamate
Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603)		3.8630organic molecular entity
mesalamine
Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.		4.2750amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols		non-steroidal anti-inflammatory drug
mesoridazine
Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group.		3.2310phenothiazines;
sulfoxide;
tertiary amino compound		dopaminergic antagonist;
first generation antipsychotic
metaproterenol
Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself.		3.5820aralkylamino compound;
phenylethanolamines;
resorcinols;
secondary alcohol;
secondary amino compound
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		5.78150guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methadone
Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.		4.3830benzenes;
diarylmethane;
ketone;
tertiary amino compound
methapyrilene
Methapyrilene: Histamine H1 antagonist with sedative action used as a hypnotic and in allergies.. methapyrilene : A member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group.		2.0510ethylenediamine derivativeanti-allergic agent;
carcinogenic agent;
H1-receptor antagonist;
sedative
methazolamide
Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.		7.73450sulfonamide;
thiadiazoles
methocarbamol
Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester.		3.7320aromatic ether;
carbamate ester;
secondary alcohol
methoxsalen
Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis.		4.6240aromatic ether;
psoralens		antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite
methoxyflurane
Methoxyflurane: An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with NITROUS OXIDE to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180). methoxyflurane : An ether in which the two groups attached to the central oxygen atom are methyl and 2,2-dichloro-1,1-difluoroethyl.		2.0510ether;
organochlorine compound;
organofluorine compound		hepatotoxic agent;
inhalation anaesthetic;
nephrotoxic agent;
non-narcotic analgesic
methyclothiazide
Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825)		3.2310benzothiadiazine
nocodazole
[no description available]		3.5920aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
methyl salicylate
methyl salicylate: used in over-the-counter liniments, ointments, lotions for relief of musculoskeletal aches and pains; has hemolytic effect on human & sheep erythrocytes; RN given refers to parent cpd; structure in Merck Index, 9th ed, #5990. methyl salicylate : A benzoate ester that is the methyl ester of salicylic acid.		2.4620benzoate ester;
methyl ester;
salicylates		flavouring agent;
insect attractant;
metabolite
methylphenidate
Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group.		4.0740beta-amino acid ester;
methyl ester;
piperidines
methyprylon
methyprylon: was heading 1973-94 (see under HYPNOTICS AND SEDATIVES 1963-72); use PIPERIDONES to search METHYPRYLON 1973-94		2.0510organic molecular entity
metiazinic acid
metiazinic acid: phenothiazine which acts as an anti-inflammatory agent; minor descriptor (75-86); on line & INDEX MEDICUS search PHENOTHIAZINES (75-86). metiazinic acid : Phenothiazine substituted at nitrogen by a methyl group and at C-2 by a carboxymethyl group.		2.1710phenothiazinesdrug allergen;
non-steroidal anti-inflammatory drug
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		4.2850benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
metolazone
Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics.		3.8830organochlorine compound;
quinazolines;
sulfonamide		antihypertensive agent;
diuretic;
ion transport inhibitor
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		11.24101aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		4.4560C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
metyrapone
Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency.		3.5920aromatic ketoneantimetabolite;
diagnostic agent;
EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		3.8830aromatic ether;
primary amino compound		anti-arrhythmia drug
mianserin
Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.		4.0740dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
miconazole
Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.. 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.		2.4620dichlorobenzene;
ether;
imidazoles
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		4.4460imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
midodrine
Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.		3.2310amino acid amide;
aromatic ether;
secondary alcohol		alpha-adrenergic agonist;
prodrug;
sympathomimetic agent;
vasoconstrictor agent
milrinone
[no description available]		3.5720bipyridines;
nitrile;
pyridone		cardiotonic drug;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
minoxidil
Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.		3.8730dialkylarylamine;
tertiary amino compound
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		4.6140benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
mitotane
Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.		3.8630diarylmethane
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		5.2990dihydroxyanthraquinoneanalgesic;
antineoplastic agent
moclobemide
Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression.		3.9130benzamides;
monochlorobenzenes;
morpholines		antidepressant;
environmental contaminant;
xenobiotic
modafinil
Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.		3.5920monocarboxylic acid amide;
sulfoxide
mofezolac
mofezolac: Cyclooxygenase 1 inhibitor; structure in first source; RN from Toxlit		2.5220methoxybenzenes
molsidomine
Molsidomine: A morpholinyl sydnone imine ethyl ester, having a nitrogen in place of the keto oxygen. It acts as NITRIC OXIDE DONORS and is a vasodilator that has been used in ANGINA PECTORIS.. molsidomine : A member of the class of oxadiazoles that is 1,2,3-oxadiazole substituted by morpholin-4-yl and (ethoxycarbonyl)azanidyl groups at positions 3 and 5, respectively. It is used as a vasodilator drug for the treatment of myocardial ischemic syndrome and congestive heart failure.		2.1310ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
moxisylyte
Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312)		3.5920monoterpenoid
entinostat
[no description available]		2.0810benzamides;
carbamate ester;
primary amino compound;
pyridines;
substituted aniline		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
deet
N,N-diethyl-m-toluamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of m-toluic acid with the nitrogen of diethylamine. First developed by the U.S. Army in 1946 for use by military personnel in insect-infested areas, it is the most widely used insect repellent worldwide.		2.0510benzamides;
monocarboxylic acid amide		environmental contaminant;
insect repellent;
xenobiotic
lm 4108
indomethacin phenethylamide: a cyclooxygenase-2 inhibitor; structure in first source		2.0510N-acylindole
acecainide
Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine.		2.4620acetamides;
benzamides		anti-arrhythmia drug
clorgyline
Clorgyline: An antidepressive agent and monoamine oxidase inhibitor related to PARGYLINE.. clorgyline : An aromatic ether that is the 2,4-dichlorophenyl ether of 3-aminopropan-1-ol in which the nitrogen is substituted by a methyl group and a prop-1-yn-3-yl group. A monoamine oxidase inhibitor, it was formerly used as an antidepressant.		3.5110aromatic ether;
dichlorobenzene;
terminal acetylenic compound;
tertiary amino compound		antidepressant;
EC 1.4.3.4 (monoamine oxidase) inhibitor
nabumetone
Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.		7.65152methoxynaphthalene;
methyl ketone		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
nadolol
[no description available]		3.6120tetralins
naftopidil
[no description available]		8.4811piperazines
nalidixic acid
[no description available]		4.43601,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
naratriptan
naratriptan: structure given in first source		3.2310heteroarylpiperidine;
sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
nefazodone
nefazodone: may be useful as an opiate adjunct		4.4360aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles		alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor
nefopam
Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26). nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain.. 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively.		6.1332benzoxazocine;
tertiary amino compound
neostigmine
Neostigmine: A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.. neostigmine : A quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor.		2.5520quaternary ammonium ionantidote to curare poisoning;
EC 3.1.1.7 (acetylcholinesterase) inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		4.2750cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nialamide
Nialamide: An MAO inhibitor that is used as an antidepressive agent.		3.5920organonitrogen compound;
organooxygen compound
nicardipine
Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.		4.0940benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
niceritrol
Niceritrol: An ester of nicotinic acid that lowers cholesterol and triglycerides in total plasma and in the VLD- and LD-lipoprotein fractions.		2.0510organic molecular entity
niclosamide
Niclosamide: An antihelmintic that is active against most tapeworms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p48). niclosamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-chlorosalicylic acid with the amino group of 2-chloro-4-nitroaniline. It is an oral anthelmintic drug approved for use against tapeworm infections.		2.0310benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide		anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		9.7690C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
niflumic acid
Niflumic Acid: An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.		3.9830aromatic carboxylic acid;
pyridines
nilutamide
[no description available]		3.8730(trifluoromethyl)benzenes;
C-nitro compound;
imidazolidinone		androgen antagonist;
antineoplastic agent
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		11.51617aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
nimodipine
Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.		4.42602-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester		antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
nisoldipine
Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris.		4.0940C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
methyl ester
nitrazepam
Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome).		2.47201,4-benzodiazepinone;
C-nitro compound		anticonvulsant;
antispasmodic drug;
drug metabolite;
GABA modulator;
sedative
nitrendipine
Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension.		2.7530C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
nitroglycerin
Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.		6.792nitroglycerolexplosive;
muscle relaxant;
nitric oxide donor;
prodrug;
tocolytic agent;
vasodilator agent;
xenobiotic
nizatidine
[no description available]		3.86301,3-thiazoles;
C-nitro compound;
carboxamidine;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
cholinergic drug;
H2-receptor antagonist
nomifensine
Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.		3.5920isoquinolinesdopamine uptake inhibitor
masoprocol
nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata)		5.4100catechols;
lignan;
tetrol		antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		4.6240fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
nortriptyline
Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.		4.140organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide
N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide: structure given in first source. NS-398 : A C-nitro compound that is N-methylsulfonyl-4-nitroaniline bearing an additional cyclohexyloxy substituent at position 2.		6.89500aromatic ether;
C-nitro compound;
sulfonamide		antineoplastic agent;
cyclooxygenase 2 inhibitor
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		4.94603-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
olprinone
olprinone: RN refers to HCl; structure given in first source		2.0810bipyridines
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		11.563813aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		8.192carbazoles
orphenadrine
Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.		3.8630ether;
tertiary amino compound		antidyskinesia agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
oxamniquine
Oxamniquine: An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martindale, The Extra Pharmacopoeia, 31st ed, p121). oxamniquine : A racemate comprising equimolar amounts of (R)- and (S)-oxamniquine. An anthelmintic, it is administered orally for the treatment of schistomiasis caused by Schistosoma mansoni (but not by other Schistosoma species); intramuscular administration is no longer used as it causes severe pain at the injection site.. {2-[(isopropylamino)methyl]-7-nitro-1,2,3,4-tetrahydroquinolin-6-yl}methanol : A member of the class of quinolines that is 1,2,3,4-tetrahydroquinoline which is substituted at positions 2, 6, and 7 by (isopropylamino)methyl, hydroxymethyl, and nitro groups, respectively.		2.0510aromatic primary alcohol;
C-nitro compound;
quinolines;
secondary amino compound
oxaprozin
Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis.		4.4601,3-oxazoles;
monocarboxylic acid		analgesic;
non-steroidal anti-inflammatory drug
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		4.07401,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
oxethazaine
[no description available]		2.0510amino acid amide
oxibendazole
oxibendazole: structure		2.0510benzimidazoles;
carbamate ester
oxidopamine
Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).		2.8330benzenetriol;
catecholamine;
primary amino compound		drug metabolite;
human metabolite;
neurotoxin
oxprenolol
Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.		2.4520aromatic ether
oxybenzone
oxybenzone : A hydroxybenzophenone that is benzophenone which is substituted at the 2- and 4-positions of one of the benzene rings by hydroxy and methoxy groups respectively.		2.0510hydroxybenzophenone;
monomethoxybenzene		dermatologic drug;
environmental contaminant;
protective agent;
ultraviolet filter;
xenobiotic
oxybutynin
oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.		11.9162acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound		antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic
oxyphenbutazone
Oxyphenbutazone: A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27). oxyphenbutazone : A metabolite of phenylbutazone obtained by hydroxylation at position 4 of one of the phenyl rings. Commonly used (as its hydrate) to treat pain, swelling and stiffness associated with arthritis and gout, it was withdrawn from the market 1984 following association with blood dyscrasis and Stevens-Johnson syndrome.		2.0510phenols;
pyrazolidines		antimicrobial agent;
antineoplastic agent;
antipyretic;
drug metabolite;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite
aminosalicylic acid
Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.		4.0940aminobenzoic acid;
phenols		antitubercular agent
pamidronate
[no description available]		4.9240phosphonoacetic acid
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		4.6980aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
papaverine
Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.		3.8730benzylisoquinoline alkaloid;
dimethoxybenzene;
isoquinolines		antispasmodic drug;
vasodilator agent
4-dichlorobenzene
dichlorobenzene : Any member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.. 1,4-dichlorobenzene : A dichlorobenzene carrying chloro groups at positions 1 and 4.		2.0510dichlorobenzeneinsecticide
pargyline
Pargyline: A monoamine oxidase inhibitor with antihypertensive properties.		2.4820aromatic amine
patulin
Patulin: 4-Hydroxy-4H-furo(3,2-c)pyran-2(6H)-one. A mycotoxin produced by several species of Aspergillus and Penicillium. It is found in unfermented apple and grape juice and field crops. It has antibiotic properties and has been shown to be carcinogenic and mutagenic and causes chromosome damage in biological systems.. patulin : A furopyran and lactone that is (2H-pyran-3(6H)-ylidene)acetic acid which is substituted by hydroxy groups at positions 2 and 4 and in which the hydroxy group at position 4 has condensed with the carboxy group to give the corresponding bicyclic lactone. A mycotoxin produced by several species of Aspergillus and Penicillium, it has antibiotic properties but has been shown to be carcinogenic and mutagenic.		2.4820furopyran;
gamma-lactone;
lactol		antimicrobial agent;
Aspergillus metabolite;
carcinogenic agent;
mutagen;
mycotoxin;
Penicillium metabolite
pca 4248
PCA 4248: structure given in first source; platelet activating factor antagonist		2.0310dihydropyridine
pd 153035
4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline: structure given in first source. PD-153035 : A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.		2.4520aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
pd 158780
[no description available]		2.0310aromatic amine;
bromobenzenes;
diamine;
pyridopyrimidine;
secondary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0310aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pemoline
Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.		4.09401,3-oxazolescentral nervous system stimulant
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		4.4230aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
pentobarbital
Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		3.8830barbituratesGABAA receptor agonist
pentoxifylline
[no description available]		4.4360oxopurine
perazine
Perazine: A phenothiazine antipsychotic with actions and uses similar to those of CHLORPROMAZINE. Extrapyramidal symptoms may be more common than other side effects.. perazine : A phenothiazine derivative in which 10H-phenothiazinecarries a 3-(4-methylpiperazin-1-yl)propyl substituent at the N-10 position.		2.0510N-alkylpiperazine;
N-methylpiperazine;
phenothiazines		dopaminergic antagonist;
phenothiazine antipsychotic drug
perhexiline
Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis.		3.5920piperidinescardiovascular drug
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		3.8730N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
phenacetin
Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione		3.3160acetamides;
aromatic ether		cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug
phenazopyridine
Phenazopyridine: A local anesthetic that has been used in urinary tract disorders. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.. phenazopyridine : A diaminopyridine that is 2,6-diaminopyridine substituted at position 3 by a phenylazo group. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.		8.9321diaminopyridine;
monoazo compound		anticoronaviral agent;
carcinogenic agent;
local anaesthetic;
non-narcotic analgesic
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		7.4881barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
phenolphthalein
Phenolphthalein: An acid-base indicator which is colorless in acid solution, but turns pink to red as the solution becomes alkaline. It is used medicinally as a cathartic.		2.0510phenols
phenoxybenzamine
Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.		3.8630aromatic amine
phentermine
Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity.		3.2310primary amineadrenergic agent;
appetite depressant;
central nervous system drug;
central nervous system stimulant;
dopaminergic agent;
sympathomimetic agent
4-phenylbutyric acid
4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation.		3.2310monocarboxylic acidantineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug
phenylbutazone
Phenylbutazone: A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.. phenylbutazone : A member of the class of pyrazolidines that is 1,2-diphenylpyrazolidine-3,5-dione carrying a butyl group at the 4-position.		2.9840pyrazolidinesantirheumatic drug;
EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor;
metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
moxonidine
moxonidine: structure given in first source		2.0510organohalogen compound;
pyrimidines
pifithrin
pifithrin: a tetrahydrobenzothiazol; inhibitor of P53 that protects mice from the side effects of cancer therapy; structure in first source		2.0510aromatic ketone
pilsicainide
pilsicainide: structure given in first source. pilsicainide : A secondary carboxamide resulting from the formal condensation of the amino group of 2,6-dimethylaniline with the carboxy group of (tetrahydro-1H-pyrrolizin-7a(5H)-yl)acetic acid. It is a sodium channel blocker which is used as an antiarrhythmic drug for the management of atrial tachyarrhythmias in Japan.		3.5720organic heterobicyclic compound;
secondary carboxamide		anti-arrhythmia drug;
sodium channel blocker
pinacidil
Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)		2.4620pyridines
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		5.2660indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		5.77150aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
pipemidic acid
Pipemidic Acid: Antimicrobial against Gram negative and some Gram positive bacteria. It is protein bound and concentrated in bile and urine and used for gastrointestinal, biliary, and urinary infections.. pipemidic acid : A pyridopyrimidine that is 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid substituted at position 2 by a piperazin-1-yl group and at position 8 by an ethyl group. A synthetic broad-spectrum antibacterial, it is used for treatment of gastrointestinal, biliary, and urinary infections.		2.0510amino acid;
monocarboxylic acid;
N-arylpiperazine;
pyridopyrimidine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
piperazine
[no description available]		2.0510azacycloalkane;
piperazines;
saturated organic heteromonocyclic parent		anthelminthic drug
pipobroman
Pipobroman: An antineoplastic agent that acts by alkylation.. pipobroman : An N-acylpiperazine that is piperazine in which each of the nitrogens has been acylated by a 3-bromopropionoyl group. An anti-cancer drug.		2.0510N-acylpiperazine;
organobromine compound;
tertiary carboxamide		alkylating agent;
antineoplastic agent
piracetam
Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent.		2.7830organonitrogen compound;
organooxygen compound
piribedil
Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.		2.0810N-arylpiperazine
polythiazide
[no description available]		3.2310benzothiadiazine
duodote
duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents		3.2310pyridinium ionantidote to organophosphate poisoning;
antidote to sarin poisoning;
cholinergic drug;
cholinesterase reactivator
pramoxine
pramoxine: RN given refers to parent cpd; structure. pramocaine : A member of the class of morpholines that is morpholine substituted at the nitrogen atom by a 3-(4-butoxyphenoxy)propyl group.		2.0410aromatic ether;
morpholines		local anaesthetic
ono 1078
pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist		2.4720chromones
pyranoprofen
pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source		2.4520pyridochromene
praziquantel
azinox: Russian drug		4.4460isoquinolines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		4.4260aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		3.8730aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
primidone
Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures.		4.0940pyrimidoneanticonvulsant;
environmental contaminant;
xenobiotic
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		11.6791benzoic acids;
sulfonamide		uricosuric drug
probucol
Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.		3.8730dithioketal;
polyphenol		anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		5.0670benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
procarbazine
Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		3.8630benzamides;
hydrazines		antineoplastic agent
prochlorperazine
Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.		4.0840N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines		alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
procyclidine
Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.		3.8730pyrrolidines;
tertiary alcohol		antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist
promazine
Promazine: A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.. promazine : A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.		2.0410phenothiazines;
tertiary amine		antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
muscarinic antagonist;
phenothiazine antipsychotic drug;
serotonergic antagonist
promethazine
Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.		4.2750phenothiazines;
tertiary amine		anti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
sedative
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		4.2750aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propantheline
Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.		3.6820xanthenes
propidium
Propidium: Quaternary ammonium analog of ethidium; an intercalating dye with a specific affinity to certain forms of DNA and, used as diiodide, to separate them in density gradients; also forms fluorescent complexes with cholinesterase which it inhibits.		2.5220phenanthridines;
quaternary ammonium ion		fluorochrome;
intercalator
propofol
Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.		4.0840phenolsanticonvulsant;
antiemetic;
intravenous anaesthetic;
radical scavenger;
sedative
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		5.05120naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
protriptyline
Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.		3.2310carbotricyclic compoundantidepressant
pyridinolcarbamate
Pyridinolcarbamate: A drug that has been given by mouth in the treatment of atherosclerosis and other vascular disorders, hyperlipidemias, and thrombo-embolic disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1408)		2.0510pyridines
pyridostigmine
[no description available]		3.2310pyridinium ion
pyrilamine
Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.		2.0310aromatic ether;
ethylenediamine derivative		H1-receptor antagonist
pyrimethamine
Maloprim: contains above 2 cpds		3.8630aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sch 16134
quazepam: structure given in first source		3.2310benzodiazepine
quetiapine
[no description available]		3.8630dibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine		adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
rabeprazole
Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.		6.2852benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-one
[no description available]		2.0810indoles
raloxifene
raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.		4.26501-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols		bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
ranitidine
[no description available]		4.460aralkylamine
opc 12759
rebamipide: structure in first source; RN refers to (+-)-isomer; inhibits gastric xanthine oxidase		4.8571secondary carboxamide
pf 5901
alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol: structure given in first source; platelet activating factor antagonist		2.0310quinolines
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		4.2750benzothiazoles
rimantadine
Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.		3.6120alkylamine
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		12.0321111,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		2.0410organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
rizatriptan
rizatriptan: structure given in first source; RN given refers to benzoate		3.2310tryptaminesanti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rofecoxib
[no description available]		21.1951540butenolide;
sulfone		analgesic;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
rolipram
[no description available]		2.0310pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
ropinirole
[no description available]		3.2310indolones;
tertiary amine		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
dopamine agonist
roxatidine acetate
roxatidine acetate: structure given in first source		3.1210piperidines
saccharin
Saccharin: Flavoring agent and non-nutritive sweetener.. saccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent.		9.853101,2-benzisothiazole;
N-sulfonylcarboxamide		environmental contaminant;
sweetening agent;
xenobiotic
salicylamide
salamide: a major impurity of hydrochlorothiazide; structure in first source		2.0510phenols;
salicylamides		antirheumatic drug;
non-narcotic analgesic
sanguinarine
benzophenanthridine alkaloid : A specific group of isoquinoline alkaloids that occur only in higher plants and are constituents mainly of the Papaveraceae family.		2.0710alkaloid antibiotic;
benzophenanthridine alkaloid;
botanical anti-fungal agent
salicylsalicylic acid
salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes.		3.2310benzoate ester;
benzoic acids;
phenols;
salicylates		antineoplastic agent;
antirheumatic drug;
EC 3.5.2.6 (beta-lactamase) inhibitor;
hypoglycemic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
sb 206553
SB 206553: a high-affinity 5-HT(2C/2B) antagonist; structure given in first source		2.0810pyrroloindole
sb 220025
SB 220025: inhibits p38 mitogen-activated protein kinase; structure in first source. SB220025 : Am member of the class of imidazoles carrying piperidin-4-yl, 4-fluophenyl and 2-aminopyrimidin-4-yl substituents at posiitons 1, 4 and 5 respectively.		2.0810aminopyrimidine;
imidazoles;
organofluorine compound;
piperidines		angiogenesis inhibitor;
anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		2.0810imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
secobarbital
Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups.		3.2310barbituratesanaesthesia adjuvant;
GABA modulator;
sedative
sevoflurane
Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.		7.4720ether;
organofluorine compound		central nervous system depressant;
inhalation anaesthetic;
platelet aggregation inhibitor
sibutramine
sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride		3.5920organochlorine compound;
tertiary amino compound		anti-obesity agent;
serotonin uptake inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		3.8730pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sk&f 86002
6-(4-fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo(2,1-b)thiazole: inhibits p38 MAP kinase		2.0810imidazoles
fluoroacetic acid
fluoroacetic acid: N1 same as NM; RN given refers to parent cpd. fluoroacetic acid : A haloacetic acid that is acetic acid in which one of the methyl hydrogens is substituted by fluorine.		2.0410haloacetic acid;
organofluorine compound		EC 4.2.1.3 (aconitate hydratase) inhibitor
iodoacetic acid
Iodoacetic Acid: A derivative of ACETIC ACID that contains one IODINE atom attached to its methyl group.. iodoacetic acid : A haloacetic acid that is acetic acid in which one of the hydrogens of the methyl group is replaced by an iodine atom.		2.830haloacetic acid;
organoiodine compound		alkylating agent
risedronic acid
Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION.		3.2310pyridines
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		4.4260ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
4-phenylbutyric acid, sodium salt
sodium phenylbutyrate : The organic sodium salt of 4-phenylbutyric acid. A prodrug for phenylacetate, it is used to treat urea cycle disorders.		2.0510organic sodium saltEC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector;
neuroprotective agent;
orphan drug;
prodrug
stearic acid
octadecanoic acid : A C18 straight-chain saturated fatty acid component of many animal and vegetable lipids. As well as in the diet, it is used in hardening soaps, softening plastics and in making cosmetics, candles and plastics.		2.5720long-chain fatty acid;
saturated fatty acid;
straight-chain saturated fatty acid		algal metabolite;
Daphnia magna metabolite;
human metabolite;
plant metabolite
imatinib
[no description available]		5.5180aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		4.7280dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
succinylcholine
Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid.		3.2310quaternary ammonium ion;
succinate ester		drug allergen;
muscle relaxant;
neuromuscular agent
sulfabenzamide
sulfabenzamide : A sulfonamide containing a benzamido substituent on nitrogen. An antibacterial/antimicrobial, it is often used in conjunction with sulfathiazole and sulfacetamide as a topical, intravaginal antibacterial preparation.		2.0510benzenes;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
antimicrobial drug
sulfadimethoxine
Sulfadimethoxine: A sulfanilamide that is used as an anti-infective agent.. sulfadimethoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 2- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position.		2.0510aromatic ether;
pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
drug allergen;
environmental contaminant;
xenobiotic
sulfamerazine
[no description available]		2.0510pyrimidines;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
drug allergen
sulfameter
Sulfameter: Long acting sulfonamide used in leprosy, urinary, and respiratory tract infections.. sulfamethoxydiazine : A sulfonamide consisting of pyrimidine having a methoxy substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 2-position.		2.0510pyrimidines;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
leprostatic drug;
renal agent
sulfamethazine
Sulfamethazine: A sulfanilamide anti-infective agent. It has a spectrum of antimicrobial action similar to other sulfonamides.. sulfamethazine : A sulfonamide consisting of pyrimidine with methyl substituents at the 4- and 6-positions and a 4-aminobenzenesulfonamido group at the 2-position.		2.0510pyrimidines;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
antiinfective agent;
antimicrobial agent;
carcinogenic agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
ligand;
xenobiotic
sulfamethizole
Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2.		3.8630sulfonamide antibiotic;
sulfonamide;
thiadiazoles		antiinfective agent;
antimicrobial agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		4.6861isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfanilamide
[no description available]		7.18430substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
drug allergen;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
sulfanitran
[no description available]		2.4620sulfonamide
sulfaphenazole
Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent.		2.7430primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
sulfapyridine
Sulfapyridine: Antibacterial, potentially toxic, used to treat certain skin diseases.. sulfapyridine : A sulfonamide consisting of pyridine with a 4-aminobenzenesulfonamido group at the 2-position.		2.0510pyridines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
dermatologic drug;
drug allergen;
environmental contaminant;
xenobiotic
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		7.26171
sulfathiazole
Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position.		3.61201,3-thiazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sulfinpyrazone
Sulfinpyrazone: A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.		2.7430pyrazolidines;
sulfoxide		uricosuric drug
sulfisoxazole
Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.. sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms.		2.0810isoxazoles;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
drug allergen
sulfobromophthalein
Sulfobromophthalein: A phenolphthalein that is used as a diagnostic aid in hepatic function determination.		2.05102-benzofurans;
organobromine compound;
organosulfonic acid;
phenols		dye
2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol
[no description available]		3.5920alkylbenzene
sulpiride
Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.		8.52442benzamides;
N-alkylpyrrolidine;
sulfonamide		antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
sulthiame
sulthiame: was heading 1964-94 (see under THIAZINES 1964-90); use THIAZINES to search SULTHIAME 1966-94		6.87310organic molecular entity
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		3.8730sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
suprofen
Suprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.. suprofen : An aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group.		2.0510aromatic ketone;
monocarboxylic acid;
thiophenes		antirheumatic drug;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
suramin
Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.. suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.		2.0510naphthalenesulfonic acid;
phenylureas;
secondary carboxamide		angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine
[no description available]		2.0810stilbenoid
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		2.7630N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		2.0810acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
tegafur
[no description available]		6.0374organohalogen compound;
pyrimidines
telenzepine
telenzepine: structure given in first source		2.0510benzodiazepine
temazepam
Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.		3.5920benzodiazepine
temozolomide
[no description available]		10.84285imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		4.0840furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
terbutaline
Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.		4.0840phenylethanolamines;
resorcinols		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hypoglycemic agent;
sympathomimetic agent;
tocolytic agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		3.6790diarylmethane
tetracaine
Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia.. tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia.		2.0510benzoate ester;
tertiary amino compound		local anaesthetic
tetraethylammonium
Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)		3.8530quaternary ammonium ion
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		12317phthalimides;
piperidones
thiabendazole
Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate		3.59201,3-thiazoles;
benzimidazole fungicide;
benzimidazoles		antifungal agrochemical;
antinematodal drug
2,4-thiazolidinedione
thiazolidine-2,4-dione: structure in first source. 1,3-thiazolidine-2,4-dione : A thiazolidenedione carrying oxo substituents at positions 2 and 4.		210thiazolidenedione
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		4.0840phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
thiotepa
Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed).		3.8830aziridines
tiapride
[no description available]		2.0810benzamides
tiaprofenic acid
tiaprofenic acid: RN given refers to parent cpd; structure. tiaprofenic acid : An aromatic ketone that is thiophene substituted at C-2 by benzoyl and at C-4 by a 1-carboxyethyl group.		2.0510aromatic ketone;
monocarboxylic acid;
thiophenes		drug allergen;
non-steroidal anti-inflammatory drug
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		6.0481monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
tilorone
Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.. tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug.		2.0810aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound		anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist
tinidazole
Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent.		4.0840imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
tiopronin
Tiopronin: Sulfhydryl acylated derivative of GLYCINE.		3.5920N-acyl-amino acid
tizanidine
tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.		5.4741benzothiadiazole;
imidazoles		alpha-adrenergic agonist;
muscle relaxant
nikethamide
Nikethamide: A central nervous system stimulant. It was formerly used in the treatment of barbiturate overdose but is now considered to be of no value for such purposes and may be dangerous. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1229)		2.0810pyridinecarboxamide
tolazamide
Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.		3.8630N-sulfonylureahypoglycemic agent;
potassium channel blocker
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		4.4160N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
tolmetin
Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.		4.2950aromatic ketone;
monocarboxylic acid;
pyrroles		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
tolnaftate
[no description available]		2.0810monothiocarbamic esterantifungal drug
tolperisone
Tolperisone: A centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1211)		2.0510aromatic ketone
ultram
2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively.		4.2650aromatic ether;
tertiary alcohol;
tertiary amino compound
tranexamic acid
Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage.		3.5920amino acid
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		9.2850monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
triamterene
Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.		3.6120pteridinesdiuretic;
sodium channel blocker
triazolam
Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.		3.620triazolobenzodiazepinesedative
triclosan
[no description available]		2.4920aromatic ether;
dichlorobenzene;
monochlorobenzenes;
phenols		antibacterial agent;
antimalarial;
drug allergen;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
fungicide;
persistent organic pollutant;
xenobiotic
trifluoperazine
[no description available]		4.4230N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
trifluperidol
Trifluperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in the treatment of PSYCHOSES including MANIA and SCHIZOPHRENIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p621)		2.0610aromatic ketone
triflupromazine
Triflupromazine: A phenothiazine used as an antipsychotic agent and as an antiemetic.. triflupromazine : A member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(dimethylamino)propyl group at the N-10 position.		2.4920organofluorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
trihexyphenidyl
Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic.		3.5820amine
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		3.8630oxazolidinoneanticonvulsant;
geroprotector
trimethobenzamide
trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans.		3.2310benzamides;
tertiary amino compound		antiemetic
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		4.5570aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		3.2310
trimipramine
Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant.		3.5820dibenzoazepine;
tertiary amino compound		antidepressant;
environmental contaminant;
xenobiotic
troglitazone
Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.		4.6680chromanes;
thiazolidinone		anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
thenoyltrifluoroacetone
Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration.		2.0810
tyramine
[no description available]		3.5620monoamine molecular messenger;
primary amino compound;
tyramines		EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
delavirdine
Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		4.120aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
undecylenic acid
undecylenic acid: a fatty acid with a terminal double bond. 10-undecenoic acid : An undecenoic acid having its double bond in the 10-position. It is derived from castor oil and is used for the treatment of skin problems.. undecenoic acid : A C11, straight-chain fatty acid carrying a C=C double bond at any position.		2.0810undecenoic acidantifungal drug;
plant metabolite
urapidil
[no description available]		2.0810piperazines
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		4.2850cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
vesnarinone
[no description available]		2.0510organic molecular entity
vigabatrin
[no description available]		3.8730gamma-amino acidanticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor
pirinixic acid
pirinixic acid: structure		2.4620aryl sulfide;
organochlorine compound;
pyrimidines
ici 204,219
zafirlukast: a leukotriene D4 receptor antagonist		4.5770carbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
zaleplon
zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.		3.6120nitrile;
pyrazolopyrimidine		anticonvulsant;
anxiolytic drug;
central nervous system depressant;
sedative
zm 336372
N-(5-(3-dimethylaminobenzamido)-2-methylphenyl)-4-hydroxybenzamide: an inhibitor of c-Raf; activates Raf-1; structure in first source		2.0310benzamides
zolpidem
Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.		3.8630imidazopyridinecentral nervous system depressant;
GABA agonist;
sedative
zomepirac
zomepirac: RN given refers to parent cpd; structure		2.4620aromatic ketone;
monocarboxylic acid;
monochlorobenzenes;
pyrroles		cardiovascular drug;
non-steroidal anti-inflammatory drug
zonisamide
Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.		7.744501,2-benzoxazoles;
sulfonamide		anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
zopiclone
zopiclone: S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position.		3.9721monochloropyridine;
pyrrolopyrazine		central nervous system depressant;
sedative
guanidine hydrochloride
[no description available]		2.0510one-carbon compound;
organic chloride salt		protein denaturant
hydrocortisone acetate
hydrocortisone acetate: RN given refers to cpd without isomeric designation		2.0510cortisol ester;
tertiary alpha-hydroxy ketone
cortisone acetate
Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.		3.5920corticosteroid hormone
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		7.0272mitomycinalkylating agent;
antineoplastic agent
oxyphenonium
Oxyphenonium: A quaternary ammonium anticholinergic agent with peripheral side effects similar to those of ATROPINE. It is used as an adjunct in the treatment of gastric and duodenal ulcer, and to relieve visceral spasms. The drug has also been used in the form of eye drops for mydriatic effect.		2.4520acylcholine
corticosterone
[no description available]		2.723011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		12.0814111beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
estriol
hormonin: estrogen replacement; each tablet contains 600 ug micronized 17beta-estradiol, 270 ug estriol and 1.4 mg estrone. chlorapatite : A phosphate mineral with the formula Ca5(PO4)3Cl.		2.051016alpha-hydroxy steroid;
17beta-hydroxy steroid;
3-hydroxy steroid		estrogen;
human metabolite;
human xenobiotic metabolite;
mouse metabolite
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		4.4260alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
cephaloridine
Cephaloridine: A cephalosporin antibiotic.. cefaloridine : A cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C.		2.4620beta-lactam antibiotic allergen;
cephalosporin;
semisynthetic derivative		antibacterial drug
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		3.5920imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		3.8630glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
thymidine
[no description available]		2.0510pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
floxuridine
Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.. floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.		2.7330nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent
piperonyl butoxide
[no description available]		2.0510benzodioxolespesticide synergist
bromouracil
Bromouracil: 5-Bromo-2,4(1H,3H)-pyrimidinedione. Brominated derivative of uracil that acts as an antimetabolite, substituting for thymine in DNA. It is used mainly as an experimental mutagen, but its deoxyriboside (BROMODEOXYURIDINE) is used to treat neoplasms.. 5-bromouracil : A pyrimidine having keto groups at the 2- and 4-positions and a bromo group at the 5-position. Used mainly as an experimental mutagen.		2.0510nucleobase analogue;
pyrimidines		mutagen
3,3',5-triiodothyroacetic acid
tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome.		2.0510
isoproterenol hydrochloride
[no description available]		2.0510catechols
hydroxyproline
Hydroxyproline: A hydroxylated form of the imino acid proline. A deficiency in ASCORBIC ACID can result in impaired hydroxyproline formation.. hydroxyproline : A proline derivative that is proline substituted by at least one hydroxy group.		2.47204-hydroxyproline;
L-alpha-amino acid zwitterion		human metabolite;
mouse metabolite;
plant metabolite
histamine dihydrochloride
Ceplene: Tradename for histamine dihydrochloride.		2.0510
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		4.08402-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
dextroamphetamine
Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.		4.3501-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0510ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
norethindrone acetate
norethisterone acetate : A 3-oxo Delta(4)-steroid that is norethisterone in which the hydroxy group has been converted to its acetate ester.		2.05103-oxo-Delta(4) steroid;
acetate ester;
terminal acetylenic compound		progestin;
synthetic oral contraceptive
spironolactone
Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.		4.41603-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester		aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
prednisolone acetate
prednisolone acetate: RN given refers to cpd with locant for acetate group in position 21 & (11 beta)-isomer		2.1110corticosteroid hormone
cyclobarbital
cyclobarbital: was heading 1977-94 (see under BARBITURATES 1977-90); CYCLOBARBITONE, HEXEMAL, & TETRAHYDROPHENOBARBITAL were see CYCLOBARBITAL 1977-94; use BARBITURATES to search CYCLOBARBITAL 1977-94; short to intermediate duration barbiturate used as hypnotic and sedative		2.0510barbiturates
aldosterone
[no description available]		10.737311beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
allobarbital
allobarbital: was heading 1976-94 (see under BARBITURATES 1976-90); ALLOBARBITONE, DIALLYLBARBITAL, DIALLYLBARBITURIC ACID, & DIALLYLMAL were see ALLOBARBITAL 1976-94; use BARBITURATES to search ALLOBARBITAL 1976-94; a barbiturate derivative with effects of intermediate duration; at lower doses, it is used as a sedative; at higher doses, it displays hypnotic effects		2.0510barbiturates
penicillamine
Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group.		3.8730non-proteinogenic alpha-amino acid;
penicillamine		antirheumatic drug;
chelator;
copper chelator;
drug allergen
trichlorfon
Trichlorfon: An organochlorophosphate cholinesterase inhibitor that is used as an insecticide for the control of flies and roaches. It is also used in anthelmintic compositions for animals. (From Merck, 11th ed). trichlorfon : A phosphonic ester that is dimethyl phosphonate in which the hydrogen atom attched to the phosphorous is substituted by a 2,2,2-trichloro-1-hydroxyethyl group.		2.0510organic phosphonate;
organochlorine compound;
phosphonic ester		agrochemical;
anthelminthic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
insecticide
cysteine
[no description available]		3.8830cysteine zwitterion;
cysteine;
L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid		EC 4.3.1.3 (histidine ammonia-lyase) inhibitor;
flour treatment agent;
human metabolite
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		13.2819111-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		5.077017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
oxandrolone
Oxandrolone: A synthetic hormone with anabolic and androgenic properties.		3.592017beta-hydroxy steroid;
3-oxo steroid;
anabolic androgenic steroid;
oxa-steroid		anabolic agent;
androgen
dehydroepiandrosterone
Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.. dehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands.		2.482017-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
androstanoid		androgen;
human metabolite;
mouse metabolite
promazine hydrochloride
[no description available]		2.0510hydrochloride
nad
[no description available]		2.0510NADgeroprotector
2-acetylaminofluorene
2-Acetylaminofluorene: A hepatic carcinogen whose mechanism of activation involves N-hydroxylation to the aryl hydroxamic acid followed by enzymatic sulfonation to sulfoxyfluorenylacetamide. It is used to study the carcinogenicity and mutagenicity of aromatic amines.		2.02102-acetamidofluorenesantimitotic;
carcinogenic agent;
epitope;
mutagen
penicillin g
Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.		4.0840penicillin allergen;
penicillin		antibacterial drug;
drug allergen;
epitope
idoxuridine
[no description available]		2.0510organoiodine compound;
pyrimidine 2'-deoxyribonucleoside		antiviral drug;
DNA synthesis inhibitor
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		9.460pilocarpineantiglaucoma drug
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		2.7830organic heterobicyclic compound;
organonitrogen heterocyclic compound
triiodothyronine
Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.		4.1402-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine		human metabolite;
mouse metabolite;
thyroid hormone
diethylnitrosamine
Diethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties.. N-nitrosodiethylamine : A nitrosamine that is N-ethylethanamine substituted by a nitroso group at the N-atom.		7.4420nitrosaminecarcinogenic agent;
hepatotoxic agent;
mutagen
carbon tetrachloride
Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.		3.1850chlorocarbon;
chloromethanes		hepatotoxic agent;
refrigerant
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		4.8571alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
4-nitroquinoline-1-oxide
4-nitroquinoline N-oxide : A quinoline N-oxide carrying a nitro substituent at position 4.		7.9640C-nitro compound;
quinoline N-oxide		carcinogenic agent
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		5.3190C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
aspartic acid
Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.		2.4820aspartate family amino acid;
aspartic acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
mouse metabolite;
neurotransmitter
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		11.8841amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
lysine
Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.		7.9740aspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid		algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
allyl isothiocyanate
allyl isothiocyanate: used in the manufacture of flavors, war gases; medical use as a counterirritant; structure. allyl isothiocyanate : An isothiocyanate with the formula CH2=CHCH2N=C=S. A colorless oil with boiling point 152degreeC, it is responsible for the pungent taste of mustard, horseradish, and wasabi.		7.0810alkenyl isothiocyanate;
isothiocyanate		antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lachrymator;
metabolite
cetrimonium bromide
cetyltrimethylammonium bromide : The organic bromide salt that is the bromide salt of cetyltrimethylammonium; one of the components of the topical antiseptic cetrimide.		2.0510organic bromide salt;
quaternary ammonium salt		detergent;
surfactant
cyanides
Cyanides: Inorganic salts of HYDROGEN CYANIDE containing the -CN radical. The concept also includes isocyanides. It is distinguished from NITRILES, which denotes organic compounds containing the -CN radical.. cyanides : Salts and C-organyl derivatives of hydrogen cyanide, HC#N.. isocyanide : The isomer HN(+)#C(-) of hydrocyanic acid, HC#N, and its hydrocarbyl derivatives RNC (RN(+)#C(-)).. cyanide : A pseudohalide anion that is the conjugate base of hydrogen cyanide.		2.0310pseudohalide anionEC 1.9.3.1 (cytochrome c oxidase) inhibitor
vincristine
[no description available]		4.4360acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		3.8630carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
sulfamic acid
sulfamic acid: standard in alkalimetry; RN given refers to parent cpd; structure. sulfamic acid : The simplest of the sulfamic acids consisting of a single sulfur atom covalently bound by single bonds to hydroxy and amino groups and by double bonds to two oxygen atoms.		4.7630sulfamic acids
sucrose
Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.		4.5351glycosyl glycosidealgal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
sweetening agent
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		3.36017-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
testosterone propionate
Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.		2.0510steroid ester
tubocurarine
Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.. tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.. isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine.		2.4720bisbenzylisoquinoline alkaloiddrug allergen;
muscle relaxant;
nicotinic antagonist
9,10-dimethyl-1,2-benzanthracene
9,10-Dimethyl-1,2-benzanthracene: Polycyclic aromatic hydrocarbon found in tobacco smoke that is a potent carcinogen.. 7,12-dimethyltetraphene : A tetraphene having methyl substituents at the 7- and 12-positions. It is a potent carcinogen and is present in tobacco smoke.		4.18160ortho-fused polycyclic arene;
tetraphenes		carcinogenic agent
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		4.0840aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
aminopyrine
Aminopyrine: A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS.. aminophenazone : A pyrazolone that is 1,2-dihydro-3H-pyrazol-3-one substituted by a dimethylamino group at position 4, methyl groups at positions 1 and 5 and a phenyl group at position 2. It exhibits analgesic, anti-inflammatory, and antipyretic properties.		2.4620pyrazolone;
tertiary amino compound		antipyretic;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
methyltestosterone
Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position.		3.592017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
enone		anabolic agent;
androgen;
antineoplastic agent
promethazine hydrochloride
[no description available]		2.0510hydrochlorideanti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
geroprotector;
H1-receptor antagonist;
local anaesthetic;
sedative
tetrabenazine
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7.		3.5920benzoquinolizine;
cyclic ketone;
tertiary amino compound
puromycin aminonucleoside
3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine: structure in first source. 3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine : Puromycin derivative that lacks the methoxyphenylalanyl group on the amine of the sugar ring.		7.05103'-deoxyribonucleoside;
adenosines
adenosine diphosphate
Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.		4.6932adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		fundamental metabolite;
human metabolite
cephalothin
Cephalothin: A cephalosporin antibiotic.. cefalotin : A semisynthetic, first-generation cephalosporin antibiotic with acetoxymethyl and (2-thienylacetyl)nitrilo moieties at positions 3 and 7, respectively, of the core structure. Administered parenterally during surgery and to treat a wide spectrum of blood infections.		2.0510azabicycloalkene;
beta-lactam antibiotic allergen;
carboxylic acid;
cephalosporin;
semisynthetic derivative;
thiophenes		antibacterial drug;
antimicrobial agent
uridine
[no description available]		2.0510uridinesdrug metabolite;
fundamental metabolite;
human metabolite
kanamycin a
Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components.		4.0940kanamycinsbacterial metabolite
bromodeoxyuridine
Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors.		2.7430pyrimidine 2'-deoxyribonucleosideantimetabolite;
antineoplastic agent
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		5.34121monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
phenylephrine
Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.		2.9840phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.9740amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
edetic acid
Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.		4.1620ethylenediamine derivative;
polyamino carboxylic acid;
tetracarboxylic acid		anticoagulant;
antidote;
chelator;
copper chelator;
geroprotector
tributyrin
tributyrin: structure. tributyrin : A triglyceride obtained by formal acylation of the three hydroxy groups of glycerol by butyric acid.		7.0710butyrate ester;
triglyceride		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug;
protective agent
phenylethyl alcohol
Phenylethyl Alcohol: An antimicrobial, antiseptic, and disinfectant that is used also as an aromatic essence and preservative in pharmaceutics and perfumery.. 2-phenylethanol : A primary alcohol that is ethanol substituted by a phenyl group at position 2.		2.2110benzenes;
primary alcohol		Aspergillus metabolite;
fragrance;
plant growth retardant;
plant metabolite;
Saccharomyces cerevisiae metabolite
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.9640amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
cysteamine
Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2.		3.5820amine;
thiol		geroprotector;
human metabolite;
mouse metabolite;
radiation protective agent
acetylcholine chloride
acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug.		3.5920quaternary ammonium salt
phlorhizin
[no description available]		2.110aryl beta-D-glucoside;
dihydrochalcones;
monosaccharide derivative		antioxidant;
plant metabolite
mepazine
mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position.		3.2310phenothiazines
methoxamine hydrochloride
[no description available]		2.0510dimethoxybenzene
niridazole
Niridazole: An antischistosomal agent that has become obsolete.		2.05101,3-thiazoles;
C-nitro compound
cloxacillin
Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6.		3.2310penicillin allergen;
penicillin;
semisynthetic derivative		antibacterial agent;
antibacterial drug
methylene blue
Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.		2.4920organic chloride saltacid-base indicator;
antidepressant;
antimalarial;
antimicrobial agent;
antioxidant;
cardioprotective agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 4.6.1.2 (guanylate cyclase) inhibitor;
fluorochrome;
histological dye;
neuroprotective agent;
physical tracer
leucine
Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.		4.8871amino acid zwitterion;
L-alpha-amino acid;
leucine;
proteinogenic amino acid;
pyruvate family amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
berlition
berlition: antioxidant preparation containing alpha-lipoic acid, used in the neuroprotective therapy of chronic brain ischemia for correction of free-radical processes. (R)-lipoic acid : The (R)-enantiomer of lipoic acid. A vitamin-like, C8 thia fatty acid with anti-oxidant properties.. lipoic acid : A heterocyclic thia fatty acid comprising pentanoic acid with a 1,2-dithiolan-3-yl group at the 5-position.		2.7530dithiolanes;
heterocyclic fatty acid;
lipoic acid;
thia fatty acid		cofactor;
nutraceutical;
prosthetic group
methacholine chloride
Methacholine Chloride: A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)		2.0710quaternary ammonium salt
aniline
[no description available]		2.0410anilines;
primary arylamine
calcium acetate
calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces.		3.2310calcium saltchelator
dimethylnitrosamine
Dimethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties. It causes serious liver damage and is a hepatocarcinogen in rodents.		2.0510nitrosaminegeroprotector;
mutagen
androstenedione
Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.		2.442017-oxo steroid;
3-oxo-Delta(4) steroid;
androstanoid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
carbaryl
Carbaryl: A carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries.. carbaryl : A carbamate ester obtained by the formal condensation of 1-naphthol with methylcarbamic acid.		2.0510carbamate ester;
naphthalenes		acaricide;
agrochemical;
carbamate insecticide;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant growth retardant
lactose
Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose.		3.4470lactose
primaquine phosphate
[no description available]		2.0510
methionine
Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.		3.5920aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid		antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical
Mebutamate
[no description available]		2.0510organic molecular entity
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		4.6680alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
gallamine triethiodide
Gallamine Triethiodide: A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)		2.0510
mebanazine
mebanazine: RN given refers to parent cpd without isomeric designation; structure		3.2310benzenes
uracil mustard
Uracil Mustard: Nitrogen mustard derivative of URACIL. It is a alkylating antineoplastic agent that is used in lymphatic malignancies, and causes mainly gastrointestinal and bone marrow damage.		2.0510aminouracil;
nitrogen mustard
oxacillin
Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.		3.2310penicillinantibacterial agent;
antibacterial drug
cycloheximide
Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.		2.9440antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol		anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
egtazic acid
Egtazic Acid: A chelating agent relatively more specific for calcium and less toxic than EDETIC ACID.. ethylene glycol bis(2-aminoethyl)tetraacetic acid : A diether that is ethylene glycol in which the hydrogens of the hydroxy groups have been replaced by 2-[bis(carboxymethyl)amino]ethyl group respectively.		2.4320diether;
tertiary amino compound;
tetracarboxylic acid		chelator
chloroform
Chloroform: A commonly used laboratory solvent. It was previously used as an anesthetic, but was banned from use in the U.S. due to its suspected carcinogenicity.. chloroform : A one-carbon compound that is methane in which three of the hydrogens are replaced by chlorines.		2.0510chloromethanes;
one-carbon compound		carcinogenic agent;
central nervous system drug;
inhalation anaesthetic;
non-polar solvent;
refrigerant
triamcinolone diacetate
triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone		2.0810corticosteroid hormone
norethindrone
Norethindrone: A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.. norethisterone : A 17beta-hydroxy steroid that is testosterone in which the hydrogen at position 17 is replaced by an ethynyl group and in which the methyl group attached to position 10 is replaced by hydrogen.		2.462017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound;
tertiary alcohol		progestin;
synthetic oral contraceptive
norethynodrel
Norethynodrel: A synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and ENDOMETRIOSIS. As a contraceptive (CONTRACEPTIVE AGENTS), it has usually been administered in combination with MESTRANOL.		2.0510oxo steroid
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		3.23104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
benziodarone
benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74)		3.5920aromatic ketone
chlorpromazine hydrochloride
[no description available]		2.0510hydrochloride;
phenothiazines		anticoronaviral agent;
phenothiazine antipsychotic drug
ampicillin
Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.		5.9120beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
mannitol
[no description available]		9.6780mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
cytarabine
[no description available]		4.4160beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
dithionitrobenzoic acid
Dithionitrobenzoic Acid: A standard reagent for the determination of reactive sulfhydryl groups by absorbance measurements. It is used primarily for the determination of sulfhydryl and disulfide groups in proteins. The color produced is due to the formation of a thio anion, 3-carboxyl-4-nitrothiophenolate.. dithionitrobenzoic acid : An organic disulfide that results from the formal oxidative dimerisation of 2-nitro-5-thiobenzoic acid. An indicator used to quantify the number or concentration of thiol groups.		2.5720nitrobenzoic acid;
organic disulfide		indicator
4-toluenesulfonamide
4-toluenesulfonamide: RN given refers to parent cpd. toluene-4-sulfonamide : A sulfonamide that is benzenesulfonamide bearing a methyl group at position 4.		4.91330sulfonamide
histidine
Histidine: An essential amino acid that is required for the production of HISTAMINE.. L-histidine : The L-enantiomer of the amino acid histidine.. histidine : An alpha-amino acid that is propanoic acid bearing an amino substituent at position 2 and a 1H-imidazol-4-yl group at position 3.		2.2110amino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
medroxyprogesterone acetate
[no description available]		2.763020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester		adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
sulfobromophthalein sodium
bromosulfophthalein sodium : An organic sodium salt that is the disodium salt of bromosulfophthalein.. bromosulfophthalein : An organosulfonic acid that consists of phthalide bearing four bromo substituents at positions 4, 5, 6 and 7 as well as two 4-hydroxy-3-sulfophenyl groups both located at position 1.		3.8530organic sodium saltdye
threonine
Threonine: An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.. threonine : An alpha-amino acid in which one of the hydrogens attached to the alpha-carbon of glycine is substituted by a 1-hydroxyethyl group.		2.0210amino acid zwitterion;
aspartate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
threonine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
mestranol
[no description available]		2.462017beta-hydroxy steroid;
aromatic ether;
terminal acetylenic compound		prodrug;
xenoestrogen
methaqualone
Methaqualone: A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604). methaqualone : A member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It became popular as a recreational drug and club drug in the late 1960s and 1970s.		2.0510quinazolinesGABA agonist;
sedative
trypan blue
VisionBlue: A trypan blue ophthalmic solution.		2.0510
chlorquinaldol
Chlorquinaldol: Local anti-infective agent used for skin, gastrointestinal, and vaginal infections with fungi, protozoa, and certain bacteria. In animals, it causes central nervous system damage and is not administered parenterally. It is also used as antiseptic, fungistat, or deodorant.. chlorquinaldol : A monohydroxyquinoline that is quinolin-8-ol which is substituted by a methyl group at position 2 and by chlorine at positions 5 and 7. An antifungal and antibacterial, it was formerly used for topical treatment of skin conditions and vaginal infections.		2.0110monohydroxyquinoline;
organochlorine compound		antibacterial drug;
antiprotozoal drug;
antiseptic drug
cordycepin
[no description available]		2.05103'-deoxyribonucleoside;
adenosines		antimetabolite;
nucleoside antibiotic
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.7530erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
nifenalol
nifenalol: adrenergic beta-blocker with good antiarrhythmic properties; also tends to lower blood pressure & provide protection against angina; minor descriptor (75-86); on-line & INDEX MEDICUS search ETHANOLAMINES (75-86); RN given refers to parent cpd without isomeric designation		2.0610C-nitro compound
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		10.05120arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
ethylamine
ethylamine : A two-carbon primary aliphatic amine.		2.0410primary aliphatic aminehuman metabolite
acetonitrile
acetonitrile: RN given refers to unlabeled cpd. acetonitrile : A nitrile that is hydrogen cyanide in which the hydrogen has been replaced by a methyl group.		2.4220aliphatic nitrile;
volatile organic compound		EC 3.5.1.4 (amidase) inhibitor;
NMR chemical shift reference compound;
polar aprotic solvent
methylene chloride
Methylene Chloride: A chlorinated hydrocarbon that has been used as an inhalation anesthetic and acts as a narcotic in high concentrations. Its primary use is as a solvent in manufacturing and food technology.. dichloromethane : A member of the class of chloromethanes that is methane in which two of the hydrogens have been replaced by chlorine. A dense, non-flammible colourless liquid at room temperature (b.p. 40degreeC, d = 1.33) which is immiscible with water, it is widely used as a solvent, a paint stripper, and for the removal of caffeine from coffee and tea.		2.4620chloromethanes;
volatile organic compound		carcinogenic agent;
polar aprotic solvent;
refrigerant
trifluoroethanol
Trifluoroethanol: A non-aqueous co-solvent that serves as tool to study protein folding. It is also used in various pharmaceutical, chemical and engineering applications.		2.0410fluoroalcohol
trichloroacetic acid
Trichloroacetic Acid: A strong acid used as a protein precipitant in clinical chemistry and also as a caustic for removing warts.. trichloroacetic acid : A monocarboxylic acid that is acetic acid in which all three methyl hydrogens are substituted by chlorine.		2.0510monocarboxylic acid;
organochlorine compound		carcinogenic agent;
metabolite;
mouse metabolite
trifluoroacetic acid
Trifluoroacetic Acid: A very strong halogenated derivative of acetic acid. It is used in acid catalyzed reactions, especially those where an ester is cleaved in peptide synthesis.. trifluoroacetic acid : A monocarboxylic acid that is the trifluoro derivative of acetic acid.		2.0410fluoroalkanoic acidhuman xenobiotic metabolite;
NMR chemical shift reference compound;
reagent
perflutren
Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines.		3.2310fluoroalkane;
fluorocarbon
triamcinolone acetonide
Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections.		7.773011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
cyclic ketal;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
fluoxymesterone
Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women.		3.231011beta-hydroxy steroid;
17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
anabolic androgenic steroid;
fluorinated steroid		anabolic agent;
antineoplastic agent
mepenzolate bromide
[no description available]		2.0410diarylmethane
allylpropymal
allylpropymal: RN given refers to parent cpd. aprobarbital : A member of the class of barbiturates that is pyrimidine-2,4,6(1H,3H,5H)-trione substituted by an isopropyl and a prop-1-en-3-yl group at position 5.		2.0510barbiturates
butobarbital
butobarbital: Butobarbital should be distinguished from Butabarbital (a synonym for Secbutabarbital)		2.0510barbiturates
methsuximide
methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation		3.2310organic molecular entity
tromethamine
Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)		3.8430primary amino compound;
triol		buffer
trichloroethylene
Trichloroethylene: A highly volatile inhalation anesthetic used mainly in short surgical procedures where light anesthesia with good analgesia is required. It is also used as an industrial solvent. Prolonged exposure to high concentrations of the vapor can lead to cardiotoxicity and neurological impairment.. triol : A chemical compound containing three hydroxy groups.		2.4620chloroethenesinhalation anaesthetic;
mouse metabolite
acrylic acid
acrylic acid: RN given refers to parent cpd. acrylic acid : A alpha,beta-unsaturated monocarboxylic acid that is ethene substituted by a carboxy group.		7.1310alpha,beta-unsaturated monocarboxylic acidmetabolite
dichloroacetic acid
[no description available]		2.0310monocarboxylic acid;
organochlorine compound		astringent;
marine metabolite
tetrabromobisphenol a
tetrabromobisphenol A: a brominated flame retardant. 3,3',5,5'-tetrabromobisphenol A : A bromobisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups and the phenyl rings are substituted by bromo groups at positions 2, 2', 6 and 6'. It is a brominated flame retardant.		3.3510brominated flame retardant;
bromobisphenol
bisphenol a
4,4'-isopropylidene diphenol: stimulates proliferative responses and cytokine productions of murine spleen cells and thymus cells in vitro. bisphenol : By usage, the methylenediphenols, HOC6H4CH2C6H4OH, commonly p,p-methylenediphenol, and their substitution products (generally derived from condensation of two equivalent amounts of a phenol with an aldehyde or ketone). The term also includes analogues in the the methylene (or substituted methylene) group has been replaced by a heteroatom.. bisphenol A : A bisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups.		3.3510bisphenolendocrine disruptor;
environmental contaminant;
xenobiotic;
xenoestrogen
dehydrocholic acid
Dehydrocholic Acid: A semisynthetic bile acid made from cholic acid. It is used as a cholagogue, hydrocholeretic, diuretic, and as a diagnostic aid.. 3,7,12-trioxo-5beta-cholanic acid : An oxo-5beta-cholanic acid in which three oxo substituents are located at positions 3, 7 and 12 on the cholanic acid skeleton.		2.051012-oxo steroid;
3-oxo-5beta-steroid;
7-oxo steroid;
oxo-5beta-cholanic acid		gastrointestinal drug
taurocholic acid
Taurocholic Acid: The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.. taurocholate : An organosulfonate oxoanion that is the conjugate base of taurocholic acid.. taurocholic acid : A bile acid taurine conjugate of cholic acid that usually occurs as the sodium salt of bile in mammals.		4.2850amino sulfonic acid;
bile acid taurine conjugate		human metabolite
rhodamine b
rhodamine B: RN & N1 from 9th CI Form Index; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7973; TETRAETHYLRHODAMINE was see RHODAMINES 1975-93; use RHODAMINES to search TETRAETHYLRHODAMINE 1975-93. rhodamine B : An organic chloride salt having N-[9-(2-carboxyphenyl)-6-(diethylamino)-3H-xanthen-3-ylidene]-N-ethylethanaminium as the counterion. An amphoteric dye commonly used as a fluorochrome.		2.0810organic chloride salt;
xanthene dye		fluorescent probe;
fluorochrome;
histological dye
cyclizine
Cyclizine: A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935). cyclizine : An N-alkylpiperazine in which one nitrogen of the piperazine ring is substituted by a methyl group, while the other is substituted by a diphenylmethyl group.		2.0510N-alkylpiperazineantiemetic;
central nervous system depressant;
cholinergic antagonist;
H1-receptor antagonist;
local anaesthetic
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		7.33716-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.9640organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
diquat
Diquat: A contact herbicide used also to produce desiccation and defoliation. (From Merck Index, 11th ed). diquat : The organic cation formed formally by addition of an ethylene bridge between the nitrogen atoms of 2,2'-bipyridine. Most often available as the dibromide.		2.0510organic cationdefoliant;
herbicide
brompheniramine
Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310organobromine compound;
pyridines		anti-allergic agent;
H1-receptor antagonist
penicillin v
Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain.		3.2310penicillin allergen;
penicillin
isosorbide dinitrate
Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action.		4.0840glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
n-vinyl-2-pyrrolidinone
N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source		5.03360pyrrolidin-2-ones
2,4-dinitrobenzenesulfonic acid
2,4-dinitrobenzenesulfonic acid: RN given refers to parent cpd; structure. 2,4-dinitrobenzenesulfonic acid : The arenesulfonic acid that is benzenesulfonic acid with two nitro substituents in the 2- and 4-positions.		210arenesulfonic acid;
C-nitro compound
pseudoephedrine
Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group.		3.2310phenylethanolamines;
secondary alcohol;
secondary amino compound		anti-asthmatic drug;
bronchodilator agent;
central nervous system drug;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
diethylpropion
Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity.		3.2310aromatic ketone;
tertiary amine		appetite depressant
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		2.4420mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
quinoline
[no description available]		2.0410azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinolines
2-naphthylamine
2-Naphthylamine: A naphthalene derivative with carcinogenic action.. 2-naphthylamine : A naphthylamine carrying the amino group at position 2.		2.0610naphthylaminecarcinogenic agent
phenothiazine
10H-phenothiazine : The 10H-tautomer of phenothiazine.		2.0510phenothiazineferroptosis inhibitor;
plant metabolite;
radical scavenger
synephrine
[no description available]		2.0510ethanolamines;
phenethylamine alkaloid;
phenols		alpha-adrenergic agonist;
plant metabolite
benzoyl peroxide
Benzoyl Peroxide: A peroxide derivative that has been used topically for BURNS and as a dermatologic agent in the treatment of ACNE and POISON IVY DERMATITIS. It is used also as a bleach in the food industry.		2.0510carbonyl compound
benzothiazole
benzothiazole: structure. benzothiazole : An organic heterobicyclic compound that is a fusion product between benzene and thiazole. The parent of the class of benzothiazoles.		2.110benzothiazolesenvironmental contaminant;
plant metabolite;
xenobiotic
2-bromophenol
bromophenol : A halophenol that is any phenol containing one or more covalently bonded bromine atoms.		2.0510bromophenolmarine metabolite
4-butyrolactone
4-Butyrolactone: One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.. tetrahydrofuranone : Any oxolane having an oxo- substituent at any position on the tetrahydrofuran ring.. gamma-butyrolactone : A butan-4-olide that is tetrahydrofuran substituted by an oxo group at position 2.		2.1310butan-4-olidemetabolite;
neurotoxin
benzenearsonic acid
benzenearsonic acid: RN given refers to parent cpd; structure		2.0610arsonic acids;
organoarsonic acid
benzenesulfonamide
[no description available]		2.0710sulfonamide
3-aminobenzotrifluoride
[no description available]		2.0410
3-trifluoromethylphenol
3-trifluoromethylphenol: structure in first source		2.0410(trifluoromethyl)benzenes
nitrobenzene
nitrobenzene : A nitroarene consisting of benzene carrying a single nitro substituent. An industrial chemical used widely in the production of aniline.		2.0810nitroarene;
nitrobenzenes
methyl gallate
methyl gallate: has both immunosuppressive and phytogenic antineoplastic activities; isolated from Acer saccharinum. methyl 3,4,5-trihydroxybenzoate : A gallate ester obtained by the formal condensation of gallic acid with methanol. It exhibits anti-oxidant, anti-tumor, anti-microbial and anti-inflammatory properties.		2.110gallate esteranti-inflammatory agent;
antioxidant;
plant metabolite
quinuclidines
Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.		2.0510quinuclidines;
saturated organic heterobicyclic parent
pyridostigmine bromide
Pyridostigmine Bromide: A cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.		2.0510pyridinium salt
4,4'-diaminodiphenylmethane
4,4'-diaminodiphenylmethane: RN given refers to parent cpd; structure. 4,4'-diaminodiphenylmethane : An aromatic amine that is diphenylmethane substituted at the 4-position of each benzene ring by an amino group.		2.4620aromatic amineallergen;
carcinogenic agent
monobenzone
monobenzone: structure. monobenzone : The monobenzyl ether of hydroquinone. It is used as a topical drug for medical depigmentation.		2.0810benzyl etherallergen;
dermatologic drug;
melanin synthesis inhibitor
phenylisothiocyanate
phenylisothiocyanate: structure. phenyl isothiocyanate : An isothiocyanate having a phenyl group attached to the nitrogen; used for amino acid sequencing in the Edman degradation.		2.0510isothiocyanateallergen;
reagent
benzonatate
benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant.		3.2310benzoate ester;
secondary amino compound;
substituted aniline		anaesthetic;
antitussive
caprolactam
Caprolactam: Cyclic amide of caproic acid used in manufacture of synthetic fibers of the polyamide type. Can cause local irritation.. epsilon-caprolactam : A member of the class of caprolactams that is azepane substituted by an oxo group at position 2.		7.1310caprolactamshuman blood serum metabolite
4-bromophenol
4-bromophenol : A bromophenol containing only hydroxy and bromo substituents that are para to one another.		2.0510bromophenolhuman urinary metabolite;
human xenobiotic metabolite;
marine metabolite;
mouse metabolite;
persistent organic pollutant;
rat metabolite
2-bromoethylamine
[no description available]		2.0510
propylamine
propylamine : A member of the class of alkylamines that is propane substituted by an amino group at C-1.		2.0410alkylamines
allyl alcohol
allyl alcohol: structure. allylic alcohol : An alcohol where the hydroxy group is attached to a saturated carbon atom adjacent to a double bond (R groups may be H, organyl, etc.).. allyl alcohol : A propenol in which the C=C bond connects C-2 and C-3. It is has been found in garlic (Allium sativum). Formerly used as a herbicide for the control of various grass and weed seeds.		2.0510primary allylic alcohol;
propenol		antibacterial agent;
fungicide;
herbicide;
insecticide;
plant metabolite
dimethyldioctadecylammonium
dimethyldioctadecylammonium: a cationic lipid analog; RN given refers to parent cpd		2.2510
vinyl acetate
[no description available]		2.5220acetate ester
bromobenzene
[no description available]		2.0510bromoarene;
bromobenzenes;
volatile organic compound		hepatotoxic agent;
mouse metabolite;
non-polar solvent
cyclohexanol
Cyclohexanols: Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.. cyclohexanols : An alcohol in which one or more hydroxy groups are attached to a cyclohexane skeleton.		3.5520cyclohexanols;
secondary alcohol		solvent
n-pentanoic acid
n-pentanoic acid: RN given refers to unlabeled parent cpd. valeric acid : A straight-chain saturated fatty acid containing five carbon atoms.		2.0510short-chain fatty acid;
straight-chain saturated fatty acid		plant metabolite
n-butylamine
n-butylamine: RN given refers to parent cpd. butan-1-amine : A primary aliphatic amine that is butane substituted by an amino group at position 1.		2.0410primary aliphatic amine
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		8.87353pyrrole;
secondary amine
furan
furan : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing four carbons and one oxygen, with formula C4H4O. It is a toxic, flammable, low-boiling (31degreeC) colourless liquid.		2.0510furans;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		carcinogenic agent;
hepatotoxic agent;
Maillard reaction product
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		8.52131mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
isopropyl myristate
isopropyl myristate: used for microemulsions; structure		2.0210fatty acid ester
piperidine
[no description available]		2.0410azacycloalkane;
piperidines;
saturated organic heteromonocyclic parent;
secondary amine		base;
catalyst;
human metabolite;
non-polar solvent;
plant metabolite;
protic solvent;
reagent
morpholine
[no description available]		2.1110morpholines;
saturated organic heteromonocyclic parent		NMR chemical shift reference compound
carbitol
carbitol: used as lubricating oil & in braking fluid, structure. diethylene glycol monoethyl ether : A primary alcohol that is ethanol substituted by a 2-ethoxyethoxy group at position 2.		2.1110diether;
glycol ether;
hydroxypolyether;
primary alcohol		protic solvent
ergotamine
Ergotamine: A vasoconstrictor found in ergot of Central Europe. It is a serotonin agonist that has been used as an oxytocic agent and in the treatment of MIGRAINE DISORDERS.. ergotamine : A peptide ergot alkaloid that is dihydroergotamine in which a double bond replaces the single bond between positions 9 and 10.		2.4520peptide ergot alkaloidalpha-adrenergic agonist;
mycotoxin;
non-narcotic analgesic;
oxytocic;
serotonergic agonist;
vasoconstrictor agent
methylergonovine
Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed)		3.2310ergoline alkaloid
imipramine hydrochloride
[no description available]		2.0510hydrochlorideantidepressant
neostigmine bromide
neostigmine bromide : The bromide salt of neostigmine.		2.4520bromide salt
phenformin
Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.		2.9840biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent
mephobarbital
Mephobarbital: A barbiturate that is metabolized to PHENOBARBITAL. It has been used for similar purposes, especially in EPILEPSY, but there is no evidence mephobarbital offers any advantage over PHENOBARBITAL.. mephobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by ethyl and phenyl groups.		2.4620barbituratesanticonvulsant
edrophonium chloride
edrophonium chloride : The chloride salt of edrophonium. A reversible inhibitor of cholinesterase with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes), it is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.		2.0510chloride salt;
quaternary ammonium salt		antidote;
diagnostic agent;
EC 3.1.1.8 (cholinesterase) inhibitor
hexachlorobenzene
Hexachlorobenzene: An agricultural fungicide and seed treatment agent.. hexachlorobenzene : A member of the class of chlorobenzenes that is benzene in which all of the hydrogens are replaced by chlorines. An agricultural fungicide introduced in the mid-1940s and formerly used as a seed treatment, its use has been banned since 1984 under the Stockholm Convention on Persistent Organic Pollutants.		2.0510aromatic fungicide;
chlorobenzenes		antifungal agrochemical;
carcinogenic agent;
persistent organic pollutant
trinitrotoluene
Trinitrotoluene: A 2,4,6-trinitrotoluene, which is an explosive chemical that can cause skin irritation and other toxic consequences.. 2,4,6-trinitrotoluene : A trinitrotoluene having the nitro groups at positions 2, 4 and 6.		2.0510trinitrotolueneexplosive
framycetin
Framycetin: A component of NEOMYCIN that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed). framycetin : A tetracyclic antibacterial agent derived from neomycin, being a glycoside ester of neamine and neobiosamine B.		2.0510aminoglycosideallergen;
antibacterial drug;
Escherichia coli metabolite
pyrazolanthrone
pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.		2.9540anthrapyrazole;
aromatic ketone;
cyclic ketone		antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector
di-n-pentyl phthalate
dipentyl phthalate : A phthalate ester that is the dipentyl ester of benzene-1,2-dicarboxylic acid.		2.0510diester;
phthalate ester		plasticiser
meglumine
Meglumine: 1-Deoxy-1-(methylamino)-D-glucitol. A derivative of sorbitol in which the hydroxyl group in position 1 is replaced by a methylamino group. Often used in conjunction with iodinated organic compounds as contrast medium.. N-methylglucamine : A hexosamine that is D-glucitol in which the hydroxy group at position 1 is substituted by the nitrogen of a methylamino group. A crystalline base, it is used in preparing salts of certain acids for use as diagnostic radiopaque media, while its antimonate is used as an antiprotozoal in the treatment of leishmaniasis.		3.2960hexosamine;
secondary amino compound
cinchophen
cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94		4.0840quinolines
indolebutyric acid
indolebutyric acid: RN given refers to parent cpd. indole-3-butyric acid : A indol-3-yl carboxylic acid that is butanoic acid carrying a 1H-indol-3-yl substituent at position 1.		3.2710indol-3-yl carboxylic acidauxin;
plant hormone;
plant metabolite
neoprontosil
neoprontosil: RN given refers to parent cpd		2.0310
phenazopyridine hydrochloride
phenazopyridine hydrochloride : A hydrochloride obtained by combining phenazopyridine with one equivalent of hydrochloric acid. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.		2.0510hydrochloridecarcinogenic agent;
local anaesthetic;
non-narcotic analgesic
tetrracaine hydrochloride
leocaine: a crystal beta-modification of the beta-dimethylaminoethyl ether of n-butylaminobenzoic acid hydrochloride		2.0510benzoate ester
carzenide
[no description available]		4.91330sulfonamide
pregnenolone
[no description available]		3.171020-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
C21-steroid		human metabolite;
mouse metabolite
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		2.0510methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
diphenhydramine hydrochloride
Antitussive Agents: Agents that suppress cough. They act centrally on the medullary cough center. EXPECTORANTS, also used in the treatment of cough, act locally.. diphenhydramine hydrochloride : The hydrochloride salt of diphenhydramine.		2.7430hydrochloride;
organoammonium salt		anti-allergic agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
sedative
nafcillin
Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group.		3.2310penicillin allergen;
penicillin		antibacterial drug
ditiocarb
Ditiocarb: A chelating agent that has been used to mobilize toxic metals from the tissues of humans and experimental animals. It is the main metabolite of DISULFIRAM.. diethyldithiocarbamic acid : A member of the class of dithiocarbamic acids that is diethylcarbamic acid in which both of the oxygens are replaced by sulfur.		2.0310dithiocarbamic acidschelator;
copper chelator
mequinol
mequinol: depigmenting agent; RN given refers to parent cpd		2.0510methoxybenzenes;
phenols		metabolite
methohexital
Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups.		3.2310acetylenic compound;
barbiturates		drug allergen;
intravenous anaesthetic
quinestrol
Quinestrol: The 3-cyclopentyl ether of ETHINYL ESTRADIOL. After gastrointestinal absorption, it is stored in ADIPOSE TISSUE, slowly released, and metabolized principally to the parent compound. It has been used in ESTROGEN REPLACEMENT THERAPY. (From AMA Drug Evaluations Annual, 1992, p1011)		2.051017-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
dydrogesterone
[no description available]		2.051020-oxo steroid;
3-oxo-Delta(4) steroid		progestin
catechin
Catechin: An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.. catechin : Members of the class of hydroxyflavan that have a flavan-3-ol skeleton and its substituted derivatives.. rac-catechin : A racemate comprising equimolar amounts of (+)- and (-)-catechin. (+)-catechin : The (+)-enantiomer of catechin and a polyphenolic antioxidant plant metabolite.		9.5570catechinantioxidant;
plant metabolite
tripelennamine hydrochloride
[no description available]		2.0510
homoarginine
L-homoarginine : An L-lysine derivative that is the L-enantiomer of homoarginine.		2.0110homoarginine;
L-lysine derivative;
non-proteinogenic L-alpha-amino acid		biomarker;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
human metabolite;
rat metabolite;
xenobiotic metabolite
perylene
Perylene: A 20-carbon dibenz(de,kl)anthracene that can be viewed as a naphthalene fused to a phenalene or as dinaphthalene. It is used as fluorescent lipid probe in the cytochemistry of membranes and is a polycyclic hydrocarbon pollutant in soil and water. Derivatives may be carcinogenic.. perylene : An ortho- and peri-fused polycyclic arene comprising of five benzene rings that is anthracene in which the d,e and k,l sides are fused to benzene rings.		2.4320ortho- and peri-fused polycyclic arene;
perylenes
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		13.024412azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
acridines
Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.		2.4920acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene		genotoxin
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		4.0840indazole
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		21.159814isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		12.136391,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
1,2,4-triazole
1,2,4-triazole: RN given refers to 1H-1,2,4-triazole		2.41101,2,4-triazole
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		5.7471diazine;
pyrazines		Daphnia magna metabolite
ethynodiol diacetate
Ethynodiol Diacetate: A synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive (CONTRACEPTIVES, ORAL).		2.0510steroid ester;
terminal acetylenic compound		contraceptive drug;
estrogen receptor modulator;
synthetic oral contraceptive
nitroblue tetrazolium
Nitroblue Tetrazolium: Colorless to yellow dye that is reducible to blue or black formazan crystals by certain cells; formerly used to distinguish between nonbacterial and bacterial diseases, the latter causing neutrophils to reduce the dye; used to confirm diagnosis of chronic granulomatous disease.		2.0310organic cation
ephedrine
Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively.		3.5920phenethylamine alkaloid;
phenylethanolamines		bacterial metabolite;
environmental contaminant;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
hydrazine
diamine : Any polyamine that contains two amino groups.		2.7430azane;
hydrazines		EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
chlormadinone acetate
Chlormadinone Acetate: An orally active synthetic progestational hormone used often in combinations as an oral contraceptive (CONTRACEPTIVES, ORAL).		2.0510corticosteroid hormone
pirinitramide
Pirinitramide: A diphenylpropylamine with intense narcotic analgesic activity of long duration. It is a derivative of MEPERIDINE with similar activity and usage.		4.3111nitrile
2,3-dimercaptosuccinic acid
[no description available]		2.0510
evans blue
Evans Blue: An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly.. Evans blue : An organic sodium salt that is the tetrasodium salt of 6,6'-{(3,3'-dimethyl[1,1'-biphenyl]-4,4'-diyl)bis[diazene-2,1-diyl]}bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate). It is sometimes used as a counterstain, especially in fluorescent methods to suppress background autofluorescence.		2.4420organic sodium saltfluorochrome;
histological dye;
sodium channel blocker;
teratogenic agent
monocrotaline
Monocrotaline: A pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes are noted after oral magnesium treatment.		7.4520pyrrolizidine alkaloid
testosterone enanthate
[no description available]		2.0510heptanoate ester;
sterol ester		androgen
aminophylline
Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio.		3.8730mixturebronchodilator agent;
cardiotonic drug
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		4.0940N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
phenyramidol
phenyramidol: considered as a drug that possibly causes hepatotoxicity		2.0510aminopyridine
flurothyl
Flurothyl: A convulsant primarily used in experimental animals. It was formerly used to induce convulsions as a alternative to electroshock therapy.		7.0310ether
carbutamide
Carbutamide: A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277)		2.0510benzenes;
sulfonamide
pseudoephedrine hydrochloride
pseudoephedrine hydrochloride : A hydrochloride that is the monohydrochloride salt of pseudoephedrine.		2.0510hydrochlorideplant metabolite
2-fluoroaniline
2-fluoroaniline: structure given in first source; RN given refers to parent compound. 2-fluoroaniline : A derivative of aniline in which the hydrogen at position 2 has been substituted by fluorine. It is used as a pharmaceutical intermediate		2.0410fluoroaniline;
primary arylamine
galantamine
Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils.		4.4230benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound		antidote to curare poisoning;
cholinergic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant metabolite
nandrolone decanoate
Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS.		3.5920steroid ester
bucladesine
[no description available]		2.05103',5'-cyclic purine nucleotide;
butanamides;
butyrate ester		agonist;
cardiotonic drug;
vasodilator agent
procarbazine hydrochloride
procarbazine hydrochloride : A hydrochloride obtained by combining procarbazine with one equivalent of hydrochloric acid. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.4720hydrochlorideantineoplastic agent
2-fluorophenol
fluorophenol : A halophenol that is any phenol containing one or more covalently bonded fluorine atoms.		2.0410
cuprizone
[no description available]		2.0710organonitrogen compound;
organooxygen compound
4-fluoroaniline
4-fluoroaniline: chemical intermediate manufactured by the Halex process; RN given refers to parent cpd; structure given in first source. 4-fluoroaniline : A primary arylamine that is the derivative of aniline in which the hydrogen at position 4 has been substituted by fluorine. It is used as an intermediate in the manufacture of pharmaceuticals, herbicides and plant growth regulators.		2.0410fluoroaniline;
primary arylamine
4-fluorophenol
4-fluorophenol: structure given in first source. 4-fluorophenol : A fluorophenol that is phenol in which the hydrogen para- to the hydroxy group has been replaced by a fluorine.		2.0410fluorophenol;
monofluorobenzenes
3-fluoroaniline
3-fluoroaniline: structure given in first source. 3-fluoroaniline : A derivative of aniline in which the hydrogen at position 3 has been substituted by fluorine. It is used as a pharmaceutical intermediate.		2.0410fluoroaniline;
primary arylamine
3-fluorophenol
3-fluorophenol: structure in first source		2.0410
2-fluoropyridine
[no description available]		2.0410
trifluoroethylamine
trifluoroethylamine: RN given refers to cpd with unspecified fluorine locants		2.0410
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.763011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
difluoroacetic acid
[no description available]		2.0410monocarboxylic acid;
organofluorine compound
perflubron
perflubron: potential anti-obesity compound; reduces food adsorption; 8-carbon perfluorocarbon radiopaque compound; an oral contrast agent for use with MRI to enhance delineation of the bowel distinguishing it from adjacent organs. perflubron : A haloalkane that is perfluorooctane in which a fluorine attached to one of the terminal carbons has been replaced by a bromine.		2.0510haloalkane;
organobromine compound;
perfluorinated compound		blood substitute;
radioopaque medium
cyproterone acetate
[no description available]		2.462020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
chlorinated steroid;
steroid ester		androgen antagonist;
geroprotector;
progestin
lithocholic acid
Lithocholic Acid: A bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.. lithocholic acid : A monohydroxy-5beta-cholanic acid with a alpha-hydroxy substituent at position 3. It is a bile acid obtained from chenodeoxycholic acid by bacterial action.. lithocholate : A bile acid anion that is the conjugate base of lithocholic acid.		2.0510bile acid;
C24-steroid;
monohydroxy-5beta-cholanic acid		geroprotector;
human metabolite;
mouse metabolite
nandrolone
Nandrolone: C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position.. nandrolone : A 3-oxo Delta(4)-steroid that is estr-4-en-3-one substituted by a beta-hydroxy group at position 17.		2.442017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
anabolic androgenic steroid		human metabolite
2-fluorobenzoic acid
2-fluorobenzoic acid: RN given refers to parent cpd. 2-fluorobenzoic acid : A 2-halobenzoic acid that is benzoic acid carrying a fluoro substituent at position 2.. fluorobenzoic acid : Any benzoic acid carrying at least one fluoro substituent on the benzene ring. Fluorobenzoic acids are important intermediates in the synthesis of antibacterial drugs.		2.04102-halobenzoic acid;
fluorobenzoic acid
2-aminopurine
2-Aminopurine: A purine that is an isomer of ADENINE (6-aminopurine).. aminopurine : Any purine having at least one amino substituent.. 2-aminopurine : The parent compound of the 2-aminopurines, comprising a purine core carrying an amino substituent at the 2-position.		2.17102-aminopurines;
nucleobase analogue		antimetabolite
4-trifluoromethylaniline
4-trifluoromethylaniline : A substituted aniline that is a benzene ring substituted with an amino group at position 1 and a trifluoromethyl group at position 4.		2.0410(trifluoromethyl)benzenes;
substituted aniline		metabolite
3-fluorobenzoic acid
[no description available]		2.0410fluorobenzoic acid
4-fluorobenzoic acid
[no description available]		2.0410fluorobenzoic acidbacterial xenobiotic metabolite
2-fluoroethylamine
2-fluoroethylamine: structure in first source		2.0410
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		210imidazolidine-2,4-dione
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		4.4122monofluorobenzenesNMR chemical shift reference compound
dextropropoxyphene
Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene.		5.46411-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoatemu-opioid receptor agonist;
opioid analgesic
limestone
Calcium Carbonate: Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.. calcium carbonate : A calcium salt with formula CCaO3.		2.0810calcium salt;
carbonate salt;
inorganic calcium salt;
one-carbon compound		antacid;
fertilizer;
food colouring;
food firming agent
glycyrrhetinic acid
[no description available]		2.0510cyclic terpene ketone;
hydroxy monocarboxylic acid;
pentacyclic triterpenoid		immunomodulator;
plant metabolite
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		4.0840bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
glycocholic acid
Glycocholic Acid: The glycine conjugate of CHOLIC ACID. It acts as a detergent to solubilize fats for absorption and is itself absorbed.. glycocholic acid : A bile acid glycine conjugate having cholic acid as the bile acid component.. glycocholate : A cholanic acid conjugate anion that is the conjugate base of glycocholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		2.0710bile acid glycine conjugatehuman metabolite
fusarium
Fusarium: A mitosporic Hypocreales fungal genus, various species of which are important parasitic pathogens of plants and a variety of vertebrates. Teleomorphs include GIBBERELLA.		2.2510
epitestosterone
Epitestosterone: The 17-alpha isomer of TESTOSTERONE, derived from PREGNENOLONE via the delta5-steroid pathway, and via 5-androstene-3-beta,17-alpha-diol. Epitestosterone acts as an antiandrogen in various target tissues. The ratio between testosterone/epitestosterone is used to monitor anabolic drug abuse.. epitestosterone : An androstanoid that is the C-17 epimer of testosterone.		2.111017alpha-hydroxy steroid;
3-oxo-Delta(4) steroid;
androstanoid		androgen antagonist;
human metabolite
plumbagin
plumbagin: a superoxide anion generator. plumbagin : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively.		2.5520hydroxy-1,4-naphthoquinone;
phenols		anticoagulant;
antineoplastic agent;
immunological adjuvant;
metabolite
chrysophanic acid
chrysophanic acid: RN given refers to parent cpd; structure in Merck, 9th ed, #2260. chrysophanol : A trihydroxyanthraquinone that is chrysazin with a methyl substituent at C-3. It has been isolated from Aloe vera and exhibits antiviral and anti-inflammatory activity.		2.110dihydroxyanthraquinoneanti-inflammatory agent;
antiviral agent;
plant metabolite
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.0810isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
osthol
osthol: from Cnidium monnieri and Angelica pubescens (both Apiaceae); structure given in first source		2.1510botanical anti-fungal agent;
coumarins		metabolite
dihydralazine
Dihydralazine: 1,4-Dihydrazinophthalazine. An antihypertensive agent with actions and uses similar to those of HYDRALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p354)		2.0510phthalazines
oxycinchophen
[no description available]		2.0310quinolines
kainic acid
Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.		8.1350dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid		antinematodal drug;
excitatory amino acid agonist
phenylpropanolamine
Phenylpropanolamine: A sympathomimetic that acts mainly by causing release of NOREPINEPHRINE but also has direct agonist activity at some adrenergic receptors. It is most commonly used as a nasal vasoconstrictor and an appetite depressant.. phenylpropanolamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group. A decongestant and appetite suppressant, it is commonly used in prescription and over-the-counter cough and cold preparations.. (-)-norephedrine : An amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1R,2S-stereoisomer). It is a plant alkaloid.		2.0510amphetamines;
phenethylamine alkaloid		plant metabolite
4-hydroxybutyric acid
4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group.		3.23104-hydroxy monocarboxylic acid;
hydroxybutyric acid		general anaesthetic;
GHB receptor agonist;
neurotoxin;
sedative
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		4.2231
thiazolidines
Thiazolidines: Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES.		3.4260thiazolidine
mustard gas
Mustard Gas: Severe irritant and vesicant of skin, eyes, and lungs. It may cause blindness and lethal lung edema and was formerly used as a war gas. The substance has been proposed as a cytostatic and for treatment of psoriasis. It has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP-85-002, 1985) (Merck, 11th ed).. bis(2-chloroethyl) sulfide : An ethyl sulfide that is diethyl sulfide in which a hydrogen from each of the terminal methyl groups is replaced by a chlorine. It is a powerful vesicant regulated under the Chemical Weapons Convention.		2.0210ethyl sulfide;
organochlorine compound		alkylating agent;
carcinogenic agent;
vesicant
oleanolic acid
[no description available]		2.3110hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
dihydroergotamine
Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension.		3.5920ergot alkaloid;
semisynthetic derivative		dopamine agonist;
non-narcotic analgesic;
serotonergic agonist;
sympatholytic agent;
vasoconstrictor agent
hematoxylin
Hematoxylin: A dye obtained from the heartwood of logwood (Haematoxylon campechianum Linn., Leguminosae) used as a stain in microscopy and in the manufacture of ink.		2.4110organic heterotetracyclic compound;
oxacycle;
polyphenol;
tertiary alcohol		histological dye;
plant metabolite
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.4720furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
hesperidin
Hesperidin: A flavanone glycoside found in CITRUS fruit peels.. hesperidin : A disaccharide derivative that consists of hesperetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.		2.51203'-hydroxyflavanones;
4'-methoxyflavanones;
dihydroxyflavanone;
disaccharide derivative;
flavanone glycoside;
monomethoxyflavanone;
rutinoside		mutagen
medroxyprogesterone
[no description available]		11.25217alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		contraceptive drug;
progestin;
synthetic oral contraceptive
androstenediol
Androstenediol: An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES).. androst-5-ene-3beta,17beta-diol : A 3beta-hydroxy-Delta(5)-steroid that is 3beta-hydroxyandrost-5-ene carrying an additional hydroxy group at position 17beta.		2.111017beta-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid		androgen;
human metabolite;
mouse metabolite;
radiation protective agent
dimenhydrinate
gravinol: has antioxidant and ant-inflammatory activities; structure in first source		3.6120diarylmethane
chlormethiazole
Chlormethiazole: A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors.		2.0510thiazoles
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		3.8530amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
levocarnitine
(R)-carnitine : The (R)-enantiomer of carnitine.		3.2310carnitineantilipemic drug;
nootropic agent;
nutraceutical;
Saccharomyces cerevisiae metabolite;
water-soluble vitamin (role)
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		5.58161dialdehydebiomarker
magnesium carbonate
magnesium carbonate: RN given refers to parent cpd (1:1). magnesium carbonate : A magnesium salt with formula CMgO3. Its hydrated forms, particularly the di-, tri-, and tetrahydrates occur as minerals.		2.9330carbonate salt;
magnesium salt;
one-carbon compound;
organic magnesium salt		antacid;
fertilizer
sulfanilylurea
sulfanilylurea: antimicrobial agent; structure		3.2310benzenes;
sulfonamide
trinitrobenzenesulfonic acid
Trinitrobenzenesulfonic Acid: A reagent that is used to neutralize peptide terminal amino groups.. 2,4,6-trinitrobenzenesulfonic acid : The arenesulfonic acid that is benzenesulfonic acid with three nitro substituents in the 2-, 4- and 6-positions.		2.9640arenesulfonic acid;
C-nitro compound		epitope;
explosive;
reagent
eosine yellowish-(ys)
Eosine Yellowish-(YS): A versatile red dye used in cosmetics, pharmaceuticals, textiles, etc., and as tissue stain, vital stain, and counterstain with HEMATOXYLIN. It is also used in special culture media.. eosin YS dye : An organic sodium salt that is 2',4',5',7'-tetrabromofluorescein in which the carboxy group and the phenolic hydroxy group have been deprotonated and the resulting charge is neutralised by two sodium ions.		2.4110organic sodium salt;
organobromine compound		fluorochrome;
histological dye
gentian violet
Gentian Violet: A dye that is a mixture of violet rosanilinis with antibacterial, antifungal, and anthelmintic properties.. crystal violet : An organic chloride salt that is the monochloride salt of crystal violet cation. It has been used in creams for the topical treatment of bacterial and fungal infections, being effective against some Gram-positive bacteria (notably Staphylococcus species) and some pathogenic fungi (including Candida species) but use declined following reports of animal carcinogenicity. It has also been used for dying wood, silk, and paper, as well as a histological stain.		2.0510organic chloride saltanthelminthic drug;
antibacterial agent;
antifungal agent;
antiseptic drug;
histological dye
amitriptyline hydrochloride
[no description available]		2.0510organic tricyclic compound
1-naphthylisothiocyanate
1-Naphthylisothiocyanate: A tool for the study of liver damage which causes bile stasis and hyperbilirubinemia acutely and bile duct hyperplasia and biliary cirrhosis chronically, with changes in hepatocyte function. It may cause skin and kidney damage.		2.4720isothiocyanateinsecticide
paeonol
paeonol: structure		2.5220methoxybenzenes;
phenols		metabolite
hematoporphyrin
Hematoporphyrins: Iron-free derivatives of heme with 4 methyl groups, 2 hydroxyethyl groups and 2 propionic acid groups attached to the pyrrole rings. Some of these PHOTOSENSITIZING AGENTS are used in the PHOTOTHERAPY of malignant NEOPLASMS.. hematoporphyrin : A dicarboxylic acid that is protoporphyrin in which the vinyl groups at positions 7 and 12 are replaced by 1-hydroxyethyl groups.		2.0510
lithium carbonate
Lithium Carbonate: A lithium salt, classified as a mood-stabilizing agent. Lithium ion alters the metabolism of BIOGENIC MONOAMINES in the CENTRAL NERVOUS SYSTEM, and affects multiple neurotransmission systems.		4.9620carbonate salt;
lithium salt		antimanic drug
formestane
[no description available]		2.462017-oxo steroid;
3-oxo-Delta(4) steroid;
enol;
hydroxy steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
lactulose
[no description available]		3.5920glycosylfructosegastrointestinal drug;
laxative
isoxsuprine hydrochloride
[no description available]		2.0510alkylbenzene
betaine hydrochloride
[no description available]		2.0510
megestrol acetate
[no description available]		6.45320-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
n,n-dimethylethylamine
[no description available]		2.0410
pamabrom
[no description available]		3.2310
1,3-indandione
1,3-indandione : A member of the class of indanones that is indane in which the hydrogens at positions 2 and 4 have been replaced by oxo groups.		2.0410aromatic ketone;
beta-diketone;
indanones
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		7.28121acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
3-hydroxyacetanilide
metacetamol : A derivative of phenol which has an acetamido substituent located meta to the phenolic -OH group. It is a non-toxic regioisomer of paracetamol with analgesic properties, but has never been marketed as a drug.		2.0510acetamides;
phenols		non-narcotic analgesic
methoxyacetic acid
methoxyacetic acid: RN given refers to parent cpd. methoxyacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a methoxy group.		2.0510ether;
monocarboxylic acid		antineoplastic agent;
apoptosis inducer;
human xenobiotic metabolite;
mutagen
Berberine chloride (TN)
[no description available]		3.1510organic molecular entity
glycochenodeoxycholic acid
Glycochenodeoxycholic Acid: A bile salt formed in the liver from chenodeoxycholate and glycine, usually as the sodium salt. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is a cholagogue and choleretic.. glycochenodeoxycholate : A N-acylglycinate that is the conjugate base of glycochenodeoxycholic acid.. glycochenodeoxycholic acid : A bile acid glycine conjugate having 3alpha,7alpha-dihydroxy-5beta-cholan-24-oyl as the bile acid component.		2.0710bile acid glycine conjugatehuman metabolite
erythromycin stearate
[no description available]		2.0510aminoglycoside
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		4.6780cyclic ketone;
erythromycin
dehydroepiandrosterone sulfate
Dehydroepiandrosterone Sulfate: The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.. dehydroepiandrosterone sulfate : A steroid sulfate that is the 3-sulfooxy derivative of dehydroepiandrosterone.		3.552017-oxo steroid;
steroid sulfate		EC 2.7.1.33 (pantothenate kinase) inhibitor;
human metabolite;
mouse metabolite
dihydroequilin
dihydroequilin: RN given refers to (17alpha)-isomer		2.1110
isosorbide
Isosorbide: 1,4:3,6-Dianhydro D-glucitol. Chemically inert osmotic diuretic used mainly to treat hydrocephalus; also used in glaucoma.		3.4511organic molecular entity
2-piperidone
2-piperidone: structure given in first source. piperidin-2-one : A delta-lactam that is piperidine which is substituted by an oxo group at position 2.		2.1510delta-lactam;
piperidones		EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor
methylnitrosourea
Methylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-methyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.		3.4270N-nitrosoureasalkylating agent;
carcinogenic agent;
mutagen;
teratogenic agent
hydroxychloroquine sulfate
[no description available]		2.4920
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		5.263117beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
vinblastine
[no description available]		4.460
diphenoxylate
Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin.		3.2310ethyl ester;
nitrile;
piperidinecarboxylate ester;
tertiary amine		antidiarrhoeal drug
1-methylpyridinium
1-methylpyridinium: RN given refers to parent cpd		3.5720methylpyridines
salicyl hydrazide
2-hydroxybenzohydrazide: structure in first source		2.110
deoxycytidine
[no description available]		14.234522pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
cyproheptadine hydrochloride (anhydrous)
cyproheptadine hydrochloride (anhydrous) : The hydrochloride salt of cyproheptadine. Note that the drug named cyproheptadine hydrochloride generally refers to cyproheptadine hydrochloride sesquihydrate.		2.0510hydrochloride
estradiol valerate
[no description available]		2.0510steroid ester
rhodamine 6g
rhodamine 6G: RN given refers to HCl		2.0310
hexamethylsilazane
hexamethylsilazane: RN given refers to parent cpd		2.0310N-silyl compoundchromatographic reagent
ethambutol hydrochloride
ethambutol dihydrochloride : The dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone.		2.0810hydrochlorideantitubercular agent
ethambutol
Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.		3.5820ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
durapatite
Durapatite: The mineral component of bones and teeth; it has been used therapeutically as a prosthetic aid and in the prevention and treatment of osteoporosis.. hydroxylapatite : A phosphate mineral with the formula Ca5(PO4)3(OH).		2.8130
sodium hydroxide
Sodium Hydroxide: A highly caustic substance that is used to neutralize acids and make sodium salts. (From Merck Index, 11th ed)		2.4110alkali metal hydroxide
arsenic trioxide
Arsenic Trioxide: An inorganic compound with the chemical formula As2O3 that is used for the treatment of ACUTE PROMYELOCYTIC LEUKEMIA in patients who have relapsed from, or are resistant to, conventional drug therapy.		2.0810
hydrofluoric acid
Hydrofluoric Acid: Hydrofluoric acid. A solution of hydrogen fluoride in water. It is a colorless fuming liquid which can cause painful burns.. hydrogen fluoride : A diatomic molecule containing covalently bonded hydrogen and fluorine atoms.. organofluorine compound : An organofluorine compound is a compound containing at least one carbon-fluorine bond.		2.4920hydrogen halide;
mononuclear parent hydride		NMR chemical shift reference compound
sorbitan monostearate
sorbitan monostearate: Stearic Acid was the HM (74-82), no longer an active MH		2.0510
antimycin a
[no description available]		2.0810benzamides;
formamides;
macrodiolide;
phenols		antifungal agent;
mitochondrial respiratory-chain inhibitor;
piscicide
vancomycin
Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.		4.2450glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
glycyrrhizic acid
glycyrrhizinic acid : A triterpenoid saponin that is the glucosiduronide derivative of 3beta-hydroxy-11-oxoolean-12-en-30-oic acid.		2.9740enone;
glucosiduronic acid;
pentacyclic triterpenoid;
tricarboxylic acid;
triterpenoid saponin		EC 3.4.21.5 (thrombin) inhibitor;
plant metabolite
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		7.51151alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
tocopherols
[no description available]		2.4320
pregnenolone carbonitrile
Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.		2.0810aliphatic nitrile
selenomethionine
[no description available]		10.9433selenoamino acid;
selenomethionines		plant metabolite
ibufenac
ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects.		3.5920monocarboxylic acidEC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
metylperon
metylperon: RN given refers to parent cpd		2.0810aromatic ketone
metaxalone
[no description available]		3.2310aromatic ether
spectinomycin
Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis.		3.2310cyclic acetal;
cyclic hemiketal;
cyclic ketone;
pyranobenzodioxin;
secondary alcohol;
secondary amino compound		antibacterial drug;
antimicrobial agent;
bacterial metabolite
1,2-dimethylimidazole
[no description available]		2.1310imidazoles
paraquat
Paraquat: A poisonous dipyridilium compound used as contact herbicide. Contact with concentrated solutions causes irritation of the skin, cracking and shedding of the nails, and delayed healing of cuts and wounds.. paraquat : An organic cation that consists of 4,4'-bipyridine bearing two N-methyl substituents loctated at the 1- and 1'-positions.		2.8630organic cationgeroprotector;
herbicide
2'-deoxyadenosine triphosphate
2'-deoxyadenosine triphosphate: RN given refers to unlabeled parent cpd		2.06102'-deoxyadenosine 5'-phosphate;
purine 2'-deoxyribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite
2-tert-butylhydroquinone
2-tert-butylhydroquinone: an anticarcinogenic and chemopreventive agent. 2-tert-butylhydroquinone : A member of the class of hydroquinones in which one of the ring hydrogens of hydroquinone is replaced by a tert-butyl group.		2.1510hydroquinonesfood antioxidant
dronabinol
Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.		5.5141benzochromene;
diterpenoid;
phytocannabinoid;
polyketide		cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
amiloride hydrochloride, anhydrous
amiloride hydrochloride : A hydrochloride obtained by combining amiloride with one molar equivalent of hydrochloric acid.		2.0810hydrochloridediuretic;
sodium channel blocker
amiloride
Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.		4.9160aromatic amine;
guanidines;
organochlorine compound;
pyrazines		diuretic;
sodium channel blocker
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		3.8630benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
7-hydroxychlorpromazine
7-hydroxychlorpromazine: RN given refers to parent cpd		2.0810phenothiazines
phenethyl isothiocyanate
phenethyl isothiocyanate: a dietary liver aldehyde dehydrogenase inhibitor; promotes urinary bladder carcinoma. phenethyl isothiocyanate : An isothiocyanate having a phenethyl group attached to the nitrogen. It is a naturally occurring compound found in some cruciferous vegetables (e.g. watercress) and is known to possess anticancer properties.		2.4620isothiocyanateantineoplastic agent;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
metabolite
fluorescein
Fluorescein: A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.. fluorescein (lactone form) : A xanthene dye that is highly fluorescent, detectable even when present in minute quantities. Used forensically to detect traces of blood, in analytical chemistry as an indicator in silver nitrate titrations and in microscopy.		2.03102-benzofurans;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
polyphenol;
xanthene dye		fluorescent dye;
radioopaque medium
dexbrompheniramine
dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310brompheniramineanti-allergic agent;
H1-receptor antagonist
sulfadoxine
Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.		2.0510pyrimidines;
sulfonamide		antibacterial drug;
antimalarial
acadesine
[no description available]		2.47201-ribosylimidazolecarboxamide;
aminoimidazole;
nucleoside analogue		antineoplastic agent;
platelet aggregation inhibitor
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		4.0940dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
arabinofuranosyluracil
[no description available]		2.0610N-glycosyl compoundmetabolite
doxifluridine
doxifluridine : A pyrimidine 5'-deoxyribonucleoside that is 5-fluorouridine in which the hydroxy group at the 5' position is replaced by a hydrogen. It is an oral prodrug of the antineoplastic agent 5-fluorouracil. Designed to circumvent the rapid degradation of 5-fluorouracil by dihydropyrimidine dehydrogenase in the gut wall, it is converted into 5-fluorouracil in the presence of pyrimidine nucleoside phosphorylase.		2.0510organofluorine compound;
pyrimidine 5'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
prodrug
dicloxacillin
Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group.		3.6120dichlorobenzene;
penicillin		antibacterial drug
fluorescein-5-isothiocyanate
Fluorescein-5-isothiocyanate: Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.. fluorescein 5-isothiocyanate : The 5-isomer of fluorescein isothiocyanate. Acts as a fluorescent probe capable of being conjugated to tissue and proteins; used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.		2.4720fluorescein isothiocyanate
benzolamide
Benzolamide: Selective renal carbonic anhydrase inhibitor. It may also be of use in certain cases of respiratory failure.		4.97350
mannose
mannopyranose : The pyranose form of mannose.		2.0310D-aldohexose;
D-mannose;
mannopyranose		metabolite
iproclozide
iproclozide: structure		2.0510aromatic ether
megestrol
Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17.		3.231017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
streptomycin
[no description available]		3.8630antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor
butylhydroxybutylnitrosamine
Butylhydroxybutylnitrosamine: A substituted carcinogenic nitrosamine.. N-butyl-N-(4-hydroxybutyl)nitrosamine : A nitrosamine that has butyl and 4-hydroxybutyl substituents. In mice, it causes high-grade, invasive cancers in the urinary bladder, but not in any other tissues.		3.3420nitrosamine;
primary alcohol		carcinogenic agent
fuberidazole
fuberidazole: fumigant; structure. fuberidazole : A ring assembly consisting of benzimidazole substituted at position 2 by a 2-furyl group. A fungicide used as a seed treatment to control Fusarium spp. in cereals.		2.110benzimidazole fungicide;
benzimidazoles;
furans		antifungal agrochemical
nitroxoline
nitroxoline: structure in Merck Index, 9th ed, #6475; RN given refers to parent cpd. nitroxoline : A monohydroxyquinoline in which the hydroxy group is positioned at C-8 with a nitro group trans to it at C-5.		2.0810C-nitro compound;
monohydroxyquinoline		antifungal agent;
antiinfective agent;
antimicrobial agent;
renal agent
clonidine hydrochloride
[no description available]		2.0510dichlorobenzene
cladribine
[no description available]		4.4260organochlorine compound;
purine 2'-deoxyribonucleoside		antineoplastic agent;
immunosuppressive agent
ethylene dimethanesulfonate
ethylene dimethanesulfonate: antispermatogenic agent; structure		2.0510
carbenicillin
Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain.		3.2310penicillin allergen;
penicillin		antibacterial drug
carbenicillin disodium
[no description available]		2.0510organic sodium salt
dehydroemetine
dehydroemetine: was MH 1991-94 (see under EMETINE 1976-90); use EMETINE to search DEHYDROEMETINE 1976-94; amebicide, derivative of emetine. dehydroemetine : A pyridoisoquinoline which was developed in response to the cardiovascular toxicity associated with emetine and results from the dehydrogenation of the heterotricylic ring of emetine. It is an antiprotozoal agent and displays antimalarial, antiamoebic, and antileishmanial properties.		2.0510aromatic ether;
isoquinolines;
pyridoisoquinoline		antileishmanial agent;
antimalarial;
antiprotozoal drug
benorilate
benorilate: was heading 1980-94 (see under SALICYLATES 1980-90); was BENORYLATE see under SALICYLATES 1975-79; BENORYLATE was see BENORILATE 1980-94; use SALICYLATES to search BENORILATE 1980-90 & BENORYLATE 1975-79; an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases; it has less severe side effects than aspirin		2.0510carbonyl compound
trimetazidine
Trimetazidine: A vasodilator used in angina of effort or ischemic heart disease.		2.0510aromatic amine
buthionine sulfoximine
Buthionine Sulfoximine: A synthetic amino acid that depletes glutathione by irreversibly inhibiting gamma-glutamylcysteine synthetase. Inhibition of this enzyme is a critical step in glutathione biosynthesis. It has been shown to inhibit the proliferative response in human T-lymphocytes and inhibit macrophage activation. (J Biol Chem 1995;270(33):1945-7). 2-amino-4-(S-butylsulfonimidoyl)butanoic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group carries an oxo, imino and butyl groups.. S-butyl-DL-homocysteine (S,R)-sulfoximine : A sulfoximide that is the sulfoximine derivative of an analogue of DL-methionine in which the S-methyl group is replaced by S-butyl.		2.1510diastereoisomeric mixture;
homocysteines;
non-proteinogenic alpha-amino acid;
sulfoximide		EC 6.3.2.2 (glutamate--cysteine ligase) inhibitor;
ferroptosis inducer
metocurine
metocurine: from Chinese herb Cyclea hainanensis Mrr		2.0810isoquinolines
floxacillin
Floxacillin: Antibiotic analog of CLOXACILLIN.. flucloxacillin : A penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain.		2.4520penicillin allergen;
penicillin		antibacterial drug
clomacran
clomacran: RN given refers to parent cpd; structure		3.2310acridines
mexiletine hydrochloride
mexiletine hydrochloride : A hydrochloride composed of equimolar amounts of mexiletine and hydrogen chloride.		2.0510hydrochlorideanti-arrhythmia drug
beclomethasone dipropionate
beclomethasone dipropionate : A steroid ester comprising beclomethasone having propionyl groups at the 17- and 21-positions.		2.051011beta-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
corticosteroid;
enone;
glucocorticoid;
propanoate ester;
steroid ester		anti-arrhythmia drug;
anti-asthmatic drug;
anti-inflammatory drug;
prodrug
vidarabine
adenine arabinoside : A purine nucleoside in which adenine is attached to arabinofuranose via a beta-N(9)-glycosidic bond.		2.4620beta-D-arabinoside;
purine nucleoside		antineoplastic agent;
bacterial metabolite;
nucleoside antibiotic
methenamine hippurate
methenamine hippurate: both parts of molecule contribute to its antibacterial action		3.2310N-acylglycine
olsalazine
olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease.		3.2310azobenzenes;
dicarboxylic acid		non-steroidal anti-inflammatory drug;
prodrug
tiadenol
tiadenol: structure		2.0510aliphatic sulfide
metoclopramide hydrochloride
metoclopramide hydrochloride : A hydrate that is the monohydrate form of metoclopramide monohydrochloride.		2.0510
2-methylquinoxaline
2-methylquinoxaline: structure given in first source. 2-methylquinoxaline : A quinoxaline derivative in which the quinoxaline (1,4-naphthyridine) skeleton is substituted at C-2 with a methyl group.		3.5110quinoxaline derivative
etidronate disodium
etidronate disodium : An organic sodium salt resulting from the replacement of two protons from etidronic acid (one from from each of the phosphonic acid groups) by sodium ions.		2.0810organic sodium saltantineoplastic agent;
bone density conservation agent;
chelator
neon
Neon: A noble gas with the atomic symbol Ne, atomic number 10, and atomic weight 20.18. It is found in the earth's crust and atmosphere as an inert, odorless gas and is used in vacuum tubes and incandescent lamps.		2.0310monoatomic neon;
noble gas atom;
p-block element atom
platinum
Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.		8.4211elemental platinum;
nickel group element atom;
platinum group metal atom
technetium
Technetium: The first artificially produced element and a radioactive fission product of URANIUM. Technetium has the atomic symbol Tc, and atomic number 43. All technetium isotopes are radioactive. Technetium 99m (m=metastable) which is the decay product of Molybdenum 99, has a half-life of about 6 hours and is used diagnostically as a radioactive imaging agent. Technetium 99 which is a decay product of technetium 99m, has a half-life of 210,000 years.		2.4320manganese group element atom
titanium
Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures.		2.7230titanium group element atom
cadmium
Cadmium: An element with atomic symbol Cd, atomic number 48, and atomic weight 112.41. It is a metal and ingestion will lead to CADMIUM POISONING.. elemental cadmium : An element in the zinc group of the periodic table with atomic number 48, atomic mass 112, M.P. 321degreeC, and B.P. 765degreeC). An odourless, tasteless, and highly poisonous soft, ductile, lustrous metal with electropositive properties. It has eight stable isotopes: (106)Cd, (108)Cd,(110)Cd, (111)Cd, (112)Cd, (113)Cd, (114)Cd and (116)Cd, with (112)Cd and (114)Cd being the most common.		7.0110cadmium molecular entity;
zinc group element atom
cerium
Cerium: An element of the rare earth family of metals. It has the atomic symbol Ce, atomic number 58, and atomic weight 140.12. Cerium is a malleable metal used in industrial applications.		2.4110f-block element atom;
lanthanoid atom
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		2.1510copper group element atom;
elemental gold
helium
Helium: A noble gas with the atomic symbol He, atomic number 2, and atomic weight 4.003. It is a colorless, odorless, tasteless gas that is not combustible and does not support combustion. It was first detected in the sun and is now obtained from natural gas. Medically it is used as a diluent for other gases, being especially useful with oxygen in the treatment of certain cases of respiratory obstruction, and as a vehicle for general anesthetics.		2.0310monoatomic helium;
noble gas atom;
s-block element atom		food packaging gas
aluminum chloride
Aluminum Chloride: A compound with the chemical formula AlCl3; the anhydrous salt is used as a catalyst in organic chemical synthesis, and hydrated salts are used topically as antiperspirants, and for the management of HYPERHYDROSIS.		2.1110aluminium coordination entityLewis acid
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		4.0840pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
magnesium sulfate
Magnesium Sulfate: A small colorless crystal used as an anticonvulsant, a cathartic, and an electrolyte replenisher in the treatment of pre-eclampsia and eclampsia. It causes direct inhibition of action potentials in myometrial muscle cells. Excitation and contraction are uncoupled, which decreases the frequency and force of contractions. (From AMA Drug Evaluations Annual, 1992, p1083). magnesium sulfate : A magnesium salt having sulfate as the counterion.		4.4122magnesium salt;
metal sulfate;
organic magnesium salt		anaesthetic;
analgesic;
anti-arrhythmia drug;
anticonvulsant;
calcium channel blocker;
cardiovascular drug;
fertilizer;
tocolytic agent
mercuric chloride
Mercuric Chloride: Mercury chloride (HgCl2). A highly toxic compound that volatizes slightly at ordinary temperature and appreciably at 100 degrees C. It is corrosive to mucous membranes and used as a topical antiseptic and disinfectant.. mercury dichloride : A mercury coordination entity made up of linear triatomic molecules in which a mercury atom is bonded to two chlorines. Water-soluble, it is highly toxic. Once used in a wide variety of applications, including preserving wood and anatomical specimens, embalming and disinfecting, as an intensifier in photography, as a mordant for rabbit and beaver furs, and freeing gold from lead, its use has markedly declined as less toxic alternatives have been developed.		2.9310mercury coordination entitysensitiser
perchloric acid
[no description available]		2.1110chlorine oxoacid
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		13.083717delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
calcium phosphate, dibasic, anhydrous
calcium phosphate, dibasic, anhydrous: molecular formula CaHPO(4), DCPA=dicalcium phosphate anhydrous; don't confuse with dichloropropionanilide which also is called DCPA; MW=136.06; has greater surface area and lower pH than DCPD (dicalcium phosphate dihydrate); occurs in nature as monetite; an intermediate in preparing hydroxyapatite		2.1510calcium phosphate
tricalcium phosphate
tricalcium phosphate: a form of tricalcium phosphate used as bioceramic bone replacement material; see also records for alpha-tricalcium phosphate, beta-tricalcium phosphate, calcium phosphate; apatitic tricalcium phosphate Ca9(HPO4)(PO4)5(OH) is the calcium orthophosphate leading to beta tricalcium phosphate Ca3(PO4)2 (b-TCP). calcium phosphate : A calcium salt composed of calcium and phosphate/diphosphate ions; present in milk and used for the mineralisation of calcified tissues.		2.5220calcium phosphate
sodium thiosulfate
sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio.		3.2310inorganic sodium saltantidote to cyanide poisoning;
antifungal drug;
nephroprotective agent
fluorine
Fluorine: A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as fluoride (FLUORIDES) to prevent dental caries.		2.5420diatomic fluorine;
gas molecular entity		NMR chemical shift reference compound
nitrous acid
Nitrous Acid: Nitrous acid (HNO2). A weak acid that exists only in solution. It can form water-soluble nitrites and stable esters. (From Merck Index, 11th ed)		2.4920nitrogen oxoacid
hydrazoic acid
[no description available]		2.0610nitrogen hydride
nickel sulfate
nickel sulfate: RN given refers to cpd with MF of Ni(2+)-H2SO4. nickel sulfate : A metal sulfate having nickel(2+) as the metal ion.		2.0810metal sulfateallergen
galactose
aldohexose : A hexose with a (potential) aldehyde group at one end.		2.4820
poloxalene
Poloxalene: A copolymer of polyethylene and polypropylene ether glycol. It is a non-ionic polyol surface-active agent used medically as a fecal softener and in cattle for prevention of bloat.. pluronic : A triblock copolymer composed of a central hydrophobic chain of poly(propylene oxide) flanked by two hydrophilic chains of poly(ethylene oxide).		2.2510epoxide
vasotocin
Vasotocin: A nonapeptide that contains the ring of OXYTOCIN and the side chain of ARG-VASOPRESSIN with the latter determining the specific recognition of hormone receptors. Vasotocin is the non-mammalian vasopressin-like hormone or antidiuretic hormone regulating water and salt metabolism.. vasotocin : A heterodetic cyclic peptide that is homologous to oxytocin and vasopressin. It is a pituitary hormone that acts as an endocrine regulator for water balance, osmotic homoeostasis and is involved in social and sexual behavior in non-mammalian vertebrates.		2.0710
silicon tetrachloride
[no description available]		2.0710
hydroiodic acid
hydrogen iodide : A diatomic molecule containing covalently bonded hydrogen and iodine atoms.		2.4920gas molecular entity;
hydrogen halide;
mononuclear parent hydride		mouse metabolite
4-chloro-7-nitrobenzofurazan
4-Chloro-7-nitrobenzofurazan: A benzofuran derivative used as a protein reagent since the terminal N-NBD-protein conjugate possesses interesting fluorescence and spectral properties. It has also been used as a covalent inhibitor of both beef heart mitochondrial ATPase and bacterial ATPase.. 4-chloro-7-nitrobenzofurazan : A benzoxadiazole that is 2,1,3-benzoxadiazole which is substituted at position 4 by chlorine and at position 7 by a nitro group.		2.5120benzoxadiazole;
C-nitro compound;
organochlorine compound		EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.6.1.3 (adenosinetriphosphatase) inhibitor;
fluorescent probe;
fluorochrome
trolamine salicylate
Arthritis: Acute or chronic inflammation of JOINTS.		16.0610711
stanozolol
Stanozolol: A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194). stanozolol : An organic heteropentacyclic compound resulting from the formal condensation of the 3-keto-aldehyde moiety of oxymetholone with hydrazine. Like oxymetholone, it is a synthetic anabolic steroid. It has both anabolic and androgenic properties, and has been used to treat hereditary angioedema and various vascular disorders. It has also been widely abused by professional athletes.		2.051017beta-hydroxy steroid;
anabolic androgenic steroid;
organic heteropentacyclic compound;
tertiary alcohol		anabolic agent;
androgen
clodronic acid
Clodronic Acid: A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification.. clodronic acid : An organochlorine compound that is methylene chloride in which both hydrogens are replaced by phosphonic acid groups. It inhibits bone resorption and soft tissue calcification, and is used (often as the disodium salt tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteolytic lesions and bone pain associated with skeletal metastases.		3.85301,1-bis(phosphonic acid);
one-carbon compound;
organochlorine compound		antineoplastic agent;
bone density conservation agent
carbendazim
carbendazim: carcinogen when combined with sodium nitrite; principle metabolite of thiophanate methyl & benomyl; structure. carbendazim : A member of the class of benzimidazoles that is 2-aminobenzimidazole in which the primary amino group is substituted by a methoxycarbonyl group. A fungicide, carbendazim controls Ascomycetes, Fungi Imperfecti, and Basidiomycetes on a wide variety of crops, including bananas, cereals, cotton, fruits, grapes, mushrooms, ornamentals, peanuts, sugarbeet, soybeans, tobacco, and vegetables.		2.0510benzimidazole fungicide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		antifungal agrochemical;
antinematodal drug;
metabolite;
microtubule-destabilising agent
mafenide acetate
[no description available]		2.0810carboxylic acid
ethionine
L-ethionine : An S-ethylhomocysteine that has S-configuration at the chiral centre.		2.0510S-ethylhomocysteineantimetabolite;
carcinogenic agent
2',3-dimethyl-4-aminobiphenyl
2',3-dimethyl-4-aminobiphenyl: RN given refers to parent cpd; structure		2.4420
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		5.9951anthraquinone
tiletamine hydrochloride
Cyclohexanones: Cyclohexane ring substituted by one or more ketones in any position.. cyclohexanones : Any alicyclic ketone based on a cyclohexane skeleton and its substituted derivatives thereof.		2.0710
xipamide
Xipamide: A sulfamoylbenzamide analog of CLOPAMIDE. It is diuretic and saluretic with antihypertensive activity. It is bound to PLASMA PROTEINS, thus has a delayed onset and prolonged action.		2.0510benzamides
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		4.4130selegiline;
terminal acetylenic compound		geroprotector
selegiline hydrochloride, (r)-isomer
[no description available]		2.0810hydrochloride;
terminal acetylenic compound		antiparkinson drug;
dopaminergic agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor
levamisole
Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.		2.44206-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazoleantinematodal drug;
antirheumatic drug;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
immunological adjuvant;
immunomodulator
clemastine
Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		3.5820monochlorobenzenes;
N-alkylpyrrolidine		anti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
thiamphenicol
[no description available]		2.4720monocarboxylic acid amide;
sulfone		antimicrobial agent;
immunosuppressive agent
pancuronium bromide
pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication.		2.0810bromide saltcholinergic antagonist;
muscle relaxant;
nicotinic antagonist
pizotyline
Pizotyline: Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.. pizotifen : A benzocycloheptathiophene that is 9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophene 4-ylidene)-1-methylpiperidine which is joined from the 4 position to the 4 position of an N-methylpiperidine moiety by a double bond. It is a sedating antihistamine, with strong serotonin antagonist and weak antimuscarinic activity. It is generally used as the malate salt for the treatment of migraine and the prevention of headache attacks during cluster periods.		2.0510benzocycloheptathiophenehistamine antagonist;
muscarinic antagonist;
serotonergic antagonist
cephalexin
Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract.		4.3730beta-lactam antibiotic allergen;
cephalosporin;
semisynthetic derivative		antibacterial drug
cromolyn sodium
Cromolyn Sodium: A chromone complex that acts by inhibiting the release of chemical mediators from sensitized MAST CELLS. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.. disodium cromoglycate : An organic sodium salt that is the disodium salt of cromoglycic acid.		3.8730organic sodium saltanti-asthmatic drug;
drug allergen
isosorbide-5-mononitrate
isosorbide-5-mononitrate: for prevention of angina pectoris; structure given in first source; a Russian drug		2.0510glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		3.5380acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
tocopheryl nicotinate
alpha-tocopheryl nicotinate: RN given refers to (2R-(2R*(2R*(4R*,8R*))-isomer		2.0510tocol
ornidazole
Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.		2.0810C-nitro compound;
imidazoles;
organochlorine compound;
secondary alcohol		antiamoebic agent;
antibacterial drug;
antiinfective agent;
antiprotozoal drug;
antitrichomonal drug;
epitope
danazol
Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.		4.094017beta-hydroxy steroid;
terminal acetylenic compound		anti-estrogen;
estrogen antagonist;
geroprotector
clonixin
Clonixin: Anti-inflammatory analgesic.. clonixin : A pyridinemonocarboxylic acid that is nicotinic acid substituted at position 2 by a (2-methyl-3-chlorophenyl)amino group. Used (as its lysine salt) for treatment of renal colic, muscular pain and moderately severe migraine attacks.		2.4620aminopyridine;
organochlorine compound;
pyridinemonocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
lipoxygenase inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
vasodilator agent
fenclozic acid
fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd		3.2310
laxagetten 4,4'-diacetoxydiphenylpyridylemethane
[no description available]		3.2310
dibenz(b,f)(1,4)oxazepine-10(11h)-carboxylic acid, 8-chloro-, 2-acetylhydrazide
Dibenz(b,f)(1,4)oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-acetylhydrazide: Inhibits the activity of prostaglandins.		2.1310
iodine
[no description available]		2.4110halide anion;
monoatomic iodine		human metabolite
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		3.8630aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
fludarabine phosphate
fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas.		3.6120nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate		antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug
disopyramide phosphate
[no description available]		2.0510organoammonium phosphate
alclofenac
alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash.		3.2310aromatic ether;
monocarboxylic acid;
monochlorobenzenes		drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
carbimazole
Carbimazole: An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.. carbimazole : A member of the class of imidazoles that is methimazole in which the nitrogen bearing a hydrogen is converted into its ethoxycarbonyl derivative. A prodrug for methimazol, carbimazole is used for the treatment of hyperthyroidism.		2.05101,3-dihydroimidazole-2-thiones;
carbamate ester		antithyroid drug;
prodrug
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		3.5920indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
ergocristine
ergocristine: an ergot alkaloid; one of the three components of ergotoxine; has alpha blocking action, stimulates smooth muscles & antagonizes serotonin; used as oxytocic & in peripheral disorders; minor descriptor (77-86); on-line & INDEX MEDICUS search EROLINES (77-86); RN given refers to ((5'alpha)-isomer). ergocristine : Ergotaman bearing benzyl, hydroxy, and isopropyl groups at the 5', 12' and 2' positions, respectively, and oxo groups at positions 3', 6', and 18. It is a natural ergot alkaloid.		2.0410ergot alkaloid
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		4.5470benzenes;
phenyl acetates
butyl acetate
butyl acetate: structure. butyl acetate : The acetate ester of butanol.		2.4820acetate estermetabolite
triamcinolone
Triamcinolone: A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739). triamcinolone : A C21-steroid hormone that is 1,4-pregnadiene-3,20-dione carrying four hydroxy substituents at positions 11beta, 16alpha, 17alpha and 21 as well as a fluoro substituent at position 9. Used in the form of its 16,17-acetonide to treat various skin infections.		2.432011beta-hydroxy steroid;
16alpha-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
oxyphenisatin
[no description available]		3.5920indoles
tetrachloroethylene
Tetrachloroethylene: A chlorinated hydrocarbon used as an industrial solvent and cooling liquid in electrical transformers. It is a potential carcinogen.		2.0510chlorocarbon;
chloroethenes		nephrotoxic agent
dimethylacetamide
hallucinogen : Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations and other alterations of mood and thinking.. N,N-dimethylacetamide : A member of the class of acetamides that is acetamide in which the hydrogens attached to the N atom have been replaced by two methyl groups respectively. Metabolite observed in cancer metabolism.		2.0210acetamides;
monocarboxylic acid amide		human metabolite
fludrocortisone
Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity.		3.231011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
fluorinated steroid;
mineralocorticoid		adrenergic agent;
anti-inflammatory drug
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		7.2261bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
butylated hydroxytoluene
2,6-di-tert-butyl-4-methylphenol : A member of the class of phenols that is 4-methylphenol substituted by tert-butyl groups at positions 2 and 6.		3.930phenolsantioxidant;
ferroptosis inhibitor;
food additive;
geroprotector
proquazone
proquazone: nonsteroid anti-inflammatory agent; structure		2.1310pyrimidines
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		2.4920C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
butachlor
butachlor : An aromatic amide that is 2-choro-N-(2,6-diethylphenyl)acetamide in which the amide nitrogen has been replaced by a butoxymethyl group.		2.0510aromatic amide;
organochlorine compound;
tertiary carboxamide		environmental contaminant;
herbicide;
xenobiotic
4-methoxyamphetamine
4-methoxyamphetamine: para-methoxy derivative to amphetamine with hallucinogenic properties; minor descriptor (75-86); on line & INDEX MEDICUS search AMPHETAMINES (75-86); RN given refers to parent compound without isomeric designation		2.4110
du-21220
Ritodrine: An adrenergic beta-2 agonist used to control PREMATURE LABOR.. 4-[2-[[1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenol : A secondary amino compound that is 4-(2-amino-1-hydroxypropyl)phenol in which one of the hydrogens attached to the nitrogen is replaced by a 2-(4-hydroxyphenyl)ethyl group.		2.0410benzyl alcohols;
polyphenol;
secondary alcohol;
secondary amino compound
rose bengal b disodium salt
[no description available]		2.0510
alkenes
[no description available]		2.0610
calcium oxalate
Calcium Oxalate: The calcium salt of oxalic acid, occurring in the urine as crystals and in certain calculi.. calcium oxalate : The calcium salt of oxalic acid, which in excess in the urine may lead to formation of oxalate calculi (kidney stones).		2.0210organic calcium salt
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		3.5680glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
dexchlorpheniramine
dexchlorpheniramine: RN given refers to parent cpd(S)-isomer		3.2310chlorphenamine
alovudine
[no description available]		2.0510pyrimidine 2',3'-dideoxyribonucleoside
clometacin
clometacin: structure		3.2310N-acylindole
azoxymethane
Azoxymethane: A potent carcinogen and neurotoxic compound. It is particularly effective in inducing colon carcinomas.		4.82120
cefazolin
Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively.		3.5920beta-lactam antibiotic allergen;
cephalosporin;
tetrazoles;
thiadiazoles		antibacterial drug
oxypeucadanin, (s)-(-)-isomer
[no description available]		2.1510epoxide;
furanocoumarin;
lactone		plant metabolite
sodium azide
Sodium Azide: A cytochrome oxidase inhibitor which is a nitridizing agent and an inhibitor of terminal oxidation. (From Merck Index, 12th ed). sodium azide : The sodium salt of hydrogen azide (hydrazoic acid).		2.4520inorganic sodium saltantibacterial agent;
explosive;
mitochondrial respiratory-chain inhibitor;
mutagen
azides
Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3.		2.7230pseudohalide anionmitochondrial respiratory-chain inhibitor
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		6.3862penicillin allergen;
penicillin		antibacterial drug
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		4.2650timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
indoramin
Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.		2.0810tryptamines
oxamethacin
oxamethacin: structure. oxametacin : A hydroxamic acid obtained by formal condensation of the carboxy group of indometacin with the amino group of hydroxylamine.		2.0310aromatic ether;
hydroxamic acid;
N-acylindole;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
tramadol
Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.		12.8837232-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanoladrenergic uptake inhibitor;
antitussive;
capsaicin receptor antagonist;
delta-opioid receptor agonist;
kappa-opioid receptor agonist;
metabolite;
mu-opioid receptor agonist;
muscarinic antagonist;
nicotinic antagonist;
NMDA receptor antagonist;
opioid analgesic;
serotonergic antagonist;
serotonin uptake inhibitor
nicergoline
Nicergoline: An ergot derivative that has been used as a cerebral vasodilator and in peripheral vascular disease. It may ameliorate cognitive deficits in CEREBROVASCULAR DISORDERS.		2.0510organic heterotetracyclic compound;
organonitrogen heterocyclic compound
oxcarbazepine
Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.		3.8730cyclic ketone;
dibenzoazepine		anticonvulsant;
drug allergen
carbidopa
carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		3.6120catechols;
hydrazines;
monocarboxylic acid		antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
moricizine hydrochloride
moricizine hydrochloride : A hydrochloride salt obtained from equimola amounts of moricizine and hydrogen chloride.		2.0510hydrochlorideanti-arrhythmia drug
moricizine
Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group.		3.2310carbamate ester;
morpholines;
phenothiazines		anti-arrhythmia drug
amineptin
amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne.		3.5920amino acid;
carbocyclic fatty acid;
carbotricyclic compound;
secondary amino compound		antidepressant;
dopamine uptake inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		5.2890azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
feprazone
Feprazone: A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15)		2.0810organic molecular entity
7-ethoxycoumarin
7-ethoxycoumarin : A member of the class of coumarins that is umbelliferone in which the hydroxy group at position 7 is replaced by an ethoxy group.		2.5720aromatic ether;
coumarins
pirprofen
pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure		3.8630pyrroline
serentil
mesoridazine besylate : The benzenesulfonate salt of mesoridazine prepared using equimolar amounts of mesoridazine and benzenesulfonic acid.		2.0510organosulfonate saltdopaminergic antagonist;
first generation antipsychotic
tobramycin
Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.		2.7630amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		11.76297taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		12.32339beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
substance p
[no description available]		5.2462peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
propafenone hydrochloride
propafenone hydrochloride : A hydrochloride that is the monohydrochloride salt of propafenone. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used in the management of supraventricular and ventricular arrhythmias.		2.0510hydrochlorideanti-arrhythmia drug
dobutamine
Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.		3.5920catecholamine;
secondary amine		beta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
penbutolol
Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.		3.2310ethanolamines
ribavirin
Rebetron: Rebetron is tradename		4.09401-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
amikacin
Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group.		3.8730alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin
flunixin
flunixin : A pyridinemonocarboxylic acid that is nicotinic acid substituted at position 2 by a 2-methyl-3-(trifluoromethyl)phenylamino group. A relatively potent non-narcotic, nonsteroidal analgesic with anti-inflammatory, anti-endotoxic and anti-pyretic properties; used in veterinary medicine (usually as the meglumine salt) for treatment of horses, cattle and pigs.		2.0610aminopyridine;
organofluorine compound;
pyridinemonocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
carbidopa
[no description available]		2.0510catechols;
hydrate;
hydrazines;
monocarboxylic acid		antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
cephradine
Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton.		3.5920beta-lactam antibiotic allergen;
cephalosporin		antibacterial drug
ticrynafen
Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis.		4.0840aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid;
thiophenes		antihypertensive agent;
hepatotoxic agent;
loop diuretic
fluproquazone
fluproquazone: structure given in first source		2.1310
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		4.0840L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
bezafibrate
[no description available]		2.4620aromatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
sq-11725
Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.. nadolol : Nadolol is a diastereoisomeric mixture consisting of equimolar amounts of the four possible 2,3-cis-isomers of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol.		2.4620
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		4.55705-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
flunixin meglumine
flunixin meglumine : An organoammonium salt obtained by combining flunixin with one molar equivalent of 1-deoxy-1-(methylamino)-D-glucitol. A relatively potent non-narcotic, nonsteroidal analgesic with anti-inflammatory, anti-endotoxic and anti-pyretic properties; used in veterinary medicine for treatment of horses, cattle and pigs.		2.0510organoammonium saltantipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
1-methyl-4-phenylpyridinium
1-Methyl-4-phenylpyridinium: An active neurotoxic metabolite of 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE. The compound reduces dopamine levels, inhibits the biosynthesis of catecholamines, depletes cardiac norepinephrine and inactivates tyrosine hydroxylase. These and other toxic effects lead to cessation of oxidative phosphorylation, ATP depletion, and cell death. The compound, which is related to PARAQUAT, has also been used as an herbicide.. N-methyl-4-phenylpyridinium : A pyridinium ion that is N-methylpyridinium having a phenyl substituent at the 4-position.		2.7330pyridinium ionapoptosis inducer;
herbicide;
human xenobiotic metabolite;
neurotoxin
lonidamine
lonidamine: structure. lonidamine : A member of the class of indazoles that is 1H-indazole that is substituted at positions 1 and 3 by 2,4-dichlorobenzyl and carboxy groups, respectively.		2.0810dichlorobenzene;
indazoles;
monocarboxylic acid		antineoplastic agent;
antispermatogenic agent;
EC 2.7.1.1 (hexokinase) inhibitor;
geroprotector
vecuronium bromide
Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent;
nicotinic antagonist
vecuronium
vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents.		3.2310acetate ester;
androstane;
quaternary ammonium ion		drug allergen;
muscle relaxant;
neuromuscular agent;
nicotinic antagonist
ng-nitroarginine methyl ester
NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.		4.13150alpha-amino acid ester;
L-arginine derivative;
methyl ester;
N-nitro compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor
dexibuprofen
dexibuprofen: structure in first source		2.0510ibuprofennon-narcotic analgesic;
non-steroidal anti-inflammatory drug
benoxaprofen
benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals.		3.86301,3-benzoxazoles;
monocarboxylic acid;
monochlorobenzenes		antipsoriatic;
antipyretic;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
hepatotoxic agent;
nephrotoxin;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
protein kinase C agonist
deoxynivalenol
deoxynivalenol : A trichothecene mycotoxin produced by Fusarium to which wheat, barley, maize (corn) and their products are susceptible to contamination.		2.6620cyclic ketone;
enone;
primary alcohol;
secondary alpha-hydroxy ketone;
trichothecene;
triol		mycotoxin
permethrin
hemoglobin Atlanta-Coventry: Leu replaced by Pro at beta75 and Leu deleted at beta141		2.4620cyclopropanecarboxylate ester;
cyclopropanes		agrochemical;
ectoparasiticide;
pyrethroid ester acaricide;
pyrethroid ester insecticide;
scabicide
exifone
[no description available]		3.2310benzophenones
pirfenidone
pirfenidone : A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis.		2.0510pyridoneantipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
[no description available]		4.2550chromanol;
monocarboxylic acid;
phenols		antioxidant;
ferroptosis inhibitor;
neuroprotective agent;
radical scavenger;
Wnt signalling inhibitor
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		3.6120[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
diisopropanolnitrosamine
diisopropanolnitrosamine: experimental carcinogen. N,N-bis(2-hydroxypropyl)nitrosamine : A nitrosamine that is dipropylamine in which the hydrogen attached to the nitrogen has been replaced by a nitroso group. It is a genotoxic carcinogen, targeting the lung, liver, thyroid, and kidney.		2.0310diol;
nitrosamine;
secondary alcohol		carcinogenic agent
desogestrel
Desogestrel: A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED).		2.472017beta-hydroxy steroid;
terminal acetylenic compound		contraceptive drug;
progestin;
synthetic oral contraceptive
flecainide acetate
flecainide acetate : An acetate salt obtained by combining flecainide with one molar equivalent of acetic acid. An antiarrhythmic agent used to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0510acetate saltanti-arrhythmia drug
nicardipine hydrochloride
[no description available]		2.0510dihydropyridinegeroprotector
muzolimine
Muzolimine: A pyrazole diuretic with long duration and high capacity of action. It was proposed for kidney failure and hypertension but was withdrawn worldwide because of severe neurological effects.		2.0510dichlorobenzene
nitazoxanide
nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug		3.6120benzamides;
carboxylic ester
sufentanil
Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid.		5.1221anilide;
ether;
piperidines;
thiophenes		anaesthesia adjuvant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
acarbose
[no description available]		5.4650tetrasaccharide derivativeEC 3.2.1.1 (alpha-amylase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
geroprotector;
hypoglycemic agent
torsemide
Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.		3.2310aminopyridine;
N-sulfonylurea;
secondary amino compound		antihypertensive agent;
loop diuretic
epirubicin
Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA.		8.88145aminoglycoside;
anthracycline antibiotic;
anthracycline;
deoxy hexoside;
monosaccharide derivative;
p-quinones;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		antimicrobial agent;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
cefmetazole
Cefmetazole: A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.. cefmetazole : A second-generation cephalosporin antibiotic having N(1)-methyltetrazol-5-ylthiomethyl, {[(cyanomethyl)sulfanyl]acetyl}amino and methoxy side-groups at positions 3, 7beta and 7alpha respectively of the parent cephem bicyclic structure.		8.5866cephalosporinantibacterial drug
desflurane
Desflurane: A fluorinated ether that is used as a volatile anesthetic for maintenance of general anesthesia.		2.0510organofluorine compoundinhalation anaesthetic
indacrinone
indacrinone: polyvalent saluretic; RN given refers to parent cpd without isomeric designation; structure		2.0510
tilomisole
tilomisole: structure given in first source		2.4110
lorcainide
[no description available]		2.0810acetamides
idarubicin
Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.		3.5920anthracycline antibiotic;
deoxy hexoside;
monosaccharide derivative
laurocapram
laurocapram: enhances percutaneous absorption of different chemicals; structure given in first source		2.4820
nitrosobis(2-oxopropyl)amine
nitrosobis(2-oxopropyl)amine: structure. nitrosobis(2-oxopropyl)amine : A nitrosamine that is iminodiacetone that is substituted by a nitroso group at the N-atom. It induces pancreatic ductal adenocarcinomas in Syrian golden hamsters (other rodents are not susceptible).		2.4520ketone;
nitrosamine		carcinogenic agent
piperacillin
Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.		3.5920penicillin allergen;
penicillin		antibacterial drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		4.7990aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		11.4160alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
cefoperazone
Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance.		3.8830cephalosporinantibacterial drug
staurosporine
[no description available]		2.4820indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
foscarnet sodium
trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.4720one-carbon compound;
organic sodium salt		antiviral drug
4-(n-methyl-n-nitrosamino)-1-(3-pyridyl)-1-butanone
4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone: structure; from tobacco smoke		2.0310nitrosamine;
pyridines
atracurium
Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups.		3.2310diester;
quaternary ammonium ion		muscle relaxant;
nicotinic antagonist
atracurium besylate
atracurium besylate : The bisbenzenesulfonate salt of atracurium.		2.0810organosulfonate salt;
quaternary ammonium salt		muscle relaxant;
nicotinic antagonist
butoconazole nitrate
butoconazole nitrate : An organic nitrate salt obtained by reaction of equimolar amounts of butaconazole and nitric acid. An antifungal agent, it is used in gynaecology for treatment of vulvovaginal infections caused by Candida species, particularly Candida albicans.		2.0510aryl sulfide;
conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
organic nitrate salt
moxalactam
Moxalactam: Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections.. moxalactam : A broad-spectrum oxacephem antibiotic in which the oxazine ring is substituted with a tetrazolylthiomethyl group and the azetidinone ring carries methoxy and 2-carboxy-2-(4-hydroxyphenyl)acetamido substituents.		2.0510cephalosporin;
oxacephem		antibacterial drug
nicorandil
Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris.		2.4720nitrate ester;
pyridinecarboxamide		potassium channel opener;
vasodilator agent
pergolide
Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		4.0920diamine;
methyl sulfide;
organic heterotetracyclic compound		antiparkinson drug;
dopamine agonist
pergolide mesylate
pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.0810methanesulfonate saltantiparkinson drug;
dopamine agonist;
geroprotector
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.4720acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
cefadroxil anhydrous
Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		5.0670cephalosporinantibacterial drug
encainide
Encainide: One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.. encainide : 4-Methoxy-N-phenylbenzamide in which the hydrogen at the 2 position of the phenyl group is substituted by a 2-(1-methylpiperidin-2-yl)ethyl group. A class Ic antiarrhythmic, the hydrochloride was used for the treatment of severe or life-threatening ventricular arrhythmias, but it was associated with increased death rates in patients who had asymptomatic heart rhythm abnormalities after a recent heart attack and was withdrawn from the market.		2.4720benzamides;
piperidines		anti-arrhythmia drug;
sodium channel blocker
talniflumate
talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma		2.0810benzofurans
fenoldopam mesylate
[no description available]		2.0810benzazepine
triclabendazole
[no description available]		2.0510aromatic ether
fialuridine
[no description available]		3.5920
cefaclor anhydrous
Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		4.640cephalosporinantibacterial drug;
drug allergen
bucindolol
bucindolol: an indolyl-tert-butyl-phenoxypropanolamine benzonitrile derivative		2.0410
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		2.0810fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
mitoxantrone hydrochloride
[no description available]		2.0510hydrochlorideantineoplastic agent
alfentanil
Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.		3.2310monocarboxylic acid amide;
piperidines		central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
sulotroban
sulotroban: thromboxane receptor antagonist		3.1210
fomesafen
fomesafen: a protoporphyrinogen oxidase-inhibiting herbicide. fomesafen : An N-sulfonylcarboxamide that is N-(methylsulfonyl)benzamide in which the phenyl ring is substituted by a nitro group at position 2 and a 2-chloro-4-(trifluoromethyl)phenoxy group at position 5. A protoporphyrinogen oxidase inhibitor, it was specially developed for use (generally as the corresponding sodium salt, fomesafen-sodium) for post-emergence control of broad-leaf weeds in soya.		2.0410aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-sulfonylcarboxamide;
organofluorine compound;
phenols		agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide
miglustat
miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group.		3.5920piperidines;
tertiary amino compound		anti-HIV agent;
EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor
haloperidol decanoate
[no description available]		3.2310organic molecular entity
cefotetan
Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms.		4.0940
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		6.84111delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
flupirtine
flupirtine: RN given refers to parent cpd without isomeric designation		2.4820aminopyridine
tolrestat
tolrestat: RN & structure given in first source		3.5920naphthalenesEC 1.1.1.21 (aldehyde reductase) inhibitor
enoximone
Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.		2.4720aromatic ketone
stepronin
[no description available]		2.0810N-acyl-amino acid
piritrexim
piritrexim: RN given refers to parent cpd; structure given in first source		2.0510
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		10.62130delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
idazoxan
Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.		2.0810benzodioxine;
imidazolines		alpha-adrenergic antagonist
remoxipride
Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.		2.0810dimethoxybenzene
balsalazide
balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond.		3.2310
pravastatin
Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		5.711003-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic)		anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic
cabergoline
Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.		3.9230N-acylureaantineoplastic agent;
antiparkinson drug;
dopamine agonist
bambuterol
bambuterol: selective inhibitor of butyrylcholinesterase & acetylcholinesterase. bambuterol : A carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.		2.0510carbamate ester;
phenylethanolamines		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
prodrug;
sympathomimetic agent;
tocolytic agent
atomoxetine hydrochloride
Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine.		2.4720hydrochlorideadrenergic uptake inhibitor;
antidepressant
atomoxetine
atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.		4.2750aromatic ether;
secondary amino compound;
toluenes		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
quinapril
Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.		6.5651dicarboxylic acid monoester;
ethyl ester;
isoquinolines;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
alpidem
[no description available]		3.5920imidazoles
raloxifene hydrochloride
Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.		4.460hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
gepirone
gepirone: RN given refers to parent cpd; structure given in first source		2.0510N-arylpiperazine
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		4.41603-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
itraconazole
Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.		5.1352aromatic ether;
conazole antifungal drug;
cyclic ketal;
dichlorobenzene;
dioxolane;
N-arylpiperazine;
triazole antifungal drug;
triazoles		EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
Hedgehog signaling pathway inhibitor;
P450 inhibitor
fosphenytoin
fosphenytoin: structure given in first & second source		3.8130imidazolidine-2,4-dione
pravadoline
[no description available]		2.0810
fluorodopa f 18
fluorodopa F 18: RN given refers to (L)-isomer		2.1710(18)F radiopharmaceutical;
6-fluoro-L-dopa
salmeterol xinafoate
Salmeterol Xinafoate: A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.		2.0810naphthoic acid
ranolazine
Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina.		3.8830aromatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
fura-2
Fura-2: A fluorescent calcium chelating agent which is used to study intracellular calcium in tissues.		2.4420
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		3.85303-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		2.0810imidazoquinolineantineoplastic agent;
interferon inducer
mk 458
MK 458: a sustained release formulation of a naphthoxazine compoud with selective D-2 dopamine receptor agonism. naxagolide hydrochloride : The hydrochloride salt of naxagolide.		2.0110hydrochlorideanticonvulsant;
antiparkinson drug;
dopamine agonist
tepoxalin
tepoxalin : A hydroxamic acid obtained by formal condensation of the carboxy group of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]propanoic acid with the amino group of N-methylhydroxylamine. It is used in veterinary medicine for the control of pain and inflammation caused by musculoskeletal disorders such as hip dysplasia and arthritis in dogs.		2.3110aromatic ether;
hydroxamic acid;
monochlorobenzenes;
pyrazoles		antipyretic;
apoptosis inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
immunomodulator;
lipoxygenase inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
esmolol
methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure.		3.5820aromatic ether;
ethanolamines;
methyl ester;
secondary alcohol;
secondary amino compound
temafloxacin
temafloxacin: structure given in first source. temafloxacin : A racemate comprising equimolar amounts of (R)- and (S)-temafloxacin. Both enantiomers both exhibit similar pharmacological profiles. Temafloxacin was briefly used (either as the free base or as the hydrochloride salt) as an antibacterial drug but was withdrawn worldwide in 1992 following reports of serious side effects, including severe hypoglycaemia, haemolytic anaemia, liver and kidney dysfunction, anaphylaxis, and death.. 1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid : A quinolone that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted at positions 1, 6, and 7 by 2,4-difluorophenyl, fluorine, and 3-methylpiperazin-1-yl groups, respectively.		2.0510amino acid;
monocarboxylic acid;
N-arylpiperazine;
organofluorine compound;
quinolone antibiotic;
quinolone;
secondary amino compound;
tertiary amino compound
clinafloxacin
clinafloxacin: structure given in first source; RN given is for monoHCl		2.0510quinolines
sertindole
sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.		2.0810heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
adapalene
Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.		2.0810adamantanes;
monocarboxylic acid;
naphthoic acid		dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
adefovir
adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection.		4.37306-aminopurines;
ether;
phosphonic acids		antiviral drug;
DNA synthesis inhibitor;
drug metabolite;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent
aromasil
[no description available]		10.16211417-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor;
environmental contaminant;
xenobiotic
sparfloxacin
[no description available]		2.7530fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
zileuton
[no description available]		10.774231-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
remacemide
remacemide: structure given in first source		2.0210stilbenoid
tebufelone
tebufelone: structure given in first source		2.0510
niguldipine
[no description available]		2.0810diarylmethane
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		5.7861methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
cidofovir anhydrous
Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients.		4.640phosphonic acids;
pyrimidone		anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent
tiagabine
Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy.		3.2310beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes		anticonvulsant;
GABA reuptake inhibitor
mibefradil
Mibefradil: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.		2.0510tetralinsT-type calcium channel blocker
sch 37370
N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine		3.1210
topotecan
Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.		5.280pyranoindolizinoquinolineantineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
eliprodil
1-(4-chlorophenyl)-2-[4-(4-fluorobenzyl)piperidin-1-yl]ethanol : A member of the class of piperidines that is piperidine substituted by a 2-(4-chlorophenyl)-2-hydroxyethyl group at position 1 and by a 4-fluorobenzyl group at position 4.		2.0810monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary alcohol;
tertiary amino compound
tenidap
tenidap: structure given in first source; RN refers to (Z)-isomer		210
bromfenac
bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.		4.5570aromatic amino acid;
benzophenones;
organobromine compound;
substituted aniline		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gemcitabine hydrochloride
[no description available]		2.0810hydrochloride;
organofluorine compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		11.882712organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
ibutilide
ibutilide: RN & structure in first source; RN refers to the fumarate salt		3.2310benzenes;
organic amino compound
aripiprazole
Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.		3.6120aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
remifentanil
Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline.		3.2310alpha-amino acid ester;
anilide;
monocarboxylic acid amide;
piperidinecarboxylate ester		intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
sedative
atorvastatin calcium anhydrous
[no description available]		2.0810organic calcium salt
atorvastatin
[no description available]		6.2240aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
lamivudine
[no description available]		4.7850monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
duloxetine hydrochloride
Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration.		7.0291duloxetine hydrochlorideantidepressant
duloxetine
[no description available]		4.5940duloxetine
irinotecan
[no description available]		13.393716carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		5.280biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
ibandronic acid
Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS.		3.2310
ziprasidone
ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.		4.35301,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
zanamivir
Zanamivir: A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE.		2.4420guanidinesantiviral agent;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor
zolmitriptan
zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.		3.6120oxazolidinone;
tryptamines		anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
adefovir dipivoxil
bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.		2.47206-aminopurines;
carbonate ester;
ether;
organic phosphonate		antiviral drug;
DNA synthesis inhibitor;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		4.6140monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		3.5920biphenyls
mk 0591
MK 0591: structure given in first source; MK 0591 was previously L-686,708; inhibits leukotriene biosynthesis by inhibiting 5-lipoxygenase activating protein		2.1110
saquinavir monomethanesulfonate
[no description available]		2.0510organic molecular entity
tiludronic acid
tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source		3.2310organochlorine compound
tirofiban
Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.		3.6320L-tyrosine derivative;
piperidines;
sulfonamide		anticoagulant;
fibrin modulating drug;
platelet glycoprotein-IIb/IIIa receptor antagonist
capecitabine
Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.		13.473214carbamate ester;
cytidines;
organofluorine compound		antimetabolite;
antineoplastic agent;
prodrug
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		3.8630adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
nitroaniline
nitroaniline: RN given refers to cpd with unspecified locant for nitro moiety. nitroaniline : A substituted aniline that carries one or more nitro groups.		2.0110
allyl formate
[no description available]		2.0510
3-n-butylphthalide
3-n-butylphthalide: isolated from phenolic part of Ligusticum wallichii Franch; structure given in first source		2.4110benzofurans
carbogen
carbogen: mixture of 95% O2 & 5% CO2		2.0210
paroxetine hydrochloride
paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug.		2.0810hydrochlorideantidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
desferrioxamine b mesylate
desferrioxamine B mesylate : A methanesulfonate salt obtained by reaction of desferrioxamine B with one molar equivalent of methanesulfonic acid. It is an iron-chelating medicine used to remove excess iron from the body. It binds to iron in the blood, which is then passed out in the urine.		2.0510methanesulfonate saltantidote;
ferroptosis inhibitor;
iron chelator
bupropion hydrochloride
[no description available]		2.4720aromatic ketone
halofuginone
[no description available]		2.0510quinazolines
diltiazem hydrochloride
Carex: fluoride (1.8%) containing varnish; no further information available 8/91. diltiazem hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of diltiazem and hydrogen chloride. A calcium-channel blocker and vasodilator, it is used in the management of angina pectoris and hypertension.		2.0510hydrochlorideantihypertensive agent;
calcium channel blocker;
vasodilator agent
venlafaxine hydrochloride
Venlafaxine Hydrochloride: A cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT.		3.5520hydrochloride
trazodone hydrochloride
Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.		2.4720hydrochlorideadrenergic antagonist;
antidepressant;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
ortho-cept
ethinyl estradiol-desogestrel combination: Ethinyl Estradiol and Desogestrell given in fixed proportions; has proved to be an effective & well-tolerated oral contraceptive, which improves cycle control & has a beneficial effect on acne		2.0510
trovafloxacin
trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure.		3.5920
verapamil hydrochloride
verapamil hydrochloride : A racemate comprising equimolar amounts of dexverapamil hydrochloride and (S)-verapamil hydrochloride.		2.4720
cefprozil
[no description available]		3.5920cephalosporin;
semisynthetic derivative		antibacterial drug
doxazosin mesylate
Cardura: Trade name in United States.		2.0810methanesulfonate saltgeroprotector
ciprofloxacin hydrochloride anhydrous
[no description available]		2.0510hydrochlorideantibacterial drug;
antiinfective agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
[no description available]		2.0510stilbenoid
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		5.39100acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		4.6880aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
amantadine hydrochloride
[no description available]		2.0510hydrochlorideantiviral agent;
dopamine agonist;
NMDA receptor antagonist
doxapram hydrochloride
[no description available]		2.0510hydrochloridecentral nervous system stimulant
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		3.6180D-glucopyranoseepitope;
mouse metabolite
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2.46202-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
bupivacaine hydrochloride
bupivacaine hydrochloride (anhydrous) : A racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride : A hydrochloride obtained by combining 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide with one molar equivalent of hydrochloric acid.		2.0810hydrochloride;
racemate		adrenergic antagonist;
amphiphile;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
local anaesthetic
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		3.2310aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
ursolic acid
[no description available]		2.4110hydroxy monocarboxylic acid;
pentacyclic triterpenoid		geroprotector;
plant metabolite
n-methylnicotinamide
N-methylnicotinamide: structure. N-methylnicotinamide : A pyridinecarboxamide that is nicotinamide in which one of the amide hydrogens is substituted by a methyl group.		2.7430pyridinecarboxamidemetabolite
1,5-anhydroglucitol
1,5-anhydroglucitol: structure. 1,5-anhydro-D-glucitol : An anhydro sugar of D-glucitol.		2.0510anhydro sugarhuman metabolite
thiazolyl blue
thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.		3.4470organic bromide saltcolorimetric reagent;
dye
thymidine 5'-triphosphate
thymidine 5'-triphosphate: RN given refers to parent cpd. dTTP : A thymidine phosphate having a triphosphate group at the 5'-position.		2.0610pyrimidine 2'-deoxyribonucleoside 5'-triphosphate;
thymidine phosphate		Escherichia coli metabolite;
mouse metabolite
betulinic acid
[no description available]		3.6120hydroxy monocarboxylic acid;
pentacyclic triterpenoid		anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite
baicalin
[no description available]		2.4620dihydroxyflavone;
glucosiduronic acid;
glycosyloxyflavone;
monosaccharide derivative		antiatherosclerotic agent;
antibacterial agent;
anticoronaviral agent;
antineoplastic agent;
antioxidant;
cardioprotective agent;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
ferroptosis inhibitor;
neuroprotective agent;
non-steroidal anti-inflammatory drug;
plant metabolite;
prodrug
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		3.9130azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
amprenavir
[no description available]		4.140carbamate ester;
sulfonamide;
tetrahydrofuryl ester		antiviral drug;
HIV protease inhibitor
oseltamivir
Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.		3.8630acetamides;
amino acid ester;
cyclohexenecarboxylate ester;
primary amino compound		antiviral drug;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
environmental contaminant;
prodrug;
xenobiotic
epigallocatechin gallate
epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis). (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin.		4.4560flavans;
gallate ester;
polyphenol		antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite
fluorexon
fluorexon: structure		2.0310xanthene dyefluorochrome
gallocatechol
gallocatechol: structure give in first source; RN given for (trans-(+-))-omer; inhibits DNA-dependent DNA & RNA polymerases. (+)-gallocatechin : A gallocatechin that has (2R,3S)-configuration. It is found in green tea and bananas.. gallocatechin : A catechin that is a flavan substituted by hydroxy groups at positions 3, 3', 4', 5, 5' and 7 (the trans isomer). It is isolated from Acacia mearnsii.		2.0110gallocatechinantioxidant;
metabolite;
radical scavenger
2'-deoxycytidine 5'-triphosphate
2'-deoxycytidine 5'-triphosphate: RN given refers to unlabeled parent cpd		2.06102'-deoxycytidine phosphate;
pyrimidine 2'-deoxyribonucleoside 5'-triphosphate		Escherichia coli metabolite;
human metabolite;
mouse metabolite
1,2-distearoyllecithin
[no description available]		2.4720
dobutamine hydrochloride
dobutamine hydrochloride : The hydrochloride salt of dobutamine. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used to increase the contractility of the heart in the management of acute heart failure.		2.0510hydrochloridebeta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
ticlopidine hydrochloride
[no description available]		2.0810hydrochloride
epirubicin hydrochloride
[no description available]		2.0810
pyrrolidine dithiocarbamate
pyrrolidine dithiocarbamic acid: spelled pyrolidine in J Nutr 1979 reference; RN given refers to parent cpd. pyrrolidine dithiocarbamate : A member of the class of dithiocarbamic acids that is the N-dithiocarboxy derivative of pyrrolidine.		2.0210dithiocarbamic acids;
pyrrolidines		anticonvulsant;
antineoplastic agent;
geroprotector;
neuroprotective agent;
NF-kappaB inhibitor;
radical scavenger
glutathione disulfide
Glutathione Disulfide: A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized.		2.7330glutathione derivative;
organic disulfide		Escherichia coli metabolite;
mouse metabolite
iopamidol
Iopamidol: A non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiological procedures.. iopamidol : A benzenedicarboxamide compound having N-substituted carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and a (2S)-2-hydroxypropanamido group at the 5-position.		2.0510benzenedicarboxamide;
organoiodine compound;
pentol		environmental contaminant;
radioopaque medium;
xenobiotic
sulconazole, mononitrate, (+-)-isomer
[no description available]		2.0510conazole antifungal drug;
imidazole antifungal drug;
organic nitrate salt
histamine phosphate
histamine phosphate : A phosphate salt that is the diphosphate salt of histamine.		3.2310phosphate salthistamine agonist
tilbroquinol
[no description available]		3.2310organohalogen compound;
quinolines
bendamustine
[no description available]		3.8730benzimidazoles
erdosteine
[no description available]		2.0510N-acyl-amino acid
st 679
[no description available]		2.4420N-acyl-amino acid
droxicam
droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.		3.2310organic heterotricyclic compound;
pyridines		cyclooxygenase 1 inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
prodrug
caroverine
caroverine: structure		2.0810quinoxaline derivative
rutecarpine
rutacarpine: from Evodia rutaecarpa; an ingredient in zhuyu hewei zhitong capsules		2.0710beta-carbolines
ebrotidine
ebrotidine: an H2-receptor antagonist and gastric mucosa protector		3.2310sulfonamide
mizolastine
[no description available]		2.0510benzimidazoles
cgs 9343b
[no description available]		2.0810benzimidazoles
intoplicine
intoplicine: structure in first source		2.0510pyridoindole
pazufloxacin
[no description available]		2.0810quinolines
repaglinide
[no description available]		4.9360piperidines
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		5.390benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
dexfenfluramine
Dexfenfluramine: The S-isomer of FENFLURAMINE. It is a serotonin agonist and is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity.. (S)-fenfluramine : The S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects.		2.0510fenfluramineappetite depressant;
serotonergic agonist;
serotonin uptake inhibitor
2-methoxyestradiol
2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2.		2.753017beta-hydroxy steroid;
3-hydroxy steroid		angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite
estradiol-3-sulfate
estradiol-3-sulfate: RN given refers to (17beta)-isomer. 17beta-estradiol 3-sulfate : A steroid sulfate obtained by the formal condensation of sulfuric acid with the 3-hydroxy group of 17beta-estradiol.		7.021017beta-hydroxy steroid;
steroid sulfate		mammalian metabolite
estradiol 17-sulfate
[no description available]		2.02103-hydroxy steroid;
phenolic steroid;
steroid sulfate		human urinary metabolite
naphthalimides
Naphthalimides: Compounds with three fused rings that appear like a naphthalene fused to piperidone or like a benz(de)isoquinoline-1,3-dione (not to be confused with BENZYLISOQUINOLINES which have a methyl separating the naphthyl from the benzyl rings). Members are CYTOTOXINS.		2.0710
benzeneboronic acid
[no description available]		2.4920boronic acids
4-amino-6-chloro-1,3-benzenedisulfonamide
4-amino-6-chloro-1,3-benzenedisulfonamide: metabolite of hydrochlorothiazide		5.04380sulfonamide
pyrazolo(3,4-d)pyrimidine
[no description available]		2.1710
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		7.741831,2,3-triazole
apaflurane
[no description available]		2.0310
isoimperatorin
isoimperatorin: tumor necrosis factor antagonist isolated from Glehniae root. isoimperatorin : A member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 5. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.		2.1510psoralensEC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite
5,6,7,8-tetrahydro-1-naphthol
5,6,7,8-tetrahydro-1-naphthol : 1-naphthol hydrogenated at C-5, -6, -7 and -8.		2.0610tetralins
disulphane
[no description available]		4.3170
trimethobenzamide monohydrochloride
[no description available]		2.0510
amiloride hydrochloride
amiloride hydrochloride dihydrate : A hydrate that is the dihydrate of amiloride hydrochloride.		2.0510hydratediuretic;
sodium channel blocker
miconazole nitrate
miconazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-miconazole nitrate. An antifungal used for the treatment of athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.		2.0810
econazole nitrate
econazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-econazole nitrate. Used to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.		2.0510
medetomidine
Medetomidine: An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE.		2.0510imidazoles
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		4.13312-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
sertraline
Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		11.8671dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor
lomefloxacin hydrochloride
lomefloxacin hydrochloride : The hydrochloride salt of lomefloxacin. It is administered by mouth to treat bacterial infections including bronchitis and urinary tract infections. It is also used topically as eye drops for the treatment of bacterial conjunctivitis, and as ear drops for the treatment of otitis externa and otitis media.		2.0510hydrochlorideantimicrobial agent;
antitubercular agent;
photosensitizing agent
sanguinarine chloride
[no description available]		2.0410
picosulfate sodium
picosulfate sodium: contains two active ingredients, sodium picosulfate and magnesium citrate, which are both laxatives; structure		2.0510aryl sulfate;
pyridines
zoledronic acid
Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.		9.791131,1-bis(phosphonic acid);
imidazoles		bone density conservation agent
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
brinzolamide
brinzolamide: an antiglaucoma agent		7.12400sulfonamide;
thienothiazine		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
dienogest
[no description available]		2.051017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
aliphatic nitrile;
steroid hormone		progesterone receptor agonist;
progestin;
synthetic oral contraceptive
flunoxaprofen
flunoxaprofen: structure given in first source. flunoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group (the S-enantiomer). Although it was shown to be effective in treatment of rheumatoid arthritis and osteoarthritis, the clinical use of flunoxaprofen was discontinued due to possible hepatotoxic side-effects.		2.05101,3-benzoxazoles;
monocarboxylic acid;
organofluorine compound		antirheumatic drug;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
protein kinase C agonist
tianeptine
tianeptine: structure given in first source. tianeptine : A racemate comprising of equimolar amounts of (R)- and (S)-tianeptine. It is an atypical antidepressant used in Europe to treat patients who respond poorly to selective serotonin reuptake inhibitors (SSRIs).. 7-[(3-chloro-6-methyl-5,5-dioxido-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid : A member of the class of dibenzothiazepines that is 3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide substituted by a (6-carboxyhexyl)amino group at position 11.. (S)-tianeptine : The S-enantiomer of tianeptine.		2.0510dibenzothiazepine;
monocarboxylic acid;
organochlorine compound
drospirenone
drospirenone: a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source		2.08103-oxo-Delta(4) steroid;
steroid lactone		aldosterone antagonist;
contraceptive drug;
progestin
artemether
Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810artemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid		antimalarial
piloty's acid
Piloty's acid: structure in first source		2.1110sulfonamide
2,4-disulfamyl-5-trifluoromethylaniline
2,4-disulfamyl-5-trifluoromethylaniline: precursor of hydroflumethiazide		4.96350
4-bromobenzenesulfonamide
4-bromobenzenesulfonamide: a metabolite of ebrotidine		2.0710
n-demethylantipyrine
[no description available]		2.110pyrazoles;
ring assembly
morphazinamide
morphazinamide: RN given refers to parent cpd; RN in Chemline for mono-HCL: 1473-73-0; structure in Merck Index		2.0510morpholines;
pyrazines;
secondary carboxamide
acamprosate
Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3.		3.2310acetamides;
organosulfonic acid		environmental contaminant;
neurotransmitter agent;
xenobiotic
isaxonine
isaxonine: promotes nerve growth		3.2310aminopyrimidine
nebivolol
2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group.		3.2310chromanes;
diol;
organofluorine compound;
secondary alcohol;
secondary amino compound
lazabemide
lazabemide: structure given in first source		3.4110
uk 68798
[no description available]		3.8830aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
hp 873
iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.		3.61201,2-benzoxazoles;
aromatic ether;
aromatic ketone;
methyl ketone;
monoamine;
organofluorine compound;
piperidines;
tertiary amino compound		dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist
dexrazoxane
Dexrazoxane: The (+)-enantiomorph of razoxane.		3.5920razoxaneantineoplastic agent;
cardiovascular drug;
chelator;
immunosuppressive agent
masoprocol
Masoprocol: A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils.. masoprocol : The meso-form of nordihydroguaiaretic acid. An antioxidant found in the creosote bush, Larrea divaricata, it is a potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. It also inhibits (though to a lesser extent) formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase.		2.7330nordihydroguaiaretic acidantineoplastic agent;
hypoglycemic agent;
lipoxygenase inhibitor;
metabolite
loxapine succinate
[no description available]		2.0810succinate saltgeroprotector
tocophersolan
tocophersolan: RN given refers to parent cpd		3.0640tocol
loperamide hydrochloride
loperamide hydrochloride : A hydrochloride obtained by combining loperamide with one equivalent of hydrochloric acid. Used for treatment of diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		2.0510hydrochlorideanticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
a 78773
A 78773: a 5-lipoxygenase inhibitor		2.0510
fenoxypropazine
[no description available]		3.2310aromatic ether
trichlorosucrose
trichlorosucrose: sweetness intensity roughly 600 times that of sucrose and is nonnutritive and noncaloric; largely unabsorbed in the gastrointestinal tract. sucralose : A disaccharide derivative consisting of 4-chloro-4-deoxy-alpha-D-galactopyranose and 1,6-dichloro-1,6-dideoxy-beta-D-fructofuranose units linked by a glycosidic bond.		210disaccharide derivative;
organochlorine compound		environmental contaminant;
sweetening agent;
xenobiotic
voriconazole
Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.		3.8730conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug		P450 inhibitor
betamipron
[no description available]		2.0810organonitrogen compound;
organooxygen compound
bufuralol
bufuralol: RN given refers to cpd without isomeric designation; structure		2.7330benzofurans
prifelone
prifelone: structure given in first source		3.1210aromatic ketone
uroxatral
[no description available]		2.0810hydrochloride
aceclofenac
[no description available]		8.0574amino acid;
carboxylic ester;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
nitrefazole
[no description available]		3.2310imidazoles
alacepril
[no description available]		2.0810dipeptide;
thioacetate ester		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
cyclobutyrol
cyclobutyrol: RN given refers to parent cpd; structure. cyclobutyrol : A hydroxy monocarboxylic acid in which the hydroxy group is geminal to a 1-carboxypropyl group on a cyclohexane ring.		2.0510hydroxy monocarboxylic acidbile therapy drug
thiocolchicoside
[no description available]		2.0810glycoside
terlipressin
terlivaz: first FDA approved injection to improve kidney function in adults with hepatorenal syndrome (HRS) with rapid reduction in kidney function.		2.0510polypeptide
ubenimex
ubenimex: growth inhibitor		9.2850
7-hydroxystaurosporine
[no description available]		7.0710
hesperetin
[no description available]		2.66203'-hydroxyflavanones;
4'-methoxyflavanones;
monomethoxyflavanone;
trihydroxyflavanone		antineoplastic agent;
antioxidant;
plant metabolite
honokiol
[no description available]		7.2510biphenyls
isoflavone
[no description available]		2.0510isoflavones
chelerythrine chloride
[no description available]		2.0410
clevudine
[no description available]		2.0510
gentamicin c1a
[no description available]		3.3110gentamycin C
dmp 323
(4R,5S,6S,7R)-4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(hydroxymethyl)benzyl]-1,3-diazepan-2-one : A 1,3-diazepanone ring with two 4-(hydroxymethyl)benzyl groups as substituents at positions N-1 and N-4, two benzyl groups at C-4 and C-7, and two hydroxy groups at C-5 and C-6 respectively.		2.0610diazepanone;
ureas		anti-HIV agent;
metabolite
grepafloxacin
grepafloxacin: structure in first source		2.0510fluoroquinolone antibiotic;
quinolines;
quinolone antibiotic
zaluzanin C
zaluzanin C: from Ainsliaea yunnanensis and Zaluzania robinsonii; structure in first source. zaluzanin C : A sesquiterpene lactone that is decahydroazuleno[4,5-b]furan-2(3H)-one substituted by methylidene groups at positions 3, 6 and 9 and a hydroxy group at position 8.		3.3110gamma-lactone;
guaiane sesquiterpenoid;
organic heterotricyclic compound;
secondary alcohol;
sesquiterpene lactone		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
metabolite
2-aminobenzenesulfonamide
[no description available]		4.31180benzenes;
sulfonamide
tetrandrine
tetrandrine: a bisbenzylisoquinoline that exhibits antifibrogenic activity		2.0510bisbenzylisoquinoline alkaloid;
isoquinolines
doripenem
Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.		3.6120carbapenems
tryptanthrine
tryptanthrine: minor constituent of traditional Chinese medicine qing dai		2.0710alkaloid antibiotic;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound
corilagin
corilagin: isolated from Geranii herba. corilagin : An ellagitannin with a hexahydroxydiphenoyl group bridging over the 3-O and 6-O of the glucose core.		2.110ellagitannin;
gallate ester		antihypertensive agent;
antioxidant;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
non-steroidal anti-inflammatory drug
2-naphthylisothiocyanate
[no description available]		2.0510
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		3.2310hydroxy-1,2-naphthoquinone
dicetylphosphate
dicetylphosphate: RN given refers to parent cpd. dicetyl hydrogen phosphate : The dihexadecyl ester of phosphoric acid.		2.0510dialkyl phosphate
rivastigmine
[no description available]		4.6940carbamate ester;
tertiary amino compound		cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent
frovatriptan
[no description available]		3.2310carbazoles
eletriptan
eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.		3.620indoles;
N-alkylpyrrolidine;
sulfone		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rosiglitazone
[no description available]		10.47110aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
tamiflu
[no description available]		2.0810phosphate salt
bexarotene
[no description available]		9.7690benzoic acids;
naphthalenes;
retinoid		antineoplastic agent
s20098
[no description available]		2.5220acetamides
flunisolide
flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones		2.081011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
primary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug;
immunosuppressive agent
sulfamide
sulfamide : The simplest of the sulfamic acids consisting of a single sulfur atom covalently bound by single bonds to two amino groups and by double bonds to two oxygen atoms.		2.7530sulfamides
4-nitrophenylglucuronide
4-nitrophenyl beta-D-glucuronide : A beta-D-glucosiduronic acid having a 4-nitrophenyl substituent at the anomeric position.		2.0410beta-D-glucosiduronic acid;
C-nitro compound		chromogenic compound
3,4-dihydroxyphenylethanol
3,4-dihydroxyphenylethanol: serotonin metabolite; structure		2.2110catechols;
primary alcohol		antineoplastic agent;
antioxidant;
metabolite
chloroquine diphosphate
[no description available]		2.0510
orphenadrine citrate
orphenadrine citrate : A citrate salt which comprises equimolar amounts of orphenadrine and citric acid.		2.0510citrate saltH1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
acetaminophen glucuronide
acetaminophen glucuronide: acetaminophen metabolite in rats. acetaminophen O-beta-D-glucosiduronic acid : A beta-D-glucosiduronic acid that is the O-glucuronide of paracetamol (acetaminophen).		2.0410beta-D-glucosiduronic aciddrug metabolite
ketorolac tromethamine
Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.		2.7530organoammonium saltanalgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor
clarithromycin
Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.		6.6382macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
5-amino-1,3,4-thiadiazole-2-sulfonamide
5-amino-1,3,4-thiadiazole-2-sulfonamide: structure in first source		5.04380
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		8.55803-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
n-(3,5-dichlorophenyl)succinimide
N-(3,5-dichlorophenyl)succinimide: nephrotoxic; post-treatment enhanced induction of renal cell tumors in rats by dimethylnitrosamine, pre-treatment inhibited induction of tumors, & alone caused interstitial nephritis but no tumors		2.0510pyrrolidines
fibrinogen
Fibrinogen: Plasma glycoprotein clotted by thrombin, composed of a dimer of three non-identical pairs of polypeptide chains (alpha, beta, gamma) held together by disulfide bonds. Fibrinogen clotting is a sol-gel change involving complex molecular arrangements: whereas fibrinogen is cleaved by thrombin to form polypeptides A and B, the proteolytic action of other enzymes yields different fibrinogen degradation products.. D-iditol : The D-enantiomer of iditol.		3.4211iditolfungal metabolite
moexipril
[no description available]		3.2310peptide
phentolamine mesylate
[no description available]		2.0510
oxybutynin hydrochloride
[no description available]		2.0510hydrochloride
homocysteine
Homocysteine: A thiol-containing amino acid formed by a demethylation of METHIONINE.. homocysteine : A sulfur-containing amino acid consisting of a glycine core with a 2-mercaptoethyl side-chain.. L-homocysteine : A homocysteine that has L configuration.		2.1310amino acid zwitterion;
homocysteine;
serine family amino acid		fundamental metabolite;
mouse metabolite
4-hydroxypropranolol
4-hydroxypropranolol: metabolite of propanolol; RN given refers to parent cpd without isomeric designation		2.0810naphthols
gliquidone
gliquidone: structure; RN given refers to parent cpd		2.0810isoquinolines
cordium
bepridil hydrochloride monohydrate : The hydrochloride monohydrate of bepridril.		2.0510hydrate;
hydrochloride
levobupivacaine
Levobupivacaine: S-enantiomer of bupivacaine that is used as a local anesthetic and for regional nerve blocks, including EPIDURAL ANESTHESIA.. levobupivacaine : The (S)-(-)-enantiomer of bupivacaine.		6.53331-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamideadrenergic antagonist;
amphiphile;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
local anaesthetic
meclizine hydrochloride
[no description available]		2.0510
zofenopril
zofenopril: structure given in first source; SQ 26900 refers to K salt & SQ 26991 to Ca salt. zofenopril : A proline derivative that is 4-(phenylsulfanyl)-L-proline in which the amine proton is replaced by a (2S)-3-(benzoylsulfanyl)-2-methylpropanoyl group. A prodrug for zofenoprilat.		3.1510aryl sulfide;
L-proline derivative;
N-acyl-L-amino acid;
thioester		anticonvulsant;
apoptosis inhibitor;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug;
vasodilator agent
mci 9038
[no description available]		3.2310peptide
lopinavir
[no description available]		4.2650amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
estrone 3-methyl ether
estrone 3-methyl ether: RN given refers to cpd with unspecified isomeric designation; structure		2.0610
glycylsarcosine
glycylsarcosine : A dipeptide obtained by formal condensation of the carboxy group of glycine with the amino group of sarcosine.		3.1510dipeptide zwitterion;
dipeptide
aminozolamide
aminozolamide: used in therapy of ocular hypertension		2.0810
6-hydroxyethoxzolamide
6-hydroxyethoxzolamide: structure given in first source		2.0810
glucuronic acid
Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form.		2.7630D-glucuronic acidalgal metabolite
1,3,4-oxadiazole
1,3,4-oxadiazole: structure in first source		2.4110
syringaresinol
[no description available]		3.3110aromatic ether;
furofuran;
lignan;
polyether;
polyphenol		plant metabolite
nepodin
nepodin: isolated from Rumex crispus		2.110naphthols
moxifloxacin hydrochloride
moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride.		2.0810hydrochlorideantibacterial drug
cobalt
Cobalt: A trace element that is a component of vitamin B12. It has the atomic symbol Co, atomic number 27, and atomic weight 58.93. It is used in nuclear weapons, alloys, and pigments. Deficiency in animals leads to anemia; its excess in humans can lead to erythrocytosis.. cobalt(1+) : A monovalent inorganic cation obtained from cobalt.. cobalt atom : A cobalt group element atom that has atomic number 27.		2.4720cobalt group element atom;
metal allergen		micronutrient
p-methoxy-n-methylphenethylamine
p-Methoxy-N-methylphenethylamine: A potent mast cell degranulator. It is involved in histamine release.. N,O-dimethyltyramine : A secondary amino compound that is tyramine in which the hydrogen of the phenolic hydroxy group has been replaced by a methyl group.		2.0410aromatic ether;
secondary amino compound		metabolite
fulvestrant
Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.		3.863017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
mizoribine
[no description available]		2.0810imidazolesanticoronaviral agent
desethylamiodarone
desethylamiodarone: metabolite of amiodarone; structure given in first source		2.4110aromatic ketone
enkephalin, d-penicillamine (2,5)-
Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.. DPDPE : A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond.		2.110heterodetic cyclic peptidedelta-opioid receptor agonist
vitamin b 6
Vitamin B 6: VITAMIN B 6 refers to several PICOLINES (especially PYRIDOXINE; PYRIDOXAL; & PYRIDOXAMINE) that are efficiently converted by the body to PYRIDOXAL PHOSPHATE which is a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, and aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into PYRIDOXAMINE phosphate. Although pyridoxine and Vitamin B 6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading (EE Snell; Ann NY Acad Sci, vol 585 pg 1, 1990). Most of vitamin B6 is eventually degraded to PYRIDOXIC ACID and excreted in the urine.		4.3911
sr141716
[no description available]		2.7830amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
bosentan anhydrous
Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.		4.4260primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
eudragit rs
Eudragit RS: copolymer of acrylic & methacrylic acid esters & quaternary ammonium groups; used for microcapsules		2.0310
fluo-3
Fluo-3: fluorescent Ca(2+) indicator; permits continuous monitoring of Ca without interference with use of UV-sensitive caged compounds		2.4620xanthene dyefluorochrome
laurdan
laurdan: RN from CA Index Guide		2.0610
paxilline
paxilline: structure given in first source; RN given refers to (2R-(2alpha,4bbeta,6aalpha,12bbeta,12calpha,14abeta))-isomer. paxilline : An indole diterpene alkaloid with formula C27H33NO4 isolated from Penicillium paxilli. It is a potent inhibitor of large conductance Ca2(+)- and voltage-activated K(+) (BK)-type channels.		3.3510diterpene alkaloid;
enone;
organic heterohexacyclic compound;
terpenoid indole alkaloid;
tertiary alcohol		anticonvulsant;
Aspergillus metabolite;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
genotoxin;
geroprotector;
mycotoxin;
Penicillium metabolite;
potassium channel blocker
selenomethionine
[no description available]		2.0510amino acid zwitterion;
selenomethionine		plant metabolite
artesunic acid
[no description available]		2.110
vinpocetine
[no description available]		2.0810
fluorocitrate
fluorocitrate: competitve inhibitor of aconitase; effects morphology of kidney tubules in fluorocitrate poisoning; RN given refers to cpd with unspecified isomeric designation		2.0210carbonyl compound
eudragit-e
Eudragit-E: a cationic polymer, used as a embolic material for arteriovenous malformations and as a taste masker		2.1510
racecadotril
racecadotril: parenterally active enkephalinase inhibitor		2.0810N-acyl-amino acid
saikosaponin d
[no description available]		3.3510
perindopril
Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline		3.5920alpha-amino acid ester;
dicarboxylic acid monoester;
ethyl ester;
organic heterobicyclic compound		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
n-monodemethyldiltiazem
N-monodemethyldiltiazem: RN given refers to (cis)-isomer; structure given in first source		2.0810benzothiazepine
deguelin
deguelin: a natural product from Mundulea sericea; RN refers to (7aS-cis)-isomer; structure given in first source. deguelin : A rotenone that is 13,13a-dihydro-3H-chromeno[3,4-b]pyrano[2,3-h]chromen-7(7aH)-one substituted by methoxy groups at positions 9 and 10, and by two methyl groups at position 3 (the 7aS,13aS-stereoisomer). It exists in abundant quantities in the bark, roots, and leaves of the Leguminosae family of plants and reported to exert anti-tumour effects in various cancers.		2.0810aromatic ether;
diether;
organic heteropentacyclic compound;
rotenones		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
mitochondrial NADH:ubiquinone reductase inhibitor;
plant metabolite
fingolimod hydrochloride
Fingolimod Hydrochloride: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.. fingolimod hydrochloride : The hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod).		2.0710hydrochlorideimmunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
fingolimod
fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.		3.6220aminodiol;
primary amino compound		antineoplastic agent;
CB1 receptor antagonist;
immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
triptolide
[no description available]		2.0810diterpenoid;
epoxide;
gamma-lactam;
organic heteroheptacyclic compound		antispermatogenic agent;
plant metabolite
parthenolide
[no description available]		2.0210germacranolide
carboxyamido-triazole
carboxyamido-triazole: structure given in first source; coccidiostat; U.S. patent No. 4,590,201		7.0210
ecteinascidin 743
[no description available]		2.0510acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound		alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite
1-hexadecyl-2-acetyl-glycero-3-phosphocholine
Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.		2.43202-acetyl-1-alkyl-sn-glycero-3-phosphocholineantihypertensive agent;
beta-adrenergic antagonist;
bronchoconstrictor agent;
hematologic agent;
vasodilator agent
sr 140333
SR 140333: SR-140603 is the (R)-antipode of SR-140333; a neurokinin-1 receptor antagonist		2.0510
deoxyglucose
Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.		2.110
tadalafil
[no description available]		4.4560benzodioxoles;
pyrazinopyridoindole		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
glycofurol
[no description available]		2.110
thromboxanes
thromboxane : A class of oxygenated oxane derivatives, originally derived from prostaglandin precursors in platelets, that stimulate aggregation of platelets and constriction of blood vessels.		6.6961
benzyloxyresorufin
[no description available]		210
voltarol
diclofenac diethylamine: structure in first source		2.1710
ponasterone a
ponasterone A: RN given refers to (2 beta,3 beta,5 beta,22R)-isomer		2.051014alpha-hydroxy steroid;
20-hydroxy steroid;
22-hydroxy steroid;
2beta-hydroxy steroid;
3beta-hydroxy steroid;
6-oxo steroid;
phytoecdysteroid
paliperidone
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia.		3.23101,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol
sc 58125
1-((4-methylsulfonyl)phenyl)-3-trifluoromethyl-5-(4-fluorophenyl)pyrazole: a COX-2 inhibitor		4.4580organofluorine compound;
pyrazoles;
sulfone		antineoplastic agent;
cyclooxygenase 2 inhibitor
nitisinone
[no description available]		3.5920(trifluoromethyl)benzenes;
C-nitro compound;
cyclohexanones;
mesotrione		EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor
plavix
[no description available]		2.4720azaheterocycle sulfate salt;
organoammonium sulfate salt		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
bw 373u86
BW 373U86: a nonpeptidic delta opioid receptor agonist		2.0110diarylmethane
marimastat
marimastat: a matrix metalloproteinase inhibitor active in patients with advanced carcinoma of the pancreas, prostate, or ovary. marimastat : A secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide.		2.0510hydroxamic acid;
secondary carboxamide		antineoplastic agent;
matrix metalloproteinase inhibitor
nitroaspirin
nitroaspirin: a nitric oxide donor		5.1931carbonyl compound
7-methoxytacrine
[no description available]		3.2710
clofarabine
[no description available]		4.0940adenosines;
organofluorine compound		antimetabolite;
antineoplastic agent
sr 48692
SR 48692: structure in first source; a neurotensin receptor-1 antagonist		2.0810N-acyl-amino acid
bw 245c
BW 245C: a selective DP receptor agonist. BW 245C : A racemate comprising equimolar amounts of (3R,4S)- and (3S,4R)-BW 245C. A hydantoin-based prostglandin analogue.. 7-[3-(3-cyclohexyl-3-hydroxypropyl)-2,5-dioxoimidazolidin-4-yl]heptanoic acid : A imidazolidine-2,4-dione that is 7-(2,5-dioxoimidazolidin-4-yl)heptanoic acid in which the imidazoline ring as substituted at position 3 by a 3-(3-cyclohexyl-3-hydroxypropyl) group.		210imidazolidine-2,4-dione;
monocarboxylic acid;
secondary alcohol
elacridar
Elacridar: inhibitor of MDR1 PROTEIN; structure given in first source		2.9840
caprylates
Caprylates: Derivatives of caprylic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain a carboxy terminated eight carbon aliphatic structure.. octanoate : A straight-chain saturated fatty acid anion that is the conjugate base of octanoic acid (caprylic acid); believed to block adipogenesis.		2.4920fatty acid anion 8:0;
straight-chain saturated fatty acid anion		human metabolite;
Saccharomyces cerevisiae metabolite
1,3,4-thiadiazole
1,3,4-thiadiazole: structure given in first source		2.2510thiadiazole
ah 6809
6-isopropoxy-9-oxoxanthene-2-carboxylic acid: structure given in UD		3.250xanthones
pramipexole
Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.		4.9440benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
valdecoxib
[no description available]		14.151294isoxazoles;
sulfonamide		antipyretic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
parecoxib
parecoxib: structure in first source. parecoxib : An N-acylsulfonamide resulting from the formal condensation of valdecoxib with propionic acid. It is a prodrug for valdecoxib.		13.413011isoxazoles;
N-sulfonylcarboxamide		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
a 63162
N-hydroxy-N-(1-(4-(phenylmethoxy)phenyl)ethyl)-acetamide: structure given in first source		2.4520
mitiglinide
mitiglinide: a rapid and short-acting hypoglycemic agent; acts on sulfonylurea receptor closing KATP channels; considered one of the glinides-an imprecise grouping; structure given in first source		2.0510benzenes;
monocarboxylic acid
ezogabine
ezogabine: structure in first source. ezogabine : A substituted aniline that is benzene-1,2,4-triamine bearing ethoxycarbonyl and 4-fluorobenzyl substituents at positions N-1 and N-4 respectively. An anticonvulsant used to treat seizures associated with epilepsy in adults.		2.7730carbamate ester;
organofluorine compound;
secondary amino compound;
substituted aniline		anticonvulsant;
potassium channel modulator
hydroxypropylmethylcellulose acetate succinate
hydroxypropylmethylcellulose acetate succinate: structure given in first source		3.2350
kadsurenone
kadsurenone: platelet-activating factor receptor antagonist from Chinese herbal plant, haifenteng; structure given in first source; RN given refers to (2s-(2alpha,3beta,3aalpha))-isomer		2.0510benzofurans
peroxynitrous acid
Peroxynitrous Acid: A potent oxidant synthesized by the cell during its normal metabolism. Peroxynitrite is formed from the reaction of two free radicals, NITRIC OXIDE and the superoxide anion (SUPEROXIDES).		2.4520nitrogen oxoacid
diethylaminosulfur trifluoride
diethylaminosulfur trifluoride: fluorinating agent for carbohydrates		2.1310
fullerene c60
Fullerenes: A polyhedral CARBON structure composed of around 60-80 carbon atoms in pentagon and hexagon configuration. They are named after Buckminster Fuller because of structural resemblance to geodesic domes. Fullerenes can be made in high temperature such as arc discharge in an inert atmosphere.. fullerene : A compound composed solely of an even number of carbon atoms, which form a cage-like fused-ring polycyclic system with twelve five-membered rings and the rest six-membered rings. The term has been broadened to include any closed cage structure consisting entirely of three-coordinate carbon atoms.		2.1710fullerenegeroprotector
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		3.93120methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
almotriptan
almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.		3.2310indoles;
sulfonamide;
tertiary amine		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
mk 0663
[no description available]		16.017910bipyridines;
organochlorine compound;
sulfone		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
gefitinib
[no description available]		8.49314aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine
N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine: structure given in first source; a selective A(3) adenosine receptor agonist. 3-iodobenzyl-5'-N-methylcarboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and one of the hydrogens of the exocyclic amino function is substituted by a 3-iodobenzyl group.		2.0510adenosines;
monocarboxylic acid amide;
organoiodine compound		adenosine A3 receptor agonist
bay x 1005
2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid: inhibits synthesis of leukotriene B4 and 5-hydroxyeicosatetraenoic acid; inhibits five-lipoxygenase activating protein(FLAP)and leukotriene A4 hydrolase(LTA4H); structure given in first source;		2.0810
sq 28603
SQ 28603: a selective neutral endopeptidase inhibitor		3.1210
angiotensin ii, des-phe(8)-
Ile(5)-angiotensin II (1-7) : An angiotensin compound consisting of the linear heptapeptide sequence L-Asp-L-Arg-L-Val-L-Tyr-L-Ile-L-His-L-Pro.		2.1110amino acid zwitterion;
angiotensin		vasodilator agent
n,n-dimethylarginine
N,N-dimethylarginine: asymmetric dimethylarginine; do not confuse with N,N'-dimethylarginine. N(omega),N(omega)-dimethyl-L-arginine : A L-arginine derivative having two methyl groups both attached to the primary amino moiety of the guanidino group.		2.5720dimethylarginine;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor
bradykinin, leu(8)-des-arg(9)-
bradykinin, Leu(8)-des-Arg(9)-: RN given refers to (L)-isomer		2.0210
tetrahydrocurcumin
tetrahydrocurcumin : A beta-diketone that is curcumin in which both of the double bonds have been reduced to single bonds.		7.1310beta-diketone;
diarylheptanoid;
polyphenol		metabolite
desloratadine
desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.		3.8930benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
desvenlafaxine
O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine.		3.2310cyclohexanols;
phenols;
tertiary amino compound		antidepressant;
drug metabolite;
marine xenobiotic metabolite
t-butyloxycarbonyl-methionyl-leucyl-phenylalanine
[no description available]		2.4520
butyloxycarbonyl-phenylalanyl-leucyl-phenylalanyl-leucyl-phenylalanine
butyloxycarbonyl-phenylalanyl-leucyl-phenylalanyl-leucyl-phenylalanine: formyl peptide antagonist and lipoxin A4 receptor antagonist		2.0210
gyki 53655
GYKI 53655: an AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate) receptor antagonist		2.0810
methotrexate
[no description available]		11.37357dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
reboxetine
Reboxetine: A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER.		7.4154aromatic ether
n-4-nitrobenzo-2-oxa-1,3-diazoledipalmitoyl phosphatidylethanolamine
[no description available]		2.0610
estrone-3-o-sulfamate
estrone-3-O-sulfamate: a steroid sulfatase inhibitor		2.4220
bmy 45778
BMY 45778: structure given in first source; partial prostacyclin agonist		2.0610bisoxazolepartial prostacyclin agonist
3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2(5h)-furanone
3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2(5H)-furanone: structure given in first source		3.5520
tamsulosin
[no description available]		3.23105-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent
rufinamide
rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source		3.2310aromatic amide;
heteroarene
antiprimod
azaspirane: structure given in first source		2.0510
sulbactam
[no description available]		2.4720penicillanic acids
exp7711
EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source		2.0610
o-demethyltramadol
O-demethyltramadol: one of the major metabolites of tramadol; structure given in first source; RN given refers to parent compound		3.5611
olmesartan medoxomil
Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.		4.140biphenyls
sauristolactam
sauristolactam: lactam of 10-aminomethyl-3-hydroxy-4-methoxyphenanthrene-1-carboxylic acid isolated from Saururus cernuus; structure given in first source		2.0510
dexpanthenol
dexpanthenol: The alcohol of pantothenic acid		3.2310amino alcohol;
monocarboxylic acid amide		cholinergic drug;
provitamin
fosamprenavir
fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir.		3.2310sulfonamideprodrug
pagoclone
RP 59037: a partial benzodiazepine receptor agonist; a cyclopyrrolone that induces hypothermia		2.0810
bmy 42393
BMY 42393: partial prostacyclin agonist		2.0610
ici d2138
ICI D2138: structure given in first source; inhibitor of leukotriene B4 synthesis		2.7330
ilomastat
CS 610: matrix metalloproteinase inhibitor; structure in first source. ilomastat : An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor		2.4820hydroxamic acid;
L-tryptophan derivative;
N-acyl-amino acid		anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
EC 3.4.24.24 (gelatinase A) inhibitor;
neuroprotective agent
omega-n-methylarginine
omega-N-Methylarginine: A competitive inhibitor of nitric oxide synthetase.. N(omega)-methyl-L-arginine : A L-arginine derivative with a N(omega)-methyl substituent.		2.9540amino acid zwitterion;
arginine derivative;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid
abiraterone
[no description available]		4.17403beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines		antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
rupatadine
rupatadine: structure given in first source; RN given refers to trihydrochloride		3.1210benzocycloheptapyridine
ml-3000
[no description available]		5.7140
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		2.0610
5-carboxyfluorescein diacetate
[no description available]		2.4620
n(alpha)-(4-toluenesulfonyl)-4-amidinophenylalanylpiperidine
N(alpha)-(4-toluenesulfonyl)-4-amidinophenylalanylpiperidine: binds to thrombin & trypsin; structure given in first source		2.0210
rhc 3164
7-chloro-5-propyl-1,2,4-triazolo(4,3-a)quinoxaline-1,4(2H,5H)-dione: structure given in first source		3.5110
febuxostat
Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout.		3.89301,3-thiazolemonocarboxylic acid;
aromatic ether;
nitrile		EC 1.17.3.2 (xanthine oxidase) inhibitor
pomalidomide
3-aminophthalimidoglutarimide: structure in first source		2.1110aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
valerylsalicylate
valerylsalicylic acid: significantly inhibited [3H]thymidine; inhibitor of normal epithelial cell proliferation and growth of malignant cells. valerylsalicylic acid : A valerate ester that is salicylic acid in which the phenolic hydrogen is replaced by a valeryl (pentanoyl) group.		2.0110benzoic acids;
salicylates;
valerate ester		cyclooxygenase 1 inhibitor
cd 437
CD 437: selective for retinoic acid receptors gamma. CD437 : A naphthoic acid that is 6-phenylnaphthylene-2-carboxyic acid in which the phenyl substituent has been substituted at positions 3 and 4 by adamant-1-yl and hydroxy groups, respectively. It acts as a selective agonist of retinoic acid receptor (RAR)gamma and induces cell cycle arrest and apoptosis in various cancer cells.		2.0810adamantanes;
monocarboxylic acid;
naphthoic acid;
phenols		apoptosis inducer;
retinoic acid receptor gamma agonist
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.0810amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
escitalopram
Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram.		8.73201-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrileantidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
lexapro
Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram.		2.0810
3-(3,5-dichlorophenyl)-1-methyl-2,5-pyrrolidinedione
[no description available]		3.9911
10-propargyl-10-deazaaminopterin
10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.		3.2310N-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
docetaxel
[no description available]		2.4620hydrate;
secondary alpha-hydroxy ketone		antineoplastic agent
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		13.073817secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
perifosine
[no description available]		7.7830ammonium betaine;
phospholipid		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
atazanavir
atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).		3.8730carbohydrazideantiviral drug;
HIV protease inhibitor
tariquidar
[no description available]		3.1510benzamides
nsc-141549
[no description available]		2.0510
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		4.93609-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		4.2750azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
ertapenem
Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.		3.2310carbapenemcarboxylic acid;
pyrrolidinecarboxamide		antibacterial drug
nepafenac
nepafenac: amide analog of amfenac; structure in first source. nepafenac : A monocarboxylic acid amide that is amfenac in which the carboxylic acid group has been converted into the corresponding carboxamide. It is a prodrug for amfenac, used in eye drops to treat pain and inflammation following cataract surgery.		2.4620monocarboxylic acid amidecyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
cox 189
lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity.		13.783112amino acid;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
secondary amino compound		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
conivaptan
conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH).		3.2310benzazepineaquaretic;
vasopressin receptor antagonist
cariporide
cariporide: a selective sodium-hydrogen exchange subtype 1 inhibitor; structure in first source		2.0510
tezosentan
tezosentan: structure in first source		2.0510
mk 767
5-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide: an antihyperlipidemic agent that also functions as an insulin sensitizer, PPARalpha agonist, and PPARgamma agonist; structure in first source		3.5520
vatalanib
[no description available]		4.0920monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
enkephalin-leu, des-tyr(1)-
enkephalin-Leu, des-Tyr(1)-: RN given refers to all (L)-isomer		2.1310
n-(3,4,5-trichlorophenyl)succinimide
[no description available]		2.0610
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		6.231aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
pralnacasan
pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source		3.2310
clevidipine
clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source		3.2310dihydropyridine
jtt 501
JTT 501: an insulin sensitizer; structure in first source		2.0510
solifenacin
[no description available]		3.2310isoquinolines
dexmethylphenidate
dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate.		3.2310methyl phenyl(piperidin-2-yl)acetateadrenergic agent
bazedoxifene acetate
[no description available]		2.0810
4-methoxyhonokiol
4-methoxyhonokiol: an NSAID isolated from Magnolia obovata; structure in first source		2.0710
moracin c
[no description available]		3.2710benzofurans
xamoterol
Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.		2.0810morpholines
disopyramide, (s)-isomer
[no description available]		2.0410
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		20.1621075methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
canertinib
[no description available]		2.0810monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
cinacalcet
cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.		3.2310(trifluoromethyl)benzenes;
naphthalenes;
secondary amino compound		calcimimetic;
P450 inhibitor
birb 796
[no description available]		2.0810aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator
bms 207940
N-((2'-(((4,5-dimethyl-3-isoxazolyl)amino)sulfonyl)-4-(2-oxazolyl)(1,1'-biphenyl)-2-yl)methyl)-N,3,3-trimethylbutanamide: an ET(A) receptor antagonist; structure in first source		3.1210
hydroxyl radical
Hydroxyl Radical: The univalent radical OH. Hydroxyl radical is a potent oxidizing agent.		2.4420oxygen hydride;
oxygen radical;
reactive oxygen species
lubiprostone
[no description available]		3.2310
methyl 5-aminolevulinate
methyl 5-aminolevulinate: esterified form of aminolevulinic acid used as PHOTOCHEMOTHERAPY. methyl 5-aminolevulinate : The methyl ester of 5-aminolevulinic acid. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells.		2.0510delta-amino acid esterantineoplastic agent;
dermatologic drug;
photosensitizing agent;
prodrug
olmesartan
olmesartan: an active metabolite of CS 866		3.8530biphenylyltetrazoleangiotensin receptor antagonist;
antihypertensive agent
telbivudine
[no description available]		3.6120pyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
jte 522
tiracoxib: The combined administration of tiracoxib with probucol significantly inhibited the tumor growth. The angiogenesis was markedly reduced; no further information available 1/31/2001. tilmacoxib : A member of the class of 1,3-oxazoles that is that is 1,3-oxazole which is substituted at positions 2, 4 and 5 by methyl, cyclohexyl, and 3-fluoro-4-sulfamoylphenyl groups, respectively.		2.41201,3-oxazoles;
organofluorine compound;
sulfonamide		cyclooxygenase 2 inhibitor
tipifarnib
[no description available]		2.8230imidazoles;
monochlorobenzenes;
primary amino compound;
quinolone		antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor
atrasentan
Atrasentan: A pyrrolidine and benzodioxole derivative that acts a RECEPTOR, ENDOTHELIN A antagonist. It has therapeutic potential as an antineoplastic agent and for the treatment of DIABETIC NEPHROPATHIES.		2.4320pyrrolidines
o-desmethylindomethacin
1-(4-chlorobenzoyl)-5-hydroxy-2-methyl-3-indoleacetic acid: has insulin sensitizing and glucose lowering activity; structure in first source		2.0310
singlet oxygen
Singlet Oxygen: An excited state of molecular oxygen generated photochemically or chemically. Singlet oxygen reacts with a variety of biological molecules such as NUCLEIC ACIDS; PROTEINS; and LIPIDS; causing oxidative damages.		2.1510chalcogen;
monoatomic oxygen;
nonmetal atom		macronutrient
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.97402,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
thiazolo(3,2-a)perimidine
thiazolo(3,2-a)perimidine: structure given in first source		2.2110
chlorzolamide
chlorzolamide: structure		4.14150
paromomycin
Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis.		3.5920amino cyclitol glycoside;
aminoglycoside antibiotic		anthelminthic drug;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
anidulafungin
Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis.		3.2310antibiotic antifungal drug;
azamacrocycle;
echinocandin;
heterodetic cyclic peptide;
semisynthetic derivative
avasimibe
[no description available]		2.0510monoterpenoid
boswellic acid
boswellic acid: ursane type; RN given refers to (3alpha,4beta)-isomer; active principle of salai guggal; see also record for salai guggal		2.110triterpenoid
4-(2-aminoethyl)benzenesulfonamide
[no description available]		5.04380
17 alpha-hydroxyprogesterone caproate
17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS.		3.2310corticosteroid hormone
varenicline
Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.		4.3830
biotin
vitamin B7 : Any member of a group of vitamers that belong to the chemical structural class called biotins that exhibit biological activity against vitamin B7 deficiency. Vitamin B7 deficiency is very rare in individuals who take a normal balanced diet. Foods rich in biotin are egg yolk, liver, cereals, vegetables (spinach, mushrooms) and rice. Symptoms associated with vitamin B7 deficiency include thinning hair, scaly skin rashes around eyes, nose and mouth, and brittle nails. The vitamers include biotin and its ionized and salt forms.		7.7830biotins;
vitamin B7		coenzyme;
cofactor;
Escherichia coli metabolite;
fundamental metabolite;
human metabolite;
mouse metabolite;
nutraceutical;
prosthetic group;
Saccharomyces cerevisiae metabolite
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		11.02142amino acid zwitterion;
angiotensin II		human metabolite
fiduxosin
fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source		3.2310
atropine
tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.		4.2650
7-hydroxy-5,11-dioxotetranorprostane-1,16-dioic acid
[no description available]		5.5244prostanoid
ropivacaine
Ropivacaine: An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons.. ropivacaine : The piperidinecarboxamide obtained by the formal condensation of N-propylpipecolic acid and 2,6-dimethylaniline.. (S)-ropivacaine : A piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond.		14.94139piperidinecarboxamide;
ropivacaine		local anaesthetic
sb 203580
[no description available]		3.1450imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
enzastaurin
[no description available]		2.0810indoles;
maleimides
erlotinib
[no description available]		5.280aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
erlotinib hydrochloride
[no description available]		12.462910hydrochloride;
terminal acetylenic compound		antineoplastic agent;
protein kinase inhibitor
piboserod
Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.		2.0810
dexketoprofen trometamol
dexketoprofen trometamol: a water-soluble tromethamine salt of the racemic ketoprofen, rac(+-)-ketoprofen		2.0110
l 163191
[no description available]		2.0810
cacalol
cacalol: a sesquiterpene contained in Cacalia delphiniifolia Sleb et Zucc; structure in first source		2.2510
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		2.0610
melagatran
[no description available]		2.0410azetidines;
carboxamidine;
dicarboxylic acid monoamide;
non-proteinogenic alpha-amino acid;
secondary amino compound		anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
serine protease inhibitor
aflatoxin b1
Aflatoxin B1: A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.. aflatoxin B1 : An aflatoxin having a tetrahydrocyclopenta[c]furo[3',2':4,5]furo[2,3-h]chromene skeleton with oxygen functionality at positions 1, 4 and 11.		2.0510aflatoxin;
aromatic ether;
aromatic ketone		carcinogenic agent;
human metabolite
bd 1047
N-(2-(3,4-Dichlorphenyl)ethyl)-N,N',N'-trimethyl-1,2-ethandiamin: sigma receptor ligand; putative sigma receptor antagonist with antidystonic activity		2.0810primary amine
carbocysteine
Carbocysteine: A compound formed when iodoacetic acid reacts with sulfhydryl groups in proteins. It has been used as an anti-infective nasal spray with mucolytic and expectorant action.. S-carboxymethyl-L-cysteine : An L-cysteine thioether that is L-cysteine in which the hydrogen of the thiol group has been replaced by a carboxymethyl group.		3.4111L-cysteine thioether;
non-proteinogenic L-alpha-amino acid		mucolytic
etravirine
[no description available]		3.5920aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
1-((4,5-bis(4-methoxyphenyl)-2-thiazoyl)carbonyl)-4-methylpiperazine
1-((4,5-bis(4-methoxyphenyl)-2-thiazoyl)carbonyl)-4-methylpiperazine: structure given in first source		2.0410
troleandomycin
Troleandomycin: A macrolide antibiotic that is similar to ERYTHROMYCIN.. troleandomycin : A semi-synthetic macrolide antibiotic obtained by acetylation of the three free hydroxy groups of oleandomycin. Troleandomycin is only found in individuals that have taken the drug.		2.4620acetate ester;
epoxide;
macrolide antibiotic;
monosaccharide derivative;
polyketide;
semisynthetic derivative		EC 1.14.13.97 (taurochenodeoxycholate 6alpha-hydroxylase) inhibitor;
xenobiotic
dronedarone
Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias.		3.23101-benzofurans;
aromatic ether;
aromatic ketone;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
environmental contaminant;
xenobiotic
ramelteon
ramelteon: melatonin MT1/MT2 receptor agonist		3.930indanes
lapatinib
[no description available]		9.9660furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
firocoxib
firocoxib: a COX-2 inhibitor; structure in first source. firocoxib : An enol ether that is the cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2-one. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in horses and dogs.		210butenolide;
cyclopropanes;
enol ether;
sulfone		antineoplastic agent;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
darunavir
Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.		3.2310carbamate ester;
furofuran;
sulfonamide		antiviral drug;
HIV protease inhibitor
cimicoxib
cimicoxib: a COX-2 inhibitor; structure in first source. cimicoxib : An imidazole substituted at positions 1, 4 and 5 by 4-aminosulfonylphenyl, chloro and 3-fluoro-4-methyoxyphenyl groups respectively. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in dogs.		3.8430aromatic ether;
imidazoles;
organochlorine compound;
organofluorine compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
deferasirox
Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions.		3.8730benzoic acids;
monocarboxylic acid;
phenols;
triazoles		iron chelator
bms204352
BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source		2.0810
ilaprazole
ilaprazole: structure in first source		8.9911benzimidazoles;
sulfoxide
tbc-11251
sitaxsentan: endothelin A receptor antagonist; structure in first source		3.8730benzodioxoles
tolvaptan
[no description available]		3.6120benzazepine;
benzenedicarboxamide		aquaretic;
vasopressin receptor antagonist
sorafenib
[no description available]		6.21120(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
lenalidomide
[no description available]		9.140aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
[no description available]		2.0810aminoquinoline
n-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide
N-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide: structure in first source. indisulam : A chloroindole that is 3-chloro-1H-indole substituted by a [(4-sulfamoylphenyl)sulfonyl]nitrilo group at position 7. It is a carbonic anhydrase inhibitor and a potential anti-cancer agent currently in clinical development.		5.1400chloroindole;
organochlorine compound;
sulfonamide		antineoplastic agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
regadenoson
[no description available]		3.2310purine nucleoside
sr 142806
[no description available]		2.0810
lacosamide
Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES.		3.6120N-acyl-amino acid
cholic acid
Cholic Acid: A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.. cholic acid : A bile acid that is 5beta-cholan-24-oic acid bearing three alpha-hydroxy substituents at position 3, 7 and 12.		2.462012alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
sitosterol, (3beta)-isomer
Sobatum: tradename; active fraction of Solanum trilobatum; reduces side-effects of radiation-induced toxicity. sitosterol : A member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3.		2.05103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
C29-steroid;
phytosterols;
stigmastane sterol		anticholesteremic drug;
antioxidant;
mouse metabolite;
plant metabolite;
sterol methyltransferase inhibitor
deoxycholic acid
Deoxycholic Acid: A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.. deoxycholic acid : A bile acid that is 5beta-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 12 respectively.		2.110bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human blood serum metabolite
equilin
Equilin: An estrogenic steroid produced by HORSES. It has a total of four double bonds in the A- and B-ring. High concentration of euilin is found in the URINE of pregnant mares.		2.111017-oxo steroid;
3-hydroxy steroid
fludrocortisone acetate
fludrocortisone acetate : An acetate ester resulting from the formal condensation of the primary hydroxy group of fludrocortisone with acetic acid. A synthetic corticosteroid, it has glucocorticoid actions about 10 times as potent as hydrocortisone, while its mineralocorticoid actions are over 100 times as potent. It is used in partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenal hyperplasia.		2.051011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
fluorinated steroid;
mineralocorticoid;
tertiary alpha-hydroxy ketone
3-nitrotyrosine
3-nitrotyrosine: RN given refers to parent cpd without isomeric designation. 3-nitrotyrosine : A nitrotyrosine comprising tyrosine having a nitro group at the 3-position on the phenyl ring.		2.01102-nitrophenols;
C-nitro compound;
nitrotyrosine;
non-proteinogenic alpha-amino acid
propargylamine
propargylamine: RN given refers to parent cpd; structure		2.110
vincaleukoblastine
[no description available]		3.9330acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
vincristine sulfate
[no description available]		2.4720organic sulfate saltantineoplastic agent;
geroprotector
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		2.9840
benzarone
benzarone: antihemorrhagic agent; structure		3.59201-benzofurans
estramustine
Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.		10.464117beta-hydroxy steroid;
carbamate ester;
organochlorine compound		alkylating agent;
antineoplastic agent;
radiation protective agent
cyclovirobuxine d
cyclovirobuxine D: active priciple of Buxus microphylla var. sinica; has anti-arrhythmic & arrhythmia-inducing actions		2.0310
noscapine
Noscapine: A naturally occurring opium alkaloid that is a centrally acting antitussive agent.. (-)-noscapine : A benzylisoquinoline alkaloid that is 1,2,3,4-tetrahydroisoquinoline which is substituted by a 4,5-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-1-yl group at position 1, a methylenedioxy group at positions 6-7 and a methoxy group at position 8. Obtained from plants of the Papaveraceae family, it lacks significant painkilling properties and is primarily used for its antitussive (cough-suppressing) effects.		2.4520aromatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound		antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite
homoharringtonine
Homoharringtonine: Semisynthetic derivative of harringtonine that acts as a protein synthesis inhibitor and induces APOPTOSIS in tumor cells. It is used in the treatment of MYELOID LEUKEMIA, CHRONIC.. omacetaxine mepesuccinate : A cephalotaxine-derived alkaloid ester obtained from Cephalotaxus harringtonia; used for the treatment of chronic or accelerated phase chronic myeloid leukaemia.		2.0510alkaloid ester;
enol ether;
organic heteropentacyclic compound;
tertiary alcohol		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
protein synthesis inhibitor
acivicin
[no description available]		2.0510isoxazoles;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		antileishmanial agent;
antimetabolite;
antimicrobial agent;
antineoplastic agent;
EC 2.3.2.2 (gamma-glutamyltransferase) inhibitor;
glutamine antagonist;
metabolite
elesclomol
[no description available]		2.0810carbohydrazide;
thiocarbonyl compound		antineoplastic agent;
apoptosis inducer
u-104
SLC-0111: a carbonic anhydrase inhibitor; structure in first source		3.4110
wortmannin
[no description available]		2.9740acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
2-guanidine-4-methylquinazoline
2-guanidine-4-methylquinazoline: structure given in first source		2.1510
trimethoprim, sulfamethoxazole drug combination
Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole.		3.411
o-(chloroacetylcarbamoyl)fumagillol
O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis.. O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative.		2.0510carbamate ester;
organochlorine compound;
semisynthetic derivative;
sesquiterpenoid;
spiro-epoxide		angiogenesis inhibitor;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
methionine aminopeptidase 2 inhibitor;
retinoic acid receptor alpha antagonist
nsc 663284
NSC 663284: structure in first source		2.0810quinolone
taurochenodeoxycholic acid
Taurochenodeoxycholic Acid: A bile salt formed in the liver by conjugation of chenodeoxycholate with taurine, usually as the sodium salt. It acts as detergent to solubilize fats in the small intestine and is itself absorbed. It is used as a cholagogue and choleretic.. taurochenodeoxycholate : An organosulfonate oxoanion that is the conjugate base of taurochenodeoxycholic acid arising from deprotonation of the sulfonate OH group; major species at pH 7.3.. taurochenodeoxycholic acid : A bile acid taurine conjugate of chenodeoxycholic acid.		2.4820bile acid taurine conjugatehuman metabolite;
mouse metabolite
bortezomib
[no description available]		7.16101amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
2-(2-nitro-1h-imidazol-1-yl)-n-(2,2,3,3,3-pentafluoropropyl)acetamide
2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)acetamide: a pentafluorinated derivative of etanidazole		210
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		10.381001,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
bardoxolone methyl
methyl 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate: structure in first source		2.0810cyclohexenones
tryptoquivaline
fumitremorgin C : An organic heteropentacyclic compound that is a mycotoxic indole alkaloid produced by several fungi. A potent and specific inhibitor of the breast cancer resistance protein multidrug transporter.		3.1510aromatic ether;
indole alkaloid;
organic heteropentacyclic compound		breast cancer resistance protein inhibitor;
mycotoxin
nexavar
[no description available]		2.0510organosulfonate salt
dihydropyridines
Dihydropyridines: Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.		2.0310
nsc 23766
[no description available]		2.0810aminopyrimidine;
aminoquinoline;
primary amino compound;
secondary amino compound;
tertiary amino compound		antiviral agent;
apoptosis inducer;
EC 3.6.5.2 (small monomeric GTPase) inhibitor;
muscarinic antagonist
leupeptins
Leupeptins: A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.		3.3160
carboplatin
[no description available]		11.141611
lithium chloride
Lithium Chloride: A salt of lithium that has been used experimentally as an immunomodulator.. lithium chloride : A metal chloride salt with a Li(+) counterion.		2.0810inorganic chloride;
lithium salt		antimanic drug;
geroprotector
glycogen
glycogen : A polydisperse, highly branched glucan composed of chains of D-glucopyranose residues in alpha(1->4) glycosidic linkage, joined together by alpha(1->6) glycosidic linkages. A small number of alpha(1->3) glycosidic linkages and some cumulative alpha(1->6) links also may occur. The branches in glycogen typically contain 8 to 12 glucose residues.		2.520
n-acetylneuraminic acid
N-Acetylneuraminic Acid: An N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria. (From Dorland, 28th ed, p1518). N-acetylneuraminic acid : An N-acylneuraminic acid where the N-acyl group is specified as acetyl.		2.0610N-acetylneuraminic acidsantioxidant;
bacterial metabolite;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
human metabolite;
mouse metabolite
bradykinin
[no description available]		3.1450oligopeptidehuman blood serum metabolite;
vasodilator agent
glucosamine
D-glucosamine : An amino sugar whose structure comprises D-glucose having an amino substituent at position 2.. 2-amino-2-deoxy-D-glucopyranose : A D-glucosamine whose structure comprises D-glucopyranose having an amino substituent at position 2.		13.143610D-glucosamineEscherichia coli metabolite;
geroprotector;
mouse metabolite
elastin
[no description available]		7.0310oligopeptide
mevalonic acid
Mevalonic Acid: A dihydroxy monocarboxylic acid and precursor in the biosynthetic pathway known as the mevalonate pathway, which produces terpenes and steroids that are vital for diverse cellular functions.. mevalonic acid : A racemate composed of equimolar amounts of (R)- and (S)-mevalonic acid.. (R)-mevalonic acid : The (R)-enantiomer of mevalonic acid.		2.05103,5-dihydroxy-3-methylpentanoic acid
naringenin
(S)-naringenin : The (S)-enantiomer of naringenin.		2.4620(2S)-flavan-4-one;
naringenin		expectorant;
plant metabolite
epiglucan
epiglucan: a highly side-chain/branched alkali-insoluble cell wall glucan from fungus such as Epicoccum nigrum, Botrytis cinerea, ascomycetes & basidiomycetes; also isolated S-4001 from Lei Wan (polyporus mylitiae), HA-beta-glucan from mushroom Pleutotus ostreatus (Fr.) Quel., and translam from seaweed Laminaria cichorioides; with commercially important functional properties including emulsification and friction reduction.		2.4110
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		3.2310heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
ouabain
Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.		3.572011alpha-hydroxy steroid;
14beta-hydroxy steroid;
5beta-hydroxy steroid;
alpha-L-rhamnoside;
cardenolide glycoside;
steroid hormone		anti-arrhythmia drug;
cardiotonic drug;
EC 2.3.3.1 [citrate (Si)-synthase] inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
ion transport inhibitor;
plant metabolite
puromycin
[no description available]		2.0510puromycinsantiinfective agent;
antimicrobial agent;
antineoplastic agent;
EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor;
EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor;
nucleoside antibiotic;
protein synthesis inhibitor
taxifolin
(+)-taxifolin : A taxifolin that has (2R,3R)-configuration.		2.0410taxifolinmetabolite
tosylphenylalanyl chloromethyl ketone
Tosylphenylalanyl Chloromethyl Ketone: An inhibitor of Serine Endopeptidases. Acts as alkylating agent and is known to interfere with the translation process.. N-tosyl-L-phenylalanyl chloromethyl ketone : The N-tosyl derivative of L-phenylalanyl chloromethyl ketone.		2.0610alpha-chloroketone;
sulfonamide		alkylating agent;
serine proteinase inhibitor
pentostatin
Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.		3.8730coformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
taurolithocholic acid
Taurolithocholic Acid: A bile salt formed in the liver from lithocholic acid conjugation with taurine, usually as the sodium salt. It solubilizes fats for absorption and is itself absorbed. It is a cholagogue and choleretic.. taurolithocholic acid : The bile acid taurine conjugate of lithocholic acid.		2.7530bile acid taurine conjugate;
monocarboxylic acid amide		human metabolite
nitroarginine
Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.		2.7430guanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
inositol 3-phosphate
inositol 3-phosphate: RN given refers to (myo)-isomer		2.0210
(+)-limonene
(4R)-limonene : An optically active form of limonene having (4R)-configuration.		2.0510limoneneplant metabolite
arbutin
hydroquinone O-beta-D-glucopyranoside : A monosaccharide derivative that is hydroquinone attached to a beta-D-glucopyranosyl residue at position 4 via a glycosidic linkage.		3.3110beta-D-glucoside;
monosaccharide derivative		Escherichia coli metabolite;
plant metabolite
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		5.55120cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		3.8730alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
griseofulvin
Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment.		4.58701-benzofurans;
antibiotic antifungal drug;
benzofuran antifungal drug;
organochlorine compound;
oxaspiro compound		antibacterial agent;
Penicillium metabolite
cefoxitin
Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase.		3.5920beta-lactam antibiotic allergen;
cephalosporin;
cephamycin;
semisynthetic derivative		antibacterial drug
digitoxin
Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain.		2.4720cardenolide glycosideEC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor
moxalactam disodium
[no description available]		2.0510
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		4.9360L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
pancuronium
Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant.		3.5820acetate ester;
steroid ester		cholinergic antagonist;
muscle relaxant;
nicotinic antagonist
hyperforin
hyperforin: a prenylated acylphloroglucinol derivative; antibiotic component of novoimanine; psychoactive agent in St. John's wort; Russian; structure;. hyperforin : A cyclic terpene ketone that is a prenylated carbobicyclic acylphloroglucinol derivative produced by St. John's Wort, Hypericum perforatum.		2.0810
abacavir
abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection.		3.59202,6-diaminopurinesantiviral drug;
drug allergen;
HIV-1 reverse transcriptase inhibitor
netilmicin
Netilmicin: Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity.		2.0510
trimethaphan camsylate
trimethaphan camsylate : The (S)-camphorsulfonate salt of trimethaphan.		2.0510
perindopril erbumine
[no description available]		2.0810addition compoundantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
miglitol
[no description available]		3.6120piperidines
amiodarone hydrochloride
[no description available]		2.0510aromatic ketone
mometasone furoate
Mometasone Furoate: A pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.		2.051011beta-hydroxy steroid;
2-furoate ester;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
organochlorine compound;
steroid ester		anti-allergic agent;
anti-inflammatory drug
metyrosine
alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma.		3.2310L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		antihypertensive agent;
EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor
rocuronium bromide
rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent
nortriptyline hydrochloride
[no description available]		2.0510organic tricyclic compoundgeroprotector
erythromycin estolate
Erythromycin Estolate: A macrolide antibiotic, produced by Streptomyces erythreus. It is the lauryl sulfate salt of the propionic ester of erythromycin. This erythromycin salt acts primarily as a bacteriostatic agent. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.		2.4620aminoglycoside sulfate salt;
erythromycin derivative		enzyme inhibitor
kanamycin sulfate
[no description available]		2.0510aminoglycoside sulfate saltantibacterial drug;
geroprotector
paromomycin sulfate
paromomycin sulfate : An aminoglycoside sulfate salt resulting from the treatment of paromomycin with sulfuric acid. A broad-spectrum antibiotic, it is used for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis.		2.0510
delavirdine mesylate
delavirdine mesylate : The monomethanesulfonic acid salt of delavirdine, a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		2.0510methanesulfonate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor
linezolid
[no description available]		3.6120acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
ryanodine
Ryanodine: A methylpyrrole-carboxylate from RYANIA that disrupts the RYANODINE RECEPTOR CALCIUM RELEASE CHANNEL to modify CALCIUM release from SARCOPLASMIC RETICULUM resulting in alteration of MUSCLE CONTRACTION. It was previously used in INSECTICIDES. It is used experimentally in conjunction with THAPSIGARGIN and other inhibitors of CALCIUM ATPASE uptake of calcium into SARCOPLASMIC RETICULUM.. ryanodine : An insecticide alkaloid isolated from South American plant Ryania speciosa.		2.0110
naringin
[no description available]		8.930(2S)-flavan-4-one;
4'-hydroxyflavanones;
dihydroxyflavanone;
disaccharide derivative;
neohesperidoside		anti-inflammatory agent;
antineoplastic agent;
metabolite
gingerol
gingerol: an active ingredient in GINGER along with SHOGAOL. a nonvolatile methoxy phenyl decanone. gingerol : A beta-hydroxy ketone that is 5-hydroxydecan-3-one substituted by a 4-hydroxy-3-methoxyphenyl moiety at position 1; believed to inhibit adipogenesis. It is a constituent of fresh ginger.		2.3110beta-hydroxy ketone;
guaiacols		antineoplastic agent;
plant metabolite
cyclopamine
[no description available]		2.0510piperidinesglioma-associated oncogene inhibitor
lignans
Lignans: A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)		3.0730
acetylleucyl-leucyl-norleucinal
acetylleucyl-leucyl-norleucinal: a proteasome inhibitor. acetylleucyl-leucyl-norleucinal : A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence.		2.0310aldehyde;
tripeptide		cysteine protease inhibitor
bq 123
cyclo(Trp-Asp-Pro-Val-Leu): derived from the modification of a natural lead of BE-18257B, an endothelin A receptor antagonist; has neuroprotective activity; amino acid sequence given in first source		2.0310cyclic peptide
e 3040
E 3040: a dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase; structure given in first source		3.1210benzothiazoles;
organic hydroxy compound;
pyridines;
secondary amino compound		anti-inflammatory drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
uricosuric drug
sc 57666
[no description available]		3.5620stilbenoid
devazepide
Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.. devazepide : An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.		2.05101,4-benzodiazepinone;
indolecarboxamide		antineoplastic agent;
apoptosis inducer;
cholecystokinin antagonist;
gastrointestinal drug
chloramphenicol palmitate
chloramphenicol palmitate: RN given refers to ((R-(R*,R*))-isomer)		2.0510hexadecanoate ester
clindamycin phosphate
[no description available]		3.2310
calcium pantothenate
[no description available]		2.0510polymer
pemirolast potassium salt
[no description available]		2.0810
eplerenone
Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.		3.61203-oxo-Delta(4) steroid;
epoxy steroid;
gamma-lactone;
methyl ester;
organic heteropentacyclic compound;
oxaspiro compound;
steroid acid ester		aldosterone antagonist;
antihypertensive agent
tolterodine
[no description available]		3.8730tertiary amineantispasmodic drug;
muscarinic antagonist;
muscle relaxant
doxorubicin hydrochloride
[no description available]		3.8730anthracycline
erythromycin ethylsuccinate
Erythromycin Ethylsuccinate: A macrolide antibiotic, produced by Streptomyces erythreus. This compound is an ester of erythromycin base and succinic acid. It acts primarily as a bacteriostatic agent. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin ethylsuccinate : A erythromycin derivative that is erythromycin A in which the hydroxy group at position 3R is substituted by a (4-ethoxy-4-oxobutanoyl)oxy group. It is used for the treatment of a wide variety of bacterial infections.		2.0510cyclic ketone;
erythromycin derivative;
ethyl ester;
succinate ester
tibolone
tibolone: used in prevention of postmenopausal osteoporosis. tibolone : Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormone receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.		2.081017beta-hydroxy steroid;
terminal acetylenic compound		bone density conservation agent;
hormone agonist
ao 128
AO 128: alpha-glucosidase inhibitor; structure given in first source		2.4720organic molecular entity
loteprednol etabonate
Loteprednol Etabonate: An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
etabonate ester;
organochlorine compound;
steroid acid ester;
steroid ester		anti-inflammatory drug
darifenacin
darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.		3.61201-benzofurans;
monocarboxylic acid amide;
pyrrolidines		antispasmodic drug;
muscarinic antagonist
fluticasone propionate
fluticasone propionate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
propanoate ester;
steroid ester;
thioester		adrenergic agent;
anti-allergic agent;
anti-asthmatic drug;
anti-inflammatory drug;
bronchodilator agent;
dermatologic drug
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		4.07140cyclodextrin
acarbose
[no description available]		2.7530amino cyclitol;
glycoside
maleic acid
maleic acid: RN given refers to parent cpd(Z)-isomer which is maleic acid; all RR's given refer to (Z)-isomer; (E)-isomer is fumaric acid. maleic acid : A butenedioic acid in which the double bond has cis- (Z)-configuration.		2.0510butenedioic acidalgal metabolite;
mouse metabolite;
plant metabolite
trichostatin a
trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES		2.7530antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		6.55141retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
arachidonic acid
icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.		10.49376icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
farnesol
Farnesol: A colorless liquid extracted from oils of plants such as citronella, neroli, cyclamen, and tuberose. It is an intermediate step in the biological synthesis of cholesterol from mevalonic acid in vertebrates. It has a delicate odor and is used in perfumery. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed). (2-trans,6-trans)-farnesol : The (2-trans,6-trans)-stereoisomer of farnesol.. farnesol : A farnesane sesquiterpenoid that is dodeca-2,6,10-triene substituted by methyl groups at positions 3, 7 and 11 and a hydroxy group at position 1.		2.5320farnesolplant metabolite
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		5.78150resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
retinol
Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).		6.1551retinol;
vitamin A		human metabolite;
mouse metabolite;
plant metabolite
cyanoginosin lr
cyanoginosin LR: cyclic heptapeptide from cyanobacterium Microcystis aeruginosa. microcystin-LR : A microcystin consisting of D-alanyl, L-leucyl, (3S)-3-methyl-D-beta-aspartyl,L-arginyl, 2S,3S,4E,6E,8S,9S)-3-amino-4,5,6,7-tetradehydro-9-methoxy-2,6,8-trimethyl-10-phenyldecanoyl, D-gamma-glutamyl, and 2,3-didehydro-N-methylalanyl residues joined into a 25-membered macrocycle. Produced by the cyanobacterium Microcystis aeruginosa, it is the most studied of the microcystins.		2.0510microcystinbacterial metabolite;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
environmental contaminant;
xenobiotic
alpha-D-fructofuranose 1,6-bisphosphate
alpha-D-fructofuranose 1,6-bisphosphate : A D-fructofuranose 1,6-bisphosphate with an alpha-configuration at the anomeric position.		2.0510D-fructofuranose 1,6-bisphosphate
docosahexaenoate
efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement. docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.. docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.. all-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19.		2.0510docosahexaenoic acid;
omega-3 fatty acid		algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical
oleic acid
Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry.		3.0340octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		4.5940macrolide lactambacterial metabolite;
immunosuppressive agent
ferulic acid
ferulate : A monocarboxylic acid anion obtained by the deprotonation of the carboxy group of ferulic acid.		2.1310ferulic acidsanti-inflammatory agent;
antioxidant;
apoptosis inhibitor;
cardioprotective agent;
MALDI matrix material;
plant metabolite
cerivastatin
cerivastatin: cerivastatin is the ((E)-(+))-isomer; structure given in first source. cerivastatin : (3R,5S)-3,5-dihydroxyhept-6-enoic acid in which the (7E)-hydrogen is substituted by a 4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl group. Formerly used (as its sodium salt) to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.		4.5370dihydroxy monocarboxylic acid;
pyridines;
statin (synthetic)
rosuvastatin
rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer).		4.0840dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrimidines;
statin (synthetic);
sulfonamide		anti-inflammatory agent;
antilipemic drug;
cardioprotective agent;
CETP inhibitor;
environmental contaminant;
xenobiotic
cocaine
Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.		2.0510benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
eicosapentaenoic acid
icosapentaenoic acid : Any straight-chain, C20 polyunsaturated fatty acid having five C=C double bonds.. all-cis-5,8,11,14,17-icosapentaenoic acid : An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17.		5.2662icosapentaenoic acid;
omega-3 fatty acid		anticholesteremic drug;
antidepressant;
antineoplastic agent;
Daphnia galeata metabolite;
fungal metabolite;
micronutrient;
mouse metabolite;
nutraceutical
thapsigargin
Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.		2.4720butyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone		calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
mycophenolic acid
Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.		3.59202-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols		anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
mupirocin
Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.		2.4420alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor
clindamycin
Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.		4.0940
fosfomycin
Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus.		3.8730epoxide;
phosphonic acids		antimicrobial agent;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		4.2750macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
geranylgeranyl pyrophosphate
geranylgeranyl pyrophosphate: RN given refers to (E,E,E)-isomer. geranylgeranyl diphosphate : A polyprenol diphosphate having geranylgeranyl as the polyprenyl component.. 2-trans,6-trans,10-trans-geranylgeranyl diphosphate : The all-trans-isomer of geranylgeranyl diphosphate.		2.0510geranylgeranyl diphosphatemouse metabolite
drf 2725
ragaglitazar: a phenoxazine analogue of phenyl propanoic acid; Ragaglitazar is a coligand of PPARalpha and PPARgamma		2.4620
gw 3965
GW 3965: a liver X receptor ligand		2.0810diarylmethane
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		2.7330aromatic amide
prostaglandin d2
Prostaglandin D2: The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.. prostaglandin D2 : A member of the class of prostaglandins D that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9 and 15 and an oxo group at position 11 (the 5Z,9alpha,13E,15S- stereoisomer).		3.74100prostaglandins Dhuman metabolite;
mouse metabolite
diethylstilbestrol
Diethylstilbestrol: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed). diethylstilbestrol : An olefinic compound that is trans-hex-3-ene in which the hydrogens at positions 3 and 4 have been replaced by p-hydroxyphenyl groups.		4.0940olefinic compound;
polyphenol		antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen
octreotide
[no description available]		3.2310
epothilone a
Epothilones: A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).		2.0310epothilone;
epoxide		antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator
eptifibatide
[no description available]		3.2310homodetic cyclic peptide;
macrocycle;
organic disulfide		anticoagulant;
platelet aggregation inhibitor
6-bromoindirubin-3'-oxime
6-bromoindirubin-3'-oxime: structure in first source. 6-bromoindirubin-3'-oxime : A member of the class of biindoles that is indirubin substituted at position 6 by a bromo group and in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime.		2.0810
purvalanol b
purvalanol B: protein kinase inhibitor; structure in first source		2.0810purvalanolprotein kinase inhibitor
y-700
[no description available]		2.0810
repsox
RepSox: inhibits TGF-beta signaling; structure in first source appears to be incorrect		2.0810pyrazolopyridine
alitretinoin
Alitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.		2.7230retinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		2.7530N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
decitabine
[no description available]		3.87302'-deoxyribonucleoside
teniposide
[no description available]		4.0940aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
kt 5720
KT 5720: indolocarbazole; synthetic derivative of K 252a. KT 5720 : An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of hexyl (3S)-3-hydroxy-2-methyltetrahydrofuran-3-carboxylate (the 2R,3S,5S product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1,5-dihydro-2H-pyrrol-2-one.		2.0210carboxylic ester;
gamma-lactam;
hemiaminal;
indolocarbazole;
organic heterooctacyclic compound;
semisynthetic derivative;
tertiary alcohol		EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor
valrubicin
[no description available]		2.4720anthracycline;
trifluoroacetamide
ketoconazole
(2R,4S)-ketoconazole : A cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine which dioxolane moiety has (2R,4S)-configuration.		4.1920cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine
purvalanol a
6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;		2.0510purvalanol
cefamandole
Cefamandole: Semisynthetic wide-spectrum cephalosporin with prolonged action, probably due to beta-lactamase resistance. It is used also as the nafate.. cefamandole : A cephalosporin compound having (R)-mandelamido and N-methylthiotetrazole side-groups.		2.4620cephalosporin;
semisynthetic derivative		antibacterial drug
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		4.2350actinomycinmutagen
tiazofurin
tiazofurin: RN given refers to (beta-D)-isomer; structure given in first source. tiazofurine : A C-glycosyl compound that is 1,3-thiazole-4-carboxamide in which the hydrogen at position 2 has been replaced by a beta-D-ribofuranosyl group. It is metabolised to thiazole-4-carboxamide adenine dinucleotide (TAD), a selective inhibitor of inosine monophosphate dehydrogenase (IMP dehydrogenase).		2.05101,3-thiazoles;
C-glycosyl compound;
monocarboxylic acid amide		antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
prodrug
azaserine
Azaserine: Antibiotic substance produced by various Streptomyces species. It is an inhibitor of enzymatic activities that involve glutamine and is used as an antineoplastic and immunosuppressive agent.. azaserine : A carboxylic ester resulting from the formal condensation of the carboxy group of diazoacetic acid with the alcoholic hydroxy group of L-serine. An antibiotic produced by a Streptomyces species.		2.0510carboxylic ester;
diazo compound;
L-serine derivative;
non-proteinogenic L-alpha-amino acid		antifungal agent;
antimetabolite;
antimicrobial agent;
antineoplastic agent;
glutamine antagonist;
immunosuppressive agent;
metabolite
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		4.0940L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
benzyloxycarbonylleucyl-leucyl-leucine aldehyde
benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.		3.4470amino aldehyde;
carbamate ester;
tripeptide		proteasome inhibitor
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		4.640nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
posaconazole
[no description available]		3.6120aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
l 743,872
[no description available]		2.1310
rubitecan
rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.		2.4720C-nitro compound;
delta-lactone;
pyranoindolizinoquinoline;
semisynthetic derivative;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
micafungin
Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy.		3.5920antibiotic antifungal drug;
echinocandin		antiinfective agent
4,4-difluoro-N-[(1S)-3-[3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]-1-cyclohexanecarboxamide
[no description available]		2.0810tropane alkaloid
riboflavin
vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms).		3.5920flavin;
vitamin B2		anti-inflammatory agent;
antioxidant;
cofactor;
Escherichia coli metabolite;
food colouring;
fundamental metabolite;
human urinary metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite
sodium bicarbonate
Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.		3.8630one-carbon compound;
organic sodium salt		antacid;
food anticaking agent
sodium acetate, anhydrous
Sodium Acetate: The trihydrate sodium salt of acetic acid, which is used as a source of sodium ions in solutions for dialysis and as a systemic and urinary alkalizer, diuretic, and expectorant.		2.0510organic sodium saltNMR chemical shift reference compound
sodium benzoate
Sodium Benzoate: The sodium salt of BENZOIC ACID. It is used as an antifungal preservative in pharmaceutical preparations and foods. It may also be used as a test for liver function.. sodium benzoate : An organic sodium salt resulting from the replacement of the proton from the carboxy group of benzoic acid by a sodium ion.		2.0510organic sodium saltalgal metabolite;
antimicrobial food preservative;
drug allergen;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
human xenobiotic metabolite;
plant metabolite
arsenic trioxide
Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius.		3.5920arsenic oxideantineoplastic agent;
insecticide
dipyrone
Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.. metamizole sodium : An organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic.		4.9381organic sodium saltanti-inflammatory agent;
antipyretic;
antirheumatic drug;
cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug;
prodrug
ditiocarb sodium
[no description available]		2.0510organic molecular entity
bromochloroacetic acid
Keratins: A class of fibrous proteins or scleroproteins that represents the principal constituent of EPIDERMIS; HAIR; NAILS; horny tissues, and the organic matrix of tooth ENAMEL. Two major conformational groups have been characterized, alpha-keratin, whose peptide backbone forms a coiled-coil alpha helical structure consisting of TYPE I KERATIN and a TYPE II KERATIN, and beta-keratin, whose backbone forms a zigzag or pleated sheet structure. alpha-Keratins have been classified into at least 20 subtypes. In addition multiple isoforms of subtypes have been found which may be due to GENE DUPLICATION.. bromochloroacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by bromine while a second is replaced by chlorine. A low-melting (27.5-31.5degreeC), hygroscopic crystalline solid, it can be formed during the disinfection (by chlorination) of water that contains bromide ions and organic matter, so can occur in drinking water as a byproduct of the disinfection process.		2.02102-bromocarboxylic acid;
monocarboxylic acid;
organochlorine compound
idarubicin hydrochloride
[no description available]		2.0510anthracycline
sr 90107
fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux.		3.2310
carbenoxolone sodium
Carbenoxolone: An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.		2.0510triterpenoid
carbenoxolone
[no description available]		2.0510
meglumine iodipamide
[no description available]		3.2310organoammonium saltradioopaque medium
cinnamaldehyde
3-phenylprop-2-enal : A member of the class of cinnamaldehydes that is prop-2-enal in which a hydrogen at position 3 has been replaced by a phenyl group. The configuration of the double bond is not specified; the name "cinnamaldehyde" is widely used to refer to the E (trans) isomer.. (E)-cinnamaldehyde : The E (trans) stereoisomer of cinnamaldehyde, the parent of the class of cinnamaldehydes.		3.99113-phenylprop-2-enal;
cinnamaldehydes		antifungal agent;
EC 4.3.1.24 (phenylalanine ammonia-lyase) inhibitor;
flavouring agent;
hypoglycemic agent;
plant metabolite;
sensitiser;
vasodilator agent
trans-4-coumaric acid
hydroxycinnamic acid : Any member of the class of cinnamic acids carrying one or more hydroxy substituents.. trans-4-coumaric acid : The trans-isomer of 4-coumaric acid.. 4-coumaric acid : A coumaric acid in which the hydroxy substituent is located at C-4 of the phenyl ring.		2.15104-coumaric acidfood component;
mouse metabolite;
plant metabolite
chalcone
trans-chalcone : The trans-isomer of chalcone.		2.1510chalconeEC 3.2.1.1 (alpha-amylase) inhibitor
isomethyleugenol
Methylation: Addition of methyl groups. In histo-chemistry methylation is used to esterify carboxyl groups and remove sulfate groups by treating tissue sections with hot methanol in the presence of hydrochloric acid. (From Stedman, 25th ed)		340isomethyleugenol
piperine
piperine : A N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum.		7.6920benzodioxoles;
N-acylpiperidine;
piperidine alkaloid;
tertiary carboxamide		food component;
human blood serum metabolite;
NF-kappaB inhibitor;
plant metabolite
squalene
Addavax: an oil-water nanoemulsion and adjuvant containing squalene, Tween 80, and sorbitane trioleate		2.4920triterpenehuman metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		4.4460stilbene
isoliquiritigenin
[no description available]		3.3110chalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
thyrotropin-releasing hormone
PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence.		3.2310peptide hormone;
tripeptide		human metabolite
(R)-(+)-sulpiride
(R)-(+)-sulpiride : An optically active form of sulpiride having (R)-configuration. The active enantiomer of the racemic drug sulpiride.		2.0210sulpiride
discodermolide
[no description available]		2.0510diterpenoid
cannabidiol
Cannabidiol: Compound isolated from Cannabis sativa extract.. cannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4.		2.5220olefinic compound;
phytocannabinoid;
resorcinols		antimicrobial agent;
plant metabolite
buprenorphine
Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.		9.5422morphinane alkaloiddelta-opioid receptor antagonist;
kappa-opioid receptor antagonist;
mu-opioid receptor agonist;
opioid analgesic
arginine vasopressin
Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.		3.8930vasopressincardiovascular drug;
hematologic agent;
mitogen
gw9662
2-chloro-5-nitrobenzanilide: pretreatment of peroxisome proliferator activated receptors with GW9662 results in the irreversible loss of ligand binding		2.0810benzamides
s 1033
[no description available]		3.930(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
calmidazolium
calmidazolium chloride : The organic choride salt of calmidazolium.		3.3510organic chloride saltapoptosis inducer;
calmodulin antagonist
trilostane
trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions.		2.081017beta-hydroxy steroid;
3-hydroxy steroid;
androstanoid;
epoxy steroid;
nitrile		abortifacient;
antineoplastic agent;
EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor
tropisetron
Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.		3.1210indolyl carboxylic acid
xe 991, anthracenone
10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone: neurotransmitter release enhancer and potassium channel blocker; structure given in first source		2.4820anthracenes
leuprolide acetate
leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0810acetate saltantineoplastic agent;
gonadotropin releasing hormone agonist
fludarabine
[no description available]		2.0510purine nucleoside
propylthiouracil
Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.		3.8730pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
prothionamide
Prothionamide: Antitubercular agent similar in action and side effects to ETHIONAMIDE. It is used mostly in combination with other agents.		2.0510pyridines
sesquiterpenes
[no description available]		2.9640
chlorprothixene
Chlorprothixene: A thioxanthine with effects similar to the phenothiazine antipsychotics.. (Z)-chlorprothixene : A chlorprothixene in which the double bond adopts a (Z)-configuration.		2.7430chlorprothixene
etomidate
Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.		3.5920ethyl ester;
imidazoles		intravenous anaesthetic;
sedative
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		4.4260aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
sb 366791
N-(3-methoxyphenyl)-4-chlorocinnamanilide: a TRPV1 antagonist; structure in first source		2.0410
levosulpiride
(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).		2.5220sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
3,6-dihydroxyflavone
3,6-dihydroxyflavone: induces apoptosis in leukemia HL-60 cells; structure in first source		3.3510
caffeic acid
trans-caffeic acid : The trans-isomer of caffeic acid.		4.09140caffeic acidgeroprotector;
mouse metabolite
rg108
RG108: DNA methyltransferase inhibitor; structure in first source		2.0810indolyl carboxylic acid
pyrantel
Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'.		3.23101,4,5,6-tetrahydropyrimidines;
carboxamidine;
thiophenes		antinematodal drug
stf 083010
[no description available]		2.0810
1-(4-chlorophenyl)-3-(4-sulfamoylphenyl)urea
[no description available]		2.0810sulfonamide
2-phenylamino-4-methyl-5-acetylthiazole
2-phenylamino-4-methyl-5-acetylthiazole: structure in first source		2.0710
N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide
[no description available]		2.0810naphthalenecarboxamide
isoeugenol
trans-isoeugenol : The trans-stereoisomer of isoeugenol.		2.1310isoeugenolplant metabolite
flunarizine
Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.		2.2110diarylmethane
thiothixene
[no description available]		3.5920N-methylpiperazineanticoronaviral agent
eszopiclone
Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use.		3.6120zopiclonecentral nervous system depressant;
sedative
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		7.24300aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
cct018159
CCT018159: structure in first source. CCT-018159 : A member of the class of pyrazoles that is 1H-pyrazole carrying 1,4-benzodioxane-6-yl and 5-ethyl-2,4-dihydroxyphenyl substituents at positions 4 and 5 respectively.		2.0810benzodioxine;
pyrazoles;
resorcinols		antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor
secinh3
SecinH3: a small molecule antagonist of cytohesins; structure in first source		2.0810triazoles
jk184
JK184: structure in first source		2.0810
benztropine
Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		3.2310diarylmethane
nootkatone
nootkatone: RN given refers to cpd without isomeric designation; structure given in first source. (+)-nootkatone : A sesquiterpenoid that is 4,4a,5,6,7,8-hexahydronaphthalen-2(3H)-one which is substituted by methyl groups at positions 4 and 4a, and by an isopropenyl group at position 6 (the 4R,4aS,6R stereoisomer).		2.0710carbobicyclic compound;
enone;
sesquiterpenoid		fragrance;
insect repellent;
plant metabolite
methimazole
Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen.		4.26501,3-dihydroimidazole-2-thionesantithyroid drug
urb 597
cyclohexyl carbamic acid 3'-carbamoylbiphenyl-3-yl ester: a fatty acid amide hydrolase inhibitor; structure in first source		2.2510biphenyls
cinnarizine
Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.		2.9840diarylmethane;
N-alkylpiperazine;
olefinic compound		anti-allergic agent;
antiemetic;
calcium channel blocker;
geroprotector;
H1-receptor antagonist;
histamine antagonist;
muscarinic antagonist
sulindac
[no description available]		2.0710
sulindac
Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.		7.98430monocarboxylic acid;
organofluorine compound;
sulfoxide		analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		4.8871capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
terbinafine
[no description available]		3.5920acetylenic compound;
allylamine antifungal drug;
enyne;
naphthalenes;
tertiary amine		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor;
sterol biosynthesis inhibitor
epalrestat
epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.		2.0810monocarboxylic acid;
thiazolidines		EC 1.1.1.21 (aldehyde reductase) inhibitor
n-(fluorenyl-9-methoxycarbonyl)leucine
N-(fluorenyl-9-methoxycarbonyl)leucine: a leumedin; RN given for (L)-isomer		2.0210
drotaverin
drotaverin: Hungarian drug; RN given refers to parent cpd; structure		2.0810isoquinolines
thioguanine anhydrous
Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.		4.56702-aminopurinesanticoronaviral agent;
antimetabolite;
antineoplastic agent
(1R,2S)-tranylcypromine hydrochloride
(1R,2S)-tranylcypromine hydrochloride : A hydrochloride obtained by combining (1R,2S)-tranylcypromine with one equivalent of hydrochloric acid.		2.0510hydrochloride
tacrine hydrochloride
[no description available]		2.5120
thiourea
Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.. thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur.		3.2710one-carbon compound;
thioureas;
ureas		antioxidant;
chromophore
sodium propionate
sodium propionate: was term of propionic acid (1986-2006). sodium propionate : An organic sodium salt comprising equal numbers of sodium and propionate ions.		2.0510organic sodium saltantifungal drug;
food preservative
D-fructopyranose
[no description available]		6.1960cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
thioacetamide
Thioacetamide: A crystalline compound used as a laboratory reagent in place of HYDROGEN SULFIDE. It is a potent hepatocarcinogen.. thioacetamide : A thiocarboxamide consiting of acetamide having the oxygen replaced by sulfur.		8.3760thiocarboxamidehepatotoxic agent
succimer
Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning.		3.2310dicarboxylic acid;
dithiol;
sulfur-containing carboxylic acid		chelator
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		10.2990cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
streptozocin
[no description available]		4.0840
capsazepine
capsazepine: modified capsaicin molecule; a capsaicin receptor antagonist. capsazepine : A benzazepine that is 2,3,4,5-tetrahydro-1H-2-benzazepine which is substituted by hydroxy groups at positions 7 and 8 and on the nitrogen atom by a 2-(p-chlorophenyl)ethylaminothiocarbonyl group. A synthetic analogue of capsaicin, it was the first reported capsaicin receptor antagonist.		2.2510benzazepine;
catechols;
monochlorobenzenes;
thioureas		capsaicin receptor antagonist
tamoxifen citrate
[no description available]		2.0810citrate saltangiogenesis inhibitor;
anticoronaviral agent
tamoxifen
[no description available]		7.01310stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
sodium taurodeoxycholate
Taurodeoxycholic Acid: A bile salt formed in the liver by conjugation of deoxycholate with taurine, usually as the sodium salt. It is used as a cholagogue and choleretic, also industrially as a fat emulsifier.. taurodeoxycholic acid : A bile acid taurine conjugate of deoxycholic acid.. taurodeoxycholate : An organosulfonate oxoanion that is the conjugate base of taurodeoxycholic acid.		2.0710bile acid taurine conjugatehuman metabolite
nadp
[no description available]		210
hc-067047
HC-067047: a TRPA1 antagonist; structure in first source		2.0810
bi-78d3
[no description available]		2.0810aryl sulfide
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		3.5920pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
gsk 3787
[no description available]		2.0810
kartogenin
kartogenin: promotes chondrocyte differentiation; structure in first source		2.1710
cancidas
[no description available]		3.2310
methyl-thiohydantoin-tryptophan
methyl-thiohydantoin-tryptophan: structure in first source		2.0810organonitrogen compound;
organooxygen compound
2-[2-chloro-6-ethoxy-4-[(3-methyl-5-oxo-1-phenyl-4-pyrazolylidene)methyl]phenoxy]acetic acid methyl ester
[no description available]		2.0810monocarboxylic acid
4-(5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1h-pyrazol-1-yl)benzenesulfonamide
[no description available]		2.0810sulfonamide
fusidic acid
Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.		2.753011alpha-hydroxy steroid;
3alpha-hydroxy steroid;
alpha,beta-unsaturated monocarboxylic acid;
steroid acid;
steroid antibiotic;
sterol ester		EC 2.7.1.33 (pantothenate kinase) inhibitor;
Escherichia coli metabolite;
protein synthesis inhibitor
lincomycin
Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis.		3.2310carbohydrate-containing antibiotic;
L-proline derivative;
monocarboxylic acid amide;
pyrrolidinecarboxamide;
S-glycosyl compound		antimicrobial agent;
bacterial metabolite
valinomycin
Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains.		2.0810cyclodepsipeptide;
macrocycle		antimicrobial agent;
antiviral agent;
bacterial metabolite;
potassium ionophore
estrone sulfate
estrone sulfate: sulfoconjugated estrone; RN given refers to parent cpd		4.255017-oxo steroid;
steroid sulfate		human metabolite;
mouse metabolite
ranitidine
Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease.		3.6620C-nitro compound;
furans;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
drug allergen;
environmental contaminant;
H2-receptor antagonist;
xenobiotic
aplaviroc
aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source		3.2310
hmr 3647
[no description available]		4.0940
latoconazole
latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source		2.0810conazole antifungal drug;
imidazole antifungal drug
maraviroc
[no description available]		3.6120tropane alkaloid
LSM-1318
[no description available]		2.0810oxa-steroid
toremifene citrate
[no description available]		2.0810stilbenoidanticoronaviral agent
toremifene
Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.		3.8530aromatic ether;
organochlorine compound;
tertiary amine		antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.9640aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
rwj 67657
RWJ 67657: inhibits p38 mitogen-activated protein kinase; structure in first source		2.0810
telaprevir
[no description available]		2.4620cyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines		antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
nelarabine
nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G).		3.6120beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside		antineoplastic agent;
DNA synthesis inhibitor;
prodrug
glycylproline
Gly-Pro : A dipeptide consisting of L-proline having a glycyl residue attached to its alpha-amino group.		3.5720dipeptide zwitterion;
dipeptide		metabolite
6-methyl-2-(phenylethynyl)pyridine
6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist. 2-methyl-6-(phenylethynyl)pyridine : A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.		2.0810acetylenic compound;
methylpyridines		anxiolytic drug;
metabotropic glutamate receptor antagonist
bms 387032
N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide: a CDK2 inhibitor with antineoplastic activity; structure in first source. N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of piperidine-4-carboxylic acid with the amino group of 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-amine. It is an ATP-competitive inhibitor of CDK2, CDK7 and CDK9 kinases and exhibits anti-cancer properties.		2.08101,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
lithium
Lithium: An element in the alkali metals family. It has the atomic symbol Li, atomic number 3, and atomic weight [6.938; 6.997]. Salts of lithium are used in treating BIPOLAR DISORDER.		10.1252alkali metal atom
cobaltous chloride
cobaltous chloride: RN given refers to unlabeled cpd; RN in Chemline for cobalt trichloride: 10241-04-0; RN for 60-labeled cpd: 14543-09-0; RN for 57-labeled cpd: 164113-89-1; RN for 58-labeled cpd: 29377-09-1; structure. cobalt dichloride : A cobalt salt in which the cobalt metal is in the +2 oxidation state and the counter-anion is chloride. It is used as an indicator for water in desiccants.		2.4720cobalt salt;
inorganic chloride		allergen;
calcium channel blocker;
sensitiser;
two-colour indicator
nitrogen dioxide
Nitrogen Dioxide: Nitrogen oxide (NO2). A highly poisonous gas. Exposure produces inflammation of lungs that may only cause slight pain or pass unnoticed, but resulting edema several days later may cause death. (From Merck, 11th ed) It is a major atmospheric pollutant that is able to absorb UV light that does not reach the earth's surface.		1.9910nitrogen oxide
maneb
Maneb: Manganese derivative of ethylenebisdithiocarbamate. It is used in agriculture as a fungicide and has been shown to cause irritation to the eyes, nose, skin, and throat.. maneb : A polymeric complex of manganese with the ethylene bis(dithiocarbamate) anionic ligand. An agrochemical fungicide, it is used to control a variety of diseases including blight, leaf spot, rust, downy mildew and scab.		2.4110
dermatan sulfate
Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units.		3.2310amino disaccharide;
glycosylgalactose derivative;
iduronic acids;
oligosaccharide sulfate
dezocine
dezocine: potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure. dezocine : (7S,8S)-7-Amino-8-methyl-5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogen at position 8 and one of the hydrogens at position 6 are substituted by each end of a tetramethylene bridge. A synthetic opioid analgesic, it has mixed opiod agonist and antagonist properties. Although it is used for pain management, it can produce opioid withdrawal syndrome in patients already dependent on other opioids, and its clinical application is limited by side effects such as dizziness.		7.3110phenols;
primary amino compound		opioid analgesic
droloxifene
[no description available]		2.0510stilbenoid
dolasetron
[no description available]		3.6120indolyl carboxylic acid
or 1259
[no description available]		2.0510hydrazone;
nitrile;
pyridazinone		anti-arrhythmia drug;
cardiotonic drug;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
vasodilator agent
monooctanoin
monooctanoin: dissolution agent for retained cholesterol bile duct stones; RN in Chemline for octanoic acid, ester with 1,2,3-propanetriol, MF unknown: 11140-04-8; RN for octanoic acid, 2,3-dihydroxypropyl ester (1-monooctanoin): 502-54-5; RN in 9th CI Form Index for (+-)-1-monooctanoin: 19670-49-6. rac-1-monooctanoylglycerol : A rac-1-monoacylglycerol comprising equal amounts of 1-octanoyl-sn-glycerol and 3-octanoyl-sn-glycerol.. 1-monooctanoylglycerol : A 1-monoglyceride that has octanoyl as the acyl group.		2.08101-monoglyceride;
octanoate ester;
rac-1-monoacylglycerol
gestodene
Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer		2.4720steroidestrogen
orlistat
Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.		3.8730beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative		anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor
idoxifene
idoxifene: structure given in first source		2.0510stilbenoid
quinine
[no description available]		5.0670cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
1,2-bis(2-aminophenoxy)ethane n,n,n',n'-tetraacetic acid acetoxymethyl ester
[no description available]		2.0210
glycodeoxycholic acid
Glycodeoxycholic Acid: A bile salt formed in the liver by conjugation of deoxycholate with glycine, usually as the sodium salt. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and choleretic.. glycodeoxycholic acid : A bile acid glycine conjugate of deoxycholic acid.		2.7630bile acid glycine conjugatehuman metabolite
rtki cpd
RTKI cpd: preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors		2.9540
cystine
[no description available]		2.2110
chaetomellic acid a
chaetomellic acid A: structure given in first source; an inhibitor of farnesyl-protein transferase		2.0610
fospropofol
[no description available]		3.2310alkylbenzene
tandutinib
[no description available]		2.0810aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
vx-745
[no description available]		2.0810aryl sulfide;
dichlorobenzene;
difluorobenzene;
pyrimidopyridazine		anti-inflammatory drug;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
corlanor
ivabradine hydrochloride : A hydrochloride obtained by combining ivabradine with one molar equivalent of hydrochloric acid. Used to treat patients with angina who have intolerance to beta blockers and/or heart failure.		2.0810hydrochloridecardiotonic drug
sr140333b
SR140333B: a neurokinin-1 receptor antagonist		2.5320
azilect
[no description available]		2.0810
rasagiline
[no description available]		3.2310indanes;
secondary amine;
terminal acetylenic compound		EC 1.4.3.4 (monoamine oxidase) inhibitor;
neuroprotective agent
deracoxib
SC 046: structure in first source. deracoxib : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3, and 5 by 4-sulfamoylphenyl, difluoromethyl and 3-fluoro-4-methoxyphenyl groups, respectively. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in dogs.		4.0550organofluorine compound;
pyrazoles;
sulfonamide		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		9.47601,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
zd 6474
CH 331: structure in first source		2.9840aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
desmethylanethol trithione
desmethylanethol trithione: metabolite of anethol trithione; structure given in first source		2.610
2,6-dibromosulfanilamide
2,6-dibromosulfanilamide: structure in first source		3.1550
salinomycin
salinomycin: from Streptomyces albus; RN given refers to parent cpd; structure		2.1110polyketide;
spiroketal		animal growth promotant;
potassium ionophore
silybin
[no description available]		2.0510
benzene-1-3-disulfonamide
[no description available]		4.25160sulfonamide
compound 968
compound 968: a glutaminase inhibitor. 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one : A partially hydrogenated benzophenanthridine carrying an oxo group at C-4, geminal methyl groups at C-2 and a 3-bromo-4-(dimethylamino)phenyl group at C-5.		2.0810benzophenanthridineEC 3.5.1.2 (glutaminase) inhibitor
phosphothreonine
Phosphothreonine: The phosphoric acid ester of threonine. Used as an identifier in the analysis of peptides, proteins, and enzymes.. O-phospho-L-threonine : A L-threonine derivative phosphorylated at the side-chain hydroxy function.		2.0110L-threonine derivative;
non-proteinogenic L-alpha-amino acid;
O-phosphoamino acid		Escherichia coli metabolite
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline: structure given in first source; neuroprotectant for cerebral ischemia; AMPA receptor antagonist		2.0310naphthalenes;
sulfonic acid derivative
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		2.0410
sb-224289
SB 224289 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid with the secondary amino group of 1'-methyl-6,7-dihydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidine]. Selective 5-HT1B receptor antagonist (pKi = 8.2). Displays >60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.		2.08101,2,4-oxadiazole;
azaspiro compound;
benzamides;
organic heterotetracyclic compound		serotonergic antagonist
gw 7647
GW 7647: a PPAR-alpha agonist; structure in first source. GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.		2.0810aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist
sodium dodecyl sulfate
Sodium Dodecyl Sulfate: An anionic surfactant, usually a mixture of sodium alkyl sulfates, mainly the lauryl; lowers surface tension of aqueous solutions; used as fat emulsifier, wetting agent, detergent in cosmetics, pharmaceuticals and toothpastes; also as research tool in protein biochemistry.. sodium dodecyl sulfate : An organic sodium salt that is the sodium salt of dodecyl hydrogen sulfate.		3.1750organic sodium saltdetergent;
protein denaturant
fh535
FH535: inhibits Wnt signaling		2.110sulfonamide
mtt formazan
MTT formazan: a blue MEM-insoluble mitochondrial byproduct; used to determine viability of cells with active mitochondrial dehydrogenase enzymes		2.0210
chloramine-t
chloramine-T: RN given refers to unlabeled parent cpd. chloramine T : An organic sodium salt derivative of toluene-4-sulfonamide with a chloro substituent in place of an amino hydrogen.		2.0510organic sodium saltallergen;
antifouling biocide;
disinfectant
l 663536
MK-886: orally active leukotriene biosynthesis inhibitor. 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid : A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at position 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.		5.25150aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes		antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist
6-cyano-7-nitroquinoxaline-2,3-dione
6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.		3.5110quinoxaline derivative
1-[6-(4-chlorophenyl)-5-imidazo[2,1-b]thiazolyl]-N-[(3,4-dichlorophenyl)methoxy]methanimine
[no description available]		2.0810imidazoles
zinc protoporphyrin ix
[no description available]		2.4920
fg 9041
FG 9041: structure given in first source		3.5110quinoxaline derivative
N4-ethyl-N6,1,2-trimethyl-N4-phenylpyrimidin-1-ium-4,6-diamine
[no description available]		2.0810aromatic amine;
tertiary amino compound
2-[[2-[2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-1-oxo-5-isoquinolinyl]oxy]propanoic acid ethyl ester
[no description available]		2.0810isoquinolines
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		2.5520
sch 79797
[no description available]		2.0810quinazolines
sc 560
SC560 : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-methoxyphenyl, trifluoromethyl and 4-chlorophenyl groups, respectively. Unlike many members of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors, SC-560 is selective for COX-1.		6.69510aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles		angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		3.8730triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
cfm 2
CFM 2: structure in first source		2.0310benzodiazepine
osteoprotegerin
Osteoprotegerin: A secreted member of the TNF receptor superfamily that negatively regulates osteoclastogenesis. It is a soluble decoy receptor of RANK LIGAND that inhibits both CELL DIFFERENTIATION and function of OSTEOCLASTS by inhibiting the interaction between RANK LIGAND and RECEPTOR ACTIVATOR OF NUCLEAR FACTOR-KAPPA B.		5.6651long-chain fatty acid
flosequinan
[no description available]		2.0510quinolines
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide: a TGF-beta type I receptor kinase activity inhibitor		2.0810benzamides;
benzodioxoles;
imidazoles;
pyridines		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
4-hydroxy-5-methyl-3(2h)-furanone
4-hydroxy-5-methyl-3-furanone : A member of the class of furans that is 5-methyl-2,3-dihydrofuran with a hydroxy group at position 4 and a keto group at position 3.		3.3110cyclic ketone;
enol;
furans		metabolite
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		4.09402-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
1-(4-Fluorophenyl)-3-(3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one
[no description available]		2.0810monobactam
diclofenac sodium
Diclofenac Sodium: The sodium form of DICLOFENAC. It is used for its analgesic and anti-inflammatory properties.. diclofenac sodium : The sodium salt of diclofenac.		5.96180organic sodium salt
imd 0354
N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first source		2.0810benzamides
1,2-diamino-4-nitrobenzene
1,2-diamino-4-nitrobenzene: reagent for determination of selenium in milk with gas chromatograph. 4-nitro-1,2-phenylenediamine : The primary amino compound that is 1,2-phenylenediamine (o-phenylenediamine) substituted at the 4- (para-) position by a nitro group.		2.0210C-nitro compound;
primary amino compound
ex 527
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide: structure in first source. 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide : A member of the class of carbazoles that is 2,3,4,9-tetrahydro-1H-carbazole which is substituted at position 1 by an aminocarbohyl group and at position 6 by a chlorine.		2.0810carbazoles;
monocarboxylic acid amide;
organochlorine compound
calceolarioside b
calceorioside B: a cardioprotective agent isolated from Akebia; structure in first source		2.0610hydroxycinnamic acidmetabolite
sphingosine
sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.		2.4920sphing-4-eninehuman metabolite;
mouse metabolite
quercetin
[no description available]		5.171307-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
bilirubin
[no description available]		3.8130biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		17.8639333prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		6.47161monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
biochanin a
[no description available]		2.04104'-methoxyisoflavones;
7-hydroxyisoflavones		antineoplastic agent;
EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
leukotriene a4
Leukotriene A4: (2S-(2 alpha,3 beta(1E,3E,5Z,8Z)))-3-(1,3,5,8-Tetradecatetraenyl)oxiranebutanoic acid. An unstable allylic epoxide, formed from the immediate precursor 5-HPETE via the stereospecific removal of a proton at C-10 and dehydration. Its biological actions are determined primarily by its metabolites, i.e., LEUKOTRIENE B4 and cysteinyl-leukotrienes. Alternatively, leukotriene A4 is converted into LEUKOTRIENE C4 by glutathione-S-transferase or into 5,6-di-HETE by the epoxide-hydrolase. (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene A4 : A leukotriene that is the (5S,6S)-epoxy derivative of (7E,9E,11Z,14Z)-icosa-7,9,11,14-tetraenoic acid.		2.0410epoxy fatty acid;
leukotriene;
long-chain fatty acid;
oxylipin;
polyunsaturated fatty acid		human metabolite;
mouse metabolite;
plant metabolite
arachidonyltrifluoromethane
arachidonyltrifluoromethane: structure given in first source; inhibits 85-kDa phospholipase A2. AACOCF3 : A fatty acid derivative that is arachidonic acid in which the OH part of the carboxy group has been replaced by a trifluoromethyl group		2.9810fatty acid derivative;
ketone;
olefinic compound;
organofluorine compound		EC 3.1.1.4 (phospholipase A2) inhibitor
apigenin
Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.		2.9840trihydroxyflavoneantineoplastic agent;
metabolite
luteolin
[no description available]		4.1403'-hydroxyflavonoid;
tetrahydroxyflavone		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		4.4260D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
scopoletin
[no description available]		2.3110hydroxycoumarinplant growth regulator;
plant metabolite
beta carotene
beta Carotene: A carotenoid that is a precursor of VITAMIN A. Beta carotene is administered to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria (PORPHYRIA, ERYTHROPOIETIC).. provitamin A : A provitamin that can be converted into vitamin A by enzymes from animal tissues.		3.5620carotenoid beta-end derivative;
cyclic carotene		antioxidant;
biological pigment;
cofactor;
ferroptosis inhibitor;
human metabolite;
mouse metabolite;
plant metabolite;
provitamin A
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		10.58161dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
thromboxane a2
Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).. thromboxane A2 : A thromboxane which is produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.		8.81151epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite
retinol palmitate
retinol palmitate: RN given refers to parent cpd; structure. retinyl palmitate : A palmitate ester of retinol with undefined geometry about the C=C bonds.. all-trans-retinyl palmitate : An all-trans-retinyl ester obtained by formal condensation of the carboxy group of palmitic (hexadecanoic acid) with the hydroxy group of all-trans-retinol. It is used in cosmetic products to treat various skin disorders such as acne, skin aging, wrinkles, dark spots, and also protect against psoriasis.		2.5120all-trans-retinyl ester;
retinyl palmitate		antioxidant;
Escherichia coli metabolite;
human xenobiotic metabolite
8,11,14-eicosatrienoic acid
8,11,14-Eicosatrienoic Acid: A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.. all-cis-icosa-8,11,14-trienoic acid : An icosatrienoic acid having three cis double bonds at positions 8, 11 and 14.		2.4720fatty acid 20:3;
long-chain fatty acid		fungal metabolite;
human metabolite;
nutraceutical
rumenic acid
9-cis,11-trans-octadecadienoic acid : An octadeca-9,11-dienoic acid having 9-cis,11-trans-stereochemistry.		2.1510octadeca-9,11-dienoic acid
quercetin 3-o-methyl ether
quercetin 3-O-methyl ether: from Rhamnus species; structure in first source. 3',4',5,7-tetrahydroxy-3-methoxyflavone : A tetrahydroxyflavone having the 4-hydroxy groups located at the 3'- 4'- 5- and 7-positions as well as a methoxy group at the 2-position.		3.3110monomethoxyflavone;
tetrahydroxyflavone		antimicrobial agent;
metabolite
alprostadil
[no description available]		2.9540prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
5-hydroxy-6,8,11,14-eicosatetraenoic acid
5(S)-HETE : A HETE having a (5S)-hydroxy group and (6E)-, (8Z)-, (11Z)- and (14Z)-double bonds.. 5-HETE : A HETE having a 5-hydroxy group and (6E)-, (8Z)-, (11Z)- and (14Z)-double bonds.		2.7230HETEhuman metabolite;
mouse metabolite
vitamin d 2
Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa.		3.8730hydroxy seco-steroid;
seco-ergostane;
vitamin D		bone density conservation agent;
nutraceutical;
plant metabolite;
rodenticide
cholecalciferol
Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.. calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone.		4.1231D3 vitamins;
hydroxy seco-steroid;
seco-cholestane;
secondary alcohol;
steroid hormone		geroprotector;
human metabolite
quercetin 3-o-glucopyranoside
quercetin 3-O-glucopyranoside: structure in first source. quercetin 3-O-beta-D-glucopyranoside : A quercetin O-glucoside that is quercetin with a beta-D-glucosyl residue attached at position 3. Isolated from Lepisorus contortus, it exhibits antineoplastic activityand has been found to decrease the rate of polymerization and sickling of red blood cells		2.4820beta-D-glucoside;
monosaccharide derivative;
quercetin O-glucoside;
tetrahydroxyflavone		antineoplastic agent;
antioxidant;
antipruritic drug;
bone density conservation agent;
geroprotector;
histamine antagonist;
osteogenesis regulator;
plant metabolite
rutin
Hydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.		3.6320disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone		antioxidant;
metabolite
bilirubin diglucuronide
[no description available]		3.1510
kaempferol
[no description available]		2.15107-hydroxyflavonol;
flavonols;
tetrahydroxyflavone		antibacterial agent;
geroprotector;
human blood serum metabolite;
human urinary metabolite;
human xenobiotic metabolite;
plant metabolite
leukotriene e4
Leukotriene E4: A biologically active principle of SRS-A that is formed from LEUKOTRIENE D4 via a peptidase reaction that removes the glycine residue. The biological actions of LTE4 are similar to LTC4 and LTD4. (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene E4 : A leukotriene that is (7E,9E,11Z,14Z)-icosa-7,9,11,14-tetraenoic acid substituted by a hydroxy group at position 5 (5S) and an L-cystein-S-yl group at position 6 (6R).		5.754amino dicarboxylic acid;
L-cysteine thioether;
leukotriene;
non-proteinogenic L-alpha-amino acid;
secondary alcohol
prostaglandin g2
[no description available]		3.110prostaglandins Ghuman metabolite;
mouse metabolite
6-ketoprostaglandin f1 alpha
6-Ketoprostaglandin F1 alpha: The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.. 6-oxoprostaglandin F1alpha : A prostaglandin Falpha that is prostaglandin F1alpha bearing a keto substituent at the 6-position.		8.82244prostaglandins Falphahuman metabolite;
mouse metabolite
11-dehydro-thromboxane b2
11-dehydro-thromboxane B2: structure given in first source. 11-dehydro-thromboxane B2 : A thromboxane obtained by formal oxidation of the hemiacetal hydroxy function of thromboxane B2.		6.8153thromboxanehuman metabolite
lipoxin a4
lipoxin A4: an antifibrolytic agent; structure given in first source; a role in ASPIRIN antiinflammatory activity. lipoxin A4 : A C20 hydroxy fatty acid having (5S)-, (6R)- and (15S)-hydroxy groups as well as (7E)- (9E)-, (11Z)- and (13E)-double bonds.		2.4220hydroxy polyunsaturated fatty acid;
lipoxin;
long-chain fatty acid		human metabolite;
metabolite
gamma-linolenic acid
gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed). gamma-linolenic acid : A C18, omega-6 acid fatty acid comprising a linolenic acid having cis- double bonds at positions 6, 9 and 12.		2.7930linolenic acid;
omega-6 fatty acid		human metabolite;
mouse metabolite;
plant metabolite
alpha-linolenic acid
linolenic acid : A two-membered subclass of octadecatrienoic acid comprising the (9Z,12Z,15Z)- and (6Z,9Z,12Z)-isomers. Linolenic acids are nutrients essential to the formation of prostaglandins and are also used in making paints and synthetic resins.. linolenate : A polyunsaturated fatty acid anion obtained by deprotonation of the carboxy group of either alpha- or gamma-linolenic acid.		2.0810linolenic acid;
omega-3 fatty acid		micronutrient;
mouse metabolite;
nutraceutical
prostaglandin e3
prostaglandin E3: Structure		2.0210prostaglandins Ehuman metabolite
prostaglandin f1
prostaglandin F1: was EN to PROSTAGLANDINS F (75-81); RN given refers to (9 alpha,11 alpha,13E,15S)-isomer		2.9440prostaglandins Falphahuman metabolite
genistein
[no description available]		8.69907-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		4.7850antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
clavulanic acid
Clavulanic Acid: A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.. clavulanate : The conjugate base of clavulanic acid.. clavulanic acid : Antibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes.		2.0510oxapenamantibacterial drug;
anxiolytic drug;
bacterial metabolite;
EC 3.5.2.6 (beta-lactamase) inhibitor
pulmicort
Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.		4.668011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen
oxymetholone
Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects.		3.8730
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		3.8730dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
montelukast
montelukast: a leukotriene D4 receptor antagonist		4.4460aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
mivacurium
Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent.		3.2310isoquinolines
timolol maleate
(S)-timolol maleate : The maleic acid salt of the active (S)-enantiomer of timolol, comprising equimolar amounts of (S)-timolol and maleic acid.		2.0510maleate saltanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
brompheniramine maleate
brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.4720maleate saltanti-allergic agent
chlorpheniramine maleate
[no description available]		2.5220organic molecular entity
clemastine fumarate
clemastine fumarate : The fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		2.0510fumarate saltanti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
dexchlorpheniramine maleate
[no description available]		2.0810organic molecular entity
olopatadine
[no description available]		2.0810
methylergonovine maleate
[no description available]		2.0510ergoline alkaloidgeroprotector
hemabate
carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy.		3.2310
mycophenolate mofetil
mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.		3.8730carboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound		anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug
entacapone
entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.		4.09402-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
paricalcitol
[no description available]		3.2310hydroxy seco-steroid;
seco-cholestane		antiparathyroid drug
astaxanthine
astaxanthine: a keto form of carotene; pigment in flesh of Scottish salmon (Salmo salar) crustacoa-lobster (Homarus gammarus, flamingo feathers; structure; a carotenoid without vitamin A activity, has shown anti-oxidant and anti-inflammatory activities. astaxanthin : A carotenone that consists of beta,beta-carotene-4,4'-dione bearing two hydroxy substituents at positions 3 and 3' (the 3S,3'S diastereomer). A carotenoid pigment found mainly in animals (crustaceans, echinoderms) but also occurring in plants. It can occur free (as a red pigment), as an ester, or as a blue, brown or green chromoprotein.		2.4420carotenol;
carotenone		animal metabolite;
anticoagulant;
antioxidant;
food colouring;
plant metabolite
lutein
Lutein: A xanthophyll found in the major LIGHT-HARVESTING PROTEIN COMPLEXES of plants. Dietary lutein accumulates in the MACULA LUTEA.. xanthophyll : A subclass of carotenoids consisting of the oxygenated carotenes.		2.0610carotenolfood colouring;
plant metabolite
isobavachalcone
isobavachalcone: RN given for (E)-isomer; structure in first source. isobavachalcone : A member of the class of chalcones that is trans-chalcone substituted by hydroxy groups at positions 4, 2' and 4' and a prenyl group at position 3'.		3.3110chalcones;
polyphenol		antibacterial agent;
metabolite;
platelet aggregation inhibitor
7-hydroxycoumarin
7-oxycoumarin: derivatives have anti-oxidant properties. umbelliferone : A hydroxycoumarin that is coumarin substituted by a hydroxy group ay position 7.		2.1510hydroxycoumarinfluorescent probe;
food component;
plant metabolite
humulene
humulene: structure given in first source. (1E,4E,8E)-alpha-humulene : The (1E,4E,8E)-isomer of alpha-humulene.		3.811alpha-humulene
baicalein
[no description available]		2.4520trihydroxyflavoneangiogenesis inhibitor;
anti-inflammatory agent;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 4.1.1.17 (ornithine decarboxylase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hormone antagonist;
plant metabolite;
prostaglandin antagonist;
radical scavenger
chrysin
chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7.		8.01407-hydroxyflavonol;
dihydroxyflavone		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite
diosmin
[no description available]		2.0510dihydroxyflavanone;
disaccharide derivative;
glycosyloxyflavone;
monomethoxyflavone;
rutinoside		anti-inflammatory agent;
antioxidant
galangin
5,7-dihydroxyflavonol: antimicrobial from the twigs of Populus nigra x Populus deltoides; structure in first source. galangin : A 7-hydroxyflavonol with additional hydroxy groups at positions 3 and 5 respectively; a growth inhibitor of breast tumor cells.		3.35107-hydroxyflavonol;
trihydroxyflavone		antimicrobial agent;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
plant metabolite
hyperoside
quercetin 3-O-beta-D-galactopyranoside : A quercetin O-glycoside that is quercetin with a beta-D-galactosyl residue attached at position 3. Isolated from Artemisia capillaris, it exhibits hepatoprotective activity.		2.110beta-D-galactoside;
monosaccharide derivative;
quercetin O-glycoside;
tetrahydroxyflavone		hepatoprotective agent;
plant metabolite
norathyriol
norathyriol: from Gentinanaceae; has vasorelaxing action on rat thoracic aorta; structure given in first source. norathyriol : A member of the class of xanthones that is 9H-xanthen-9-one substituted by hydroxy groups at positions 1, 3, 6 and 7. Isolated from Garcinia mangostana and Maclura pomifera, it exhibits inhibitory activity against protein kinase C.		3.3110polyphenol;
xanthones		antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
plant metabolite
morin
morin: a light yellowish pigment found in the wood of old fustic (Chlorophora tinctoria). morin : A pentahydroxyflavone that is 7-hydroxyflavonol bearing three additional hydroxy substituents at positions 2' 4' and 5.		2.46207-hydroxyflavonol;
pentahydroxyflavone		angiogenesis modulating agent;
anti-inflammatory agent;
antibacterial agent;
antihypertensive agent;
antineoplastic agent;
antioxidant;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
hepatoprotective agent;
metabolite;
neuroprotective agent
myricitrin
myricitrin: isolated from root bark of Myrica cerifera L.; structure. myricitrin : A glycosyloxyflavone that consists of myricetin attached to a alpha-L-rhamnopyranosyl residue at position 3 via a glycosidic linkage. Isolated from Myrica cerifera, it exhibits anti-allergic activity.		3.3110alpha-L-rhamnoside;
glycosyloxyflavone;
monosaccharide derivative;
pentahydroxyflavone		anti-allergic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
plant metabolite
wogonin
wogonin: structure in first source. wogonin : A dihydroxy- and monomethoxy-flavone in which the hydroxy groups are positioned at C-5 and C-7 and the methoxy group is at C-8.		2.5120dihydroxyflavone;
monomethoxyflavone		angiogenesis inhibitor;
antineoplastic agent;
cyclooxygenase 2 inhibitor;
plant metabolite
coumestrol
Coumestrol: A daidzein derivative occurring naturally in forage crops which has some estrogenic activity.. coumestrol : A member of the class of coumestans that is coumestan with hydroxy substituents at positions 3 and 9.		2.0710coumestans;
delta-lactone;
polyphenol		anti-inflammatory agent;
antioxidant;
plant metabolite
daidzein
[no description available]		2.07107-hydroxyisoflavonesantineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
phytoestrogen;
plant metabolite
pterostilbene
[no description available]		7.610diether;
methoxybenzenes;
stilbenol		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger
cynarine
cynarine: active principle of the artichoke; functions primarily as a cholagogue and choleretic and also as antilipemic agent		2.0510alkyl caffeate ester;
quinic acid		plant metabolite
caffeic acid phenethyl ester
phenethyl caffeate : An alkyl caffeate ester in which 2-phenylethyl is the alkyl component.		2.1310alkyl caffeate esteranti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
antiviral agent;
immunomodulator;
metabolite;
neuroprotective agent
acteoside
acteoside: a protein kinase C inhibitor with hepatoprotective, anti-asthmatic, and analgesic activities; a phenylethanoid glycoside related to isoacteoside; from leaves of Lippia multiflora (Verbenaceae). acteoside : A glycoside that is the alpha-L-rhamnosyl-(1->3)-beta-D-glucoside of hydroxytyrosol in which the hydroxy group at position 4 of the glucopyranosyl moiety has undergone esterification by formal condensation with trans-caffeic acid.		3.3110catechols;
cinnamate ester;
disaccharide derivative;
glycoside;
polyphenol		anti-inflammatory agent;
antibacterial agent;
antileishmanial agent;
neuroprotective agent;
plant metabolite
Licarin A
[no description available]		2.0510benzofurans
ellagic acid
[no description available]		8.2550catechols;
cyclic ketone;
lactone;
organic heterotetracyclic compound;
polyphenol		antioxidant;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor;
EC 2.4.1.1 (glycogen phosphorylase) inhibitor;
EC 2.5.1.18 (glutathione transferase) inhibitor;
EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor;
EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor;
EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
food additive;
fungal metabolite;
geroprotector;
plant metabolite;
skin lightening agent
flupenthixol
cis-flupenthixol : A flupenthixol in which the double bond adopts a cis-configuration.		2.9740flupenthixoldopaminergic antagonist
sdz psc 833
valspodar: nonimmunosuppressive cyclosporin analog which is a potent multidrug resistance modifier; 7-10 fold more potent than cyclosporin A; a potent P glycoprotein inhibitor; MW 1215		2.4720homodetic cyclic peptide
estradiol-17 beta-glucuronide
17beta-estradiol 17-glucosiduronic acid : A steroid glucosiduronic acid that consists of 17beta-estradiol having a beta-glucuronyl residue attached at position 17 via a glycosidic linkage.		3.85303-hydroxy steroid;
steroid glucosiduronic acid
l 660,711
[no description available]		2.7630quinolines
prostaglandin a1
[no description available]		2.730prostaglandins A
coenzyme q10
coenzyme Q10: Ubiquinone ring with a chain of 10 isoprene units; redox equilibrium with ubiqunol serving in mitochondrial inner membrane to transfer electrons; presence during reconstitution of acetylcholine receptor into phospholipid vesicles yields vesicles active in catalyzing carbamylcholine-sensitive Na+ flux; coenzyme Q10 depletion has been noted with use of statins. coenzyme Q10 : A ubiquinone having a side chain of 10 isoprenoid units. In the naturally occurring isomer, all isoprenyl double bonds are in the E- configuration.		2.4420ubiquinonesantioxidant;
ferroptosis inhibitor;
human metabolite
anandamide
anandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine.		2.520endocannabinoid;
N-acylethanolamine 20:4		human blood serum metabolite;
neurotransmitter;
vasodilator agent
4',7-dihydroxyflavone
4',7-dihydroxyflavone: inducer of nod gene. 4',7-dihydroxyflavone : A dihydroxyflavone in which the two hydroxy substituents are located at positions 4' and 7.		2.1510dihydroxyflavonemetabolite
astragalin
kaempferol-3-O-glucoside: isolated from the pit of Mahkota dewa; structure in first source. kaempferol 3-O-beta-D-glucoside : A kaempferol O-glucoside in which a glucosyl residue is attached at position 3 of kaempferol via a beta-glycosidic linkage.		2.110beta-D-glucoside;
kaempferol O-glucoside;
monosaccharide derivative;
trihydroxyflavone		plant metabolite;
trypanocidal drug
geranylgeranylacetone
geranylgeranylacetone: structure in first source; RN given refers to isomeric cpd without isomeric designation; mixture of (5E,9E,13E) & (5Z,9E,13E)-isomers. teprenone : A terpene ketone in which a (9E,13E)-geranylgernayl group is bonded to one of the alpha-methyls of acetone (it is a mixture of 5E- and 5Z-geoisomers in a 3:2 ratio).		2.0310
pelubiprofen
pelubiprofen: RN & structure given in first source; RN not in Chemline 3/84		9.411
travoprost
Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.		2.0810(trifluoromethyl)benzenes;
isopropyl ester;
prostaglandins Falpha		antiglaucoma drug;
antihypertensive agent;
ophthalmology drug;
prodrug;
prostaglandin receptor agonist
tranilast
tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.		2.7530amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide		anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
7432 s
Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections.		3.2310cephalosporin;
dicarboxylic acid		antibacterial drug
8-epi-prostaglandin f2alpha
8-epi-prostaglandin F2alpha: a potent preglomerular vasoconstrictor acting principally through thromboxane A2 receptor activation. 8-epi-prostaglandin F2alpha : An isoprostane that is prostaglandin F2alpha having inverted stereochemistry at the 8-position.		2.7130F2-isoprostanebiomarker;
bronchoconstrictor agent;
vasoconstrictor agent
glyceryl 2-arachidonate
glyceryl 2-arachidonate: binds to cannabinoid receptors; structure in first source. 2-arachidonoylglycerol : An endocannabinoid and an endogenous agonist of the cannabinoid receptors (CB1 and CB2). It is an ester formed from omega-6-arachidonic acid and glycerol.		2.07102-acylglycerol 20:4;
endocannabinoid		human metabolite
4,4'-dihydroxystilbene
[no description available]		2.1710stilbene-4,4'-diol
menatetrenone
menaquinone-4 : A menaquinone whose side-chain contains 4 isoprene units in an all-trans-configuration.		2.0510menaquinoneanti-inflammatory agent;
antioxidant;
bone density conservation agent;
human metabolite;
neuroprotective agent
imipenem
[no description available]		2.0810carbapenems
etretinate
retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.		2.4720enoate ester;
ethyl ester;
retinoid		keratolytic drug
isotretinoin
Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases.		8.3683retinoic acidantineoplastic agent;
keratolytic drug;
teratogenic agent
misoprostol
Misoprostol: A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties.. misoprostol : A diastereoisomeric mixture composed of approximately equal amounts of a double racemate of four of the sixteen possible diastereoisomers of methyl (13E)-11,16-dihydroxy-16-methyl-9-oxoprost-13-en-1-oate that is racemic prostaglandin E1 which is lacking the hydroxy group at position 15, but which has an additional hydroxy group at position 16. It is a synthetic prostaglandin E1 analogue, used in the treatment of gastric and duodenal ulcers. A weak abortifacient, it is also used for cervical ripening prior to surgical termination of pregnancy. The (11R,16S)-diastereoisomer is the pharmacologically active form.		8.78132
ketotifen fumarate
ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.		2.0810organoammonium saltanti-asthmatic drug;
H1-receptor antagonist
epoprostenol
[no description available]		3.2310prostaglandins Imouse metabolite
indocyanine green
[no description available]		3.58201,1-diunsubstituted alkanesulfonate;
benzoindole;
cyanine dye
dinoprost tromethamine
[no description available]		2.0810organic molecular entity
ozagrel
ozagrel: RN refers to (E)-isomer		2.0510cinnamic acids
triprolidine
Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders.		3.2310N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
pitavastatin
pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.		9.0840cyclopropanes;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
quinolines;
statin (synthetic)		antioxidant
rosuvastatin calcium
S 4522: structure in first source		2.0810N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine;
organic calcium salt		anti-inflammatory agent;
cardioprotective agent;
CETP inhibitor
terbinafine hydrochloride
terbinafine hydrochloride : A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride.		2.0810allylamine antifungal drug;
hydrochloride		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor
ethamolin
monoethanolamine oleate: used for treatment of pyogenic granuloma		3.2310long-chain fatty acid
alatrofloxacin mesylate
[no description available]		3.5920
13-hydroxy-9,11-octadecadienoic acid
13-hydroxy-9,11-octadecadienoic acid: chemorepellant factor which maintains blood vessel wall thromboresistance; RN given refers to unspecified stereoisomer		2.4220octadecadienoic acid
16,16-dimethylprostaglandin e2
16,16-Dimethylprostaglandin E2: A synthetic prostaglandin E analog that protects the gastric mucosa, prevents ulceration, and promotes the healing of peptic ulcers. The protective effect is independent of acid inhibition. It is also a potent inhibitor of pancreatic function and growth of experimental tumors.. 16,16-dimethylprostaglandin E2 : A prostanoid that is prostaglandin E2 in which both of the hydrogens at position 16 have been replaced by methyl groups. A synthetic analogue of prostaglandin E2, it is a potent inhibitor of pancreatic function and growth of experimental tumors. It also protects the gastric mucosa, prevents ulceration, and promotes the healing of peptic ulcers.		2.0510cyclopentanones;
monocarboxylic acid;
prostanoid;
secondary allylic alcohol		anti-ulcer drug;
gastrointestinal drug;
radiation protective agent
2,3-dinor-6-ketoprostaglandin f1alpha
2,3-dinor-6-ketoprostaglandin F1alpha: formed from 6-keto-PGF1alpha by Mycobacterium rhodochrous; RN given refers to (1R-(1alph,2beta(1E,3S*)))-isomer; structure given in first source. 2,3-dinor-6-oxoprostaglandin F1alpha : A prostanoid that is prostaglandin F1alpha lacking two methylenes in the carboxyalkyl chain and bearing an oxo group at the 6-position.		7.12534-oxo monocarboxylic acid;
prostanoid;
secondary alcohol		metabolite
prostaglandin e2 ethanolamide
prostaglandin E2 ethanolamide: structure in first source		2.0710prostanoid
thromboxane b2
Thromboxane B2: A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).. thromboxane B2 : A member of the class of thromboxanes B that is (5Z,13E)-thromboxa-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15.		10.242710thromboxanes Bhuman metabolite;
mouse metabolite
20-hydroxy-5,8,11,14-eicosatetraenoic acid
20-hydroxy-5,8,11,14-eicosatetraenoic acid: stimulator of renal sodium, potassium atpase; RN given is for the (all-Z) isomer. 20-HETE : A HETE that consists of arachidonic acid bearing a hydroxy substituent at position 20.		2.5720HETE;
hydroxy monocarboxylic acid		human metabolite;
mouse metabolite
4-hydroxy-2-nonenal
4-hydroxy-2-nonenal: cytotoxic product from peroxidation of liver microsomal lipids; RN given refers to cpd without isomeric designation. 4-hydroxynon-2-enal : An enal consisting of non-2-ene having an oxo group at the 1-position and a hydroxy group at the 4-position.. 4-hydroxynonenal : A monounsaturated fatty aldehyde that is nonanal that has undergone dehydrogenation to introduce a double bond at any position in the aliphatic chain and in which a hydrogen at position 4 has been replaced by a hydroxy group.		2.42204-hydroxynon-2-enal;
4-hydroxynonenal
1-monooleoyl-rac-glycerol
Peceol: lipid excipient containing readily dispersible mixture of mono- & diglycerides of oleic acid. 1-oleoylglycerol : A 1-monoglyceride where the acyl group is oleoyl.. monooleoylglycerol : A monoglyceride in which the acyl group is oleoyl with the position of acylation unspecified.		3.03401-acylglycerol 18:1;
monooleoylglycerol		plant metabolite
sphingosine 1-phosphate
sphingosine 1-phosphate: RN given refers to (R-(R*,S*-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1		2.110sphingoid 1-phosphatemouse metabolite;
signalling molecule;
sphingosine-1-phosphate receptor agonist;
T-cell proliferation inhibitor;
vasodilator agent
n-palmitoylsphingosine
N-palmitoylsphingosine: structure given in first source; RN given refers to (R*,S*-(E))-isomer. N-hexadecanoylsphingosine : A N-acylsphingosine in which the ceramide N-acyl group is specified as hexadecanoyl (palmitoyl).		2.0510Cer(d34:1);
N-acylsphingosine;
N-palmitoyl-sphingoid base		human blood serum metabolite;
Mycoplasma genitalium metabolite
codeine
[no description available]		4.5670morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		5.6390homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
phenoxybenzamine hydrochloride
[no description available]		2.0510organic molecular entity
phenylephrine hydrochloride
Nose: A part of the upper respiratory tract. It contains the organ of SMELL. The term includes the external nose, the nasal cavity, and the PARANASAL SINUSES.. phenylephrine hydrochloride : A hydrochloride that is the monohydrochloride salt of phenylephrine.		3.3911hydrochloride
natamycin
[no description available]		2.4720antibiotic antifungal drug;
dicarboxylic acid monoester;
epoxide;
macrolide antibiotic;
monosaccharide derivative;
polyene antibiotic		antifungal agrochemical;
antimicrobial food preservative;
apoptosis inducer;
bacterial metabolite;
ophthalmology drug
acitretin
Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9.		4.0940acitretin;
alpha,beta-unsaturated monocarboxylic acid;
retinoid		keratolytic drug
cyproterone
Cyproterone: An anti-androgen that, in the form of its acetate (CYPROTERONE ACETATE), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females.		2.041017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
chlorinated steroid;
tertiary alpha-hydroxy ketone		androgen antagonist
dorzolamide
dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer. dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.		7.18430sulfonamide;
thiophenes		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
dothiepin
[no description available]		2.0510dothiepin
estropipate
estropipate: used therapeutically in menopausal patients		3.2310piperazinium salt;
steroid sulfate
hydrocodone
Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.. hydrocodone : A morphinane-like compound that is a semi-synthetic opioid synthesized from codeine.		11.5863morphinane-like compound;
organic heteropentacyclic compound		antitussive;
mu-opioid receptor agonist;
opioid analgesic
hydromorphone
Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class.		5.3130morphinane alkaloid;
organic heteropentacyclic compound		mu-opioid receptor agonist;
opioid analgesic
levetiracetam
Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine.		4.2850pyrrolidin-2-onesanticonvulsant;
environmental contaminant;
xenobiotic
ly 163892
loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.		3.5920carbacephem;
zwitterion		antibacterial drug;
antimicrobial agent
nabilone
nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure		3.2310
nalmefene
nalmefene: RN given refers to 5-alpha isomer		2.4720morphinane alkaloid
nalorphine
Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.		2.0510morphinane alkaloid
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		3.8730morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
oxycodone
Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain.		19.273521organic heteropentacyclic compound;
semisynthetic derivative		antitussive;
mu-opioid receptor agonist;
opioid analgesic
oxymorphone
Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)		3.5920morphinane alkaloid
vitamin k 1
Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones.		3.2310phylloquinones;
vitamin K		cofactor;
human metabolite;
plant metabolite
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		8.65191antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		8.48530cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
trospium chloride
trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder.		3.2310
brefeldin a
[no description available]		2.4820macrolide antibioticPenicillium metabolite
ophiocordin
azepinostatin: isolated from Fusarium merismoides; structure in first source; RN assigned by CAS - 63590-19-2 (ophiocordin; azepinostatin is not the same as ophiocordin)		2.0610
alvocidib
alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.		2.0510dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound		antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
seocalcitol
seocalcitol: structure given in first source		2.0510
fenretinide
Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids.		3.1450monocarboxylic acid amide;
retinoid		antineoplastic agent;
antioxidant
geldanamycin
[no description available]		2.44201,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound		antimicrobial agent;
antineoplastic agent;
antiviral agent;
cysteine protease inhibitor;
Hsp90 inhibitor
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		14.766232morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
aftin-4
aftin-4: increases production of amyloid-beta protein (1-42)		2.0710
demycarosylturimycin h
[no description available]		2.4720
ter 199
[no description available]		2.0810
7-benzylidenenaltrexone
7-benzylidenenaltrexone: structure given in first source; a highly selective delta1-opioid receptor antagonist		2.0110phenanthrenes
a 192621
A 192621: ET(B) receptor antagonist		2.0310
acipimox
acipimox: lipolysis inhibitor		2.0810pyrazinecarboxylic acid
ah 23848
AH 23848: thromboxane antagonist. AH23848 : A racemate comprising equimolar amounts of (1R,2R,5S)- and (1S,2S,5R)-enantiomers of (4Z)-7-{5-[([1,1'-biphenyl]-4-yl)methoxy]-2-(morpholin-4-yl)-3-oxocyclopentyl}hept-4-enoic acid. The hemicalcium salt is a potent, specific thromboxane receptor-blocking drug that is orally active and has a long duration of action.. (1R,2R,5S)-AH23848 : A (4Z)-7-{5-[([1,1'-biphenyl]-4-yl)methoxy]-2-(morpholin-4-yl)-3-oxocyclopentyl}hept-4-enoic acid in which the stereocentres at positions 1, 2 and 5 have R-, R- and S-configuration respectively.		2.0610(4Z)-7-{5-[([1,1'-biphenyl]-4-yl)methoxy]-2-(morpholin-4-yl)-3-oxocyclopentyl}hept-4-enoic acid
arachidonylcyclopropylamide
arachidonylcyclopropylamide: a potent and selective agonist of neuronal cannabinoid receptor; structure in first source		2.0810
atosiban
[no description available]		2.4820oligopeptide
benzphetamine
Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity.		3.2310amphetamines;
tertiary amine		adrenergic uptake inhibitor;
appetite depressant;
dopamine uptake inhibitor;
sympathomimetic agent
beta-funaltrexamine
beta-funaltrexamine: RN given refers to parent cpd(E)-isomer; structure given in first source		2.0710morphinane alkaloid
bimatoprost
Bimatoprost: A cloprostenol-derived amide that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.		2.0810monocarboxylic acid amideantiglaucoma drug;
antihypertensive agent
upf 596
UPF 596: structure in first source		2.0610
clobetasol
Clobetasol: A derivative of PREDNISOLONE with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than FLUOCINONIDE, it is used topically in treatment of PSORIASIS but may cause marked adrenocortical suppression.. clobetasol : A 3-oxo-Delta(1),Delta(4)-steroid that is 16beta-methylpregna-1,4-diene-3,20-dione bearing hydroxy groups at the 11beta and 17alpha positions, fluorine at position 9, and a chlorine substituent at position 21. It is used as its 17alpha-propionate ester to treat various skin disorders, including exzema and psoriasis.		2.011011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
fluorinated steroid;
glucocorticoid;
tertiary alpha-hydroxy ketone		anti-inflammatory drug;
SMO receptor agonist
denopamine
denopamine: structure given in first source		2.0410dimethoxybenzene
deamino arginine vasopressin
Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR.		3.2310heterodetic cyclic peptidediagnostic agent;
renal agent;
vasopressin receptor agonist
dexmedetomidine
[no description available]		3.930medetomidinealpha-adrenergic agonist;
analgesic;
non-narcotic analgesic;
sedative
fr 173657
FR 173657: structure given in first source		2.0410
goserelin
Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer.		3.2310organic molecular entity
iloprost
Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.. iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.		2.9840carbobicyclic compound;
monocarboxylic acid;
secondary alcohol		platelet aggregation inhibitor;
vasodilator agent
l 365260
L 365260: a CCK-B antagonist; structure given in first source; potent & selective CCK-B & gastrin receptor ligand; L 365260 and L 365346 are (R)- and (S)-stereoisomers, respectively		3.1210benzodiazepine
15-deoxy-delta(12,14)-prostaglandin j2
15-deoxy-delta(12,14)-prostaglandin J2: 15-deoxy-PGJ2 is also available; check for double bonds (indicated by delta) at 12 and 14 positions. 15-deoxy-Delta(12,14)-prostaglandin J2 : A prostaglandin J derivative comprising prostaglandin J2 lacking the 15-hydroxy group and having C=C double bonds at the 12- and 14-positions.		210prostaglandins Jelectrophilic reagent;
insulin-sensitizing drug;
metabolite
latanoprost
Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.		2.0810isopropyl ester;
prostaglandins Falpha;
triol		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
ly 320135
LY 320135: cannabinoid receptor antagonist; structure in first source		2.0810benzofurans
lysophosphatidic acid
lysophosphatidic acid: RN given refers to parent cpd. 1-oleoyl-sn-glycerol 3-phosphate : A 1-acyl-sn-glycerol 3-phosphate having oleoyl as the 1-O-acyl group.. lysophosphatidic acid : A member of the class of lysophosphatidic acids obtained by hydrolytic removal of one of the two acyl groups of any phosphatidic acid. A 'closed' class.		2.43201-acyl-sn-glycerol 3-phosphate
lysophosphatidylcholines
lysophosphatidylcholine : An acylglycerophosphocholine resulting from partial hydrolysis of a phosphatidylcholine, which removes one of the fatty acyl groups. The structure is depicted in the image where R1 = acyl, R2 = H or where R1 = H, R2 = acyl.		2.17101-O-acyl-sn-glycero-3-phosphocholine
nalbuphine
Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.		3.2310organic heteropentacyclic compoundmu-opioid receptor antagonist;
opioid analgesic
nateglinide
Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.		3.6120phenylalanine derivative
pd 166285
[no description available]		2.0810
seglitide
seglitide: more potent than somatostatin for inhibition of insulin, glucagon & growth hormone release; used experimentally in treatment of Alzheimer's disease; somatostatin receptor antagonist		2.0410
vinorelbine
[no description available]		3.8630acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
silodosin
silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source		3.2310indolecarboxamide
kn 62
KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II		2.0810piperazines
su 6656
SU 6656: a c-Src kinase inhibitor; used to probe growth signaling; structure in first source. SU6656 : A member of the class of oxindoles that is 3-methyleneoxindole in which the hydrogeh at position 5 has been replaced by a dimethylaminosulfonyl group and in which one of the hydrogens of the methylene group has been replaced by a 4,5,6,7-tetrahydro-indol-2-yl group. It is a specific inhibitor of Src family kinase.		2.0810
bisdemethoxycurcumin
curcumin III: structure in first source. bisdemethoxycurcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by 4-hydroxycinnamoyl groups.		2.0210beta-diketone;
diarylheptanoid;
enone;
polyphenol		EC 3.2.1.1 (alpha-amylase) inhibitor;
metabolite
syringin
syringin: a phenylpropanoid glycoside; see also eleutherosides & lyoniside for eleutheroside A: 474-58-8. syringin : A monosaccharide derivative that is trans-sinapyl alcohol attached to a beta-D-glucopyranosyl residue at position 1 via a glycosidic linkage.		2.8930beta-D-glucoside;
dimethoxybenzene;
monosaccharide derivative;
primary alcohol		hepatoprotective agent;
plant metabolite
kaempferol-3-o-rutinoside
kaempferol-3-O-rutinoside: isolated from the methanolic extract of the whole plants of Diodia teres through repeated silica gel and Sephadex LH-20 column chromatography; structure in first source. kaempferol-3-rutinoside : A kaempferol O-glucoside that is kaempferol attached to a rutinosyl [6-deoxy-alpha-L-mannosyl-(1->6)-beta-D-glucosyl] residue at position 3 via a glycosidic linkage. It has been isolated from the leaves of Solanum campaniforme.		2.110disaccharide derivative;
kaempferol O-glucoside;
rutinoside;
trihydroxyflavone		metabolite;
plant metabolite;
radical scavenger
muromonab-cd3
cudraflavone B: antiproliferative from Cudrania tricuspidata. cudraflavone B : An extended flavonoid that consists of a pyranochromane skeleton that is 2H,6H-pyrano[3,2-g]chromen-6-one substituted by geminal methyl groups at position 2, a 2,4-dihydroxyphenyl group at position 8, a hydroxy group at position 5 and a prenyl group at position 7. Isolated from Morus alba and Morus species it exhibits anti-inflammatory activity.		3.3110extended flavonoid;
pyranochromane;
trihydroxyflavone		anti-inflammatory agent;
plant metabolite
furazolidone
[no description available]		2.4620
fluvoxamine
Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder.		5.8261(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
serotonin uptake inhibitor
ag-490
[no description available]		2.0310catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide		anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
bosutinib
4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source		3.1210aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
semaxinib
semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group.		2.4720olefinic compound;
oxindoles;
pyrroles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
orantinib
orantinib: an antiangiogenic agent. orantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.		2.0510
su 11248
[no description available]		4.4560monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
palbociclib
[no description available]		2.0810aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
jnj-7706621
[no description available]		2.0810sulfonamide
nifuroxazide
nifuroxazide: structure		2.1510benzoic acids
ergosterol-5,8-peroxide
ergosterol-5,8-peroxide: also inhibits sulfatase; isolated from fungus Cercospora kikuchii; structure given in first source. ergosterol peroxide : An ergostanoid that is ergosta-6,22-dien-3-ol with a peroxy group between positions 5 and 8 (the 3beta,5alpha,8alpha,22E stereoisomer). Isolated from Ganoderma lucidum and Cordyceps sinensis, it exhibits antimycobacterial, trypanocidal and antineoplastic activities.		3.31103beta-sterol;
ergostanoid;
organic peroxide;
phytosterols		antimycobacterial drug;
antineoplastic agent;
metabolite;
trypanocidal drug
guttiferone e
guttiferone E: isolated from the fruits of Garcinia pyrifera collected in Malaysia; structure in first source		3.3110
lead
Lead: A soft, grayish metal with poisonous salts; atomic number 82, atomic weight 207.2, symbol Pb.		7.0210carbon group element atom;
elemental lead;
metal atom		neurotoxin
sulindac sulfide
sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source. sulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.		8.1750aryl sulfide;
monocarboxylic acid;
organofluorine compound		antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug
11-hydroxy-5,8,12,14-eicosatetraenoic acid
11-hydroxy-5,8,12,14-eicosatetraenoic acid: RN given refers to cpd without isomeric designation		2.4420
12-hydroxy-5,8,10,14-eicosatetraenoic acid
12-Hydroxy-5,8,10,14-eicosatetraenoic Acid: A lipoxygenase metabolite of ARACHIDONIC ACID. It is a highly selective ligand used to label mu-opioid receptors in both membranes and tissue sections. The 12-S-HETE analog has been reported to augment tumor cell metastatic potential through activation of protein kinase C. (J Pharmacol Exp Ther 1995; 274(3):1545-51; J Natl Cancer Inst 1994; 86(15):1145-51)		2.4620
15-hydroxy-5,8,11,13-eicosatetraenoic acid
15-hydroxy-5,8,11,13-eicosatetraenoic acid: potent & selective inhibitor of platelet lipoxygenase; RN given refers to cpd without isomeric designation		2.5420
bay 11-7082
(E)-3-tosylacrylonitrile : A nitrile that is acrylonitrile in which the hydrogen located beta,trans to the cyano group is replaced by a tosyl group. It is an inhibitor of cytokine-induced IkappaB-alpha phosphorylation in cells.		3.2150nitrile;
sulfone		apoptosis inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor
bay 11-7085
BAY11-7085 : A sulfone that is benzene substituted by [(E)-2-cyanoethenyl]sulfonyl and tert-butyl groups at position 1 and 4, respectively. It is an irreversible inhibitor of IkappaB-alpha phosphorylation in cells (IC50 = 10 muM) and prevents the activation of NF-kappaB.		2.2510benzenes;
nitrile;
sulfone		anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
ferroptosis inducer;
NF-kappaB inhibitor
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.		4.4260dihydroxy monocarboxylic acid;
indoles;
organofluorine compound
molsidomine
[no description available]		2.4720ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid: A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)		3.3911
octylmethoxycinnamate
[no description available]		2.0510cinnamate ester
barium
Barium: An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.		2.0310alkaline earth metal atom;
elemental barium
lichexanthone
lichexanthone: a dihydropyranexanthone derived from the natural xanthone; structure in first source. lichexanthone : A member of the class of xanthones that is 9H-xanthen-9-one substituted by a hydroxy group at position 1, a methyl group at position 8 and methoxy groups at positions 3 and 6. It has been isolated from the bark of Cupania cinerea.		3.3110aromatic ether;
phenols;
xanthones		plant metabolite
levorphanol
Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.		3.2310morphinane alkaloid
arsenic
Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed)		7.520metalloid atom;
pnictogen		micronutrient
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		4.7690cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
dextromethorphan
Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.		8.191026-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
butorphanol
Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.		3.6120morphinane alkaloidantitussive;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
cefixime
[no description available]		3.8730cephalosporinantibacterial drug;
drug allergen
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		5.9371dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
benazepril
benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.		3.5920benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		9.2850azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
verteporfin
(2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid.		3.2310
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		4.5470dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
sulfur
Sulfur: An element that is a member of the chalcogen family. It has an atomic symbol S, atomic number 16, and atomic weight [32.059; 32.076]. It is found in the amino acids cysteine and methionine.		2.7220chalcogen;
nonmetal atom		macronutrient
glyceryl behenate
1-behenoylglycerol : A fatty acid ester resulting from the formal condensation of the hydroxy group at position-1 of glycerol with the carboxy group of docosanoic acid.		2.03101-monoglyceride;
fatty acid ester		antineoplastic agent;
plant metabolite
zimeldine
Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385)		3.2310styrenes
enalapril maleate
enalapril maleate : The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.		2.0810maleate saltantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		5.1680dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
vinblastine sulfate
[no description available]		2.0510
nitrofurazone
Nitrofurazone: A topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial WOUNDS AND INJURIES and skin infections. Nitrofurazone has also been administered orally in the treatment of TRYPANOSOMIASIS.. nitrofurazone : A semicarbazone resulting from the formal condensation of semicarbazide with 5-nitrofuraldehyde. A broad spectrum antibacterial drug, although with little activity against Pseudomonas species, it is used as a local application for burns, ulcers, wounds and skin infections.		2.4720
trientine hydrochloride
[no description available]		3.5920
n-methylscopolamine bromide
scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide.		3.2310
sinomenine
sinomenine: isolated from root of Sinomenium acutum; antirheumatic, antineuralgic		2.110morphinane alkaloid
ecdysterone
Ecdysterone: A steroid hormone that regulates the processes of MOLTING or ecdysis in insects. Ecdysterone is the 20-hydroxylated ECDYSONE.. 20-hydroxyecdysone : An ecdysteroid that is ecdysone substituted by a hydroxy group at position 20.		2.051014alpha-hydroxy steroid;
20-hydroxy steroid;
22-hydroxy steroid;
25-hydroxy steroid;
2beta-hydroxy steroid;
3beta-sterol;
ecdysteroid;
phytoecdysteroid		animal metabolite;
plant metabolite
deoxyribose
[no description available]		2.0310deoxypentosehuman metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
cisplatin
[no description available]		2.0810diamminedichloroplatinumantineoplastic agent;
apoptosis inducer;
cross-linking reagent;
ferroptosis inducer;
genotoxin;
mutagen;
nephrotoxin;
photosensitizing agent
fumarates
Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)		4.3822butenedioate;
C4-dicarboxylate		human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
bleomycin
[no description available]		3.5920bleomycinantineoplastic agent;
metabolite
cysteine
Cysteine: A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.. L-cysteinium : The L-enantiomer of cysteinium.. cysteine : A sulfur-containing amino acid that is propanoic acid with an amino group at position 2 and a sulfanyl group at position 3.		3.411cysteiniumfundamental metabolite
silicon
Silicon: A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086].		7.1110carbon group element atom;
metalloid atom;
nonmetal atom
dextromethorphan hydrobromide
dextromethorphan hydrobromide : The hydrobromide and monohydrate of the antitussive drug dextromethorphan.		2.0510hydrate;
hydrobromide
indinavir sulfate
[no description available]		2.0510azaheterocycle sulfate salt
enalaprilat anhydrous
Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.		3.8730dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ramiprilat
ramiprilat : A dipeptide that is the active metabolite of ramipril. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.		2.0210azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid;
dipeptide		bradykinin receptor B2 agonist;
cardioprotective agent;
drug metabolite;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor
imidapril
imidapril: structure given in first source. imidapril : A member of the class of imidazolidines that is (4S)-1-methyl-2-oxoimidazolidine-4-carboxylic acid in which the hydrogen of the imidazolidine nitrogen has been substituted by (1S)-1-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}ethyl group. It is the prodrug for imidaprilat, an ACE inhibitor used for the treatment of chronic heart failure.		2.0510dicarboxylic acid monoester;
dipeptide;
ethyl ester;
imidazolidines;
N-acylurea;
secondary amino compound		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
s-trans,trans-farnesylthiosalicylic acid
farnesylthiosalicylic acid: structure in first source		2.5320sesquiterpenoid
demethoxycurcumin
demethoxycurcumin: corresponds to curcumin with one methoxy group replaced by hydrogen; isolated from rhizomes of Curcuma longa. demethoxycurcumin : A beta-diketone that is curcumin in which one of the methoxy groups is replaced by hydrogen. It is found in Curcuma zedoaria and Etlingera elatior.		2.1310beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antineoplastic agent;
metabolite
zerumbone
zerumbone: RN given for (E,E,E)-isomer; structure in first source. zerumbone : A sesquiterpenoid and cyclic ketone that is (1E,4E,8E)-alpha-humulene which is substituted by an oxo group at the carbon atom attached to two double bonds. It is obtained by steam distillation from a type of edible ginger, Zingiber zerumbet Smith, grown particularly in southeast Asia.		2.110cyclic ketone;
sesquiterpenoid		anti-inflammatory agent;
glioma-associated oncogene inhibitor;
plant metabolite
sulindac sulfone
sulindac sulfone: inhibits K-ras-dependent cyclooxygenase-2; sulfated analog of indomethacin;; CP248 is an antineoplastic agent that fosters microtubule depolymerization; structure in first source. sulindac sulfone : A sulfone metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. It inhibits the development and induces regression of premalignant adenomatous polyps. Lipoxygenase and Cox-2 inhibitor.		4.6480monocarboxylic acid;
organofluorine compound;
sulfone		apoptosis inducer;
cyclooxygenase 2 inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
ximelagatran
ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.		3.8630amidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide		anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor
cefuroxime
[no description available]		3.23103-(carbamoyloxymethyl)cephalosporin;
furans;
oxime O-ether		drug allergen
ceftriaxone
[no description available]		3.59201,2,4-triazines;
1,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 3.5.2.6 (beta-lactamase) inhibitor
cefepime
Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.2310cephalosporin;
oxime O-ether		antibacterial drug
1,3,5,6-tetrahydroxyxanthone
1,3,5,6-tetrahydroxyxanthone: from roots of Cudrania cochinchinensis		3.3110
pafuramidine
pafuramidine: a prodrug of furamidine		3.2310
ceftazidime
[no description available]		3.5920cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
Norartocarpetin
[no description available]		3.3110flavones
24-ethyl-4-cholesten-3-one
stigmast-4-en-3-one: from the bark of Anacardium occidentale (cashew); structure in first source		3.3110C29-steroid;
steroid		metabolite
trandolapril
trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.		4.0940dicarboxylic acid monoester;
dipeptide;
ethyl ester;
organic heterobicyclic compound;
secondary amino compound;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
lofepramine hydrochloride
[no description available]		3.5110
pregabalin
Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.		13.823415gamma-amino acidanticonvulsant;
calcium channel blocker
alvimopan anhydrous
alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain		3.6120peptide
aliskiren
aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.		5.7932monocarboxylic acid amide;
monomethoxybenzene		antihypertensive agent
vx680
[no description available]		2.0810N-arylpiperazine
naltrindole
naltrindole: delta opioid receptor antagonist		2.0710isoquinolines
guanabenz acetate
[no description available]		2.0510dichlorobenzenegeroprotector
famotidine
[no description available]		4.26501,3-thiazoles;
guanidines;
sulfonamide		anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
fenoterol
fenoterol hydrobromide : The hydrobromide salt of fenoterol. A beta2-adrenergic agonist, it is used as a bronchodilator in the management of reversible airway obstruction.		2.0510hydrobromidebeta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
resiniferatoxin
resiniferatoxin: phorbol related diterpene ester; potent agonist of vanilloid TRPV1 receptors. resiniferatoxin : A heteropentacyclic compound found in Euphorbia poissonii with molecular formula C37H40O9. It is an agonist of the transient receptor potential cation channel subfamily V member 1 (TrpV1).		2.1510carboxylic ester;
diterpenoid;
enone;
monomethoxybenzene;
organic heteropentacyclic compound;
ortho ester;
phenols;
tertiary alpha-hydroxy ketone		analgesic;
neurotoxin;
plant metabolite;
TRPV1 agonist
carbocyanines
Carbocyanines: Compounds that contain three methine groups. They are frequently used as cationic dyes used for differential staining of biological materials.		2.1710cyanine dye;
organic iodide salt		fluorochrome
lyoniside
daucosterol : A steroid saponin that is sitosterol attached to a beta-D-glucopyranosyl residue at position 3 via a glycosidic linkage. It has bee isolated from Panax japonicus var. major and Breynia fruticosa.		3.3110beta-D-glucoside;
monosaccharide derivative;
steroid saponin		plant metabolite
cefotaxime
Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.		3.59201,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen
aztreonam
[no description available]		3.8630beta-lactam antibiotic allergen;
monobactam		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
3,4-dihydroxy-xanthone
3,4-dihydroxy-xanthone: structure given in first source		2.0210
proguanil
Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells.		2.0510biguanides;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
am-356
methanandamide: structure given in first source; RN given refers to (all-Z)-(+-)-isomer		2.0310fatty amide
cci 15641
[no description available]		2.0810cephalosporin
22,23-dihydroavermectin b(1)a
22,23-dihydroavermectin B(1)a: C48H74O14; major component of IVERMECTIN; MW 875.093; structure given in first source. 22,23-dihydroavermectin B1a : A macrocyclic lactone that is avermectin B1a in which the double bond present in the spirocyclic ring system has been reduced to a single bond. It is the major component of ivermectin.		3.3510macrocyclic lactone;
spiroketal
rifamycin sv
rifamycin SV: RN given refers to parent cpd; structure in Merck Index, 9th ed, #8009. rifamycin SV : A member of the class of rifamycins that exhibits antibiotic and antitubercular properties.		2.4720acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterotetracyclic compound;
polyphenol;
rifamycins		antimicrobial agent;
antitubercular agent;
bacterial metabolite
ginkgolide b
[no description available]		2.0510
tetrodotoxin
Tetrodotoxin: An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.. tetrodotoxin : A quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.		2.0310azatetracycloalkane;
oxatetracycloalkane;
quinazoline alkaloid		animal metabolite;
bacterial metabolite;
marine metabolite;
neurotoxin;
voltage-gated sodium channel blocker
selenium
Selenium: An element with the atomic symbol Se, atomic number 34, and atomic weight 78.97. It is an essential micronutrient for mammals and other animals but is toxic in large amounts. Selenium protects intracellular structures against oxidative damage. It is an essential component of GLUTATHIONE PEROXIDASE.		6.9874chalcogen;
nonmetal atom		micronutrient
benzeneselenol
benzeneselenol: RN given refers to parent cpd		3.4110
radium
Radium: A radioactive element of the alkaline earth series of metals. It has the atomic symbol Ra and atomic number 88. Radium is the product of the disintegration of URANIUM and is present in pitchblende and all ores containing uranium. It is used clinically as a source of beta and gamma-rays in radiotherapy, particularly BRACHYTHERAPY.		3.4311alkaline earth metal atom
cefpodoxime
[no description available]		3.2310carboxylic acid;
cephalosporin		antibacterial drug
palonosetron
Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.		3.2310azabicycloalkane;
delta-lactam;
organic heterotricyclic compound		antiemetic;
serotonergic antagonist
(3S,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
Fluvastatin: An indole-heptanoic acid derivative that inhibits HMG COA REDUCTASE and is used to treat HYPERCHOLESTEROLEMIA. In contrast to other statins, it does not appear to interact with other drugs that inhibit CYP3A4.. (3S,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid diastereoisomer in which both chiral centres have S configuration.. fluvastatin : A racemate comprising equimolar amounts of (3R,5S)- and (3S,5R)-fluvastatin. An HMG-CoA reductase inhibitor, it is used (often as the corresponding sodium salt) to reduce triglycerides and LDL-cholesterol, and increase HDL-chloesterol, in the treatment of hyperlipidaemia.		4.0540(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
epoprostenol sodium
[no description available]		2.0510prostanoid
tenofovir disoproxil fumarate
tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.		2.0810fumarate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
d 4476
[no description available]		2.0810imidazoles
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.4520maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
cyc 116
4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine: an aurora kinase inhibitor; structure in first source		2.0810
diphenoxylate hydrochloride
diphenoxylate hydrochloride : The hydrochloride salt of diphenoxylate.		2.0510hydrochlorideantidiarrhoeal drug
bay 19-8004
BAY 19-8004: a PDE4 inhibitor; structure in first source		2.0810
dexbrompheniramine maleate
dexbrompheniramine maleate : The maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810brompheniramine maleateanti-allergic agent;
H1-receptor antagonist
6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid
6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid: combined thromboxane A2 receptor & thromboxane synthesis inhibitor; structure given in first source; RN given refers to (E)-isomer		3.1210
rifaximin
[no description available]		3.6120acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterohexacyclic compound;
rifamycins;
semisynthetic derivative		antimicrobial agent;
gastrointestinal drug;
orphan drug
bafilomycin a1
bafilomycin A1: from Streptomyces griseus; structure given in first source. bafilomycin A1 : The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.		2.0810cyclic hemiketal;
macrolide antibiotic;
oxanes		apoptosis inducer;
autophagy inhibitor;
bacterial metabolite;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor;
ferroptosis inhibitor;
fungicide;
potassium ionophore;
toxin
ergonovine maleate
ergometrine maleate : A maleate salt resulting form the reaction of equimolar amounts of maleic acid and ergometrine. It is used in the active management of the third stage of labour, and to prevent or treat postpartum of postabortal haemorrhage caused by uterine atony: by maintaining uterine contraction and tone, blood vessels in the uterine wall are compressed and blood flow reduced.		2.0510maleate saltdiagnostic agent;
oxytocic
involucrin
involucrin: soluble precursor protein of cross-linked envelope characteristic of epidermal s. corneum synthesized by keratinocytes in natural & cultured human epithelia; see also related records for prekeratin & stratum corneum basic protein precursor		2.0210
plastochromanol 8
plastochromanol 8: has antiproliferative activity against 3T3-L1 cells and anti-adipogenic activity; structure; plastochromanol 3 is gamma-tocotrienol		2.4620
bwa 4c
[no description available]		2.4620
goniothalamin
goniothalamin: has antineoplastic activity; structure given in first source		2.8430
acuminatin
acuminatin: from Epimedium acuminatum; Chemline give RN 41744-39-2 for acuminatin, but the compound has a different structure than the one given in journal. acuminatin : A neolignan that is 5-[(1E)-prop-1-en-1-yl]-2,3-dihydro-1-benzofuran carrying additional 3,4-dimethoxyphenyl, methyl and methoxy substituents at positions 2, 3 and 7 respectively.		2.05101-benzofurans;
dimethoxybenzene;
neolignan;
olefinic compound;
ring assembly		fungal metabolite;
plant metabolite
licarin b
licarin B: neolignan; RN given for (2S-(2alpha,3beta,5(E)))-isomer; isolated from seeds of Myristica fragrans; structure in first source		2.0510
everolimus
[no description available]		3.6120cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
elaiophylin
[no description available]		3.5110lactol;
macrodiolide;
monosaccharide derivative		antifungal agent;
autophagy inhibitor;
bacterial metabolite
ixabepilone
[no description available]		3.59201,3-thiazoles;
beta-hydroxy ketone;
epoxide;
lactam;
macrocycle		antineoplastic agent;
microtubule-destabilising agent
13-oxo-9,11-octadecadienoic acid
13-oxo-9Z,11E-ODE : An oxooctadecadienoic acid that consists of 9Z,11E-octadecadienoic acid bearing an additional 13-keto substituent. In addtion it has been found as a natural product found in Carthamus oxyacantha.		3.311013-oxo-9,11-octadecadienoic acidmetabolite;
mouse metabolite
azalomycin-f
azalomycin-F: a macrocyclic lactone antibiotic		3.5110
axitinib
[no description available]		2.0810aryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
pai 039
tiplaxtinin: inhibitor of plasminogen activator inhibitor-1		2.0810indole-3-acetic acids
salvianolic acid B
salvianolic acid B: isolated from Salvia miltiorrhiza. salvianolic acid B : A member of the class of 1-benzofurans that is an antioxidant and free radical scavenging compound extracted from S. miltiorrhiza		7.05101-benzofurans;
catechols;
dicarboxylic acid;
enoate ester;
polyphenol		anti-inflammatory agent;
antidepressant;
antineoplastic agent;
antioxidant;
apoptosis inducer;
autophagy inhibitor;
cardioprotective agent;
hepatoprotective agent;
hypoglycemic agent;
neuroprotective agent;
osteogenesis regulator;
plant metabolite
azlocillin
Azlocillin: A semisynthetic ampicillin-derived acylureido penicillin.. azlocillin : A semisynthetic penicillin having a 6beta-{(2R)-2-[(2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl}amino side-group. It is an antibiotic used in treating infections caused by Pseudomonas aeruginosa, Escherichia coli and Haemophilus influenzae.		2.0510penicillin allergen;
penicillin;
semisynthetic derivative		antibacterial drug
tanespimycin
CP 127374: analog of herbimycin A		2.98401,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor
verlukast
verlukast: LTD4 receptor antagonist		2.0710
gw 1929
GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first source		2.0310benzophenones
cefpodoxime proxetil
cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.		2.0810carboxylic acid;
carboxylic ester;
cephalosporin		antibacterial drug;
prodrug
ceftizoxime
[no description available]		4.120cephalosporinantibacterial drug
2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole
[no description available]		2.0310aryl sulfide
1-methyl-d-lysergic acid butanolamide
[no description available]		3.2310ergot alkaloid;
monocarboxylic acid amide		serotonergic antagonist;
sympatholytic agent;
vasoconstrictor agent
fluphenazine
[no description available]		2.0810
gw2974
GW2974: quinazoline derivative, which is able to block the activation of both the EGFR and erbB2		2.0810pyridopyrimidine
dantrolene sodium
dantrolene sodium (anhydrous) : The anhydrous sodium salt of dantrolene.		2.4620
nitrofurantoin
Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA.		4.5570imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
tubacin
tubacin: inhibits histone deacetylase 6; structure in first source		2.15101,3-oxazoles
nifurtimox
Nifurtimox: A nitrofuran thiazine that has been used against TRYPANOSOMIASIS.		2.0510nitrofuran antibiotic
ispinesib
[no description available]		2.0810benzamides
6-hydroxybenzothiazide-2-sulfonamide
6-hydroxybenzothiazide-2-sulfonamide: structure given in first source		3.5780
morphinans
Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.		2.110isoquinoline alkaloid fundamental parent;
morphinane alkaloid
dantrolene
[no description available]		3.2310
roxithromycin
(E)-roxithromycin : A major geometrical isomer of roxithromycin.		2.4720roxithromycinenvironmental contaminant;
xenobiotic
cefdinir
[no description available]		3.6120cephalosporin;
ketoxime		antibacterial drug
etonogestrel
[no description available]		3.231017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin
bisoprolol, fumarate (1:1) salt
[no description available]		2.0810
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		2.0810artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
ci 940
leptomycin : A complex, very long chain, polyunsaturated fatty acid whose core structure comprises 8-oxononadeca-2,10,12,16,18-pentaenoic acid having methyl substituents at positions 3, 5, 7, 9, 11 and 15 and a 3,6-dihydropyran-6-one-2-yl group at position 19.		2.0310hydroxy polyunsaturated fatty acid;
leptomycin		antifungal agent;
bacterial metabolite
beraprost
beraprost: stable prostacyclin analog; structure given in first source. beraprost : An organic heterotricyclic compound that is (3aS,8bS)-2,3,3a,8b-tetrahydro-1H-benzo[b]cyclopenta[d]furan in which the hydrogens at positions 1R, 2R and 5 are replaced by (3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl, hydroxy and 3-carboxypropyl groups, respectively. It is a prostaglandin receptor agonist which is approved to treat pulmonary arterial hypertension in Asia.		2.0510enyne;
monocarboxylic acid;
organic heterotricyclic compound;
secondary alcohol;
secondary allylic alcohol		anti-inflammatory agent;
antihypertensive agent;
platelet aggregation inhibitor;
prostaglandin receptor agonist;
vasodilator agent
lanreotide
[no description available]		2.0510
etoposide phosphate
[no description available]		2.0810furonaphthodioxole
ciclesonide
ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis		2.0810organic molecular entity
temsirolimus
[no description available]		3.8930macrolide lactam
dutasteride
Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.		3.6120(trifluoromethyl)benzenes;
aza-steroid;
delta-lactam		antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
tekturna
[no description available]		2.0810fumarate saltantihypertensive agent
pd 184352
2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source		2.0810aminobenzoic acid
lu 208075
ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension		3.5920diarylmethane
bibx 1382bs
BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001		3.6120substituted aniline
vildagliptin
[no description available]		2.0810amino acid amide
indacaterol
indacaterol: a beta2 adrenoceptor agonist; indacaterol is the (R)-isomer; structure in first source. indacaterol : A monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary disease.		2.0810indanes;
monohydroxyquinoline;
quinolone;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
fesoterodine
fesoterodine: a muscarinic antagonist for treatment of overactive bladder		3.2310diarylmethane
hdac-42
HDAC-42: structure in first source		2.0810amidobenzoic acid
bromopyruvate
[no description available]		2.03102-oxo monocarboxylic acid anion
acetylcarnitine
O-acetyl-L-carnitine : An O-acyl-L-carnitine where the acyl group specified is acetyl. It facilitates movement of acetyl-CoA into the matrices of mammalian mitochondria during the oxidation of fatty acids.		2.0510O-acetylcarnitine;
saturated fatty acyl-L-carnitine		human metabolite;
Saccharomyces cerevisiae metabolite
staurosporine
staurosporinium : Conjugate acid of staurosporine.		7.4620ammonium ion derivative
taxane
taxane: produced by Taxomyces andreanae		8.8321diterpene;
terpenoid fundamental parent
[4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone
[no description available]		2.0810benzamides;
N-acylpiperidine
sgd 301-76
[no description available]		2.0810conazole antifungal drug;
imidazole antifungal drug;
organic nitrate salt		antiinfective agent
fluvoxamine maleate
[no description available]		2.0810(trifluoromethyl)benzenes
formazans
Formazans: Colored azo compounds formed by the reduction of tetrazolium salts. Employing this reaction, oxidoreductase activity can be determined quantitatively in tissue sections by allowing the enzymes to act on their specific substrates in the presence of tetrazolium salts.		2.0210
thioacetazone
Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives.		2.0810
s 1743
Esomeprazole: The S-isomer of omeprazole.. esomeprazole : A 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole that has S configuration at the sulfur atom. An inhibitor of gastric acid secretion, it is used (generally as its sodium or magnesium salt) for the treatment of gastro-oesophageal reflux disease, dyspepsia, peptic ulcer disease, and Zollinger-Ellison syndrome.		8.9588magnesium saltanti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
nifurtoinol
nifurtoinol : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group and at position 3 by a hydroxymethyl group.		2.0510hydrazone;
imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
gemifloxacin
Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position.		3.23101,8-naphthyridine derivative;
fluoroquinolone antibiotic;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
topoisomerase IV inhibitor
dexlansoprazole
Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE.		3.6120benzimidazoles;
sulfoxide
gemifloxacin mesylate
gemifloxacin mesylate : The mesylate salt of gemifloxacin.		2.0810methanesulfonate saltantimicrobial agent;
topoisomerase IV inhibitor
fosinopril
[no description available]		4.3730
armodafinil
armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.		3.23102-[(diphenylmethyl)sulfinyl]acetamidecentral nervous system stimulant;
eugeroic
clasto-lactacystin beta-lactone
clasto-lactacystin beta-lactone: active metabolite of lactacystin; inhibits 20 S proteasome; structure in first source		3.5110
iniparib
[no description available]		2.0810carbonyl compound;
organohalogen compound
mk 0752
[no description available]		2.0810
gw 501516
GW 501516: a selective PPARdelta agonist; structure in first source. GW 501516 : An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.		2.08101,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound		carcinogenic agent;
PPARbeta/delta agonist
eflucimibe
eflucimibe: a powerful and systemic acylcoenzyme A: cholesterol acyltransferase inhibitor		2.0510
av 412
[no description available]		2.0810
ag-041r
AG-041R: structure in first source		2.0810
telatinib
[no description available]		2.0810
bimosiamose
bimosiamose: a selectin inhibitor		2.0310
cp 547632
3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide: inhibits vascular endothelial growth factor receptor-2 tyrosine kinase; structure in first source		2.0810
cajanine
cajanine: isolated from Cajanus cajan L.; structure in first source		3.3110stilbenoid
apricoxib
apricoxib: a COX-2 inhibitor; structure in first source		4.1231
spc-839
SPC-839: an inhibitor of activator protein 1; structure in first source		2.0810
cj 13610
CJ 13610: structure in first source		2.0510
lenvatinib
lenvatinib : A member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to radioiodine.		2.0810aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist
ono 8711
ONO 8711: a prostaglandin E receptor EP1 antagonist; structure in first source		2.0510
andarine
[no description available]		2.0810acetamides;
anilide
gw843682x
[no description available]		2.0810(trifluoromethyl)benzenes
pd 0325901
mirdametinib: has antineoplastic activity; appears to be a MEK inhibitor. PD 0325901 : A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position 2 by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer).		2.0810difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound		antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
midostaurin
midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine.		2.0810benzamides;
gamma-lactam;
indolocarbazole;
organic heterooctacyclic compound		antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor
gw406381x
GW406381X: cyclooxygenase-2 inhibitor		4.3830
sincalide
Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.		4.3830oligopeptide
tapentadol
Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.		3.2310alkylbenzene
(5z)-4-bromo-5-(bromomethylene)-3-butyl-2(5h)-furanone
4-bromo-5Z-(bromomethylene)-3-butylfuran-2-one: structure in first source		3.3110
ag 14361
[no description available]		2.0810benzimidazoles
etomoxir
[no description available]		2.0510aromatic ether
tqx 173
[no description available]		3.5110
sb 265610
[no description available]		2.0810
cg100649
CG100649: a cyclooxygenase-2 inhibitor with both anti-inflammatory and antineoplastic activities; structure in first source		11.9642
4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide
4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide: a long-acting COX-2 inhibitor; structure in first source. mavacoxib : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-sulfamoylphenyl, trifluoromethyl and 4-fluorophenyl groups, respectively. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine to treat pain and inflammation in dogs with degenerative joint disease.		4.3570organofluorine compound;
pyrazoles;
sulfonamide		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
11-keto-boswellic acid
[no description available]		2.110
ursodoxicoltaurine
tauroursodeoxycholate : An organosulfonate oxoanion that is the conjugate base of tauroursodeoxycholic acid arising from deprotonation of the sulfonate OH group; major species at pH 7.3.. tauroursodeoxycholic acid : A bile acid taurine conjugate derived from ursoodeoxycholic acid.		2.0710bile acid taurine conjugateanti-inflammatory agent;
apoptosis inhibitor;
bone density conservation agent;
cardioprotective agent;
human metabolite;
neuroprotective agent
gambogic acid
gambogic acid: RN given refers to (1R-(1alpha,1(Z),3abeta,5alpha,11beta,14aS*))-isomer		2.0410pyranoxanthonesmetabolite
upamostat
[no description available]		2.5220
efipladib
efipladib: structure in first source		2.4520
pentagastrin
Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.		3.8530organic molecular entity
sc-75416
SC-75416: a benzopyran (chromene) COX-2 inhibitor		2.110
fr 148083
5Z-7-oxozeaenol : A macrolide that is the 7-oxo derivative of zeaenol (the 5Z stereoisomer). Isolated from Fungi, it exhibits cytotoxic, antibacterial and inhibitory activity against NF-kappaB.		2.0810aromatic ether;
macrolide;
phenols;
secondary alcohol;
secondary alpha-hydroxy ketone		antibacterial agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		5.72191aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
sc 236
4-(5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide: SC58236 = SC236 re email from Harris, Ray 		4.88130
osi 930
OSI 930: inhibits both receptor tyrosine kinase Kit and kinase insert domain receptor; structure in first source		2.0810aromatic amide
ki 20227
[no description available]		2.0810
cefditoren
cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections.		3.2310carboxylic acid;
cephalosporin		antibacterial drug
scio-469
SCIO-469: a small-molecule p38 mitogen-activated protein (MAP) kinase inhibitor for potential oral therapy for inflammatory disorders; in phase lib clinical trials for rheumatoid arthritis 4/2004. talmapimod : An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties.		2.0810aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
ticagrelor
Ticagrelor: An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION.. ticagrelor : A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.		2.0810aryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines		P2Y12 receptor antagonist;
platelet aggregation inhibitor
ssr 69071
SSR 69071: structure in first source		2.0810pyridopyrimidine
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		2.0810aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
4-methylene-2-octyl-5-oxofuran-3-carboxylic acid
4-methylene-2-octyl-5-oxofuran-3-carboxylic acid: an anorectic fatty acid synthase inhibitor; structure in first source. (2R,3S)-C75 : A 4-methylidene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acid that has 2R,3S-configuration.		2.13104-methylidene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acid;
gamma-lactone
dehydroxymethylepoxyquinomicin
dehydroxymethylepoxyquinomicin: an NF-kappaB inhibitor; structure in first source		2.0710
molindone hydrochloride
[no description available]		2.0510indoles
way 133537
[no description available]		2.0610
naproxen-n-butyl nitrate
naproxen-n-butyl nitrate: a nitric oxide-releasing NSAID derivative. naproxcinod : A carboxylic ester obtained by formal condensation of the carboxy group of naproxen with the hydroxy group of 4-(nitrooxy)butanol. A cyclooxygenase-inhibiting nitric oxide donator that is metabolised to naproxen and a nitric oxide donating moiety, effective in treatment of osteoarthritis.		2.7230carboxylic ester;
methoxynaphthalene;
nitrate ester		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
nitric oxide donor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
pi103
PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce		2.0810aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
sb 210313
[no description available]		2.0810
dapagliflozin
[no description available]		2.4110aromatic ether;
C-glycosyl compound;
monochlorobenzenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
gw 4064
[no description available]		2.0810stilbenoid
dpc 423
[no description available]		2.0610
bms 248360
[no description available]		3.1210
gentamicin sulfate
[no description available]		2.0510
sa 4503
[no description available]		2.0810
ic 87114
IC 87114: structure in first source		2.08106-aminopurines;
biaryl;
quinazolines		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
zibotentan
ZD4054: a potent endothelin receptor A antagonist that inhibits ovarian carcinoma cell proliferation		2.0810phenylpyridine
tivozanib
N-(2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-N'-(5-methyl-3-isoxazolyl)urea: KNR-951 is the HCl, monohydrate salt; an antineoplastic agent; structure in first source		2.0810aromatic ether
l-873724
L-873724: a selective inhibitor of cathepsin K; structure in first source		2.0410
hki 272
[no description available]		2.4920nitrile;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
dolastatin 15
dolastatin 15: from Dolabella auricularia; seven subunit depsipeptide		2.7730
motexafin gadolinium
[no description available]		2.0310
sorbitan monooleate
[no description available]		2.1110fatty acid ester
fk 881
3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole: structure in first source		2.3110
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		2.4920N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
bibr 1532
[no description available]		2.0810
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide
[no description available]		2.0810
pifithrin-alpha
[no description available]		2.0310
rucaparib
AG14447: Poly(ADP-ribose) polymerase inhibitor; structure in first source		2.0810azepinoindole;
caprolactams;
organofluorine compound;
secondary amino compound		antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
cediranib
[no description available]		2.0810aromatic ether
gw0742
GW 610742: structure in first source		2.0810monocarboxylic acid
ono 8713
ONO 8713: EP1 receptors antagonist; structure in first source		2.0310
pasireotide
pasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease.		2.0610homodetic cyclic peptide;
peptide hormone		antineoplastic agent
bpc 157
BPC 157: amino acid sequence given in first source; a 15-amino acid fragment of a gastric peptide, BPC, with hepatoprotective effects		7.5520
ps1145
PS1145: IkappaB kinase inhibitor; structure in first source		2.0810beta-carbolines
cp 31398
CP 31398: structure in first source		2.0510
bay 41-8543
BAY 41-8543: structure in first source		2.0810pyrazolopyridine
chir 99021
Chir 99021: structure in first source. CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively.		2.0810aminopyridine;
aminopyrimidine;
cyanopyridine;
diamine;
dichlorobenzene;
imidazoles;
secondary amino compound		EC 2.7.11.26 (tau-protein kinase) inhibitor
l-161982
L-161982: A prostanoid EP4 receptor antagonist		2.1510biphenyls
vortioxetine
Vortioxetine: A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression.. vortioxetine : An N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.		6.6553aryl sulfide;
N-arylpiperazine		antidepressant;
anxiolytic drug;
serotonergic agonist;
serotonergic antagonist
sb 525334
6-(2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline: a TGF-betaR kinase inhibitor		2.0810quinoxaline derivative
way-362450
[no description available]		2.0810indoles
osu 03012
OSU 03012: a PDK-1 inhibitor; structure in first source		5.56120antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
masitinib
[no description available]		2.08101,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines		antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor
bx795
BX795: structure in first source		2.0810ureas
snap 6201
[no description available]		2.0610
2,4,2',4'-Tetrahydroxychalcone
[no description available]		3.3110chalcones
pazopanib
pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.		4.1340aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
sepantronium
sepantronium: a survivin suppressant with antineoplastic activity. sepantronium : An organic cation that is 1-(2-methoxyethyl)-2-methyl-1H-naphtho[2,3-d]imidazole-4,9-dione in which the nitrogen at position 3 of the napthoimidazole moiety has been alkylated by a pyrazin-2-ylmethyl group.		2.0810organic cation
azd 6244
AZD 6244: a MEK inhibitor		2.7730benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
furanone c-30
furanone C-30: structure in first source		3.3110
am 1241
AM 1241: a CB(2) receptor-selective agonist; no further information available 11/2001		2.1110
prasugrel hydrochloride
Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels.		3.2310
1-(2-(1-adamantyl)ethyl)-1-pentyl-3-(3-(4-pyridyl)propyl)urea
1-(2-(1-adamantyl)ethyl)-1-pentyl-3-(3-(4-pyridyl)propyl)urea: structure in first source		2.0810
heptakis(2,6-o-dimethyl)beta-cyclodextrin
heptakis(2,6-O-dimethyl)beta-cyclodextrin: stimulant for Bordetella pertussis Phase I		2.4320
apixaban
[no description available]		2.0810aromatic ether;
lactam;
piperidones;
pyrazolopyridine		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
bibw 2992
[no description available]		2.3110aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide
N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide : A member of the class of biphenyls that is the amide obtained by formal condensation of the carboxy group of 2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)[1,1'-biphenyl]-4-carboxylic acid with the amino group of 3-cyanoaniline.		2.08101,3,4-oxadiazoles;
benzamides;
biphenyls;
nitrile		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
jte 013
JTE 013: an Edg-5 antagonist. JTE-013 : A semicarbazide derivative that is semicarbazide in which the amino group at position 2 is replaced by a [1,3-dimethyl-4-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-6-yl]amino group and the amino group adjacent to the carbonyl is replaced by a (2,6-dichloropyridin-4-yl)amino group. It is a potent S1P2 antagonist (IC50 = 17.6 nM).		3.4110chloropyridine;
pyrazolopyridine		anti-asthmatic agent;
anti-inflammatory agent;
antineoplastic agent;
osteogenesis regulator;
pro-angiogenic agent;
sphingosine-1-phosphate receptor 2 antagonist
ar c155858
AR C155858: an MCT1 inhibitor; structure in first source		2.0810
sb-649915
SB-649915: potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor		3.1210
aee 788
AEE 788: structure in first source		2.99406-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineangiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist;
trypanocidal drug
saracatinib
[no description available]		2.0810aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent
sd-208
[no description available]		2.0810
ko 143
[no description available]		2.4620beta-carbolines;
tert-butyl ester
vx 702
VX 702: a p38 MAP kinase inhibitor		2.0810phenylpyridine
angiotensin amide
Angiotensin Amide: The octapeptide amide of bovine angiotensin II used to increase blood pressure by vasoconstriction.		210oligopeptide
3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole
3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole: inhibits cyclooxygenase-1; structure in first source		2.110
cay 10404
3-(4-methylsulfonylphenyl)-4-phenyl-5-trifluoromethylisoxazole: a cyclooxygenase-2 (Cox-2) inhibitor		210sulfonic acid derivative
volasertib
BI 6727: a polo-like kinase inhibitor with broad antitumor activity; structure in first source		2.0810
PB28
PB28 : A member of the class of tetralins that is tetralin that is substituted by 3-(4-cyclohexylpiperazin-1-yl)propyl and methoxy groups at positions 1 and 5, respectively. It is a sigma 2 (sigma2) receptor agonist (Ki = 0.68 nM) and exhibits antineoplastic and anti SARS-CoV-2 activities.		2.0810aromatic ether;
piperazines;
tetralins		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist
amg 009
AMG 009: an anti-inflammatory agent; structure in first source		2.0810
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		3.3660
vinflunine
vinflunine: inhibits tubulin assembly; structure in first source. vinflunine : An organic heteropentacyclic compound and an organic heterotetracyclic compound that is vinorelbine in which the tetrahydropyridine moiety of the heterotetracyclic part of the molecule has been redced to the corresponding piperidine, and in which the ethyl group attached to this ring has been replaced by a 1,1-difluoroethyl group.		2.0510acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
semisynthetic derivative;
vinca alkaloid		antineoplastic agent
cefotaxime sodium
[no description available]		2.0810organic sodium salt
baci-im
[no description available]		3.8630homodetic cyclic peptide;
polypeptide;
zwitterion		antibacterial agent;
antimicrobial agent
ribose
ribopyranose : The pyranose form of ribose.		2.4110D-ribose;
ribopyranose
acebutolol
alpha-D-glucosyl-(1->4)-alpha-D-mannose : An alpha-D-glucosyl-(1->4)-D-mannopyranose in which the anomeric hydroxy group has alpha configuration.		2.0710alpha-D-glucosyl-(1->4)-D-mannopyranose
lactulose
Lactulose: A synthetic disaccharide used in the treatment of constipation and hepatic encephalopathy. It has also been used in the diagnosis of gastrointestinal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p887). lactulose : A synthetic galactosylfructose disaccharide used in the treatment of constipation and hepatic encephalopathy.		210
azd 7762
[no description available]		2.0810aromatic amide;
thiophenes
krp-203
[no description available]		2.0810
mk 0354
[no description available]		2.0810
regorafenib
[no description available]		2.0810(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide		antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor
acetyl-11-ketoboswellic acid
acetyl-11-ketoboswellic acid: a 5-lipoxygenase inhibitor; structure given in first source		2.5220triterpenoid
acetic acid 2-[4-methyl-8-(4-morpholinylsulfonyl)-1,3-dioxo-2-pyrrolo[3,4-c]quinolinyl]ethyl ester
[no description available]		2.0810pyrroloquinoline
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
[no description available]		2.0810methoxybenzenes;
substituted aniline
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide
N-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide: MK-0364 is the (1S,2S)-isomer; a cannabinoid-1 receptor inverse agonist; structure in first source		2.4620stilbenoid
abt-737
[no description available]		2.7830aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound		anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
brivanib
[no description available]		2.0810aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist
icg 001
[no description available]		2.0810peptide
bms 477118
[no description available]		3.2310adamantanes;
azabicycloalkane;
monocarboxylic acid amide;
nitrile;
tertiary alcohol		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
mp470
[no description available]		2.0810N-arylpiperazine
nystatin a1
Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.		4.7850nystatins
mk 2866
[no description available]		3.5111
nu 7441
8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one: structure in first source		2.0810dibenzothiophenes
at 7519
4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide : A member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine.		2.0810dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
marizomib
marizomib: a proteasome inhibitor from a marine bacterium Salinospora; structure in first source		3.5110beta-lactone;
gamma-lactam;
organic heterobicyclic compound;
organochlorine compound;
salinosporamide		antineoplastic agent;
proteasome inhibitor
bi 2536
[no description available]		2.0810
3-o-acetyl-beta-boswellic acid
3-O-acetyl-beta-boswellic acid: isolated from Boswellia serrata; structure in first source		2.110
a 784168
1-(3-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethylsulfonyl)phenyl)-1,2,3,6-tetrahydropyridine-4-carboxamide: a TRPV1 antagonist		2.0810
danusertib
[no description available]		2.0810piperazines
N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide
[no description available]		2.0810benzamides
N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide
[no description available]		2.0810benzamides
abt 869
[no description available]		2.0810aromatic amine;
indazoles;
phenylureas		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
pyrazolone
pyrazolone: non-steroid antirheumatic agent. pyrazolone : A member of the class of pyrazoles in which one of the carbons of the pyrazole ring is substituted by an oxo group.		2.2510
mw-151
2-(4-(4-methyl-6-phenylpyridazin-3-yl)piperazin-1-yl)pyrimidine: attenuates proinflammatory cytokine production		2.4110
dorsomorphin
dorsomorphin: an AMPK inhibitor. dorsomorphin : A pyrazolopyrimidine that is pyrazolo[1,5-a]pyrimidine which is substituted at positions 3 and 6 by pyridin-4-yl and p-[2-(piperidin-1-yl)ethoxy]phenyl groups, respectively. It is a potent, selective, reversible, and ATP-competitive inhibitor of AMPK (AMP-activated protein kinase, EC 2.7.11.31) and a selective inhibitor of bone morphogenetic protein (BMP) signaling.		2.0810aromatic ether;
piperidines;
pyrazolopyrimidine;
pyridines		bone morphogenetic protein receptor antagonist;
EC 2.7.11.31 {[hydroxymethylglutaryl-CoA reductase (NADPH)] kinase} inhibitor
ac 261066
[no description available]		2.0810
boeravinone e
boeravinone E: from Boerhaavia diffusa L; structure in first source		2.0810
quisinostat
[no description available]		2.1310indoles
2,5-dimethylcelecoxib
2,5-dimethylcelecoxib: non-COX-2 inhibitory structural analog of celecoxib		5.94180
carfilzomib
[no description available]		2.0810epoxide;
morpholines;
tetrapeptide		antineoplastic agent;
proteasome inhibitor
apremilast
[no description available]		2.0810aromatic ether;
N-acetylarylamine;
phthalimides;
sulfone		non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor
cytidine diphosphate choline
[no description available]		2.0510nucleotide-(amino alcohol)s;
phosphocholines		human metabolite;
mouse metabolite;
neuroprotective agent;
psychotropic drug;
Saccharomyces cerevisiae metabolite
sitagliptin phosphate
Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.		2.4110
gw9508
GW9508: structure in first source		2.0810aromatic amine
jnj 26854165
[no description available]		2.0810
pf 573228
6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one: structure in first source		2.0810quinolines
gw 2580
5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine: a cFMS kinase inhibitor; structure in first source		3.6520
milnacipran
[no description available]		4.0720acetamides
idelalisib
idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source. idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia.		2.520aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
crizotinib
Crizotinib: A piperidine and aminopyridine derivative that acts as an inhibitor of RECEPTOR PROTEIN-TYROSINE KINASES, including ANAPLASTIC LYMPHOMA KINASE (ALK) and HEPATOCYTE GROWTH FACTOR RECEPTOR (HGFR; c-Met). It is used in the treatment of NON-SMALL CELL LUNG CANCER.. crizotinib : A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC)		2.08103-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amineantineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
5-(5,6-dimethoxy-1-benzimidazolyl)-3-[(2-methylsulfonylphenyl)methoxy]-2-thiophenecarbonitrile
[no description available]		2.0810benzimidazoles
4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Vx-11e: ERK1-2 inhibitor		2.0810aromatic amide;
heteroarene
osi 906
[no description available]		2.0810cyclobutanes;
quinolines
vindesine
[no description available]		2.0510
ly2109761
[no description available]		2.0810
chir-265
[no description available]		2.0810aromatic ether
motesanib
[no description available]		2.0810pyridinecarboxamide
az-628
AZ-628: a multikinase inhibitor; structure in first source		2.0810benzamides
imrecoxib
Imrecoxib: structure in first source		5.7863
trametinib
[no description available]		2.4920acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pf-562,271
[no description available]		2.0810indoles
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		2.7630
calcimycin
Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.		2.7130benzoxazole
veliparib
[no description available]		2.0810benzimidazolesEC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
ku-0060648
[no description available]		2.0810dibenzothiophenes
scopolamine hydrobromide
[no description available]		3.8630
dactolisib
dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.		2.4920imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
palomid 529
[no description available]		2.0810
pf 03491390
[no description available]		2.0510
roburic acid
roburic acid : A tetracyclic triterpenoid with formula C30H40O2 that is isolated from the roots of Gentiana dahurica and Gentiana macrophylla.		2.110monocarboxylic acid;
olefinic compound;
tetracyclic triterpenoid		plant metabolite
thienopyrimidine
thienopyrimidine: structure in first source. thienopyrimidine : A class of aromatic heterobicyclic compounds each of which contains a pyrimidine ring ortho fused to a 5-membered thiophene ring.		2.610
acid phosphatase
Acid Phosphatase: An enzyme that catalyzes the conversion of an orthophosphoric monoester and water to an alcohol and orthophosphate. EC 3.1.3.2.		2.9740
chikusetsu saponin iva
chikusetsu saponin IVa: from the tubers of Hemsleya pengxianensis (Cucurbitaceae)		3.3110triterpenoid saponinmetabolite
boeravinone b
boeravinone B: from Boerhaavia diffusa L; structure in first source		2.0810
physalaemin
Physalaemin: An oligopeptide isolated from the skin of Physalaemus fuscumaculatus, a South American frog. It is a typical kinin, resembling SUBSTANCE P in structure and action and has been proposed as a sialagogue, antihypertensive, and vasodilator.		2.0210
rabeprazole sodium
[no description available]		2.0810organic sodium salt
icatibant
icatibant: a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer. icatibant : A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acute attacks of hereditary angioedema in adult patients.		2.4220
tosedostat
[no description available]		2.0810carboxylic ester;
hydroxamic acid;
secondary carboxamide
alisol b
[no description available]		3.3510triterpenoid
cyanidin-3-o-beta-glucopyranoside
cyanidin-3-O-beta-glucopyranoside: a natural compound distributed in several fruits & vegetables, such as strawberry, rhubarb, cherry, red cabbage, red onion, cranberries, etc.		2.1510
parecoxib sodium
[no description available]		2.7130
mdv 3100
[no description available]		2.5220(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent
ku 60019
[no description available]		2.0810
gsk 461364
GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1		2.0810(trifluoromethyl)benzenes
n-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide: a MEK inhibitor; structure in first source		2.0810
nvp-tae684
[no description available]		2.0810piperidines
4-(4-(3-adamantan-1-ylureido)cyclohexyloxy)benzoic acid
[no description available]		2.5420
a 803467
A 803467: an Nav1.8 sodium channel blocker; structure in first source		2.1310
amodiaquine hydrochloride
[no description available]		2.7530
clindamycin hydrochloride
[no description available]		2.0510S-glycosyl compound
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		4.14150
mf63 compound
MF63 compound: a phenanthrene imidazole identified as a potent, selective, and orally active mPGES-1 inhibitor; structure in first source		2.5320
4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide
4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide: structure in first source		2.0810
gsk 269962a
[no description available]		2.0810
calcitonin
[no description available]		7.2110
melitten
Melitten: Basic polypeptide from the venom of the honey bee (Apis mellifera). It contains 26 amino acids, has cytolytic properties, causes contracture of muscle, releases histamine, and disrupts surface tension, probably due to lysis of cell and mitochondrial membranes.		2.0310
ceruletide
Ceruletide: A specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction.. ceruletide : A decapeptide comprising 5-oxoprolyl, glutamyl, aspartyl, O-sulfotyrosyl, threonyl, glycyl, tryptopyl, methionyl, aspartyl and phenylalaninamide residues in sequence. Found in the skins of certain Australian amphibians, it is an analogue of the gastrointestinal peptide hormone cholecystokinin and stimulates gastric, biliary, and pancreatic secretion. It is used in cases of paralysis of the intestine (paralytic ileus) and as a diagnostic aid in pancreatic malfunction.		2.4220oligopeptidediagnostic agent;
gastrointestinal drug
bivalirudin
bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.		3.6120polypeptideanticoagulant;
EC 3.4.21.5 (thrombin) inhibitor
somatostatin
[no description available]		2.0810heterodetic cyclic peptide;
peptide hormone
tannins
gallotannin : A class of hydrolysable tannins obtained by condensation of the carboxy group of gallic acid (and its polymeric derivatives) with the hydroxy groups of a monosaccharide (most commonly glucose).		2.0510tannin
enfuvirtide
Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes.		3.2310
ganirelix
[no description available]		3.2310polypeptide
gr 82334
GR 82334: tachykinin NK-1 receptor antagonist		2.0210
alamethicin
Alamethicin: A cyclic nonadecapeptide antibiotic that can act as an ionophore and is produced by strains of Trichoderma viride. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)		2.0310
gastrins
Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.		2.9440
gramicidin a
Gramicidin: A group of peptide antibiotics from BACILLUS brevis. Gramicidin C or S is a cyclic, ten-amino acid polypeptide and gramicidins A, B, D are linear. Gramicidin is one of the two principal components of TYROTHRICIN.		2.0310
glucagon
Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.		2.0310peptide hormone
teriparatide
[no description available]		3.2310polypeptide
salmon calcitonin
[no description available]		3.2310heterodetic cyclic peptide;
peptide hormone;
polypeptide		bone density conservation agent;
metabolite
irl 1620
sovateltide: a potent, specific ligand for the endothelin-B receptor		2.0310
oligonucleotides
[no description available]		7.4520
ly-146032
[no description available]		3.6120heterodetic cyclic peptide;
lipopeptide antibiotic;
lipopeptide;
macrocycle;
macrolide		antibacterial drug;
bacterial metabolite;
calcium-dependent antibiotics
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt		3.2310polypeptide
exenatide
[no description available]		3.2310
warfarin sodium
warfarin sodium : A racemate comprising equal amounts of (R)- and (S)-warfarin sodium. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.		2.0810
cellulose
DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications.		8.81100glycoside
quinine sulfate
[no description available]		2.0510hydrate
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		3.1450
phosphatidylcholines
Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.		3.32601,2-diacyl-sn-glycero-3-phosphocholine
a-83-01
A-83-01: an ALK-5 inhibitor; structure in first source		2.0810
3-[(1-methyl-3-indolyl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one
[no description available]		2.0810indoles
vx-770
ivacaftor: a CFTR potentiator; structure in first source. ivacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis.		2.0810aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone		CFTR potentiator;
orphan drug
buparlisib
NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source		2.0810aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
azd 1480
[no description available]		2.0810
fedratinib
fedratinib: a selective small-molecule inhibitor of JAK2		2.0810sulfonamide
gsk690693
[no description available]		2.08101,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol		antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
cnf 2024
[no description available]		2.08102-aminopurines;
aromatic ether;
organochlorine compound;
pyridines		antineoplastic agent;
Hsp90 inhibitor
ku 0063794
Ku 0063794: an mTOR inhibitor; structure in first source		2.0810benzyl alcohols;
monomethoxybenzene;
morpholines;
pyridopyrimidine;
tertiary amino compound		antineoplastic agent;
mTOR inhibitor
azd 7545
AZD 7545: an anilide tertiary carbinol; a pyruvate dehydrogenase kinase 2 inhibitor. AZD7545 : A sulfone that is benzene substituted by [4-(dimethylcarbamoyl)phenyl]sulfonyl, chloro and [(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino groups at positions 1, 3 and 4, respectively. It is a potent and non-ATP-competitive inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC50 of 6.4 nM and exhibits glucose-lowering activity. Also inhibits PDHK1 at higher levels (IC50 = 36.8 nM).		2.0810benzamides;
monochlorobenzenes;
organofluorine compound;
secondary carboxamide;
sulfone;
tertiary alcohol;
tertiary carboxamide		EC 2.7.11.2 - [pyruvate dehydrogenase (acetyl-transferring)] kinase inhibitor;
hypoglycemic agent
nutlin-3b
[no description available]		2.0810Nutlin;
piperazinone		anticoronaviral agent
pravastatin sodium
pravastatin sodium : An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.0810organic sodium salt;
statin (semi-synthetic)		anticholesteremic drug
alendronate sodium
[no description available]		2.0810
sodium salicylate
[no description available]		7.9740organic molecular entity
sphingosine kinase
[no description available]		2.0810
ubiquinone
Ubiquinone: A lipid-soluble benzoquinone which is involved in ELECTRON TRANSPORT in mitochondrial preparations. The compound occurs in the majority of aerobic organisms, from bacteria to higher plants and animals.		2.0210
mavatrep
mavatrep: a transient receptor potential vanilloid 1 antagonist; structure in first source		2.1110
pf 04217903
[no description available]		2.0810quinolines
gdc 0941
pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring.		2.0810indazoles;
morpholines;
piperazines;
sulfonamide;
thienopyrimidine		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
sm 164
SM 164: a bivalent Smac mimetic with antineoplastic activity; structure in first source		2.0810benzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles		antineoplastic agent;
apoptosis inducer;
radiosensitizing agent
sl 80.0750
[no description available]		2.0810
calpain
Calpain: Cysteine proteinase found in many tissues. Hydrolyzes a variety of endogenous proteins including NEUROPEPTIDES; CYTOSKELETAL PROTEINS; proteins from SMOOTH MUSCLE; CARDIAC MUSCLE; liver; platelets; and erythrocytes. Two subclasses having high and low calcium sensitivity are known. Removes Z-discs and M-lines from myofibrils. Activates phosphorylase kinase and cyclic nucleotide-independent protein kinase. This enzyme was formerly listed as EC 3.4.22.4.		7.4520
cefotiam hydrochloride
[no description available]		2.0510
Norartocarpanone
[no description available]		3.3110flavanones
chitosan
[no description available]		4.11140
ph 797804
PH 797804: an NSAID; structure in first source. PH 797804 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1-yl}-4-methylbenzoic acid with the amino group of methylamine.		2.0810aromatic ether;
benzamides;
organobromine compound;
organofluorine compound;
pyridone		anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
pha 408
PHA 408: an IKK-2 antagonist; structure in first source		2.0810
15-deoxyprostaglandin j2
15-deoxyprostaglandin J2: 15d-PGJ2 abbreviation is also used for 15-deoxy-delta(12,14)PGJ2		2.4220
gsk 1016790a
GSK1016790A : A tertiary carboxamide that is piperazine in which one of the amino groups has undergone condensation with the carboxy group of N-[(2,4-dichlorophenyl)sulfonyl]-L-serine, while the other has undergone condensation with the carboxy group of N-(1-benzothiophen-2-ylcarbonyl)-L-leucine. It is a cell-permeable, potent and selective agonist of the TRPV4 (transient receptor potential vanilloid 4) channel.		2.08101-benzothiophenes;
aromatic primary alcohol;
dichlorobenzene;
N-acylpiperazine;
sulfonamide;
tertiary carboxamide		TRPV4 agonist
gsk1482160
[no description available]		2.0510
mesna
Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE.		3.8730organosulfonic acid
tofisopam
[no description available]		2.0610organic sodium saltantipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
potassium aminobenzoate
[no description available]		2.0510
bucladesine
Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed). bucladesine : A 3',5'-cyclic purine nucleotide that is the 2'-butanoate ester and 6-N-butanoyl derivative of 3',5'-cyclic AMP.		2.48203',5'-cyclic purine nucleotide
ampicillin sodium
[no description available]		2.0510organic sodium salt
cerivastatin sodium
cerivastatin sodium : The sodium salt of cerivastatin. Formerly used to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.		2.0510organic sodium salt;
statin (synthetic)
clavulanate potassium
potassium clavulanate : A potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases.		2.0810potassium saltantibacterial drug;
antimicrobial agent;
EC 3.5.2.6 (beta-lactamase) inhibitor
taurocholic acid, monosodium salt
[no description available]		3.5520bile salt
sodium lactate
Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion.		3.2310lactate salt;
organic sodium salt		food acidity regulator;
food preservative
piperacillin sodium
[no description available]		2.0810organic sodium salt
monensin
[no description available]		2.0510
sodium iothalamate
[no description available]		3.2310
methicillin sodium
[no description available]		2.0510organic sodium salt
nafcillin sodium
[no description available]		2.0510organic sodium salt
oxacillin sodium
[no description available]		2.4720organic sodium salt
penicillin g sodium
[no description available]		2.0510organic sodium salt
cefamandole nafate
cefamandole sodium : An organic sodium salt that is the sodium salt of cefamandole.		2.0510organic sodium saltantibacterial drug
sodium diatrizoate
histopaque: used for separating mononuclear & other cells. sodium amidotrizoate : The sodium salt of a benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, often as a mixture with the meglumine salt, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.		2.0510organic sodium salt;
organoiodine compound		radioopaque medium
cephapirin sodium
cephapirin sodium : The sodium salt of cephapirin. A first-generation cephalosporin antibiotic, it is effective against gram-negative and gram-positive organisms. Being more resistant to beta-lactamases than penicillins, it is effective agains most staphylococci, though not methicillin-resistant staphylococci.		2.0510cephalosporin;
organic sodium salt		antibacterial drug
sodium cephalothin
[no description available]		2.0510organic sodium salt
cefazolin sodium
cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.		2.0810organic sodium salt
dicloxacillin sodium
[no description available]		2.0510hydrate
sodium glutamate
Sodium Glutamate: One of the FLAVORING AGENTS used to impart a meat-like flavor.. monosodium glutamate : An organic sodium salt that is the monosodium salt of glutamic acid.		2.4620monosodium glutamateflavouring agent
merocyanine dye
merocyanine dye: fluorescent dye used for studying axons 2 position on pyrimidine ring may be S or O; RN given refers to Na salt; structure		2.0610
ro13-9904
Ceftriaxone: A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.. ceftriaxone : A third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.		2.110
azlocillin sodium
[no description available]		2.4720organic sodium salt
olaparib
[no description available]		3.6320cyclopropanes;
monofluorobenzenes;
N-acylpiperazine;
phthalazines		antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
(E)-1,7-Bis(4-hydroxyphenyl)hept-4-en-3-one
[no description available]		3.3110diarylheptanoid
srt1720
[no description available]		2.0810
plx 4720
PLX 4720: a B-Raf(V600E) kinase inhibitor; structure in first source		2.0810aromatic ketone;
difluorobenzene;
organochlorine compound;
pyrrolopyridine;
sulfonamide		antineoplastic agent;
B-Raf inhibitor
beta-Elemonic acid
beta-elemonic acid: extracted from Boswellia carterii		2.110triterpenoid
cx 4945
[no description available]		2.0810
cudc 101
7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide: a histone deacetylase inhibitor; structure in first source		2.0810
s-adenosylmethionine
(R)-S-adenosyl-L-methionine : An S-adenosyl-L-methionine that has R-configuration.. S-adenosyl-L-methionine zwitterion : A zwitterionic tautomer of S-adenosyl-L-methionine arising from shift of the proton from the carboxy group to the amino group.. (R)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has R-configuration; major species at pH 7.3.. (S)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has S-configuration; major species at pH 7.3.. S-adenosyl-L-methionine : A sulfonium compound that is the S-adenosyl derivative of L-methionine. It is an intermediate in the metabolic pathway of methionine.		3.411organic cation;
sulfonium compound		coenzyme;
cofactor;
human metabolite;
micronutrient;
Mycoplasma genitalium metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
mln 8237
MLN 8237: an aurora kinase A inhibitor		2.0810benzazepine
lde225
sonidegib: specific Smoothened/Smo antagonist. sonidegib : A member of the classo of biphenyls that is the amide obtained by formal condensation of the carboxy group of 2-methyl-4'-(trifluoromethoxy)[1,1'-biphenyl]-3-carboxylic acid with the amino group of 6-(2,6-dimethylmorpholin-4-yl)pyridin-3-amine. Used (as its phosphate salt) for treatment of locally advanced basal cell carcinoma.		2.0810aminopyridine;
aromatic ether;
benzamides;
biphenyls;
morpholines;
organofluorine compound;
tertiary amino compound		antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist
gdc 0449
HhAntag691: inhibits the hedgehog pathway and ABC transporters; has antineoplastic activity		2.0810benzamides;
monochlorobenzenes;
pyridines;
sulfone		antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist;
teratogenic agent
sgx 523
[no description available]		2.0810aryl sulfide;
biaryl;
pyrazoles;
quinolines;
triazolopyridazine		c-Met tyrosine kinase inhibitor;
nephrotoxic agent
bms 777607
N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide: a Met kinase inhibitor; structure in first source		2.0810aromatic amide
sgi 1776
SGI 1776: a Pim kinase inhibitor; structure in first source		2.0810imidazoles
ys 121
2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid: inhibits microsomal prostaglanding E2 synthase; structure in first source		2.7630medium-chain fatty acid
pci 32765
ibrutinib: a Btk protein inhibitor. ibrutinib : A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of the enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.		2.0810acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
florbetapir f 18
florbetapir: a PET agent for Abeta plaques; structure in first source. florbetapir F-18 : An aromatic ether consisting of a pyridine ring substituted at position 2 by a 2-{2-[2-((18)F)fluoroethoxy]ethoxy}ethoxy group and at position 5 and a 2-(4-methylaminophenyl)vinyl group. A positron emission tomography imaging ligand for the detection of amyloid aggregation associated with Alzheimer disease.		2.0810(18)F radiopharmaceutical;
aromatic ether;
organofluorine compound;
pyridines;
substituted aniline		radioactive imaging agent
ponatinib
[no description available]		2.0810(trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine		antineoplastic agent;
tyrosine kinase inhibitor
ethyl cellulose
[no description available]		2.7330glycoside
amg 900
N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine: a pan-aurora kinase inhibitor; structure in first source		2.0810
mk-1775
adavosertib: a Wee1 kinase inhibitor; structure in first source		2.0810piperazines
bag956
BAG956: an imidazo[4,5-c]quinoline; dual PI3K/PDK-1 inhibitor, used in antileukemic therapies		2.0810
quizartinib
[no description available]		2.0810benzoimidazothiazole;
isoxazoles;
morpholines;
phenylureas		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
necroptosis inhibitor
N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]-oxomethyl]-5-isoxazolyl]phenyl]carbamic acid tert-butyl ester
CAY10603: a HDAC6 inhibitor		2.0810carbamate ester
tak 733
[no description available]		2.0810
mk 2206
MK 2206: a protein kinase inhibitor and antineoplastic agent		2.7830organic heterotricyclic compoundEC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
navitoclax
[no description available]		2.5120aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
sns 314
SNS 314: an aurora kinase inhibitor; structure in first source		2.0810ureas
jzl 184
JZL 184: inhibits monoacylglycerol lipase; structure in first source		2.0810benzodioxoles
quetiapine fumarate
Quetiapine Fumarate: A dibenzothiazepine and ANTIPSYCHOTIC AGENT that targets the SEROTONIN 5-HT2 RECEPTOR; HISTAMINE H1 RECEPTOR, adrenergic alpha1 and alpha2 receptors, as well as the DOPAMINE D1 RECEPTOR and DOPAMINE D2 RECEPTOR. It is used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER and DEPRESSIVE DISORDER.		2.2110fumarate salt
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide
N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide: a Janus kinase 1 and Janus kinase 2 inhibitor; structure in first source. momelotinib : A benzamide obtained by formal condensation of the carboxy group of 4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzoic acid with the primary amino group of aminoacetonitrile. It is an ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 nM and 18 nM, respectively. Used for the treatment of patients with intermediate- or high-risk myelofibrosis.		2.0810aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound		anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		3.1410
atb-346
2-(6-methoxy-napthalen-2-yl)-propionic acid 4-thiocarbamoyl-phenyl ester: NSAIDs; structure in first source		2.4920
dcc-2036
rebastinib: an inhibitor of Tie2 tyrosine kinase receptor and antineoplastic agent		2.0810organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines		tyrosine kinase inhibitor
ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4h-chromene-3-carboxylate
ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate: has antineoplastic activity; structure in first source		3.3510
cetrorelix
cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.		3.2310oligopeptideantineoplastic agent;
GnRH antagonist
cabozantinib
cabozantinib: a multikinase inhibitor. cabozantinib : A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.		2.0810aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide
[no description available]		2.0810benzamides
incb-018424
[no description available]		2.4920nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
mannans
[no description available]		2.7330
bix 01294
[no description available]		2.0810piperidines
pexidartinib
pexidartinib: inhibits both CSF1R and c-kit receptor tyrosine kinase; structure in first source. pexidartinib : A pyrrolopyridine that is 5-chloro-1H-pyrrolo[2,3-b]pyridine which is substituted by a [6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino)pyridin-3-yl]methyl group at position 3. It is a potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, KIT, and FLT3 (IC50 of 20 nM, 10 nM and 160 nM, respectively). Approved by the FDA for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT).		3.4110aminopyridine;
organochlorine compound;
organofluorine compound;
pyrrolopyridine;
secondary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
pf 3845
PF 3845: inhibits fatty acid amide hydrolase		2.0810piperidines
gsk 2126458
omipalisib: inhibitor of mTOR protein. omipalisib : A member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors.		2.0810aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide		anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent
ixazomib
ixazomib: a proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708; structure in first source. ixazomib : A glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixazomib citrate, it is used in combination therapy for treatment of multiple myeloma.		2.0810benzamides;
boronic acids;
dichlorobenzene;
glycine derivative		antineoplastic agent;
apoptosis inducer;
drug metabolite;
orphan drug;
proteasome inhibitor
ldn 193189
LDN 193189: inhibits bone morphogenetic protein signaling		2.0810pyrimidines
cem 101
solithromycin: an antibacterial fluoroketolide; structure in first source		3.3510
(E)-sinapaldehyde 4-O-beta-D-glucopyranoside
(E)-sinapaldehyde 4-O-beta-D-glucopyranoside : A beta-D-glucoside resulting from the formal condensation of the phenolic hydroxy group of (E)-sinapaldehyde with beta-D-glucose.		2.3110beta-D-glucoside;
cinnamaldehydes;
dimethoxybenzene;
monosaccharide derivative		plant metabolite
11,12-epoxy-5,8,14-eicosatrienoic acid
11,12-epoxy-5,8,14-eicosatrienoic acid: RN given refers to cpd without isomeric designation. (11S,12R)-EET : An 11,12-EET in which the epoxy moiety has 11S,12R-configuration.. 11,12-EET : An EET obtained by formal epoxidation of the 11,12-double bond of arachidonic acid.		2.021011,12-EEThuman xenobiotic metabolite
plx4032
[no description available]		3.0240aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide		antineoplastic agent;
B-Raf inhibitor
(2S)-2-[[2-(2,3-dihydro-1H-inden-5-yloxy)-9-[(4-phenylphenyl)methyl]-6-purinyl]amino]-3-phenyl-1-propanol
[no description available]		2.0810biphenyls
gsk 1363089
GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source		2.0810aromatic ether
kin-193
[no description available]		2.0810pyridopyrimidine
biselyngbyaside
biselyngbyaside: antineoplastic from the marine cyanobacterium Lyngbya sp.; structure in first source		3.3510
bay 869766
[no description available]		2.0810
4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester
WYE-354: an mTOR inhibitor; structure in first source		2.0810carbamate ester
cinerin c
cinerin C: isolated from Pleurothyrium cinereum; structure in first source		2.0510
piperidines
Piperidines: A family of hexahydropyridines.		4.43200
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinone
ML-265: a small molecule activator of PKM2		2.0810organic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		9.8371
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]aniline
[no description available]		2.0810benzenes;
sulfonamide
cp 466722
[no description available]		2.0810quinazolines
CAY10626
[no description available]		2.0810ureas
thiopental sodium
[no description available]		2.0810organochlorine compound;
piperazines;
pyrimidines		antineoplastic agent;
tyrosine kinase inhibitor
LSM-2536
[no description available]		3.5110piperazines
mme
[no description available]		2.4110
fosinopril
Fosinopril: A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.. fosinopril : A phosphinate ester-containing N-acyl derivative of (4S)-cyclohexyl-L-proline. It is used for the treatment of hypertension and heart failure. A pro-drug, it is hydrolysed in vivo to the corresponding phosphininc acid, fosinoprilat, which is the active metabolite.		2.0110
cinerin a
cinerin A: isolated from Pleurothyrium cinereum; structure in first source		2.0510
endrin
Endrin: An organochlorine compound that was formerly used as an insecticide. Its manufacture and use has been discontinued in the United States. (From Merck Index, 11th ed). endrin : An organochlorine compound resulting from the epoxidation of the double bond of isodrin. It is the endo, endo stereoisomer of dieldrin. It is an insecticide mainly used on field crops such as cotton and grains and has also been used as a rodenticide to control mice and voles. The product is banned in many countries since it is a persistent organic pollutant.		2.4110
blz 945
[no description available]		3.4110
pha 793887
[no description available]		2.0810piperidinecarboxamide
nvp-bsk805
[no description available]		2.0810
xmd 8-92
XMD8-92 : A dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one carrying at C-2 on the pyrimidine ring a [2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino substituent. It is an inhibitor of the BMK1 kinase pathway.		2.0810pyrimidobenzodiazepineprotein kinase inhibitor
jq1 compound
[no description available]		2.0810carboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer
jnj38877605
[no description available]		2.0810quinolines
N-[3-(1,3-benzothiazol-2-yl)-5,6-dihydro-4H-thieno[2,3-c]pyrrol-2-yl]acetamide
[no description available]		2.0810benzothiazoles
lgk974
LGK974: a potent and specific small-molecule inhibitor of Porcupine (PORCN) acyltransferase. LGK974 : A carboxamide, the structure of which is that of acetamide substituted on carbon by a 2',3-dimethyl-2,4'-bipyridin-5-yl group and on nitrogen by a 5-(pyrazin-2-yl)pyridin-2-yl group. It is a highly potent, selective and orally bioavailable Porcupine inhibitor (a Wnt signalling inhibitor).		2.1110bipyridines;
pyrazines;
pyridines;
secondary carboxamide		Wnt signalling inhibitor
calcipotriene
calcipotriene: a topical dermatologic for the treatment of moderate plaque psoriasis; structure in first source. calcipotriol hydrate : A hydrate that is the monohydrate form of calcipotriol. It is used in combination with betamethasone dipropionate, a corticosteroid, for the topical treatment of plaque psoriasis in adult patients.		2.0310hydrateantipsoriatic
torin 1
torin 1 : A member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties.		2.0810N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines		antineoplastic agent;
mTOR inhibitor
ly2940680
[no description available]		2.0810
tubastatin a
[no description available]		2.1510hydroxamic acid;
pyridoindole;
tertiary amino compound		EC 3.5.1.98 (histone deacetylase) inhibitor
1-[4-fluoro-3-(trifluoromethyl)phenyl]-3-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)urea
[no description available]		2.0810ureas
ro 4929097
[no description available]		2.0810dibenzoazepine;
dicarboxylic acid diamide;
lactam;
organofluorine compound		EC 3.4.23.46 (memapsin 2) inhibitor
gsk4112
GSK4112: a Rev-erbalpha agonist; structure in first source		2.0810
methylcellulose
Methylcellulose: Methylester of cellulose. Methylcellulose is used as an emulsifying and suspending agent in cosmetics, pharmaceutics and the chemical industry. It is used therapeutically as a bulk laxative.		8.86110
torin 2
torin 2 : A member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties.		2.0810aminopyridine;
organofluorine compound;
primary amino compound;
pyridoquinoline		antineoplastic agent;
mTOR inhibitor
pf-4708671
[no description available]		2.0810
natriuretic peptide, brain
Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.		3.8430polypeptide
acy-1215
ricolinostat: an HDAC6 inhibitor; structure in first source		2.1710pyrimidinecarboxylic acid
heme
Heme: The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.. ferroheme : Any iron(II)--porphyrin coordination complex.. ferroheme b : Heme b in which the iron has oxidation state +2.. heme : A heme is any tetrapyrrolic chelate of iron.		2.0810
N-[2-(3-oxo-4H-quinoxalin-2-yl)-4-propan-2-ylphenyl]-2-thiophenecarboxamide
[no description available]		3.5110aromatic amide
N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide
[no description available]		2.0810benzamides;
N-acylpiperidine
2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide
2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide : A member of the class of quinazolines that is quinazoline substituted by {3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl}amino and 3-(2-methoxyacetamido)prop-1-en-1-yl groups at positions 4 and 6, respectively.		2.0810aromatic ether;
methylpyridines;
olefinic compound;
quinazolines;
secondary amino compound;
secondary carboxamide;
toluenes
belinostat
[no description available]		2.0810olefinic compound
chondroitin
Chondroitin: A mucopolysaccharide constituent of chondrin. (Grant & Hackh's Chemical Dictionary, 5th ed)		5.8461
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		8.68182ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
raltegravir
[no description available]		3.23101,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor
aspulvinone E
4-hydroxy-5-(4-hydroxybenzylidene)-3-(4-hydroxyphenyl)furan-2(5H)-one : A member of the class of butenolides that is furan-2(5H)-one substituted by 4-hydroxyphenyl, hydroxy and 4-hydroxybenzylidene groups at positions 3, 4 and 5, respectively.. aspulvinone E : A 4-hydroxy-5-(4-hydroxybenzylidene)-3-(4-hydroxyphenyl)furan-2(5H)-one in which the double bond adopts a Z-configuration. It is a marine metabolite isolated from the fungus Aspergillus terreus and exhibits antiviral activity.		3.51104-hydroxy-5-(4-hydroxybenzylidene)-3-(4-hydroxyphenyl)furan-2(5H)-one;
aspulvinone		antiviral agent;
Aspergillus metabolite;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
marine metabolite
novobiocin
Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189). novobiocin : A coumarin-derived antibiotic obtained from Streptomyces niveus.		4.2650carbamate ester;
ether;
hexoside;
hydroxycoumarin;
monocarboxylic acid amide;
monosaccharide derivative;
phenols		antibacterial agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Escherichia coli metabolite;
hepatoprotective agent
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		4.5570
chlortetracycline
Chlortetracycline: A TETRACYCLINE with a 7-chloro substitution.. chlortetracycline : A member of the class of tetracyclines with formula C22H23ClN2O8 isolated from Streptomyces aureofaciens.		2.0510
oxytetracycline, anhydrous
Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.		3.5920
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		8.95142
salicylates
Salicylates: The salts or esters of salicylic acids, or salicylate esters of an organic acid. Some of these have analgesic, antipyretic, and anti-inflammatory activities by inhibiting prostaglandin synthesis.. hydroxybenzoate : Any benzoate derivative carrying a single carboxylate group and at least one hydroxy substituent.. salicylates : Any salt or ester arising from reaction of the carboxy group of salicylic acid, or any ester resulting from the condensation of the phenolic hydroxy group of salicylic acid with an organic acid.. salicylate : A monohydroxybenzoate that is the conjugate base of salicylic acid.		4.4360monohydroxybenzoateplant metabolite
dicumarol
Dicumarol: An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases.		2.0510hydroxycoumarinanticoagulant;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
Hsp90 inhibitor;
vitamin K antagonist
piroxicam
[no description available]		9.04301benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
roquinimex
roquinimex: structure in first source		2.0810aromatic amide
acenocoumarol
Acenocoumarol: A coumarin that is used as an anticoagulant. Its actions and uses are similar to those of WARFARIN. (From Martindale, The Extra Pharmacopoeia, 30th ed, p233). acenocoumarol : A hydroxycoumarin that is warfarin in which the hydrogen at position 4 of the phenyl substituent is replaced by a nitro group.		2.4620C-nitro compound;
hydroxycoumarin;
methyl ketone		anticoagulant;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		12.4568101,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
mobiflex
tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.		4.1331heteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
isoxicam
isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome.		2.4720benzothiazine;
isoxazoles;
monocarboxylic acid amide		antirheumatic drug;
non-steroidal anti-inflammatory drug
ethyl 1-benzyl-3-hydroxy-2(5h)-oxopyrrole-4-carboxylate
ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate: RN & structure given in first source		2.0810carboxylic acid;
pyrroline
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		7.47212benzenes;
hydroxycoumarin;
methyl ketone
demeclocycline
Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		3.2310
phenprocoumon
Phenprocoumon: Coumarin derivative that acts as a long acting oral anticoagulant.. phenprocoumon : A hydroxycoumarin that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenylpropyl group.		2.0510hydroxycoumarinanticoagulant;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor
tipranavir
tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor.		4.0940sulfonamideantiviral drug;
HIV protease inhibitor
chlortetracycline hydrochloride
Alexomycin: a thiopeptide; a cyclic peptide antibiotic produced by Streptomyces arginensis isolated from the soil		2.0510
rolitetracycline
Rolitetracycline: A pyrrolidinylmethyl TETRACYCLINE.. rolitetracycline : A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group.		2.0510
sudoxicam
sudoxicam: proposed ant-inflammatory agent; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZINES (75-86)		2.0510
teriflunomide
[no description available]		1.9910(trifluoromethyl)benzenes;
aromatic amide;
enamide;
enol;
nitrile;
secondary carboxamide		drug metabolite;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
tyrosine kinase inhibitor
methacycline monohydrochloride
[no description available]		2.0510
minocycline hydrochloride
[no description available]		2.4720
demeclocycline hydrochloride
demeclocycline hydrochloride : The hydrochloride salt of demeclocycline. A tetracycline antibiotic, it is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		2.0510
tigecycline
[no description available]		3.6120
(S)-warfarin
(S)-warfarin : A 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one that has (S)-configuration (the racemate is warfarin, an anticoagulant drug and rodenticide).		2.08104-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one
lornoxicam
lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.		2.7530heteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine		antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
a 769662
[no description available]		2.0810biphenyls
pf 9184
[no description available]		2.0710
almagate
pegaptanib: a 28-base ribonucleic acid aptamer covalently linked to two branched 20-kD polyethylene glycol moieties to block the activity of extracellular VEGF, specifically the 165-amino-acid isoform (VEGF165); for treatment of neovascular age-related macular degeneration		2.0310
omega-agatoxin iva
omega-Agatoxin IVA: A neuropeptide toxin from the venom of the funnel web spider, Agelenopsis aperta. It inhibits CALCIUM CHANNELS, P-TYPE by altering the voltage-dependent gating so that very large depolarizations are needed for channel opening. It also inhibits CALCIUM CHANNELS, Q-TYPE.		2.0310
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		10.4770
kaolinite
Kaolin: The most common mineral of a group of hydrated aluminum silicates, approximately H2Al2Si2O8-H2O. It is prepared for pharmaceutical and medicinal purposes by levigating with water to remove sand, etc. (From Merck Index, 11th ed) The name is derived from Kao-ling (Chinese: high ridge), the original site. (From Grant & Hackh's Chemical Dictionary, 5th ed). kaolin : An aluminosilicate soft white mineral named after the hill in China (Kao-ling) from which it was mined for centuries. In its natural state kaolin is a white, soft powder consisting principally of the mineral kaolinite, and varying amounts of other minerals such as muscovite, quartz, feldspar, and anatase. It is used in the manufacture of china and porcelain and also widely used in the production of paper, rubber, paint, drying agents, and many other products.		2.0310aluminosilicate mineral;
mixture		antidiarrhoeal drug;
excipient
clay
Clay: A naturally-occurring rock or soil constituent characterized by particles with a diameter of less than 0.005 mm. It is composed primarily of hydrous aluminum silicates, trace amounts of metal OXIDES, and organic matter.		2.1510
charybdotoxin
[no description available]		2.2110
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		6.23172
LimKi 3
LIMKi3: LIMK inhibitor. LimKi 3 : A member of the class of pyrazoles that is 1-(2,6-dichlorophenyl)-1H-pyrazole which is substituted by a difluoromethyl group at position 3 and by a 2-(isobutyrylamino)-1,3-thiazol-5-yl group at position 5. It is a a potent cell-permeable inhibitor of LIM kinase 1 and 2.		2.08101,3-thiazoles;
dichlorobenzene;
organofluorine compound;
pyrazoles;
secondary carboxamide		LIM kinase inhibitor
1-[4-amino-7-[3-(2-methoxyethylamino)propyl]-5-(4-methylphenyl)-6-pyrrolo[2,3-d]pyrimidinyl]-2-fluoroethanone
[no description available]		2.0810pyrroles
okadaic acid
Okadaic Acid: A specific inhibitor of phosphoserine/threonine protein phosphatase 1 and 2a. It is also a potent tumor promoter. It is produced by DINOFLAGELLATES and causes diarrhetic SHELLFISH POISONING.. okadaic acid : A polycyclic ether that is produced by several species of dinoflagellates, and is known to accumulate in both marine sponges and shellfish. A polyketide, polyether derivative of a C38 fatty acid, it is one of the primary causes of diarrhetic shellfish poisoning (DSP). It is a potent inhibitor of specific protein phosphatases and is known to have a variety of negative effects on cells.		2.0210ketal
2-[5-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-4-methoxy-2-pyrrolylidene]indole
[no description available]		2.0810dipyrrins
N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]-2-propenamide
[no description available]		2.0810tryptamines
3-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]-6-(phenylmethylene)piperazine-2,5-dione
[no description available]		2.0810pyrazines
gsk837149a
GSK837149A: structure in first source		2.0810
N-[4-(3-chloro-4-fluoroanilino)-7-[[(3S)-3-oxolanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
[no description available]		2.0810quinazolines
N-[4-(3-chloro-4-fluoroanilino)-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
[no description available]		2.0810quinazolines
wnt-c59
2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide: a PORCN acyltransferase inhibitor; structure in first source		2.520
5-[1-(2-hydroxyethyl)-3-pyridin-4-yl-4-pyrazolyl]-2,3-dihydroinden-1-one oxime
[no description available]		2.0810indanes
pf-543
PF-543: Sphingosine Kinase 1 Selective Inhibitor; structure in first source		2.3110sulfonamide
g007-lk
G007-LK: potent and specific small-molecule tankyrase inhibitor; structure in first source		2.1110
ajmaline
[no description available]		2.0510
hunanamycin a
hunanamycin A: antibiotic from a marine-derived Bacillus hunanensis; structure in first source		3.5110
agar
Agar: A complex sulfated polymer of galactose units, extracted from Gelidium cartilagineum, Gracilaria confervoides, and related red algae. It is used as a gel in the preparation of solid culture media for microorganisms, as a bulk laxative, in making emulsions, and as a supporting medium for immunodiffusion and immunoelectrophoresis.. agar : A complex mixture of polysaccharides extracted from species of red algae. Its two main components are agarose and agaropectin. Agarose is the component responsible for the high-strength gelling properties of agar, while agaropectin provides the viscous properties.		2.4110
arsenic trisulfide
[no description available]		2.1110
ziyuglycoside ii
ziyuglycoside II: isolated from Sanguisorba officinalis; structure in first source		2.1710
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		5.5200
contraceptives, postcoital
Contraceptives, Postcoital: Contraceptive substances to be used after COITUS. These agents include high doses of estrogenic drugs; progesterone-receptor blockers; ANTIMETABOLITES; ALKALOIDS, and PROSTAGLANDINS.		2.0110
caseins
Caseins: A mixture of related phosphoproteins occurring in milk and cheese. The group is characterized as one of the most nutritive milk proteins, containing all of the common amino acids and rich in the essential ones.		2.4920
fertinex
[no description available]		3.2310
limbrel
flavocoxid: a mixture of baicalin and catechin used as an NSAID		2.1310
benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone
benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone: an interleukin-1beta converting enzyme (ICE)-like protease inhibitor		2.0710
nitrophenols
Nitrophenols: PHENOLS carrying nitro group substituents.		3.0240
handelin
handelin: Chinese drug isolated from flowers of Chrysanthemum indicum L.; structure given in first source		2.110sesterterpenoid
snx 482
SNX 482: from venom of tarantula, Hysterocrates gigas; amino acid sequence in first source		2.0310
angiotensin i
Angiotensin I: A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.. angiotensin I : A ten amino acid peptide formed by renin cleavage of angiotensinogen. Angiotensin I has no direct biological function except that high levels can stimulate catecholamine production. It is metabolized to its biologically active byproduct angiotensin II, a potent vasoconstrictor, by angiotensin converting enzyme (ACE) through cleavage of the two terminal amino acids.. angiotensin I dizwitterion : A peptide zwitterion that is the dizwitterionic form of angiotensin I having both carboxy groups deprotonated and the aspartyl amino group and arginine side-chain protonated. It is the major species at pH 7.3.		2.1110angiotensin;
peptide zwitterion		human metabolite;
neurotransmitter agent
hyaluronoglucosaminidase
Hyaluronoglucosaminidase: An enzyme that catalyzes the random hydrolysis of 1,4-linkages between N-acetyl-beta-D-glucosamine and D-glucuronate residues in hyaluronate. (From Enzyme Nomenclature, 1992) There has been use as ANTINEOPLASTIC AGENTS to limit NEOPLASM METASTASIS.		310
lipofectamine
Lipofectamine: mediates gene transfer; a polycationic lipid reagent		2.0710
ginkgolide b
[no description available]		2.0310
vitamin b 12
Vitamin B 12: A cobalt-containing coordination compound produced by intestinal micro-organisms and found also in soil and water. Higher plants do not concentrate vitamin B 12 from the soil and so are a poor source of the substance as compared with animal tissues. INTRINSIC FACTOR is important for the assimilation of vitamin B 12.		2.110
transforming growth factor alpha
Transforming Growth Factor alpha: An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR.		2.5920
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		4.4360
silybin
Silybin: The major active component of silymarin flavonoids extracted from seeds of the MILK THISTLE, Silybum marianum; it is used in the treatment of HEPATITIS; LIVER CIRRHOSIS; and CHEMICAL AND DRUG INDUCED LIVER INJURY, and has antineoplastic activity; silybins A and B are diastereomers.		2.4720
lactoferrin
Lactoferrin: An iron-binding protein that was originally characterized as a milk protein. It is widely distributed in secretory fluids and is found in the neutrophilic granules of LEUKOCYTES. The N-terminal part of lactoferrin possesses a serine protease which functions to inactivate the TYPE III SECRETION SYSTEM used by bacteria to export virulence proteins for host cell invasion.		7.8930
icg 001
ICG 001: PRI-724 is an enantiomer of ICG-001; binds to cAMP response element-binding protein; structure in first source		2.0810
thromboplastin
Thromboplastin: Constituent composed of protein and phospholipid that is widely distributed in many tissues. It serves as a cofactor with factor VIIa to activate factor X in the extrinsic pathway of blood coagulation.		3.4270
lewis y antigen
[no description available]		2.1110
chondroitin sulfates
Chondroitin Sulfates: Derivatives of chondroitin which have a sulfate moiety esterified to the galactosamine moiety of chondroitin. Chondroitin sulfate A, or chondroitin 4-sulfate, and chondroitin sulfate C, or chondroitin 6-sulfate, have the sulfate esterified in the 4- and 6-positions, respectively. Chondroitin sulfate B (beta heparin; DERMATAN SULFATE) is a misnomer and this compound is not a true chondroitin sulfate.		11.812512
entecavir
entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B.		3.87302-aminopurines;
oxopurine;
primary alcohol;
secondary alcohol		antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
chir 258
[no description available]		2.0810
acyclovir
Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.		5.08702-aminopurines;
oxopurine		antimetabolite;
antiviral drug
osi 027
OSI 027: inhibits both mTORC1 and mTORC2; structure in first source		2.0810
levoleucovorin
Levoleucovorin: A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.. (6S)-5-formyltetrahydrofolic acid : The pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid.		10.6413125-formyltetrahydrofolic acidantineoplastic agent;
metabolite
cyclic gmp
Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.		3.83303',5'-cyclic purine nucleotide;
guanyl ribonucleotide		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
deoxyguanosine triphosphate
[no description available]		2.0610deoxyguanosine phosphate;
guanyl deoxyribonucleotide;
purine 2'-deoxyribonucleoside 5'-triphosphate		Arabidopsis thaliana metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
guanosine diphosphate
Guanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.		2.0610guanosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
inosine
[no description available]		2.0510inosines;
purines D-ribonucleoside		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		10.95100folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
3-methyladenine
N3-methyladenine: structure in first source		2.0810
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		12.83122cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		6.62100benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		15.2255dacarbazine
didanosine
Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.		4.0940purine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor;
geroprotector;
HIV-1 reverse transcriptase inhibitor
ganciclovir
[no description available]		4.44602-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
valtrex
[no description available]		2.0810organic molecular entity
valacyclovir
Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES.		4.5940L-valyl esterantiviral drug
sildenafil
sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position.		4.2850piperazines;
pyrazolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
olanzapine
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		10.9371benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
penciclovir
penciclovir : A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclovir, is used for oral administration.		2.05102-aminopurines;
propane-1,3-diols		antiviral drug
oxypurinol
Oxypurinol: A xanthine oxidase inhibitor.. alloxanthine : A pyrazolopyrimidine that is 4,5,6,7-tetrahydro-H-pyrazolo[3,4-d]pyrimidine substituted by oxo groups at positions 4 and 6.		2.0510pyrazolopyrimidinedrug metabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor
zaprinast
zaprinast: anaphylaxis inhibitor; structure		2.0310triazolopyrimidines
raltitrexed
[no description available]		2.7630N-acyl-amino acid
vardenafil
vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine.		3.5720imidazotriazine;
N-alkylpiperazine;
N-sulfonylpiperazine		EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		11.77101nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
hli 373
[no description available]		2.0810
citrovorum factor
[no description available]		3.8730tetrahydrofolic acid
leucovorin
5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5.		3.8630formyltetrahydrofolic acidEscherichia coli metabolite;
mouse metabolite
rifapentine
rifapentine: cyclopentyl derivative of rifampicin		3.6120N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug
alanosine
[no description available]		2.0510
bl 4162a
anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions.		3.5920imidazoquinazolineanticoagulant;
antifibrinolytic drug;
cardiovascular drug;
platelet aggregation inhibitor
tegaserod
tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source		3.2310carboxamidine;
guanidines;
hydrazines;
indoles		gastrointestinal drug;
serotonergic agonist
norclozapine
norclozapine: structure given in first source. N-desmethylclozapine : A dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist.		2.0810dibenzodiazepine;
organochlorine compound;
piperazines		delta-opioid receptor agonist;
metabolite;
serotonergic antagonist
pemetrexed
pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).		6.4141N-acyl-L-glutamic acid;
pyrrolopyrimidine		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
tirapazamine
Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4.		2.0510aromatic amine;
benzotriazines;
N-oxide		antibacterial agent;
antineoplastic agent;
apoptosis inducer
sildenafil citrate
Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.		3.1850citrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
valganciclovir
Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine.		3.5920L-valyl ester;
purines		antiviral drug;
prodrug
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		10.3290(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
fosaprepitant
fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid.		3.2310(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
phosphoramide;
triazoles		antiemetic;
neurokinin-1 receptor antagonist;
prodrug
tegaserod maleate
[no description available]		2.0810maleate saltserotonergic agonist
rifabutin
[no description available]		4.0940
xav939
XAV939: selectively inhibits beta-catenin-mediated transcription; structure in first source. XAV939 : A thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group.		2.520(trifluoromethyl)benzenes;
thiopyranopyrimidine		tankyrase inhibitor
2-carboxyarabinitol 1-phosphate
[no description available]		2.0810
trypan blue
Trypan Blue: A diazo-naphthalene sulfonate that is widely used as a stain.. trypan blue : An organosulfonate salt that is the tetrasodium salt of 3,3'-[(3,3'-dimethylbiphenyl-4,4'-diyl)didiazene-2,1-diyl]bis(5-amino-4-hydroxynaphthalene-2,7-disulfonic acid).		2.0610
nintedanib
nintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.		7.8830
methylnitronitrosoguanidine
Methylnitronitrosoguanidine: A nitrosoguanidine derivative with potent mutagenic and carcinogenic properties.. N-methyl-N'-nitro-N-nitrosoguanidine : An N-nitroguanidine compound having nitroso and methyl substituents at the N'-position		2.9440nitroso compoundalkylating agent
l 742694
L 742694: a neurokinin-1 receptor antagonist; structure given in first source		2.0410
cupferron
cupferron: superoxide dismutase inhibitor; RN given refers to parent cpd; structure		7.520
hydrazinocurcumin
hydrazinocurcumin: structure in first source. hydrazinocurcumin : A pyrazole obtained by cyclocodensation of the two carbonyl groups of curcumin with hydrazine.		2.0210aromatic ether;
olefinic compound;
polyphenol;
pyrazoles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
alpha-cyclopiazonic acid
[no description available]		3.3510alpha-cyclopiazonic acids
ver 52296
luminespib : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(2,4-dihydroxy-5-isopropylphenyl)-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxylic acid with the amino group of ethylamine.		2.0810aromatic amide;
isoxazoles;
monocarboxylic acid amide;
morpholines;
resorcinols		angiogenesis inhibitor;
antineoplastic agent;
Hsp90 inhibitor
levomefolate calcium
levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid.		3.2310organic calcium saltantidepressant
sb-590885
N-{5-[2-{4-[2-(dimethylamino)ethoxy]phenyl}-4-(pyridin-4-yl)-1H-imidazol-5-yl]-2,3-dihydro-1H-inden-1-ylidene}hydroxylamine : A ketoxime that is the oxime of indan-1-one in which the hydrogen at position 5 has been replaced by an imidazol-5-yl group which has itself been substituted at positions 2 and 4 by p-[2-(dimethylamino)ethoxy]phenyl and pyridin-4-yl groups, respectively.		2.0810aromatic ether;
imidazoles;
ketoxime;
pyridines;
tertiary amino compound
pf-477736
PF 00477736: a Chk1 inhibitor; structure in first source. PF-00477736 : A diazepinoindole that is 8-amino-4,5-dihydro-6H-[1,2]diazepino[4,5,6-cd]indol-6-one which is substituted at position 2 by a 1-methylpyrazol-4-yl group and in which the amino group at position 8 has undergone condensation with the carboxy group of (2R)-2-cyclohexylglycine to give the corresponding carboxamide. It is an inhibitor of checkpoint kinase 1 (Chk 1).		2.0810
fenobam
fenobam: in USAN fenobam refers to monohydrate		2.0810ureas
cholestyramine resin
Cholestyramine Resin: A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.		3.3911
eye
[no description available]		2.4820
maltodextrin
maltodextrin : A dextrin in which the D-glucose units are linked by alpha-(1->4) glycosidic bonds.		2.0810
acetylcellulose
acetylcellulose: coating compound. cellulose acetate : A glucan derivative obtained through the esterification of cellulose by acetic anhydride or acetic acid, resulting in the substitution of some of the hydroxy groups of cellulose by acetyl groups. It is used in a variety of applications including base material for photographic film, clothing, membrane filters, coatings, food packaging, and as a frame material for eyeglasses.		2.1710
concanavalin a
Concanavalin A: A MANNOSE/GLUCOSE binding lectin isolated from the jack bean (Canavalia ensiformis). It is a potent mitogen used to stimulate cell proliferation in lymphocytes, primarily T-lymphocyte, cultures.		7.5220
trypsinogen
Trypsinogen: The inactive proenzyme of trypsin secreted by the pancreas, activated in the duodenum via cleavage by enteropeptidase. (Stedman, 25th ed)		2.0110
leptin
Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.		2.7430
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		3.1950
phenanthrenes
Phenanthrenes: POLYCYCLIC AROMATIC HYDROCARBONS composed of three fused BENZENE rings.. phenanthrenes : Any benzenoid aromatic compound that consists of a phenanthrene skeleton and its substituted derivatives thereof.		2.4920
ConditionIndicatedRelationship StrengthStudiesTrials
Adjuvant Arthritis
[description not available]		010.1642
Rheumatoid Arthritis
[description not available]		018.417634
Allodynia
[description not available]		08.97512
Arthritis, Degenerative
[description not available]		020.8426176
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		120.417634
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		122.8426176
Anasarca
[description not available]		013.311815
Pyrexia
[description not available]		07.86231
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		013.311815
Fever
An abnormal elevation of body temperature, usually as a result of a pathologic process.		012.86231
Polyarthritis
[description not available]		017.0711717
Arthritis
Acute or chronic inflammation of JOINTS.		017.0711717
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		013.063473
Foot Diseases
Anatomical and functional disorders affecting the foot.		0210
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		06.13113
Innate Inflammatory Response
[description not available]		018.425834
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		120.425834
Ache
[description not available]		020.822778
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		122.822778
Gastroduodenal Ulcer
[description not available]		015.646618
Peptic Ulcer
Ulcer that occurs in the regions of the GASTROINTESTINAL TRACT which come into contact with GASTRIC JUICE containing PEPSIN and GASTRIC ACID. It occurs when there are defects in the MUCOSA barrier. The common forms of peptic ulcers are associated with HELICOBACTER PYLORI and the consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		120.3513236
Acute Disease
Disease having a short and relatively severe course.		011.484611
Intraocular Pressure
The pressure of the fluids in the eye.		02.4620
Gastric Ulcer
[description not available]		013.21816
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		013.21816
Gastritis
Inflammation of the GASTRIC MUCOSA, a lesion observed in a number of unrelated disorders.		03.6490
Cancer of Prostate
[description not available]		013.979320
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		115.979320
Cancer of Colon
[description not available]		012.341226
Colonic Neoplasms
Tumors or cancer of the COLON.		118.3136618
Diseases, Metabolic
[description not available]		02.9410
Metabolic Diseases
Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)		02.9410
Chronic Illness
[description not available]		016.846841
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		016.846841
Granulomas
[description not available]		03.6990
Granuloma
A relatively small nodular inflammatory lesion containing grouped mononuclear phagocytes, caused by infectious and noninfectious agents.		03.6990
Ulcer
A lesion on the surface of the skin or a mucous surface, produced by the sloughing of inflammatory necrotic tissue.		04.58230
Extravascular Hemolysis
[description not available]		03.3360
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		03.3360
Adverse Drug Event
[description not available]		017.59289
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		012.59289
Primary Peritonitis
[description not available]		03.78100
Peritonitis
INFLAMMATION of the PERITONEUM lining the ABDOMINAL CAVITY as the result of infectious, autoimmune, or chemical processes. Primary peritonitis is due to infection of the PERITONEAL CAVITY via hematogenous or lymphatic spread and without intra-abdominal source. Secondary peritonitis arises from the ABDOMINAL CAVITY itself through RUPTURE or ABSCESS of intra-abdominal organs.		08.78100
Degenerative Diseases, Central Nervous System
[description not available]		05.0791
Neurodegenerative Diseases
Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.		05.0791
Pleurisy
INFLAMMATION of PLEURA, the lining of the LUNG. When PARIETAL PLEURA is involved, there is pleuritic CHEST PAIN.		02.9440
Acute Liver Injury, Drug-Induced
[description not available]		09.68332
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		09.68332
Brucella Infection
[description not available]		03.8721
Brucellosis
Infection caused by bacteria of the genus BRUCELLA mainly involving the MONONUCLEAR PHAGOCYTE SYSTEM. This condition is characterized by fever, weakness, malaise, and weight loss.		08.8721
Disease
A definite pathologic process with a characteristic set of signs and symptoms. It may affect the whole body or any of its parts, and its etiology, pathology, and prognosis may be known or unknown.		02.0510
Breast Cancer
[description not available]		016.5114441
Breast Neoplasms
Tumors or cancer of the human BREAST.		122.79432123
Encephalitis, Polio
[description not available]		02.0610
Poliomyelitis
An acute infectious disease of humans, particularly children, caused by any of three serotypes of human poliovirus (POLIOVIRUS). Usually the infection is limited to the gastrointestinal tract and nasopharynx, and is often asymptomatic. The central nervous system, primarily the spinal cord, may be affected, leading to rapidly progressive paralysis, coarse FASCICULATION and hyporeflexia. Motor neurons are primarily affected. Encephalitis may also occur. The virus replicates in the nervous system, and may cause significant neuronal loss, most notably in the spinal cord. A rare related condition, nonpoliovirus poliomyelitis, may result from infections with nonpoliovirus enteroviruses. (From Adams et al., Principles of Neurology, 6th ed, pp764-5)		02.0610
Infections, Salmonella
[description not available]		02.0610
Benign Neoplasms
[description not available]		016.5411419
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		121.2422838
Inflammatory Breast Cancer
[description not available]		02.5220
Inflammatory Breast Neoplasms
Metastatic breast cancer characterized by EDEMA and ERYTHEMA of the affected breast due to LYMPHATIC METASTASIS and eventual obstruction of LYMPHATIC VESSELS by the cancer cells.		02.5220
Constriction, Pathological
[description not available]		05.4751
Constriction, Pathologic
The condition of an anatomical structure's being constricted beyond normal dimensions.		05.4751
B16 Melanoma
[description not available]		03.3660
Lung Injury, Acute
[description not available]		02.0710
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		02.0710
Dermatomycoses
Superficial infections of the skin or its appendages by any of various fungi.		02.0710
Scalp Dermatoses
Skin diseases involving the SCALP.		02.0710
Granulocytic Leukemia
[description not available]		02.0710
Leukemia, Myeloid
Form of leukemia characterized by an uncontrolled proliferation of the myeloid lineage and their precursors (MYELOID PROGENITOR CELLS) in the bone marrow and other sites.		02.0710
Angiogenesis, Pathologic
[description not available]		014.329410
American Trypanosomiasis
[description not available]		02.0810
Chagas Disease
Infection with the protozoan parasite TRYPANOSOMA CRUZI, a form of TRYPANOSOMIASIS endemic in Central and South America. It is named after the Brazilian physician Carlos Chagas, who discovered the parasite. Infection by the parasite (positive serologic result only) is distinguished from the clinical manifestations that develop years later, such as destruction of PARASYMPATHETIC GANGLIA; CHAGAS CARDIOMYOPATHY; and dysfunction of the ESOPHAGUS or COLON.		02.0810
Leishmania Infection
[description not available]		02.4620
Leishmaniasis
A disease caused by any of a number of species of protozoa in the genus LEISHMANIA. There are four major clinical types of this infection: cutaneous (Old and New World) (LEISHMANIASIS, CUTANEOUS), diffuse cutaneous (LEISHMANIASIS, DIFFUSE CUTANEOUS), mucocutaneous (LEISHMANIASIS, MUCOCUTANEOUS), and visceral (LEISHMANIASIS, VISCERAL).		02.4620
Cancer of Cervix
[description not available]		011.2247
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		115.734814
Nerve Pain
[description not available]		05.11150
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		17.11150
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		020.919650
Carcinoma, Non-Small Cell Lung
[description not available]		016.478834
Cancer of Lung
[description not available]		018.318050
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		118.478834
Lung Neoplasms
Tumors or cancer of the LUNG.		120.318050
Vibrio cholerae Infection
[description not available]		02.4620
Cholera
An acute diarrheal disease endemic in India and Southeast Asia whose causative agent is VIBRIO CHOLERAE. This condition can lead to severe dehydration in a matter of hours unless quickly treated.		02.4620
Cronobacter Infections
[description not available]		02.1310
Enterobacteriaceae Infections
Infections with bacteria of the family ENTEROBACTERIACEAE.		02.1310
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
Dermatitis
Any inflammation of the skin.		04.3770
Acute Confusional Senile Dementia
[description not available]		014.835021
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		116.835021
Dermatoses
[description not available]		06.6362
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		06.6362
Congenital Zika Syndrome
[description not available]		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Colorectal Cancer
[description not available]		019.3417357
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		125.69519171
Apoplexy
[description not available]		09.86242
Acute Ischemic Stroke
[description not available]		02.4110
Cerebral Ischemia
[description not available]		03.4870
Ischemic Stroke
Stroke due to BRAIN ISCHEMIA resulting in interruption or reduction of blood flow to a part of the brain. When obstruction is due to a BLOOD CLOT formed within in a cerebral blood vessel it is a thrombotic stroke. When obstruction is formed elsewhere and moved to block a cerebral blood vessel (see CEREBRAL EMBOLISM) it is referred to as embolic stroke. Wake-up stroke refers to ischemic stroke occurring during sleep while cryptogenic stroke refers to ischemic stroke of unknown origin.		02.4110
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		03.4870
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		111.86242
Astrocytoma, Grade IV
[description not available]		010.45305
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		112.45305
Nasopharyngeal Carcinoma
A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.		03.570
Cancer of Nasopharynx
[description not available]		07.05162
Nasopharyngeal Neoplasms
Tumors or cancer of the NASOPHARYNX.		19.05162
Necrotizing Enterocolitis
[description not available]		07.4920
Enterocolitis, Necrotizing
ENTEROCOLITIS with extensive ulceration (ULCER) and NECROSIS. It is observed primarily in LOW BIRTH WEIGHT INFANT.		02.4920
Osteoarthritis of Knee
[description not available]		026.3216112
Osteoarthritis, Knee
Noninflammatory degenerative disease of the knee joint consisting of three large categories: conditions that block normal synchronous movement, conditions that produce abnormal pathways of motion, and conditions that cause stress concentration resulting in changes to articular cartilage. (Crenshaw, Campbell's Operative Orthopaedics, 8th ed, p2019)		123.3216112
Cruveilhier-Baumgarten Syndrome
Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS.		02.8330
Hypertension, Portal
Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.		02.8330
Adenomatous Polyposis Coli, Familial
[description not available]		014.334511
Adenomatous Polyposis Coli
A polyposis syndrome due to an autosomal dominant mutation of the APC genes (GENES, APC) on CHROMOSOME 5. The syndrome is characterized by the development of hundreds of ADENOMATOUS POLYPS in the COLON and RECTUM of affected individuals by early adulthood.		119.019022
Bone Spur
[description not available]		02.8630
ACL Injuries
[description not available]		0542
Plica Syndrome
[description not available]		03.3460
Synovitis
Inflammation of the SYNOVIAL MEMBRANE.		03.3460
Cardiac Toxicity
[description not available]		09.8960
Cardiotoxicity
Damage to the HEART or its function secondary to exposure to toxic substances such as drugs used in CHEMOTHERAPY; IMMUNOTHERAPY; or RADIATION.		09.8960
Arthritis, Juvenile Chronic
[description not available]		07.8282
Autoimmune Disease
[description not available]		03.3860
Colitis Gravis
[description not available]		06.96142
Bowel Diseases, Inflammatory
[description not available]		04.2360
Hypogammaglobulinemia
[description not available]		02.3110
Common Variable Hypogammaglobulinemia
[description not available]		02.3110
Agammaglobulinemia
An immunologic deficiency state characterized by an extremely low level of generally all classes of gamma-globulin in the blood.		02.3110
Arthritis, Juvenile
Arthritis in children, with onset before 16 years of age. The terms juvenile rheumatoid arthritis (JRA) and juvenile idiopathic arthritis (JIA) refer to classification systems for chronic arthritis in children. Only one subtype of juvenile arthritis (polyarticular-onset, rheumatoid factor-positive) clinically resembles adult rheumatoid arthritis and is considered its childhood equivalent.		19.8282
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		03.3860
Colitis, Ulcerative
Inflammation of the COLON that is predominantly confined to the MUCOSA. Its major symptoms include DIARRHEA, rectal BLEEDING, the passage of MUCUS, and ABDOMINAL PAIN.		06.96142
Inflammatory Bowel Diseases
Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.		04.2360
Common Variable Immunodeficiency
Heterogeneous group of immunodeficiency syndromes characterized by hypogammaglobulinemia of most isotypes, variable B-cell defects, and the presence of recurrent bacterial infections.		02.3110
Microsatellite Instability
The occurrence of highly polymorphic mono- and dinucleotide MICROSATELLITE REPEATS in somatic cells. It is a form of genome instability associated with defects in DNA MISMATCH REPAIR.		010.4322
Lymph Node Metastasis
[description not available]		08.1154
Cancer of Mouth
[description not available]		011.34396
Mouth Neoplasms
Tumors or cancer of the MOUTH.		113.34396
2019 Novel Coronavirus Disease
[description not available]		05.7551
Acute Post-operative Pain
[description not available]		021.91264188
Coxarthrosis
[description not available]		016.685322
Pain, Postoperative
Pain during the period after surgery.		021.91264188
Osteoarthritis, Hip
Noninflammatory degenerative disease of the hip joint which usually appears in late middle or old age. It is characterized by growth or maturational disturbances in the femoral neck and head, as well as acetabular dysplasia. A dominant symptom is pain on weight-bearing or motion.		118.685322
Disease Exacerbation
[description not available]		016.079531
Cytokine Release Syndrome
A severe immune reaction characterized by excessive release of CYTOKINES. Symptoms include DYSPNEA; FEVER; HEADACHE; HYPOTENSION; NAUSEA; RASH; TACHYCARDIA; HYPOXIA; HYPERFERRITINEMIA, and MULTIPLE ORGAN FAILURE. It is associated with viral infections, SEPSIS; AUTOIMMUNE DISEASES and a variety of factors used in IMMUNOTHERAPY.		03.2310
Dementia Praecox
[description not available]		014.773932
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		116.773932
Adenoma, Basal Cell
[description not available]		014.855425
Adenoma
A benign epithelial tumor with a glandular organization.		116.855425
Peritoneal Carcinomatosis
[description not available]		06.34104
Appendiceal Cancer
[description not available]		04.231
Local Neoplasm Recurrence
[description not available]		014.646127
Appendiceal Neoplasms
Tumors or cancer of the APPENDIX.		04.231
Peritoneal Neoplasms
Tumors or cancer of the PERITONEUM.		18.34104
Pain, Chronic
[description not available]		012.09228
Low Back Ache
[description not available]		013.32713
Low Back Pain
Acute or chronic pain in the lumbar or sacral regions, which may be associated with musculo-ligamentous SPRAINS AND STRAINS; INTERVERTEBRAL DISK DISPLACEMENT; and other conditions.		115.32713
Chronic Pain
Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain.		119.09228
Arthritis, Spinal
[description not available]		04.3731
Ectopic Ossification
[description not available]		09.84253
Temporomandibular Disorders
[description not available]		06.2241
Temporomandibular Joint Disorders
A variety of conditions affecting the anatomic and functional characteristics of the temporomandibular joint. Factors contributing to the complexity of temporomandibular diseases are its relation to dentition and mastication and the symptomatic effects in other areas which account for referred pain to the joint and the difficulties in applying traditional diagnostic procedures to temporomandibular joint pathology where tissue is rarely obtained and x-rays are often inadequate or nonspecific. Common diseases are developmental abnormalities, trauma, subluxation, luxation, arthritis, and neoplasia. (From Thoma's Oral Pathology, 6th ed, pp577-600)		18.2241
Adenocarcinoma, Basal Cell
[description not available]		013.79628
Neoplastic Processes
The pathological mechanisms and forms taken by tissue during degeneration into a neoplasm and its subsequent activity.		02.4110
Invasiveness, Neoplasm
[description not available]		09.32448
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		013.79628
Pericementitis
[description not available]		05.692
Periodontitis
Inflammation and loss of connective tissues supporting or surrounding the teeth. This may involve any part of the PERIODONTIUM. Periodontitis is currently classified by disease progression (CHRONIC PERIODONTITIS; AGGRESSIVE PERIODONTITIS) instead of age of onset. (From 1999 International Workshop for a Classification of Periodontal Diseases and Conditions, American Academy of Periodontology)		05.692
Anankastic Personality
[description not available]		06.2843
Obsessive-Compulsive Disorder
An anxiety disorder characterized by recurrent, persistent obsessions or compulsions. Obsessions are the intrusive ideas, thoughts, or images that are experienced as senseless or repugnant. Compulsions are repetitive and seemingly purposeful behavior which the individual generally recognizes as senseless and from which the individual does not derive pleasure although it may provide a release from tension.		18.2843
Schistosoma mansoni Infection
[description not available]		07.7620
Schistosomiasis mansoni
Schistosomiasis caused by Schistosoma mansoni. It is endemic in Africa, the Middle East, South America, and the Caribbean and affects mainly the bowel, spleen, and liver.		07.7620
ER-Negative PR-Negative HER2-Negative Breast Cancer
[description not available]		03.2230
Triple Negative Breast Neoplasms
Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.		03.2230
Anhedonia
Inability to experience pleasure due to impairment or dysfunction of normal psychological and neurobiological mechanisms. It is a symptom of many PSYCHOTIC DISORDERS (e.g., DEPRESSIVE DISORDER, MAJOR; and SCHIZOPHRENIA).		02.4110
Depression
Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.		010.752811
Cephalgia Syndromes
[description not available]		03.4520
Bilateral Headache
[description not available]		06.9182
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		011.9182
Headache Disorders
Various conditions with the symptom of HEADACHE. Headache disorders are classified into major groups, such as PRIMARY HEADACHE DISORDERS (based on characteristics of their headache symptoms) and SECONDARY HEADACHE DISORDERS (based on their etiologies). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)		08.4520
Addiction, Opioid
[description not available]		06.2661
Opioid-Related Disorders
Disorders related to or resulting from abuse or misuse of OPIOIDS.		06.2661
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		011.084610
Tendinitis
Inflammation of TENDONS. It is characterized by the degeneration of tendons accompanied by an inflammatory repair response, fibroblastic proliferation, and formation of granulation tissue. Tendinitis is not a clinical diagnosis and can be confirmed only by histopathological findings.		09.5851
Tendinopathy
Clinical syndrome describing overuse tendon injuries characterized by a combination of PAIN, diffuse or localized swelling, and impaired performance.		09.5851
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		05.0952
Pneumonia
Infection of the lung often accompanied by inflammation.		05.0952
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		04.9860
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		04.9860
Labor, Premature
[description not available]		05.7373
Brain Inflammation
[description not available]		09.5551
Delayed Effects, Prenatal Exposure
[description not available]		02.5820
Encephalitis
Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.		04.5551
Atrophy, Muscle
[description not available]		03.0730
Muscular Atrophy
Derangement in size and number of muscle fibers occurring with aging, reduction in blood supply, or following immobilization, prolonged weightlessness, malnutrition, and particularly in denervation.		03.0730
Brain Swelling
[description not available]		06.8651
Brain Hemorrhage, Cerebral
[description not available]		07.7281
Brain Edema
Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)		011.8651
Cerebral Hemorrhage
Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.		19.7281
Hematoma
A collection of blood outside the BLOOD VESSELS. Hematoma can be localized in an organ, space, or tissue.		08.7130
Chemotherapy-Induced Acral Erythema
[description not available]		010.651311
Hand-Foot Syndrome
Chemotherapy-induced dermal side effects that are associated with the use of various CYTOSTATIC AGENTS. Symptoms range from mild ERYTHEMA and/or PARESTHESIA to severe ulcerative dermatitis with debilitating pain involving typically palmoplantar and intertriginous areas. These cutaneous manifestations are sometimes accompanied by nail anomalies.		112.651311
Esophageal Squamous Cell Carcinoma
A carcinoma that originates usually from cells on the surface of the middle and lower third of the ESOPHAGUS. Tumor cells exhibit typical squamous morphology and form large polypoid lesions. Mutations in RNF6, LZTS1, TGFBR2, DEC1, and WWOX1 genes are associated with this cancer.		03.9721
Cancer of Esophagus
[description not available]		011.663110
Esophageal Neoplasms
Tumors or cancer of the ESOPHAGUS.		113.663110
Acute Bacterial Prostatitis
[description not available]		04.7761
Pelvic Pain
Pain in the pelvic region of genital and non-genital origin.		09.6251
Cystitis
Inflammation of the URINARY BLADDER, either from bacterial or non-bacterial causes. Cystitis is usually associated with painful urination (dysuria), increased frequency, urgency, and suprapubic pain.		02.4110
Prostatitis
Infiltration of inflammatory cells into the parenchyma of PROSTATE. The subtypes are classified by their varied laboratory analysis, clinical presentation and response to treatment.		04.7761
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		011.23448
Cancer of Stomach
[description not available]		010.636513
Stomach Neoplasms
Tumors or cancer of the STOMACH.		010.636513
Complication, Postoperative
[description not available]		010.61295
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		010.61295
Blood Pressure, High
[description not available]		013.567112
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		115.567112
Fatty Liver, Nonalcoholic
[description not available]		03.2450
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		08.2450
Recrudescence
[description not available]		012.763414
Drug Withdrawal Symptoms
[description not available]		03.811
Cannabis Abuse
[description not available]		03.811
Marijuana Abuse
Use of marijuana associated with abnormal psychological, social, and or occupational functioning.		03.811
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		03.811
Hyperlipemia
[description not available]		03.2250
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		03.2250
Acute Pain
Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing.		115.9273
Alopecia Cicatrisata
[description not available]		02.4820
Abdominal Migraine
[description not available]		05.4172
Alopecia
Absence of hair from areas where it is normally present.		02.4820
Migraine Disorders
A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)		17.4172
Craniofacial Pain
[description not available]		06.8251
Facial Pain
Pain in the facial region including orofacial pain and craniofacial pain. Associated conditions include local inflammatory and neoplastic disorders and neuralgic syndromes involving the trigeminal, facial, and glossopharyngeal nerves. Conditions which feature recurrent or persistent facial pain as the primary manifestation of disease are referred to as FACIAL PAIN SYNDROMES.		113.8251
Colitis
Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.		04.19160
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		04.35170
Ankylosing Spondylarthritis
[description not available]		012.042511
Spondylitis, Ankylosing
A chronic inflammatory condition affecting the axial joints, such as the SACROILIAC JOINT and other intervertebral or costovertebral joints. It occurs predominantly in young males and is characterized by pain and stiffness of joints (ANKYLOSIS) with inflammation at tendon insertions.		114.042511
ALS - Amyotrophic Lateral Sclerosis
[description not available]		07.8193
Amyotrophic Lateral Sclerosis
A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94)		19.8193
Libman-Sacks Disease
[description not available]		05.13100
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		05.13100
Acute Kidney Failure
[description not available]		06.6181
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		011.6181
Adrenal Cancer
[description not available]		02.7630
Pheochromocytoma, Extra-Adrenal
[description not available]		02.5120
Pheochromocytoma
A usually benign, well-encapsulated, lobular, vascular tumor of chromaffin tissue of the ADRENAL MEDULLA or sympathetic paraganglia. The cardinal symptom, reflecting the increased secretion of EPINEPHRINE and NOREPINEPHRINE, is HYPERTENSION, which may be persistent or intermittent. During severe attacks, there may be HEADACHE; SWEATING, palpitation, apprehension, TREMOR; PALLOR or FLUSHING of the face, NAUSEA and VOMITING, pain in the CHEST and ABDOMEN, and paresthesias of the extremities. The incidence of malignancy is as low as 5% but the pathologic distinction between benign and malignant pheochromocytomas is not clear. (Dorland, 27th ed; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1298)		02.5120
Carcinoma, Squamous Cell of Head and Neck
[description not available]		05.7361
Carcinoma, Epidermoid
[description not available]		014.118718
Cancer of Head
[description not available]		012.33511
Squamous Cell Carcinoma of Head and Neck
The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.		17.7361
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		014.118718
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		114.33511
Gout
Metabolic disorder characterized by recurrent acute arthritis, hyperuricemia and deposition of sodium urate in and around the joints, sometimes with formation of URIC ACID calculi.		15.8840
Edema-Proteinuria-Hypertension Gestosis
[description not available]		03.1440
Pre-Eclampsia
A complication of PREGNANCY, characterized by a complex of symptoms including maternal HYPERTENSION and PROTEINURIA with or without pathological EDEMA. Symptoms may range between mild and severe. Pre-eclampsia usually occurs after the 20th week of gestation, but may develop before this time in the presence of trophoblastic disease.		110.1440
Cardiac Death
[description not available]		03.3340
Disc, Herniated
[description not available]		07.4376
Intervertebral Disc Displacement
An INTERVERTEBRAL DISC in which the NUCLEUS PULPOSUS has protruded through surrounding ANNULUS FIBROSUS. This occurs most frequently in the lower lumbar region.		07.4376
Degenerative Disc Disease
[description not available]		05.1681
Intervertebral Disc Degeneration
Degenerative changes in the INTERVERTEBRAL DISC due to aging or structural damage, especially to the vertebral end-plates.		010.1681
Allergy, Drug
[description not available]		011.164316
Airway Hyper-Responsiveness
[description not available]		03.8721
Drug Hypersensitivity
Immunologically mediated adverse reactions to medicinal substances used legally or illegally.		011.164316
Respiratory Tract Diseases
Diseases involving the RESPIRATORY SYSTEM.		03.8230
Adenoma, Prostatic
[description not available]		05.8842
Hyperplasia
An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.		010.06145
Prostatic Hyperplasia
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.		112.8842
Dermatitis Medicamentosa
[description not available]		09.58335
Exanthem
[description not available]		05.7471
Exanthema
Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.		05.7471
Malignant Melanoma
[description not available]		09.75265
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		111.75265
Pyogenic Sacroiliitis
[description not available]		02.610
Chronic Insomnia
[description not available]		02.610
Agitation, Psychomotor
[description not available]		02.610
Spondylisthesis
[description not available]		02.610
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		06.0852
Sleep Initiation and Maintenance Disorders
Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition.		02.610
Psychomotor Agitation
A feeling of restlessness associated with increased motor activity. This may occur as a manifestation of nervous system drug toxicity or other conditions.		02.610
Autism Spectrum Disorder
Wide continuum of associated cognitive and neurobehavioral disorders, including, but not limited to, three core-defining features: impairments in socialization, impairments in verbal and nonverbal communication, and restricted and repetitive patterns of behaviors. (from DSM-V)		03.5210
Allergic Reaction
[description not available]		02.4920
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		02.4920
Pus
[description not available]		03.9911
Hypomania
[description not available]		03.9911
Affective Psychosis, Bipolar
[description not available]		012.612612
Bipolar Disorder
A major affective disorder marked by severe mood swings (manic or major depressive episodes) and a tendency to remission and recurrence.		114.612612
Indigestion
[description not available]		08.25126
Dyspepsia
Impaired digestion, especially after eating.		08.25126
Injuries, Tendon
[description not available]		09.0994
Hepatocellular Carcinoma
[description not available]		08.85431
Cancer of Liver
[description not available]		012.215710
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		110.85431
Liver Neoplasms
Tumors or cancer of the LIVER.		114.215710
Autoimmune Chronic Hepatitis
[description not available]		02.610
Hepatitis, Autoimmune
A chronic self-perpetuating hepatocellular INFLAMMATION of unknown cause, usually with HYPERGAMMAGLOBULINEMIA and serum AUTOANTIBODIES.		02.610
Nerve Root Avulsion
[description not available]		03.4120
Radiculopathy
Disease involving a spinal nerve root (see SPINAL NERVE ROOTS) which may result from compression related to INTERVERTEBRAL DISK DISPLACEMENT; SPINAL CORD INJURIES; SPINAL DISEASES; and other conditions. Clinical manifestations include radicular pain, weakness, and sensory loss referable to structures innervated by the involved nerve root.		03.4120
Spinal Stenosis
Narrowing of the spinal canal.		09.1121
Cytomegalic Inclusion Disease
[description not available]		02.610
Cytomegalovirus Infections
Infection with CYTOMEGALOVIRUS, characterized by enlarged cells bearing intranuclear inclusions. Infection may be in almost any organ, but the salivary glands are the most common site in children, as are the lungs in adults.		02.610
Cytomegalovirus
A genus of the family HERPESVIRIDAE, subfamily BETAHERPESVIRINAE, infecting the salivary glands, liver, spleen, lungs, eyes, and other organs, in which they produce characteristically enlarged cells with intranuclear inclusions. Infection with Cytomegalovirus is also seen as an opportunistic infection in AIDS.		02.7930
Anterior Cervical Pain
[description not available]		02.5220
Hyperkyphosis
[description not available]		02.610
Lordosis
The anterior concavity in the curvature of the lumbar and cervical spine as viewed from the side. The term usually refers to abnormally increased curvature (hollow back, saddle back, swayback). It does not include lordosis as normal mating posture in certain animals ( = POSTURE + SEX BEHAVIOR, ANIMAL).		02.610
Neck Pain
Discomfort or more intense forms of pain that are localized to the cervical region. This term generally refers to pain in the posterior or lateral regions of the neck.		02.5220
Hyperoxia
An abnormal increase in the amount of oxygen in the tissues and organs.		07.9740
Chronic Lung Injury
[description not available]		02.610
Angioneurotic Edema
[description not available]		06.184
Hives
[description not available]		06.75135
Angioedema
Swelling involving the deep DERMIS, subcutaneous, or submucosal tissues, representing localized EDEMA. Angioedema often occurs in the face, lips, tongue, and larynx.		011.184
Urticaria
A vascular reaction of the skin characterized by erythema and wheal formation due to localized increase of vascular permeability. The causative mechanism may be allergy, infection, or stress.		06.75135
Astrocytosis
[description not available]		02.610
Aqueductal Stenosis
[description not available]		02.610
Depression, Involutional
Form of depression in those MIDDLE AGE with feelings of ANXIETY.		010.42127
Depressive Disorder, Major
Disorder in which five (or more) of the following symptoms have been present during the same 2-week period and represent a change from previous functioning; at least one of the symptoms is either (1) depressed mood or (2) loss of interest or pleasure. Symptoms include: depressed mood most of the day, nearly every daily; markedly diminished interest or pleasure in activities most of the day, nearly every day; significant weight loss when not dieting or weight gain; Insomnia or hypersomnia nearly every day; psychomotor agitation or retardation nearly every day; fatigue or loss of energy nearly every day; feelings of worthlessness or excessive or inappropriate guilt; diminished ability to think or concentrate, or indecisiveness, nearly every day; or recurrent thoughts of death, recurrent suicidal ideation without a specific plan, or a suicide attempt. (DSM-5)		112.42127
Aura
[description not available]		02.5420
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.5420
Koch's Disease
[description not available]		04.0721
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		111.0721
Bone Cancer
[description not available]		014.74265
Osteogenic Sarcoma
[description not available]		04.93130
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		09.74265
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		04.93130
Cirrhosis, Liver
[description not available]		06.23172
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		011.23172
Pulmonary Consumption
[description not available]		02.4920
Tuberculosis, Pulmonary
MYCOBACTERIUM infections of the lung.		02.4920
Cirrhosis
[description not available]		04.6290
Contracture
Prolonged shortening of the muscle or other soft tissue around a joint, preventing movement of the joint.		07.8830
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		09.6290
Lymphatic Abnormalities
Congenital or acquired structural abnormalities of the lymphatic system (LYMPHOID TISSUE) including the lymph vessels.		02.2110
Airway Obstruction
Any hindrance to the passage of air into and out of the lungs.		02.4620
Dysphagia
[description not available]		04.8721
Deglutition Disorders
Difficulty in SWALLOWING which may result from neuromuscular disorder or mechanical obstruction. Dysphagia is classified into two distinct types: oropharyngeal dysphagia due to malfunction of the PHARYNX and UPPER ESOPHAGEAL SPHINCTER; and esophageal dysphagia due to malfunction of the ESOPHAGUS.		04.8721
Metastase
[description not available]		017.365212
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		012.365212
Acute Onset Aura Migraine
[description not available]		02.2110
Migraine with Aura
A subtype of migraine disorder, characterized by recurrent attacks of reversible neurological symptoms (aura) that precede or accompany the headache. Aura may include a combination of sensory disturbances, such as blurred VISION; HALLUCINATIONS; VERTIGO; NUMBNESS; and difficulty in concentrating and speaking. Aura is usually followed by features of the COMMON MIGRAINE, such as PHOTOPHOBIA; PHONOPHOBIA; and NAUSEA. (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)		02.2110
Chemical Dependence
[description not available]		02.2110
Substance-Related Disorders
Disorders related to substance use or abuse.		02.2110
Infections, Staphylococcal
[description not available]		03.0440
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		03.0440
Cancer of Pancreas
[description not available]		012.686013
Carcinoma, Ductal, Pancreatic
[description not available]		04.8471
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		114.686013
Carcinoma, Pancreatic Ductal
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.		04.8471
Femoracetabular Impingement
A pathological mechanical process that can lead to hip failure. It is caused by abnormalities of the ACETABULUM and/or FEMUR combined with rigorous hip motion, leading to repetitive collisions that damage the soft tissue structures.		04.0421
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		014.814219
Refractory Depression
[description not available]		05.9922
Depressive Disorder, Treatment-Resistant
Failure to respond to two or more trials of antidepressant monotherapy or failure to respond to four or more trials of different antidepressant therapies. (Campbell's Psychiatric Dictionary, 9th ed.)		05.9922
Amyotrophy, Thenar, Of Carpal Origin
[description not available]		04.3741
Carpal Tunnel Syndrome
Entrapment of the MEDIAN NERVE in the carpal tunnel, which is formed by the flexor retinaculum and the CARPAL BONES. This syndrome may be associated with repetitive occupational trauma (CUMULATIVE TRAUMA DISORDERS); wrist injuries; AMYLOID NEUROPATHIES; rheumatoid arthritis (see ARTHRITIS, RHEUMATOID); ACROMEGALY; PREGNANCY; and other conditions. Symptoms include burning pain and paresthesias involving the ventral surface of the hand and fingers which may radiate proximally. Impairment of sensation in the distribution of the median nerve and thenar muscle atrophy may occur. (Joynt, Clinical Neurology, 1995, Ch51, p45)		04.3741
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		03.99130
Testicular Diseases
Pathological processes of the TESTIS.		02.5920
Morbid Obesity
[description not available]		05.1431
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		02.4920
Obesity, Morbid
The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.		05.1431
Idiopathic Parkinson Disease
[description not available]		04.1631
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		04.1631
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		112.42131
Cancer of the Tongue
[description not available]		04.35190
Tongue Neoplasms
Tumors or cancer of the TONGUE.		04.35190
Pain, Breakthrough
[description not available]		03.5720
Breakthrough Pain
Acute pain that comes on rapidly despite the use of pain medication.		03.5720
Androgen-Independent Prostatic Cancer
[description not available]		04.2431
Prostatic Neoplasms, Castration-Resistant
Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.		16.2431
Cancer of Ovary
[description not available]		08.83265
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		113.887815
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		05.6232
6th Nerve Palsy
[description not available]		02.2510
Diplopia
A visual symptom in which a single object is perceived by the visual cortex as two objects rather than one. Disorders associated with this condition include REFRACTIVE ERRORS; STRABISMUS; OCULOMOTOR NERVE DISEASES; TROCHLEAR NERVE DISEASES; ABDUCENS NERVE DISEASES; and diseases of the BRAIN STEM and OCCIPITAL LOBE.		02.2510
Herpes Zoster, Ocular
[description not available]		02.2510
Herpes Zoster Ophthalmicus
Virus infection of the Gasserian ganglion and its nerve branches characterized by pain and vesicular eruptions with much swelling. Ocular involvement is usually heralded by a vesicle on the tip of the nose. This area is innervated by the nasociliary nerve.		02.2510
Benign Neoplasms, Brain
[description not available]		010.885010
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		112.885010
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		03.2150
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		03.2150
Joint Pain
[description not available]		011.442412
Arthralgia
Pain in the joint.		011.442412
Cholera Infantum
[description not available]		018.5811243
Inflammatory Pseudotumor
[description not available]		02.2510
Granuloma, Plasma Cell
A slow-growing benign pseudotumor in which plasma cells greatly outnumber the inflammatory cells.		02.2510
Glial Cell Tumors
[description not available]		06.58252
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		18.58252
Epithelial Ovarian Cancer
[description not available]		05.6963
Carcinoma, Ovarian Epithelial
A malignant neoplasm that originates in cells on the surface EPITHELIUM of the ovary and is the most common form of ovarian cancer. There are five histologic subtypes: papillary serous, endometrioid, mucinous, clear cell, and transitional cell. Mutations in BRCA1, OPCML, PRKN, PIK3CA, AKT1, CTNNB1, RRAS2, and CDH1 genes are associated with this cancer.		05.6963
Lymphangiomyomatosis
[description not available]		04.5511
Lymphangioleiomyomatosis
A disease characterized by the progressive invasion of SMOOTH MUSCLE CELLS into the LYMPHATIC VESSELS, and the BLOOD VESSELS. The majority of the cases occur in the LUNGS of women of child-bearing age, eventually blocking the flow of air, blood, and lymph. The common symptom is shortness of breath (DYSPNEA).		111.5511
Injuries
Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.		02.2510
Wounds and Injuries
Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.		14.2510
Desmoid
[description not available]		03.4770
Fibromatosis, Aggressive
A childhood counterpart of abdominal or extra-abdominal desmoid tumors, characterized by firm subcutaneous nodules that grow rapidly in any part of the body but do not metastasize. The adult form of abdominal fibromatosis is FIBROMATOSIS, ABDOMINAL. (Stedman, 25th ed)		03.4770
Arthropathies
[description not available]		05.341
Joint Diseases
Diseases involving the JOINTS.		05.341
Acute Edematous Pancreatitis
[description not available]		05.79112
Pancreatitis
INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.		05.79112
Burns
Injuries to tissues caused by contact with heat, steam, chemicals (BURNS, CHEMICAL), electricity (BURNS, ELECTRIC), or the like.		02.2510
Cancer of Skin
[description not available]		011.41477
Skin Neoplasms
Tumors or cancer of the SKIN.		011.41477
Menstruation, Painful
[description not available]		06.0252
Dysmenorrhea
Painful menstruation.		18.0252
Amentia
[description not available]		03.4220
Bleeding
[description not available]		05.2680
Cardiovascular Stroke
[description not available]		013.59743
Dementia
An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.		03.4220
Hemorrhage
Bleeding or escape of blood from a vessel.		112.2680
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		013.59743
Endometrial Diseases
[description not available]		07.8354
Uterine Diseases
Pathological processes involving any part of the UTERUS.		07.8354
Urogenital Prolapse
[description not available]		02.2510
Pelvic Organ Prolapse
Abnormal descent of a pelvic organ resulting in the protrusion of the organ beyond its normal anatomical confines. Symptoms often include vaginal discomfort, DYSPAREUNIA; URINARY STRESS INCONTINENCE; and FECAL INCONTINENCE.		02.2510
Gastric Diseases
[description not available]		05.9491
Infections, Coronavirus
[description not available]		03.5720
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		02.2510
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		03.5720
Bone Marrow Diseases
Diseases involving the BONE MARROW.		02.5520
Bone Diseases
Diseases of BONES.		05.3441
Injuries, Spinal Cord
[description not available]		02.2510
Spinal Cord Injuries
Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).		02.2510
Remission, Spontaneous
A spontaneous diminution or abatement of a disease over time, without formal treatment.		03.6411
HPV Infection
[description not available]		06.8364
Infections, Respiratory
[description not available]		05.1552
Respiratory Tract Infections
Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases.		05.1552
Papillomavirus Infections
Neoplasms of the skin and mucous membranes caused by papillomaviruses. They are usually benign but some have a high risk for malignant progression.		18.8364
Weight Reduction
[description not available]		0340
Weight Loss
Decrease in existing BODY WEIGHT.		0340
Cancer of Intestines
[description not available]		05.9791
Intestinal Neoplasms
Tumors or cancer of the INTESTINES.		05.9791
Abdominal Aortic Aneurysm
[description not available]		07.9840
Aortic Aneurysm, Abdominal
An abnormal balloon- or sac-like dilatation in the wall of the ABDOMINAL AORTA which gives rise to the visceral, the parietal, and the terminal (iliac) branches below the aortic hiatus at the diaphragm.		02.9840
Affective Disorders
[description not available]		02.2510
Mood Disorders
Those disorders that have a disturbance in mood as their predominant feature.		02.2510
Bladder Cancer
[description not available]		08.9285
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		110.9285
Impotence
[description not available]		02.520
Erectile Dysfunction
The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.		07.520
Colitis-Associated Cancer
[description not available]		02.3110
Carcinoma, Anaplastic
[description not available]		08.34263
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		08.34263
Atherosclerotic Parkinsonism
[description not available]		02.3110
Parkinson Disease, Secondary
Conditions which feature clinical manifestations resembling primary Parkinson disease that are caused by a known or suspected condition. Examples include parkinsonism caused by vascular injury, drugs, trauma, toxin exposure, neoplasms, infections and degenerative or hereditary conditions. Clinical features may include bradykinesia, rigidity, parkinsonian gait, and masked facies. In general, tremor is less prominent in secondary parkinsonism than in the primary form. (From Joynt, Clinical Neurology, 1998, Ch38, pp39-42)		02.3110
Cerebral Infarction, Middle Cerebral Artery
[description not available]		02.6320
Infarction, Middle Cerebral Artery
NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.		02.6320
Aortic Stenosis
[description not available]		02.2510
Calcification, Pathologic
[description not available]		02.8330
Aortic Valve Stenosis
A pathological constriction that can occur above (supravalvular stenosis), below (subvalvular stenosis), or at the AORTIC VALVE. It is characterized by restricted outflow from the LEFT VENTRICLE into the AORTA.		02.2510
Calcinosis
Pathologic deposition of calcium salts in tissues.		02.8330
Aspirin Induced Asthma
[description not available]		02.3110
Radius Fractures
Fractures of the RADIUS.		03.811
Inguinal Hernia
[description not available]		08.711
Hernia, Inguinal
An abdominal hernia with an external bulge in the GROIN region. It can be classified by the location of herniation. Indirect inguinal hernias occur through the internal inguinal ring. Direct inguinal hernias occur through defects in the ABDOMINAL WALL (transversalis fascia) in Hesselbach's triangle. The former type is commonly seen in children and young adults; the latter in adults.		03.711
Bone Loss, Osteoclastic
[description not available]		04.08140
Cardiac Remodeling, Ventricular
[description not available]		03.1750
Bone Fractures
[description not available]		04.9221
Fracture, Pathologic
[description not available]		04.6211
Aseptic Necrosis of Bone
[description not available]		04.6211
Intra-Articular Fractures
Fractures of the articular surface of a bone.		04.6211
Osteonecrosis
Death of a bone or part of a bone, either atraumatic or posttraumatic.		04.6211
Fractures, Bone
Breaks in bones.		04.9221
Cirrhoses, Experimental Liver
[description not available]		03.4570
Enlarged Spleen
[description not available]		02.3110
Hangman Fracture
[description not available]		03.711
Spinal Fractures
Broken bones in the vertebral column.		03.711
Anxiety Neuroses
[description not available]		02.3110
Anxiety Disorders
Persistent and disabling ANXIETY.		07.3110
Enthesopathy
A disorder occurring at the site of insertion of TENDONS or LIGAMENTS into bones or JOINT CAPSULES.		02.3110
Psoriasis Arthropathica
[description not available]		04.3741
Arthritis, Psoriatic
A type of inflammatory arthritis associated with PSORIASIS, often involving the axial joints and the peripheral terminal interphalangeal joints. It is characterized by the presence of HLA-B27-associated SPONDYLARTHROPATHY, and the absence of rheumatoid factor.		04.3741
Emesis, Postoperative
[description not available]		013.042622
Postoperative Nausea and Vomiting
Emesis and queasiness occurring after anesthesia.		013.042622
Diabetes Mellitus, Adult-Onset
[description not available]		04.6861
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		04.6861
Acute Brain Injuries
[description not available]		02.4620
Hemorrhage, Subarachnoid
[description not available]		02.5520
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		02.4620
Subarachnoid Hemorrhage
Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.		02.5520
Central Nervous System Disease
[description not available]		03.2310
Central Nervous System Diseases
Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.		03.2310
B-Cell Lymphoma
[description not available]		0340
Lymphoma, B-Cell
A group of heterogeneous lymphoid tumors generally expressing one or more B-cell antigens or representing malignant transformations of B-lymphocytes.		0340
Emesis
[description not available]		05.0531
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		08.7384
Vomiting
The forcible expulsion of the contents of the STOMACH through the MOUTH.		05.0531
Urinary Retention
Inability to empty the URINARY BLADDER with voiding (URINATION).		08.8721
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		08.71385
Chondromalacia
Softening and degeneration of the CARTILAGE.		03.5311
Cartilage Diseases
Pathological processes involving the chondral tissue (CARTILAGE).		03.5311
Long Sleeper Syndrome
[description not available]		04.4511
Sleep Wake Disorders
Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle.		04.4511
Ewing Sarcoma
[description not available]		06.5252
Sarcoma, Ewing
A malignant tumor of the bone which always arises in the medullary tissue, occurring more often in cylindrical bones. The tumor occurs usually before the age of 20, about twice as frequently in males as in females.		06.5252
Hemorrhage, Peptic Ulcer
[description not available]		08.7146
Alloxan Diabetes
[description not available]		03.6590
Hematochezia
The passage of bright red blood from the rectum. The blood may or may not be mixed with formed stool in the form of blood, blood clots, bloody stool or diarrhea.		012.56397
Gastrointestinal Hemorrhage
Bleeding in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.		012.56397
Intestinal Diseases
Pathological processes in any segment of the INTESTINE from DUODENUM to RECTUM.		06.0574
Cancer-Associated Pain
[description not available]		04.4922
Cancer Pain
Pain that may be caused by or related to cellular, tissue, and systemic changes that occur during NEOPLASM growth, tissue invasion, and METASTASIS.		09.4922
Carcinoma, Oat Cell
[description not available]		06.6541
Carcinoma, Small Cell
An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)		06.6541
Interstitial Nephritis
[description not available]		04.5490
Nephritis, Interstitial
Inflammation of the interstitial tissue of the kidney. This term is generally used for primary inflammation of KIDNEY TUBULES and/or surrounding interstitium. For primary inflammation of glomerular interstitium, see GLOMERULONEPHRITIS. Infiltration of the inflammatory cells into the interstitial compartment results in EDEMA, increased spaces between the tubules, and tubular renal dysfunction.		04.5490
Back Ache
[description not available]		07.673
Back Pain
Acute or chronic pain located in the posterior regions of the THORAX; LUMBOSACRAL REGION; or the adjacent regions.		114.673
Condition, Preneoplastic
[description not available]		012.773812
Precancerous Conditions
Pathological conditions that tend eventually to become malignant.		012.773812
Cachexia
General ill health, malnutrition, and weight loss, usually associated with chronic disease.		09.941610
Hepato-Pulmonary Syndrome
[description not available]		02.1510
Hepatopulmonary Syndrome
A syndrome characterized by the clinical triad of advanced chronic liver disease, pulmonary vascular dilatations, and reduced arterial oxygenation (HYPOXEMIA) in the absence of intrinsic cardiopulmonary disease. This syndrome is common in the patients with LIVER CIRRHOSIS or portal hypertension (HYPERTENSION, PORTAL).		02.1510
Cancer of the Thymus
[description not available]		03.0910
Thymus Neoplasms
Tumors or cancer of the THYMUS GLAND.		03.0910
Blood Loss, Surgical
Loss of blood during a surgical procedure.		010.3129
Anesthesia
A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.		04.4511
Break-Bone Fever
[description not available]		02.1510
Dengue
An acute febrile disease transmitted by the bite of AEDES mosquitoes infected with DENGUE VIRUS. It is self-limiting and characterized by fever, myalgia, headache, and rash. SEVERE DENGUE is a more virulent form of dengue.		07.1510
Choroid Neovascularization
[description not available]		02.4820
Age-Related Macular Degeneration
[description not available]		03.940
Macular Degeneration
Degenerative changes in the RETINA usually of older adults which results in a loss of vision in the center of the visual field (the MACULA LUTEA) because of damage to the retina. It occurs in dry and wet forms.		15.940
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		07.76231
Cancer of Larynx
[description not available]		04.3670
Laryngeal Neoplasms
Cancers or tumors of the LARYNX or any of its parts: the GLOTTIS; EPIGLOTTIS; LARYNGEAL CARTILAGES; LARYNGEAL MUSCLES; and VOCAL CORDS.		04.3670
Encephalopathy, Toxic
[description not available]		02.5320
Rheumatism
[description not available]		05.76110
Rheumatic Diseases
Disorders of connective tissue, especially the joints and related structures, characterized by inflammation, degeneration, or metabolic derangement.		17.76110
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		09.34149
Acropachy, Hereditary
[description not available]		02.1510
Hypertrophy
General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).		02.4720
Adenocarcinoma, Alveolar
[description not available]		02.1510
Adenocarcinoma, Bronchiolo-Alveolar
A carcinoma derived from epithelium of terminal bronchioles, in which the neoplastic tissue extends along the alveolar walls and grows in small masses within the alveoli. Involvement may be uniformly diffuse and massive, or nodular, or lobular. The neoplastic cells are cuboidal or columnar and form papillary structures. Mucin may be demonstrated in some of the cells and in the material in the alveoli, which also includes denuded cells. Metastases in regional lymph nodes, and in even more distant sites, are known to occur, but are infrequent. (From Stedman, 25th ed)		02.1510
Out-of-Hospital Cardiac Arrest
Occurrence of heart arrest in an individual when there is no immediate access to medical personnel or equipment.		02.1510
Cognitive Decline
[description not available]		07.8430
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		02.8430
Autosomal Dominant Juvenile Parkinson Disease
[description not available]		02.4920
Parkinsonian Disorders
A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.		02.4920
Arteriosclerosis, Coronary
[description not available]		07.5184
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		07.5184
Hypercalciuria
Excretion of abnormally high level of CALCIUM in the URINE, greater than 4 mg/kg/day.		02.1510
Aldosteronism with Hyperplasia of the Adrenal Cortex
[description not available]		02.4920
Extramembranous Glomerulopathy
[description not available]		02.4620
Glomerulonephritis, Membranous
A type of glomerulonephritis that is characterized by the accumulation of immune deposits (COMPLEMENT MEMBRANE ATTACK COMPLEX) on the outer aspect of the GLOMERULAR BASEMENT MEMBRANE. It progresses from subepithelial dense deposits, to basement membrane reaction and eventual thickening of the basement membrane.		02.4620
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		18.71121
Altitude Hypoxia
Low ambient oxygen tension associated with ALTITUDE.		02.1510
Altitude Sickness
Multiple symptoms associated with reduced oxygen at high ALTITUDE.		02.1510
Musculoskeletal Pain
Discomfort stemming from muscles, LIGAMENTS, tendons, and bones.		05.6832
Herpes Simplex Virus Infection
[description not available]		02.1710
Herpes Simplex
A group of acute infections caused by herpes simplex virus type 1 or type 2 that is characterized by the development of one or more small fluid-filled vesicles with a raised erythematous base on the skin or mucous membrane. It occurs as a primary infection or recurs due to a reactivation of a latent infection. (Dorland, 27th ed.)		02.1710
De Quervain Disease
Stenosing tenosynovitis of the abductor pollicis longus and extensor pollicis brevis tendons in the first dorsal wrist compartment. The presenting symptoms are usually pain and tenderness at the radial styloid. The cause is almost always related to OVERUSE INJURY or is associated with RHEUMATOID ARTHRITIS.		02.1710
Ganglion Cysts
Nodular tumor-like lesions or mucoid flesh, arising from tendon sheaths, LIGAMENTS, or JOINT CAPSULE, especially of the hands, wrists, or feet. They are not true cysts as they lack epithelial wall. They are distinguished from SYNOVIAL CYSTS by the lack of communication with a joint cavity or the SYNOVIAL MEMBRANE.		02.1710
Flexor Tendon Entrapment
[description not available]		02.1710
Anochlesia
[description not available]		02.1710
Nervous System Disorders
[description not available]		07.9774
Nervous System Diseases
Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.		07.9774
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		09.36156
Atherogenesis
[description not available]		06.25121
Atheroma
[description not available]		03.4220
Aortic Diseases
Pathological processes involving any part of the AORTA.		02.5720
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		06.25121
Cervix Dysplasia
[description not available]		07.2642
Uterine Cervical Dysplasia
Abnormal development of immature squamous EPITHELIAL CELLS of the UTERINE CERVIX, a term used to describe premalignant cytological changes in the cervical EPITHELIUM. These atypical cells do not penetrate the epithelial BASEMENT MEMBRANE.		07.2642
Cancer of Gastrointestinal Tract
[description not available]		07.1982
Anorexia
The lack or loss of APPETITE accompanied by an aversion to food and the inability to eat. It is the defining characteristic of the disorder ANOREXIA NERVOSA.		07.1354
Weight Gain
Increase in BODY WEIGHT over existing weight.		05.5244
Asthma, Bronchial
[description not available]		08.5166
Symptom Cluster
[description not available]		08.14104
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		08.5166
Nasal Polyps
Focal accumulations of EDEMA fluid in the NASAL MUCOSA accompanied by HYPERPLASIA of the associated submucosal connective tissue. Polyps may be NEOPLASMS, foci of INFLAMMATION, degenerative lesions, or malformations.		02.1710
Syndrome
A characteristic symptom complex.		08.14104
Congenital Limb Deformities
[description not available]		02.1710
Hallux Abductovalgus
[description not available]		03.9121
Fibrodysplasia Ossificans Progressiva
[description not available]		02.1710
Hallux Valgus
Lateral displacement of the great toe (HALLUX), producing deformity of the first METATARSOPHALANGEAL JOINT with callous, bursa, or BUNION formation over the bony prominence.		03.9121
Myositis Ossificans
A disease characterized by bony deposits or the ossification of muscle tissue.		02.1710
Benign Psychomotor Epilepsy, Childhood
[description not available]		02.520
Absence Seizure
[description not available]		06.14111
Epilepsy, Temporal Lobe
A localization-related (focal) form of epilepsy characterized by recurrent seizures that arise from foci within the TEMPORAL LOBE, most commonly from its mesial aspect. A wide variety of psychic phenomena may be associated, including illusions, hallucinations, dyscognitive states, and affective experiences. The majority of complex partial seizures (see EPILEPSY, COMPLEX PARTIAL) originate from the temporal lobes. Temporal lobe seizures may be classified by etiology as cryptogenic, familial, or symptomatic. (From Adams et al., Principles of Neurology, 6th ed, p321).		02.520
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		011.14111
Experimental Neoplasms
[description not available]		06.44151
Papilloma, Squamous Cell
[description not available]		05.661
Papilloma
A circumscribed benign epithelial tumor projecting from the surrounding surface; more precisely, a benign epithelial neoplasm consisting of villous or arborescent outgrowths of fibrovascular stroma covered by neoplastic cells. (Stedman, 25th ed)		112.661
Varicocele
A condition characterized by the dilated tortuous veins of the SPERMATIC CORD with a marked left-sided predominance. Adverse effect on male fertility occurs when varicocele leads to an increased scrotal (and testicular) temperature and reduced testicular volume.		07.1710
Glenoid Labral Tears
[description not available]		03.5611
Rotator Cuff Injuries
Injuries to the ROTATOR CUFF of the shoulder joint.		15.5611
Carcinoma, Ductal, Breast
An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST.		06.9474
Itching
[description not available]		05.8342
Dermatitis, Radiation-Induced
[description not available]		03.8521
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		010.8342
Radiodermatitis
A cutaneous inflammatory reaction occurring as a result of exposure to ionizing radiation.		03.8521
Experimental Hepatoma
[description not available]		03.5680
Adenomatous Polyps
Benign neoplasms derived from glandular epithelium. (From Stedman, 25th ed)		012.392117
Polyps
Discrete abnormal tissue masses that protrude into the lumen of the DIGESTIVE TRACT or the RESPIRATORY TRACT. Polyps can be spheroidal, hemispheroidal, or irregular mound-shaped structures attached to the MUCOUS MEMBRANE of the lumen wall either by a stalk, pedunculus, or by a broad base.		03.5611
Becker Muscular Dystrophy
[description not available]		02.1710
Muscular Dystrophy, Duchenne
An X-linked recessive muscle disease caused by an inability to synthesize DYSTROPHIN, which is involved with maintaining the integrity of the sarcolemma. Muscle fibers undergo a process that features degeneration and regeneration. Clinical manifestations include proximal weakness in the first few years of life, pseudohypertrophy, cardiomyopathy (see MYOCARDIAL DISEASES), and an increased incidence of impaired mentation. Becker muscular dystrophy is a closely related condition featuring a later onset of disease (usually adolescence) and a slowly progressive course. (Adams et al., Principles of Neurology, 6th ed, p1415)		02.1710
Cholangiocellular Carcinoma
[description not available]		03.6490
Cholangiocarcinoma
A malignant tumor arising from the epithelium of the BILE DUCTS.		03.6490
Cyst
[description not available]		02.5220
Actinic Keratosis
[description not available]		05.341
Cancer, Radiation-Induced
[description not available]		04.5590
Keratosis, Actinic
White or pink lesions on the arms, hands, face, or scalp that arise from sun-induced DNA DAMAGE to KERATINOCYTES in exposed areas. They are considered precursor lesions to superficial SQUAMOUS CELL CARCINOMA.		17.341
Epithelial Neoplasms
[description not available]		05.1352
Camurati-Engelmann Disease
[description not available]		03.0910
Osteoid Osteoma
[description not available]		03.6930
Osteomyelitis
INFLAMMATION of the bone as a result of infection. It may be caused by a variety of infectious agents, especially pyogenic (PUS - producing) BACTERIA.		03.0910
Cancer of Endometrium
[description not available]		04.1531
Endometrial Neoplasms
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.		04.1531
Lung Adenocarcinoma
[description not available]		02.1710
Adenocarcinoma of Lung
A carcinoma originating in the lung and the most common lung cancer type in never-smokers. Malignant cells exhibit distinct features such as glandular epithelial, or tubular morphology. Mutations in KRAS, EGFR, BRAF, and ERBB2 genes are associated with this cancer.		02.1710
Enteritis
Inflammation of any segment of the SMALL INTESTINE.		02.1710
Liver Steatosis
[description not available]		08.4770
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		08.4770
Sarcoma, Epithelioid
[description not available]		02.5220
Carcinosarcoma
A malignant neoplasm that contains elements of carcinoma and sarcoma so extensively intermixed as to indicate neoplasia of epithelial and mesenchymal tissue. (Stedman, 25th ed)		02.1710
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		14.5220
Carcinoma, Transitional Cell
A malignant neoplasm derived from TRANSITIONAL EPITHELIAL CELLS, occurring chiefly in the URINARY BLADDER; URETERS; or RENAL PELVIS.		07.19112
Injury, Ischemia-Reperfusion
[description not available]		09.23225
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		09.23225
Bile Duct Obstruction
[description not available]		04.3370
MODS
[description not available]		03.1450
Cholangitis
Inflammation of the biliary ductal system (BILE DUCTS); intrahepatic, extrahepatic, or both.		02.2110
Cholestasis
Impairment of bile flow due to obstruction in small bile ducts (INTRAHEPATIC CHOLESTASIS) or obstruction in large bile ducts (EXTRAHEPATIC CHOLESTASIS).		09.3370
Multiple Organ Failure
A progressive condition usually characterized by combined failure of several organs such as the lungs, liver, kidney, along with some clotting mechanisms, usually postinjury or postoperative.		03.1450
Vascular Diseases
Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.		04.4322
Teeth, Impacted
[description not available]		07.3455
Patellar Dislocation
Displacement of the PATELLA from the femoral groove.		03.5911
Disbacteriosis
[description not available]		02.5420
Infections, Paramyxoviridae
[description not available]		02.2110
Paramyxoviridae Infections
Infections with viruses of the family PARAMYXOVIRIDAE. This includes MORBILLIVIRUS INFECTIONS; RESPIROVIRUS INFECTIONS; PNEUMOVIRUS INFECTIONS; HENIPAVIRUS INFECTIONS; AVULAVIRUS INFECTIONS; and RUBULAVIRUS INFECTIONS.		02.2110
Ovarian Hyperstimulation Syndrome, Familial Gestational Spontaneous
[description not available]		02.2110
Ovarian Hyperstimulation Syndrome
A complication of OVULATION INDUCTION in infertility treatment. It is graded by the severity of symptoms which include OVARY enlargement, multiple OVARIAN FOLLICLES; OVARIAN CYSTS; ASCITES; and generalized EDEMA. The full-blown syndrome may lead to RENAL FAILURE, respiratory distress, and even DEATH. Increased capillary permeability is caused by the vasoactive substances, such as VASCULAR ENDOTHELIAL GROWTH FACTORS, secreted by the overly-stimulated OVARIES.		02.2110
Dermatosclerosis
[description not available]		02.2110
Sclerosis, Systemic
[description not available]		02.4620
Scleroderma, Localized
A term used to describe a variety of localized asymmetrical SKIN thickening that is similar to those of SYSTEMIC SCLERODERMA but without the disease features in the multiple internal organs and BLOOD VESSELS. Lesions may be characterized as patches or plaques (morphea), bands (linear), or nodules.		02.2110
Scleroderma, Systemic
A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.		02.4620
Bleb
[description not available]		02.5720
Cancer of the Fallopian Tube
[description not available]		04.4722
Fallopian Tube Neoplasms
Benign or malignant neoplasms of the FALLOPIAN TUBES. They are uncommon. If they develop, they may be located in the wall or within the lumen as a growth attached to the wall by a stalk.		04.4722
Acute Myelogenous Leukemia
[description not available]		0340
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		0340
Cockayne-Touraine Disease
[description not available]		02.2510
Epidermolysis Bullosa Dystrophica
Form of epidermolysis bullosa characterized by atrophy of blistered areas, severe scarring, and nail changes. It is most often present at birth or in early infancy and occurs in both autosomal dominant and recessive forms. All forms of dystrophic epidermolysis bullosa result from mutations in COLLAGEN TYPE VII, a major component fibrils of BASEMENT MEMBRANE and EPIDERMIS.		02.2510
Calcium Pyrophosphate Deposition Disease
[description not available]		02.2110
Necrotizing Pyelonephritis
[description not available]		02.2110
Discitis
Inflammation of an INTERVERTEBRAL DISC or disk space which may lead to disk erosion. Until recently, discitis has been defined as a nonbacterial inflammation and has been attributed to aseptic processes (e.g., chemical reaction to an injected substance). However, recent studies provide evidence that infection may be the initial cause, but perhaps not the promoter, of most cases of discitis. Discitis has been diagnosed in patients following discography, myelography, lumbar puncture, paravertebral injection, and obstetrical epidural anesthesia. Discitis following chemonucleolysis (especially with chymopapain) is attributed to chemical reaction by some and to introduction of microorganisms by others.		02.2110
Chondrocalcinosis
Presence of CALCIUM PYROPHOSPHATE in the connective tissues such as the cartilaginous structures of joints. When accompanied by GOUT-like symptoms, it is referred to as pseudogout.		02.2110
Pyelonephritis
Inflammation of the KIDNEY involving the renal parenchyma (the NEPHRONS); KIDNEY PELVIS; and KIDNEY CALICES. It is characterized by ABDOMINAL PAIN; FEVER; NAUSEA; VOMITING; and occasionally DIARRHEA.		02.2110
Cells, Neoplasm Circulating
[description not available]		05.4653
Bronchopulmonary Dysplasia
A chronic lung disease developed after OXYGEN INHALATION THERAPY or mechanical ventilation (VENTILATION, MECHANICAL) usually occurring in certain premature infants (INFANT, PREMATURE) or newborn infants with respiratory distress syndrome (RESPIRATORY DISTRESS SYNDROME, NEWBORN). Histologically, it is characterized by the unusual abnormalities of the bronchioles, such as METAPLASIA, decrease in alveolar number, and formation of CYSTS.		02.0810
CACH Syndrome
[description not available]		02.0810
B Virus Infection
[description not available]		02.0810
Active Hyperemia
[description not available]		08.0565
Hyperemia
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).		08.0565
Blood Loss, Postoperative
[description not available]		06.0552
Deep Vein Thrombosis
[description not available]		05.4451
Venous Thrombosis
The formation or presence of a blood clot (THROMBUS) within a vein.		05.4451
Alveolitis, Fibrosing
[description not available]		03.6430
Pulmonary Fibrosis
A process in which normal lung tissues are progressively replaced by FIBROBLASTS and COLLAGEN causing an irreversible loss of the ability to transfer oxygen into the bloodstream via PULMONARY ALVEOLI. Patients show progressive DYSPNEA finally resulting in death.		08.6430
Carcinoma, Lobular
A type of BREAST CANCER where the abnormal malignant cells form in the lobules, or milk-producing glands, of the breast.		05.6332
Infections, Helicobacter
[description not available]		09.28197
Helicobacter Infections
Infections with organisms of the genus HELICOBACTER, particularly, in humans, HELICOBACTER PYLORI. The clinical manifestations are focused in the stomach, usually the gastric mucosa and antrum, and the upper duodenum. This infection plays a major role in the pathogenesis of type B gastritis and peptic ulcer disease.		09.28197
Experimental Mammary Neoplasms
[description not available]		04.9340
HMN (Hereditary Motor Neuropathy) Proximal Type I
[description not available]		02.0810
Spinal Muscular Atrophies of Childhood
A group of recessive inherited diseases that feature progressive muscular atrophy and hypotonia. They are classified as type I (Werdnig-Hoffman disease), type II (intermediate form), and type III (Kugelberg-Welander disease). Type I is fatal in infancy, type II has a late infantile onset and is associated with survival into the second or third decade. Type III has its onset in childhood, and is slowly progressive. (J Med Genet 1996 Apr:33(4):281-3)		02.0810
Lentiginosis, Perioral
[description not available]		03.6630
Peutz-Jeghers Syndrome
A hereditary disease caused by autosomal dominant mutations involving CHROMOSOME 19. It is characterized by the presence of INTESTINAL POLYPS, consistently in the JEJUNUM, and mucocutaneous pigmentation with MELANIN spots of the lips, buccal MUCOSA, and digits.		03.6630
Lymphoma of Mucosa-Associated Lymphoid Tissue
[description not available]		02.110
Lymphoma, B-Cell, Marginal Zone
Extranodal lymphoma of lymphoid tissue associated with mucosa that is in contact with exogenous antigens. Many of the sites of these lymphomas, such as the stomach, salivary gland, and thyroid, are normally devoid of lymphoid tissue. They acquire mucosa-associated lymphoid tissue (MALT) type as a result of an immunologically mediated disorder.		02.110
Bile Duct Cancer
[description not available]		03.1250
Bile Duct Neoplasms
Tumors or cancer of the BILE DUCTS.		03.1250
Histoplasma capsulatum Infection
[description not available]		07.0810
Histoplasmosis
Infection resulting from exposure to the fungus HISTOPLASMA. It is worldwide in distribution and particularly common in the central and eastern states, especially areas around the Ohio and Mississippi River valleys.		02.0810
Amnesia-Memory Loss
[description not available]		02.0810
Behavior Disorders
[description not available]		02.4520
Amnesia
Pathologic partial or complete loss of the ability to recall past experiences (AMNESIA, RETROGRADE) or to form new memories (AMNESIA, ANTEROGRADE). This condition may be of organic or psychologic origin. Organic forms of amnesia are usually associated with dysfunction of the DIENCEPHALON or HIPPOCAMPUS. (From Adams et al., Principles of Neurology, 6th ed, pp426-7)		02.0810
Mental Disorders
Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function.		02.4520
Gouty Arthritis
[description not available]		09.1531
Arthritis, Gouty
Arthritis, especially of the great toe, as a result of gout. Acute gouty arthritis often is precipitated by trauma, infection, surgery, etc. The initial attacks are usually monoarticular but later attacks are often polyarticular. Acute and chronic gouty arthritis are associated with accumulation of MONOSODIUM URATE in and around affected joints.		04.1531
Intestinal Polyps
Discrete abnormal tissue masses that protrude into the lumen of the INTESTINE. A polyp is attached to the intestinal wall either by a stalk, pedunculus, or by a broad base.		07.3393
FMR1-Related Primary Ovarian Insufficiency
[description not available]		02.0810
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		010.9493
Menopause
The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.		04.1231
Primary Ovarian Insufficiency
Cessation of ovarian function after MENARCHE but before the age of 40, without or with OVARIAN FOLLICLE depletion. It is characterized by the presence of OLIGOMENORRHEA or AMENORRHEA, elevated GONADOTROPINS, and low ESTRADIOL levels. It is a state of female HYPERGONADOTROPIC HYPOGONADISM. Etiologies include genetic defects, autoimmune processes, chemotherapy, radiation, and infections. The most commonly known genetic cause is the expansion of a CGG repeat to 55 to 199 copies in the 5' untranslated region in the X-linked FMR1 gene.		02.0810
Preterm Birth
[description not available]		02.7630
Premature Birth
CHILDBIRTH before 37 weeks of PREGNANCY (259 days from the first day of the mother's last menstrual period, or 245 days after FERTILIZATION).		02.7630
Genetic Predisposition
[description not available]		08.24133
Diabetic Retinopathy
Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.		05.7371
Nociceptive Pain
Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.		03.4220
Deficiency, Pyridoxine
[description not available]		04.3911
Amyloid Deposits
[description not available]		02.4420
Conjunctival Diseases
Diseases involving the CONJUNCTIVA.		02.110
Uveitis
Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)		02.520
Cancer of Duodenum
[description not available]		05.2121
Lower Urinary Tract Symptom
[description not available]		04.4422
Anaplastic Astrocytoma
[description not available]		02.7730
Astrocytoma
Neoplasms of the brain and spinal cord derived from glial cells which vary from histologically benign forms to highly anaplastic and malignant tumors. Fibrillary astrocytomas are the most common type and may be classified in order of increasing malignancy (grades I through IV). In the first two decades of life, astrocytomas tend to originate in the cerebellar hemispheres; in adults, they most frequently arise in the cerebrum and frequently undergo malignant transformation. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2013-7; Holland et al., Cancer Medicine, 3d ed, p1082)		07.7730
Adhesive Capsulitis
[description not available]		04.422
Bursitis
Inflammation or irritation of a SYNOVIAL BURSA, the fibrous sac that acts as a cushion between moving structures of bones, muscles, tendons or skin.		09.422
Acne Inversa
[description not available]		0310
Hidradenitis Suppurativa
A chronic suppurative and cicatricial disease of the apocrine glands occurring chiefly in the axillae in women and in the groin and anal regions in men. It is characterized by poral occlusion with secondary bacterial infection, evolving into abscesses which eventually rupture. As the disease becomes chronic, ulcers appear, sinus tracts enlarge, fistulas develop, and fibrosis and scarring become evident.		0310
Keratoacanthoma
A benign, non-neoplastic, usually self-limiting epithelial lesion closely resembling squamous cell carcinoma clinically and histopathologically. It occurs in solitary, multiple, and eruptive forms. The solitary and multiple forms occur on sunlight exposed areas and are identical histologically; they affect primarily white males. The eruptive form usually involves both sexes and appears as a generalized papular eruption.		02.110
Cancer of the Thyroid
[description not available]		06.5261
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		06.5261
Carcinoma, Neuroendocrine
A group of carcinomas which share a characteristic morphology, often being composed of clusters and trabecular sheets of round blue cells, granular chromatin, and an attenuated rim of poorly demarcated cytoplasm. Neuroendocrine tumors include carcinoids, small (oat) cell carcinomas, medullary carcinoma of the thyroid, Merkel cell tumor, cutaneous neuroendocrine carcinoma, pancreatic islet cell tumors, and pheochromocytoma. Neurosecretory granules are found within the tumor cells. (Segen, Dictionary of Modern Medicine, 1992)		02.4920
Allergic Encephalomyelitis
[description not available]		02.4620
MS (Multiple Sclerosis)
[description not available]		02.4820
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		07.4820
Cerebral Primitive Neuroectodermal Tumor
[description not available]		02.7330
Brain Stem Neoplasms, Primary
[description not available]		02.7730
Benign Cerebellar Neoplasms
[description not available]		02.9940
Anterior Circulation Transient Ischemic Attack
[description not available]		02.7330
Arachnoidal Cerebellar Sarcoma, Circumscribed
[description not available]		03.3360
Anaplastic Ependymoma
[description not available]		02.0810
Adult Optic Nerve Glioma
[description not available]		02.0810
Choroid Plexus Neoplasms, Primary
[description not available]		02.0810
Ischemic Attack, Transient
Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)		02.7330
Ependymoma
Glioma derived from EPENDYMOGLIAL CELLS that tend to present as malignant intracranial tumors in children and as benign intraspinal neoplasms in adults. It may arise from any level of the ventricular system or central canal of the spinal cord. Intracranial ependymomas most frequently originate in the FOURTH VENTRICLE and histologically are densely cellular tumors which may contain ependymal tubules and perivascular pseudorosettes. Spinal ependymomas are usually benign papillary or myxopapillary tumors. (From DeVita et al., Principles and Practice of Oncology, 5th ed, p2018; Escourolle et al., Manual of Basic Neuropathology, 2nd ed, pp28-9)		02.0810
Medulloblastoma
A malignant neoplasm that may be classified either as a glioma or as a primitive neuroectodermal tumor of childhood (see NEUROECTODERMAL TUMOR, PRIMITIVE). The tumor occurs most frequently in the first decade of life with the most typical location being the cerebellar vermis. Histologic features include a high degree of cellularity, frequent mitotic figures, and a tendency for the cells to organize into sheets or form rosettes. Medulloblastoma have a high propensity to spread throughout the craniospinal intradural axis. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2060-1)		15.3360
Choroid Plexus Neoplasms
Benign or malignant tumors which arise from the choroid plexus of the ventricles of the brain. Papillomas (see PAPILLOMA, CHOROID PLEXUS) and carcinomas are the most common histologic subtypes, and tend to seed throughout the ventricular and subarachnoid spaces. Clinical features include headaches, ataxia and alterations of consciousness, primarily resulting from associated HYDROCEPHALUS. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2072; J Neurosurg 1998 Mar;88(3):521-8)		02.0810
Neuroectodermal Tumors, Primitive
A group of malignant tumors of the nervous system that feature primitive cells with elements of neuronal and/or glial differentiation. Use of this term is limited by some authors to central nervous system tumors and others include neoplasms of similar origin which arise extracranially (i.e., NEUROECTODERMAL TUMORS, PRIMITIVE, PERIPHERAL). This term is also occasionally used as a synonym for MEDULLOBLASTOMA. In general, these tumors arise in the first decade of life and tend to be highly malignant. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2059)		02.7330
Brain Stem Neoplasms
Benign and malignant intra-axial tumors of the MESENCEPHALON; PONS; or MEDULLA OBLONGATA of the BRAIN STEM. Primary and metastatic neoplasms may occur in this location. Clinical features include ATAXIA, cranial neuropathies (see CRANIAL NERVE DISEASES), NAUSEA, hemiparesis (see HEMIPLEGIA), and quadriparesis. Primary brain stem neoplasms are more frequent in children. Histologic subtypes include GLIOMA; HEMANGIOBLASTOMA; GANGLIOGLIOMA; and EPENDYMOMA.		02.7730
Optic Nerve Glioma
Glial cell derived tumors arising from the optic nerve, usually presenting in childhood.		02.0810
Cancer of Rectum
[description not available]		06.3976
Rectal Neoplasms
Tumors or cancer of the RECTUM.		19.681412
Bronchospasm
[description not available]		05.2541
Bronchial Spasm
Spasmodic contraction of the smooth muscle of the bronchi.		05.2541
Candida Infection
[description not available]		02.520
Candidiasis
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)		02.520
Auricular Fibrillation
[description not available]		02.9740
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		02.9740
Heart Disease, Ischemic
[description not available]		05.86122
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		05.86122
Electrolytes
Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)		04.942
Autosomal Hemophilia A
[description not available]		03.8521
Hemarthrosis
Bleeding into the joints. It may arise from trauma or spontaneously in patients with hemophilia.		03.4811
Hemophilia A
The classic hemophilia resulting from a deficiency of factor VIII. It is an inherited disorder of blood coagulation characterized by a permanent tendency to hemorrhage.		03.8521
Hypopharyngeal Cancer
[description not available]		02.7630
Hypopharyngeal Neoplasms
Tumors or cancer of the HYPOPHARYNX.		02.7630
Hypesthesia
Absent or reduced sensitivity to cutaneous stimulation.		04.4111
Dysesthesia
[description not available]		04.7721
Canine Diseases
[description not available]		03.3360
Carcinoma, Basal Cell, Pigmented
[description not available]		06.7883
Atypical Ductal Hyperplasia
[description not available]		04.1431
Carcinoma, Basal Cell
A malignant skin neoplasm that seldom metastasizes but has potentialities for local invasion and destruction. Clinically it is divided into types: nodular, cicatricial, morphaic, and erythematoid (pagetoid). They develop on hair-bearing skin, most commonly on sun-exposed areas. Approximately 85% are found on the head and neck area and the remaining 15% on the trunk and limbs. (From DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1471)		06.7883
Carcinoma, Intraductal, Noninfiltrating
A noninvasive (noninfiltrating) carcinoma of the breast characterized by a proliferation of malignant epithelial cells confined to the mammary ducts or lobules, without light-microscopy evidence of invasion through the basement membrane into the surrounding stroma.		04.1431
Granulocytic Leukemia, Chronic
[description not available]		03.1650
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		03.1650
Apnea, Obstructive Sleep
[description not available]		06.0133
Anoxemia
[description not available]		06.9992
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		06.9992
Sleep Apnea, Obstructive
A disorder characterized by recurrent apneas during sleep despite persistent respiratory efforts. It is due to upper airway obstruction. The respiratory pauses may induce HYPERCAPNIA or HYPOXIA. Cardiac arrhythmias and elevation of systemic and pulmonary arterial pressures may occur. Frequent partial arousals occur throughout sleep, resulting in relative SLEEP DEPRIVATION and daytime tiredness. Associated conditions include OBESITY; ACROMEGALY; MYXEDEMA; micrognathia; MYOTONIC DYSTROPHY; adenotonsilar dystrophy; and NEUROMUSCULAR DISEASES. (From Adams et al., Principles of Neurology, 6th ed, p395)		06.0133
Neuralgia, Sciatic
[description not available]		02.4620
Sciatica
A condition characterized by pain radiating from the back into the buttock and posterior/lateral aspects of the leg. Sciatica may be a manifestation of SCIATIC NEUROPATHY; RADICULOPATHY (involving the SPINAL NERVE ROOTS; L4, L5, S1, or S2, often associated with INTERVERTEBRAL DISK DISPLACEMENT); or lesions of the CAUDA EQUINA.		02.4620
Elevated Cholesterol
[description not available]		03.3260
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		08.3260
Hyperactivity, Motor
[description not available]		02.110
Depression, Endogenous
[description not available]		011.681610
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		113.681610
Fibroid
[description not available]		02.110
Cancer of the Uterus
[description not available]		02.4720
Leiomyoma
A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues.		07.110
Uterine Neoplasms
Tumors or cancer of the UTERUS.		14.4720
Colonic Polyps
Discrete tissue masses that protrude into the lumen of the COLON. These POLYPS are connected to the wall of the colon either by a stalk, pedunculus, or by a broad base.		07.12121
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		09.41104
Puerperal Disorders
Disorders or diseases associated with PUERPERIUM, the six-to-eight-week period immediately after PARTURITION in humans.		02.110
Ureterolithiasis
Formation of stones in the URETER.		03.4811
Lipidoses
Conditions characterized by abnormal lipid deposition due to disturbance in lipid metabolism, such as hereditary diseases involving lysosomal enzymes required for lipid breakdown. They are classified either by the enzyme defect or by the type of lipid involved.		02.110
Mucositis, Oral
[description not available]		04.7821
Stomatitis
INFLAMMATION of the soft tissues of the MOUTH, such as MUCOSA; PALATE; GINGIVA; and LIP.		16.7821
Adhesions, Tissue
[description not available]		03.3260
Carcinoma, Lewis Lung
A carcinoma discovered by Dr. Margaret R. Lewis of the Wistar Institute in 1951. This tumor originated spontaneously as a carcinoma of the lung of a C57BL mouse. The tumor does not appear to be grossly hemorrhagic and the majority of the tumor tissue is a semifirm homogeneous mass. (From Cancer Chemother Rep 2 1972 Nov;(3)1:325) It is also called 3LL and LLC and is used as a transplantable malignancy.		03.1750
Drug Overdose
Accidental or deliberate use of a medication or street drug in excess of normal dosage.		02.4720
Bone Cysts
Benign unilocular lytic areas in the proximal end of a long bone with well defined and narrow endosteal margins. The cysts contain fluid and the cyst walls may contain some giant cells. Bone cysts usually occur in males between the ages 3-15 years.		02.110
Injuries, Knee
[description not available]		02.110
Knee Injuries
Injuries to the knee or the knee joint.		02.110
Spinal Neoplasms
New abnormal growth of tissue in the SPINE.		02.7530
Colitis, Granulomatous
[description not available]		03.3620
Crohn Disease
A chronic transmural inflammation that may involve any part of the DIGESTIVE TRACT from MOUTH to ANUS, mostly found in the ILEUM, the CECUM, and the COLON. In Crohn disease, the inflammation, extending through the intestinal wall from the MUCOSA to the serosa, is characteristically asymmetric and segmental. Epithelioid GRANULOMAS may be seen in some patients.		03.3620
Carcinoma 256, Walker
A transplantable carcinoma of the rat that originally appeared spontaneously in the mammary gland of a pregnant albino rat, and which now resembles a carcinoma in young transplants and a sarcoma in older transplants. (Stedman, 25th ed)		02.4720
Dementias, Transmissible
[description not available]		02.1310
Agnogenic Myeloid Metaplasia
[description not available]		02.1110
Lassitude
[description not available]		05.4553
Fatigue
The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.		05.4553
Primary Myelofibrosis
A de novo myeloproliferation arising from an abnormal stem cell. It is characterized by the replacement of bone marrow by fibrous tissue, a process that is mediated by CYTOKINES arising from the abnormal clone.		02.1110
Animal Mammary Carcinoma
[description not available]		04.76110
Bladder Pain Syndrome
[description not available]		02.5220
Cystitis, Interstitial
A condition with recurring discomfort or pain in the URINARY BLADDER and the surrounding pelvic region without an identifiable disease. Severity of pain in interstitial cystitis varies greatly and often is accompanied by increased urination frequency and urgency.		02.5220
Analgesic Overuse Headache
[description not available]		03.511
Bechterew Syndrome
[description not available]		02.1110
Spondylarthropathies
Heterogeneous group of arthritic diseases sharing clinical and radiologic features. They are associated with the HLA-B27 ANTIGEN and some with a triggering infection. Most involve the axial joints in the SPINE, particularly the SACROILIAC JOINT, but can also involve asymmetric peripheral joints. Subsets include ANKYLOSING SPONDYLITIS; REACTIVE ARTHRITIS; PSORIATIC ARTHRITIS; and others.		02.1110
Pulmonary Arterial Remodeling
[description not available]		02.5220
Cystic Fibrosis of Pancreas
[description not available]		02.1110
Cystic Fibrosis
An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.		02.1110
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		02.1110
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		02.1110
Heart Valve Diseases
Pathological conditions involving any of the various HEART VALVES and the associated structures (PAPILLARY MUSCLES and CHORDAE TENDINEAE).		02.1110
Hypertension, Renal
Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.		02.4520
Deafness, Transitory
[description not available]		02.1110
Pulsatile Tinnitus
[description not available]		02.1110
Tinnitus
A nonspecific symptom of hearing disorder characterized by the sensation of buzzing, ringing, clicking, pulsations, and other noises in the ear. Objective tinnitus refers to noises generated from within the ear or adjacent structures that can be heard by other individuals. The term subjective tinnitus is used when the sound is audible only to the affected individual. Tinnitus may occur as a manifestation of COCHLEAR DISEASES; VESTIBULOCOCHLEAR NERVE DISEASES; INTRACRANIAL HYPERTENSION; CRANIOCEREBRAL TRAUMA; and other conditions.		02.1110
Hearing Loss
A general term for the complete or partial loss of the ability to hear from one or both ears.		02.1110
Armstrong Syndrome
[description not available]		02.1110
Nerve Degeneration
Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.		02.9640
Lumbar Osteoarthritis
[description not available]		02.1110
Osteoarthritis, Spine
A degenerative joint disease involving the SPINE. It is characterized by progressive deterioration of the spinal articular cartilage (CARTILAGE, ARTICULAR), usually with hardening of the subchondral bone and outgrowth of bone spurs (OSTEOPHYTE).		02.1110
Anaphylactic Reaction
[description not available]		05.91132
Anaphylaxis
An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.		05.91132
Acute Coronary Syndrome
An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.		04.8421
Liver Dysfunction
[description not available]		02.4820
Liver Diseases
Pathological processes of the LIVER.		02.4820
Intradural-Extramedullary Spinal Cord Neoplasms
[description not available]		02.1110
Spinal Cord Neoplasms
Benign and malignant neoplasms which occur within the substance of the spinal cord (intramedullary neoplasms) or in the space between the dura and spinal cord (intradural extramedullary neoplasms). The majority of intramedullary spinal tumors are primary CNS neoplasms including ASTROCYTOMA; EPENDYMOMA; and LIPOMA. Intramedullary neoplasms are often associated with SYRINGOMYELIA. The most frequent histologic types of intradural-extramedullary tumors are MENINGIOMA and NEUROFIBROMA.		02.1110
Rhabdoid Tumor
A rare but highly lethal childhood tumor found almost exclusively in infants. Histopathologically, it resembles RHABDOMYOSARCOMA but the tumor cells are not of myogenic origin. Although it arises primarily in the kidney, it may be found in other parts of the body. The rhabdoid cytomorphology is believed to be the expression of a very primitive malignant cell. (From Holland et al., Cancer Medicine, 3d ed, p2210)		07.1110
Hypercapnia
A clinical manifestation of abnormal increase in the amount of carbon dioxide in arterial blood.		03.8721
Colon Cancer, Familial Nonpolyposis
[description not available]		04.7721
Colorectal Neoplasms, Hereditary Nonpolyposis
A group of autosomal-dominant inherited diseases in which COLON CANCER arises in discrete adenomas. Unlike FAMILIAL POLYPOSIS COLI with hundreds of polyps, hereditary nonpolyposis colorectal neoplasms occur much later, in the fourth and fifth decades. HNPCC has been associated with germline mutations in mismatch repair (MMR) genes. It has been subdivided into Lynch syndrome I or site-specific colonic cancer, and LYNCH SYNDROME II which includes extracolonic cancer.		04.7721
Cerebral Microangiopathies
[description not available]		02.1110
Cerebral Small Vessel Diseases
Pathological processes or diseases where cerebral MICROVESSELS show abnormalities. They are often associated with aging, hypertension and risk factors for lacunar infarcts (see LACUNAR INFARCTION); LEUKOARAIOSIS; and CEREBRAL HEMORRHAGE.		02.1110
Retrolental Fibroplasia
[description not available]		02.1110
Neovascularization, Optic Disc
[description not available]		02.4820
Retinopathy of Prematurity
A bilateral retinopathy occurring in premature infants treated with excessively high concentrations of oxygen, characterized by vascular dilatation, proliferation, and tortuosity, edema, and retinal detachment, with ultimate conversion of the retina into a fibrous mass that can be seen as a dense retrolental membrane. Usually growth of the eye is arrested and may result in microophthalmia, and blindness may occur. (Dorland, 27th ed)		02.1110
Retinal Neovascularization
Formation of new blood vessels originating from the retinal veins and extending along the inner (vitreal) surface of the retina.		02.4820
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		04.3741
Scoliosis
An appreciable lateral deviation in the normally straight vertical line of the spine. (Dorland, 27th ed)		03.511
Alcohol Problem
[description not available]		02.1110
Airflow Obstruction, Chronic
[description not available]		02.1110
Chronic Kidney Diseases
[description not available]		02.1110
Gallstone Disease
[description not available]		02.1110
Cholelithiasis
Presence or formation of GALLSTONES in the BILIARY TRACT, usually in the gallbladder (CHOLECYSTOLITHIASIS) or the common bile duct (CHOLEDOCHOLITHIASIS).		02.1110
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		02.1110
Alcohol-Related Disorders
Disorders related to or resulting from abuse or misuse of alcohol.		02.1110
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		02.1110
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		02.1110
Leucocythaemia
[description not available]		03.1550
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		03.1550
Age-Related Osteoporosis
[description not available]		04.2160
Osteoporosis
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.		04.2160
Complications of Diabetes Mellitus
[description not available]		02.4820
Neointima
The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.		09.9542
Coronary Restenosis
Recurrent narrowing or constriction of a coronary artery following surgical procedures performed to alleviate a prior obstruction.		09.39105
Cardiac Failure
[description not available]		07.43191
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		07.43191
Postherpetic Neuralgia
[description not available]		04.8221
Neuralgia, Postherpetic
Pain in nerves, frequently involving facial SKIN, resulting from the activation the latent varicella-zoster virus (HERPESVIRUS 3, HUMAN). The two forms of the condition preceding the pain are HERPES ZOSTER OTICUS; and HERPES ZOSTER OPHTHALMICUS. Following the healing of the rashes and blisters, the pain sometimes persists.		04.8221
Cushing's Syndrome
[description not available]		02.1310
Cushing Syndrome
A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent.		02.1310
Ureteral Obstruction
Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy.		02.7330
Overweight
A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat.		02.1110
Acute Generalised Exanthematous Pustulosis
[description not available]		02.1310
Aggressive Systemic Mastocytosis
A form of systemic mastocytosis in which patients have impaired organ functions due to multifocal infiltrates of pathological MAST CELLS in bone marrow, liver, spleen, gastrointestinal tract, or skeletal system. The cytomorphology shows a low to high grade.		02.1110
Mastocytosis, Systemic
A group of disorders caused by the abnormal proliferation of MAST CELLS in a variety of extracutaneous tissues including bone marrow, liver, spleen, lymph nodes, and gastrointestinal tract. Systemic mastocytosis is commonly seen in adults. These diseases are categorized on the basis of clinical features, pathologic findings, and prognosis.		02.1110
Hypercoagulability
[description not available]		03.0310
Hemorrhagic Diathesis
[description not available]		03.0310
Hemorrhagic Disorders
Spontaneous or near spontaneous bleeding caused by a defect in clotting mechanisms (BLOOD COAGULATION DISORDERS) or another abnormality causing a structural flaw in the blood vessels (HEMOSTATIC DISORDERS).		03.0310
Thrombophilia
A disorder of HEMOSTASIS in which there is a tendency for the occurrence of THROMBOSIS.		03.0310
Tooth Mobility
Horizontal and, to a lesser degree, axial movement of a tooth in response to normal forces, as in occlusion. It refers also to the movability of a tooth resulting from loss of all or a portion of its attachment and supportive apparatus, as seen in periodontitis, occlusal trauma, and periodontosis. (From Jablonski, Dictionary of Dentistry, 1992, p507 & Boucher's Clinical Dental Terminology, 4th ed, p313)		04.7821
Colicky Pain
[description not available]		06.1462
Abdominal Pain
Sensation of discomfort, distress, or agony in the abdominal region.		06.1462
Di Guglielmo Disease
[description not available]		02.7330
Leukemia, Erythroblastic, Acute
A myeloproliferative disorder characterized by neoplastic proliferation of erythroblastic and myeloblastic elements with atypical erythroblasts and myeloblasts in the peripheral blood.		02.7330
Chronic Idiopathic Intestinal Pseudo-Obstruction
[description not available]		03.511
Anastomotic Leak
Breakdown of the connection and subsequent leakage of effluent (fluids, secretions, air) from a SURGICAL ANASTOMOSIS of the digestive, respiratory, genitourinary, and cardiovascular systems. Most common leakages are from the breakdown of suture lines in gastrointestinal or bowel anastomosis.		03.511
Intestinal Pseudo-Obstruction
A type of ILEUS, a functional not mechanical obstruction of the INTESTINES. This syndrome is caused by a large number of disorders involving the smooth muscles (MUSCLE, SMOOTH) or the NERVOUS SYSTEM.		03.511
Inflammatory Response Syndrome, Systemic
[description not available]		02.1310
Systemic Inflammatory Response Syndrome
A systemic inflammatory response to a variety of clinical insults, characterized by two or more of the following conditions: (1) fever		02.1310
Curling Ulcer
Acute stress DUODENAL ULCER, usually observed in patients with extensive third-degree burns.		09.93126
Duodenal Diseases
Pathological conditions in the DUODENUM region of the small intestine (INTESTINE, SMALL).		02.520
Duodenal Ulcer
A PEPTIC ULCER located in the DUODENUM.		09.93126
Envenomation, Scorpion
[description not available]		02.1310
Acute Febrile Neutrophilic Dermatosis
[description not available]		02.9540
Adenoma Sebaceum
Facial ANGIOFIBROMA in tuberous sclerosis		02.1310
Tuberous Sclerosis
Autosomal dominant neurocutaneous syndrome classically characterized by MENTAL RETARDATION; EPILEPSY; and skin lesions (e.g., adenoma sebaceum and hypomelanotic macules). There is, however, considerable heterogeneity in the neurologic manifestations. It is also associated with cortical tuber and HAMARTOMAS formation throughout the body, especially the heart, kidneys, and eyes. Mutations in two loci TSC1 and TSC2 that encode hamartin and tuberin, respectively, are associated with the disease.		02.1310
Congestive Ophthalmopathy
[description not available]		02.4820
Graves Ophthalmopathy
An autoimmune disorder of the EYE, occurring in patients with Graves disease. Subtypes include congestive (inflammation of the orbital connective tissue), myopathic (swelling and dysfunction of the extraocular muscles), and mixed congestive-myopathic ophthalmopathy.		14.4820
Absence Status
[description not available]		02.9740
Status Epilepticus
A prolonged seizure or seizures repeated frequently enough to prevent recovery between episodes occurring over a period of 20-30 minutes. The most common subtype is generalized tonic-clonic status epilepticus, a potentially fatal condition associated with neuronal injury and respiratory and metabolic dysfunction. Nonconvulsive forms include petit mal status and complex partial status, which may manifest as behavioral disturbances. Simple partial status epilepticus consists of persistent motor, sensory, or autonomic seizures that do not impair cognition (see also EPILEPSIA PARTIALIS CONTINUA). Subclinical status epilepticus generally refers to seizures occurring in an unresponsive or comatose individual in the absence of overt signs of seizure activity. (From N Engl J Med 1998 Apr 2;338(14):970-6; Neurologia 1997 Dec;12 Suppl 6:25-30)		02.9740
Hyperhomocysteinemia
Condition in which the plasma levels of homocysteine and related metabolites are elevated (		02.1310
Tonsillitis
Inflammation of the tonsils, especially the PALATINE TONSILS but the ADENOIDS (pharyngeal tonsils) and lingual tonsils may also be involved. Tonsillitis usually is caused by bacterial infection. Tonsillitis may be acute, chronic, or recurrent.		16.4311
Insulin Sensitivity
[description not available]		04.5351
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		09.5351
Chemotherapy-Induced Febrile Neutropenia
FEVER accompanied by a significant reduction in NEUTROPHIL count associated with CHEMOTHERAPY.		04.4311
Fibrocartilaginous Dysplasia of Bone
[description not available]		02.1510
Fibrous Dysplasia of Bone
A disease of bone marked by thinning of the cortex by fibrous tissue containing bony spicules, producing pain, disability, and gradually increasing deformity. Only one bone may be involved (FIBROUS DYSPLASIA, MONOSTOTIC) or several (FIBROUS DYSPLASIA, POLYOSTOTIC).		02.1510
B-Cell Leukemia
[description not available]		02.1510
Cancer, Second Primary
[description not available]		03.8521
Hepatitis, Animal
INFLAMMATION of the LIVER in non-human animals.		02.4720
C gattii Infection
[description not available]		02.1310
Cryptococcosis
Fungal infection caused by genus CRYPTOCOCCUS.		07.1310
Acute Lymphoid Leukemia
[description not available]		02.4820
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		02.4820
Adenocarcinoma Of Kidney
[description not available]		05.6263
Cancer of Kidney
[description not available]		05.7573
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		17.6263
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		05.7573
Blood Clot
[description not available]		011.12224
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		011.12224
Blood Poisoning
[description not available]		02.1510
Acute Mesenteric Arterial Embolus
[description not available]		02.1510
Sepsis
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.		02.1510
Endotoxemia
A condition characterized by the presence of ENDOTOXINS in the blood. On lysis, the outer cell wall of gram-negative bacteria enters the systemic circulation and initiates a pathophysiologic cascade of pro-inflammatory mediators.		07.4420
Angiitis
[description not available]		03.8621
Cold Panniculitis
[description not available]		02.4920
Vasculitis
Inflammation of any one of the blood vessels, including the ARTERIES; VEINS; and rest of the vasculature system in the body.		03.8621
Apnea, Sleep
[description not available]		02.1510
Sleep Apnea Syndromes
Disorders characterized by multiple cessations of respirations during sleep that induce partial arousals and interfere with the maintenance of sleep. Sleep apnea syndromes are divided into central (see SLEEP APNEA, CENTRAL), obstructive (see SLEEP APNEA, OBSTRUCTIVE), and mixed central-obstructive types.		02.1510
Barrett Epithelium
[description not available]		06.7112
Barrett Esophagus
A condition with damage to the lining of the lower ESOPHAGUS resulting from chronic acid reflux (ESOPHAGITIS, REFLUX). Through the process of metaplasia, the squamous cells are replaced by a columnar epithelium with cells resembling those of the INTESTINE or the salmon-pink mucosa of the STOMACH. Barrett's columnar epithelium is a marker for severe reflux and precursor to ADENOCARCINOMA of the esophagus.		06.7112
Amnesia, Pre-Ictal
[description not available]		03.3620
Hypertrophy, Right Ventricular
Enlargement of the RIGHT VENTRICLE of the heart. This increase in ventricular mass is often attributed to PULMONARY HYPERTENSION and is a contributor to cardiovascular morbidity and mortality.		02.0410
Pulmonary Hypertension
[description not available]		02.4620
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		02.4620
Eosinophilia, Tropical
[description not available]		02.7230
Idiopathic Inflammatory Myopathies
[description not available]		02.0410
Eosinophilia
Abnormal increase of EOSINOPHILS in the blood, tissues or organs.		07.7230
Myositis
Inflammation of a muscle or muscle tissue.		02.0410
Pain, Intractable
Persistent pain that is refractory to some or all forms of treatment.		02.0410
Metaplasia
A condition in which there is a change of one adult cell type to another similar adult cell type.		07.0762
Nycturia
[description not available]		04.3411
Nocturia
Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS).		09.3411
Hemorrhagic Shock
[description not available]		07.4620
Root Resorption
Resorption in which cementum or dentin is lost from the root of a tooth owing to cementoclastic or osteoclastic activity in conditions such as trauma of occlusion or neoplasms. (Dorland, 27th ed)		07.7330
Endometrioma
An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst.		04.3470
Sterility, Female
[description not available]		03.6330
Endometriosis
A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.		04.3470
Infertility, Female
Diminished or absent ability of a female to achieve conception.		03.6330
Hepatic Failure
[description not available]		02.4520
Liver Failure
Severe inability of the LIVER to perform its normal metabolic functions, as evidenced by severe JAUNDICE and abnormal serum levels of AMMONIA; BILIRUBIN; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; LACTATE DEHYDROGENASES; and albumin/globulin ratio. (Blakiston's Gould Medical Dictionary, 4th ed)		07.4520
Hemangioendothelioma, Epithelioid
A tumor of medium-to-large veins, composed of plump-to-spindled endothelial cells that bulge into vascular spaces in a tombstone-like fashion. These tumors are thought to have borderline aggression, where one-third develop local recurrences, but only rarely metastasize. It is unclear whether the epithelioid hemangioendothelioma is truly neoplastic or an exuberant tissue reaction, nor is it clear if this is equivalent to Kimura's disease (see ANGIOLYMPHOID HYPERPLASIA WITH EOSINOPHILIA). (Segen, Dictionary of Modern Medicine, 1992)		02.0410
Alveolar Bone Atrophy
[description not available]		02.9440
Gingivitis
Inflammation of gum tissue (GINGIVA) without loss of connective tissue.		02.0410
Grippe
[description not available]		02.0410
Infections, Orthomyxoviridae
[description not available]		02.7430
Influenza, Human
An acute viral infection in humans involving the respiratory tract. It is marked by inflammation of the NASAL MUCOSA; the PHARYNX; and conjunctiva, and by headache and severe, often generalized, myalgia.		14.0410
Orthomyxoviridae Infections
Virus diseases caused by the ORTHOMYXOVIRIDAE.		02.7430
Skin Aging
The process of aging due to changes in the structure and elasticity of the skin over time. It may be a part of physiological aging or it may be due to the effects of ultraviolet radiation, usually through exposure to sunlight.		02.4620
Adenosis of Breast
[description not available]		02.0410
Fibrocystic Breast Disease
A common and benign breast disease characterized by varying degree of fibrocystic changes in the breast tissue. There are three major patterns of morphological changes, including FIBROSIS, formation of CYSTS, and proliferation of glandular tissue (adenosis). The fibrocystic breast has a dense irregular, lumpy, bumpy consistency.		02.0410
Hormone-Dependent Neoplasms
[description not available]		06.7783
Soft Tissue Neoplasms
Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.		05.4453
Age-Related Memory Disorders
[description not available]		04.5251
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		16.5251
Segond Fracture
[description not available]		02.0410
Tibial Fractures
Fractures of the TIBIA.		02.0410
Argentaffinoma
[description not available]		02.0510
Adenoma, beta-Cell
[description not available]		02.0510
Carcinoid Tumor
A usually small, slow-growing neoplasm composed of islands of rounded, oxyphilic, or spindle-shaped cells of medium size, with moderately small vesicular nuclei, and covered by intact mucosa with a yellow cut surface. The tumor can occur anywhere in the gastrointestinal tract (and in the lungs and other sites); approximately 90% arise in the appendix. It is now established that these tumors are of neuroendocrine origin and derive from a primitive stem cell. (From Stedman, 25th ed & Holland et al., Cancer Medicine, 3d ed, p1182)		02.0510
Insulinoma
A benign tumor of the PANCREATIC BETA CELLS. Insulinoma secretes excess INSULIN resulting in HYPOGLYCEMIA.		02.0510
Inadequate Sleep
[description not available]		02.0510
Anterior Horn Cell Disease
[description not available]		02.9610
Motor Neuron Disease
Diseases characterized by a selective degeneration of the motor neurons of the spinal cord, brainstem, or motor cortex. Clinical subtypes are distinguished by the major site of degeneration. In AMYOTROPHIC LATERAL SCLEROSIS there is involvement of upper, lower, and brainstem motor neurons. In progressive muscular atrophy and related syndromes (see MUSCULAR ATROPHY, SPINAL) the motor neurons in the spinal cord are primarily affected. With progressive bulbar palsy (BULBAR PALSY, PROGRESSIVE), the initial degeneration occurs in the brainstem. In primary lateral sclerosis, the cortical neurons are affected in isolation. (Adams et al., Principles of Neurology, 6th ed, p1089)		02.9610
Stenosing Tendovaginitis
[description not available]		03.4311
Tendon Entrapment
Narrowing or stenosis of a tendon's retinacular sheath. It occurs most often in the hand or wrist but can also be found in the foot or ankle. The most common types are DE QUERVAIN DISEASE and TRIGGER FINGER DISORDER.		03.4311
Biliary Tract Cancer
[description not available]		09.422
Thrombopenia
[description not available]		03.4311
Biliary Tract Neoplasms
Tumors or cancer in the BILIARY TRACT including the BILE DUCTS and the GALLBLADDER.		04.422
Thrombocytopenia
A subnormal level of BLOOD PLATELETS.		03.4311
Nephrosis
Pathological processes of the KIDNEY without inflammatory or neoplastic components. Nephrosis may be a primary disorder or secondary complication of other diseases. It is characterized by the NEPHROTIC SYNDROME indicating the presence of PROTEINURIA and HYPOALBUMINEMIA with accompanying EDEMA.		07.0510
Carcinoma, Intraepithelial
[description not available]		04.1331
Carcinoma in Situ
A lesion with cytological characteristics associated with invasive carcinoma but the tumor cells are confined to the epithelium of origin, without invasion of the basement membrane.		04.1331
Attachment Loss, Periodontal
[description not available]		03.8321
Prosthesis Durability
[description not available]		04.1131
Carcinoma, Small Cell Lung
[description not available]		03.4311
Small Cell Lung Carcinoma
A form of highly malignant lung cancer that is composed of small ovoid cells (SMALL CELL CARCINOMA).		03.4311
Carcinoma, Medullary
A carcinoma composed mainly of epithelial elements with little or no stroma. Medullary carcinomas of the breast constitute 5%-7% of all mammary carcinomas; medullary carcinomas of the thyroid comprise 3%-10% of all thyroid malignancies. (From Dorland, 27th ed; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1141; Segen, Dictionary of Modern Medicine, 1992)		02.0510
Hemorrhage, Uterine
[description not available]		03.4311
Uterine Hemorrhage
Bleeding from blood vessels in the UTERUS, sometimes manifested as vaginal bleeding.		03.4311
Hamartoma
A focal malformation resembling a neoplasm, composed of an overgrowth of mature cells and tissues that normally occur in the affected area.		02.0510
Cell Transformation, Viral
An inheritable change in cells manifested by changes in cell division and growth and alterations in cell surface properties. It is induced by infection with a transforming virus.		02.0510
Christmas Disease
[description not available]		02.4420
Hemophilia B
A deficiency of blood coagulation factor IX inherited as an X-linked disorder. (Also known as Christmas Disease, after the first patient studied in detail, not the holy day.) Historical and clinical features resemble those in classic hemophilia (HEMOPHILIA A), but patients present with fewer symptoms. Severity of bleeding is usually similar in members of a single family. Many patients are asymptomatic until the hemostatic system is stressed by surgery or trauma. Treatment is similar to that for hemophilia A. (From Cecil Textbook of Medicine, 19th ed, p1008)		02.4420
Lesion of Sciatic Nerve
[description not available]		02.4420
Endothelioma, Vascular
[description not available]		02.0510
Kaposi Sarcoma
[description not available]		02.0510
Hemangioendothelioma
A neoplasm derived from blood vessels, characterized by numerous prominent endothelial cells that occur singly, in aggregates, and as the lining of congeries of vascular tubes or channels. Hemangioendotheliomas are relatively rare and are of intermediate malignancy (between benign hemangiomas and conventional angiosarcomas). They affect men and women about equally and rarely develop in childhood. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1866)		02.0510
Sarcoma, Kaposi
A multicentric, malignant neoplastic vascular proliferation characterized by the development of bluish-red cutaneous nodules, usually on the lower extremities, most often on the toes or feet, and slowly increasing in size and number and spreading to more proximal areas. The tumors have endothelium-lined channels and vascular spaces admixed with variably sized aggregates of spindle-shaped cells, and often remain confined to the skin and subcutaneous tissue, but widespread visceral involvement may occur. Kaposi's sarcoma occurs spontaneously in Jewish and Italian males in Europe and the United States. An aggressive variant in young children is endemic in some areas of Africa. A third form occurs in about 0.04% of kidney transplant patients. There is also a high incidence in AIDS patients. (From Dorland, 27th ed & Holland et al., Cancer Medicine, 3d ed, pp2105-7) HHV-8 is the suspected cause.		02.0510
Aberrant Tissue
[description not available]		02.9610
Dysembryoma
[description not available]		02.9610
Abscess
Accumulation of purulent material in tissues, organs, or circumscribed spaces, usually associated with signs of infection.		02.9610
Teratoma
A true neoplasm composed of a number of different types of tissue, none of which is native to the area in which it occurs. It is composed of tissues that are derived from three germinal layers, the endoderm, mesoderm, and ectoderm. They are classified histologically as mature (benign) or immature (malignant). (From DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1642)		02.9610
Colonic Diseases
Pathological processes in the COLON region of the large intestine (INTESTINE, LARGE).		03.1350
Hematoma, Subdural, Cranial
[description not available]		02.0510
Carcinomatous Meningitis
[description not available]		02.0510
Hematoma, Subdural, Intracranial
Accumulation of blood in the SUBDURAL SPACE over the CEREBRAL HEMISPHERE.		02.0510
Meningeal Carcinomatosis
Primary or secondary neoplasm in the ARACHNOID or SUBARACHNOID SPACE. It appears as a diffuse fibrotic thickening of the MENINGES associated with variable degrees of inflammation.		02.0510
Smoking Cessation
Discontinuing the habit of SMOKING.		03.8521
Injury, Myocardial Reperfusion
[description not available]		04.8171
Orthopedic Disorders
[description not available]		03.3620
Musculoskeletal Diseases
Diseases of the muscles and their associated ligaments and other connective tissue and of the bones and cartilage viewed collectively.		03.3620
T-Cell Lymphoma
[description not available]		07.0510
Lymphoma, T-Cell
A group of heterogeneous lymphoid tumors representing malignant transformations of T-lymphocytes.		02.0510
Experimental Radiation Injuries
[description not available]		02.4520
Abdominal Cramps
[description not available]		03.4311
Astroblastoma
[description not available]		02.0510
Neoplasms, Neuroepithelial
Neoplasms composed of neuroepithelial cells, which have the capacity to differentiate into NEURONS, oligodendrocytes, and ASTROCYTES. The majority of craniospinal tumors are of neuroepithelial origin. (From Dev Biol 1998 Aug 1;200(1):1-5)		02.0510
Encapsulating Peritoneal Sclerosis
[description not available]		02.0510
Ileus
A condition caused by the lack of intestinal PERISTALSIS or INTESTINAL MOTILITY without any mechanical obstruction. This interference of the flow of INTESTINAL CONTENTS often leads to INTESTINAL OBSTRUCTION. Ileus may be classified into postoperative, inflammatory, metabolic, neurogenic, and drug-induced.		03.4311
Intermittent Claudication
A symptom complex characterized by pain and weakness in SKELETAL MUSCLE group associated with exercise, such as leg pain and weakness brought on by walking. Such muscle limpness disappears after a brief rest and is often relates to arterial STENOSIS; muscle ISCHEMIA; and accumulation of LACTATE.		03.4311
Cancer of the Vulva
[description not available]		02.0510
Vulvar Neoplasms
Tumors or cancer of the VULVA.		02.0510
Poisoning
Used with drugs, chemicals, and industrial materials for human or animal poisoning, acute or chronic, whether the poisoning is accidental, occupational, suicidal, by medication error, or by environmental exposure.		02.4420
Atrophy
Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.		03.8321
Bowel Incontinence
[description not available]		03.4411
Gangrene
Death and putrefaction of tissue usually due to a loss of blood supply.		03.4411
Injuries, Radiation
[description not available]		05.0331
Fecal Incontinence
Failure of voluntary control of the anal sphincters, with involuntary passage of feces and flatus.		03.4411
Proctitis
INFLAMMATION of the MUCOUS MEMBRANE of the RECTUM, the distal end of the large intestine (INTESTINE, LARGE).		03.4411
Germinoblastoma
[description not available]		02.7330
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		07.7330
Foreign-Body Granuloma
[description not available]		02.0510
Foreign-Body Migration
Migration of a foreign body from its original location to some other location in the body.		02.0510
Alcoholic Cirrhosis
[description not available]		02.4320
Alcoholic Liver Diseases
[description not available]		02.0510
Alcoholic Fatty Liver
[description not available]		02.0510
Liver Cirrhosis, Alcoholic
FIBROSIS of the hepatic parenchyma due to chronic excess ALCOHOL DRINKING.		02.4320
Liver Diseases, Alcoholic
Liver diseases associated with ALCOHOLISM. It usually refers to the coexistence of two or more subentities, i.e., ALCOHOLIC FATTY LIVER; ALCOHOLIC HEPATITIS; and ALCOHOLIC CIRRHOSIS.		02.0510
Chondrosarcoma
A slowly growing malignant neoplasm derived from cartilage cells, occurring most frequently in pelvic bones or near the ends of long bones, in middle-aged and old people. Most chondrosarcomas arise de novo, but some may develop in a preexisting benign cartilaginous lesion or in patients with ENCHONDROMATOSIS. (Stedman, 25th ed)		07.0510
Central Retinal Edema, Cystoid
[description not available]		03.4411
Macular Edema
Fluid accumulation in the outer layer of the MACULA LUTEA that results from intraocular or systemic insults. It may develop in a diffuse pattern where the macula appears thickened or it may acquire the characteristic petaloid appearance referred to as cystoid macular edema. Although macular edema may be associated with various underlying conditions, it is most commonly seen following intraocular surgery, venous occlusive disease, DIABETIC RETINOPATHY, and posterior segment inflammatory disease. (From Survey of Ophthalmology 2004; 49(5) 470-90)		08.4411
Fifth Phacomatosis
[description not available]		03.4411
Basal Cell Nevus Syndrome
Hereditary disorder consisting of multiple basal cell carcinomas, odontogenic keratocysts, and multiple skeletal defects, e.g., frontal and temporoparietal bossing, bifurcated and splayed ribs, kyphoscoliosis, fusion of vertebrae, and cervicothoracic spina bifida. Genetic transmission is autosomal dominant.		03.4411
Parodontosis
[description not available]		02.0510
Periodontal Diseases
Pathological processes involving the PERIODONTIUM including the gum (GINGIVA), the alveolar bone (ALVEOLAR PROCESS), the DENTAL CEMENTUM, and the PERIODONTAL LIGAMENT.		02.0510
Angina at Rest
[description not available]		03.8321
Anterior Choroidal Artery Infarction
[description not available]		02.0510
Death, Sudden
The abrupt cessation of all vital bodily functions, manifested by the permanent loss of total cerebral, respiratory, and cardiovascular functions.		02.0510
Angina, Unstable
Precordial pain at rest, which may precede a MYOCARDIAL INFARCTION.		03.8321
Cerebral Infarction
The formation of an area of NECROSIS in the CEREBRUM caused by an insufficiency of arterial or venous blood flow. Infarcts of the cerebrum are generally classified by hemisphere (i.e., left vs. right), lobe (e.g., frontal lobe infarction), arterial distribution (e.g., INFARCTION, ANTERIOR CEREBRAL ARTERY), and etiology (e.g., embolic infarction).		02.0510
Thromboembolism
Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.		06.7291
Diffuse Mixed Small and Large Cell Lymphoma
[description not available]		04.6732
Diffuse Large B-Cell Lymphoma
[description not available]		03.8521
Lymphoma, Non-Hodgkin
Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease.		04.6732
Lymphoma, Large B-Cell, Diffuse
Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation.		03.8521
Anguilluliasis
[description not available]		02.0510
Strongyloidiasis
Infection with nematodes of the genus STRONGYLOIDES. The presence of larvae may produce pneumonitis and the presence of adult worms in the intestine could lead to moderate to severe diarrhea.		02.0510
Central Nervous System Neoplasm
[description not available]		02.4420
Central Nervous System Neoplasms
Benign and malignant neoplastic processes that arise from or secondarily involve the brain, spinal cord, or meninges.		14.4420
Autoimmune Diabetes
[description not available]		05.2543
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		05.2543
Uveitis, Anterior
Inflammation of the anterior uvea comprising the iris, angle structures, and the ciliary body. Manifestations of this disorder include ciliary injection, exudation into the anterior chamber, iris changes, and adhesions between the iris and lens (posterior synechiae). Intraocular pressure may be increased or reduced.		02.0510
Carbon Tetrachloride Poisoning
Poisoning that results from ingestion, injection, inhalation, or skin absorption of CARBON TETRACHLORIDE.		02.4320
Centriacinar Emphysema
[description not available]		02.0510
Chronic Paroxysmal Hemicrania
[description not available]		02.0510
Kashin-Beck Disease
Disabling osteochondrodysplasia with OSTEOSCLEROSIS, cone-shaped METAPHYSIS, and shortening of the DIAPHYSIS. It is endemic in parts of Siberia and northern China. Mineral deficiencies (e.g., selenium, iodine), fungal cereal contamination, and water contamination may be contributing factors in its etiology.		08.4511
Neoplasms, Squamous Cell
Neoplasms of the SQUAMOUS EPITHELIAL CELLS. The concept does not refer to neoplasms located in tissue composed of squamous elements.		03.8421
Aberrant Crypt Foci
Clusters of colonic crypts that appear different from the surrounding mucosa when visualized after staining. They are of interest as putative precursors to colorectal adenomas and potential biomarkers for colorectal carcinoma.		02.0610
Glioblastoma with Sarcomatous Component
[description not available]		02.4420
Gliosarcoma
Rare mixed tumors of the brain and rarely the spinal cord which contain malignant neuroectodermal (glial) and mesenchymal components, including spindle-shaped fibrosarcoma cells. These tumors are highly aggressive and present primarily in adults as rapidly expanding mass lesions. They may arise in tissue that has been previously irradiated. (From Br J Neurosurg 1995 Apr;9(2):171-8)		02.4420
Benign Supratentorial Neoplasms
[description not available]		04.3611
Mesothelioma
A tumor derived from mesothelial tissue (peritoneum, pleura, pericardium). It appears as broad sheets of cells, with some regions containing spindle-shaped, sarcoma-like cells and other regions showing adenomatous patterns. Pleural mesotheliomas have been linked to exposure to asbestos. (Dorland, 27th ed)		02.7230
Mycosis Fungoides
A chronic, malignant T-cell lymphoma of the skin. In the late stages, the LYMPH NODES and viscera are affected.		02.0510
Angiosarcoma
[description not available]		07.0510
Hemangiosarcoma
A rare malignant neoplasm characterized by rapidly proliferating, extensively infiltrating, anaplastic cells derived from blood vessels and lining irregular blood-filled or lumpy spaces. (Stedman, 25th ed)		02.0510
African Lymphoma
[description not available]		02.7330
Burkitt Lymphoma
A form of undifferentiated malignant LYMPHOMA usually found in central Africa, but also reported in other parts of the world. It is commonly manifested as a large osteolytic lesion in the jaw or as an abdominal mass. B-cell antigens are expressed on the immature cells that make up the tumor in virtually all cases of Burkitt lymphoma. The Epstein-Barr virus (HERPESVIRUS 4, HUMAN) has been isolated from Burkitt lymphoma cases in Africa and it is implicated as the causative agent in these cases; however, most non-African cases are EBV-negative.		02.7330
Dyslipidemia
[description not available]		02.0610
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		02.0610
Esophageal Reflux
[description not available]		07.7430
Gastroesophageal Reflux
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.		07.7430
Ureteral Calculi
Stones in the URETER that are formed in the KIDNEY. They are rarely more than 5 mm in diameter for larger renal stones cannot enter ureters. They are often lodged at the ureteral narrowing and can cause excruciating renal colic.		03.8421
Adult Periodontitis
[description not available]		03.4511
Hemorrhage, Gingival
[description not available]		04.422
Gingival Hemorrhage
The flowing of blood from the marginal gingival area, particularly the sulcus, seen in such conditions as GINGIVITIS, marginal PERIODONTITIS, injury, and ASCORBIC ACID DEFICIENCY.		04.422
Cardiac Diseases
[description not available]		04.4580
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		04.4580
Nephrotic Syndrome
A condition characterized by severe PROTEINURIA, greater than 3.5 g/day in an average adult. The substantial loss of protein in the urine results in complications such as HYPOPROTEINEMIA; generalized EDEMA; HYPERTENSION; and HYPERLIPIDEMIAS. Diseases associated with nephrotic syndrome generally cause chronic kidney dysfunction.		02.7230
Angiospasm, Intracranial
[description not available]		02.7630
Vasospasm, Intracranial
Constriction of arteries in the SKULL due to sudden, sharp, and often persistent smooth muscle contraction in blood vessels. Intracranial vasospasm results in reduced vessel lumen caliber, restricted blood flow to the brain, and BRAIN ISCHEMIA that may lead to hypoxic-ischemic brain injury (HYPOXIA-ISCHEMIA, BRAIN).		02.7630
Goldblatt Syndrome
[description not available]		02.7230
Hypertension, Renovascular
Hypertension due to RENAL ARTERY OBSTRUCTION or compression.		02.7230
Chronic Kidney Failure
[description not available]		04.1131
Hyperparathyroidism
A condition of abnormally elevated output of PARATHYROID HORMONE (or PTH) triggering responses that increase blood CALCIUM. It is characterized by HYPERCALCEMIA and BONE RESORPTION, eventually leading to bone diseases. PRIMARY HYPERPARATHYROIDISM is caused by parathyroid HYPERPLASIA or PARATHYROID NEOPLASMS. SECONDARY HYPERPARATHYROIDISM is increased PTH secretion in response to HYPOCALCEMIA, usually caused by chronic KIDNEY DISEASES.		02.0610
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		04.1131
Akinetic-Rigid Variant of Huntington Disease
[description not available]		02.4420
Huntington Disease
A familial disorder inherited as an autosomal dominant trait and characterized by the onset of progressive CHOREA and DEMENTIA in the fourth or fifth decade of life. Common initial manifestations include paranoia; poor impulse control; DEPRESSION; HALLUCINATIONS; and DELUSIONS. Eventually intellectual impairment; loss of fine motor control; ATHETOSIS; and diffuse chorea involving axial and limb musculature develops, leading to a vegetative state within 10-15 years of disease onset. The juvenile variant has a more fulminant course including SEIZURES; ATAXIA; dementia; and chorea. (From Adams et al., Principles of Neurology, 6th ed, pp1060-4)		02.4420
Rhabdomyosarcoma
A malignant solid tumor arising from mesenchymal tissues which normally differentiate to form striated muscle. It can occur in a wide variety of sites. It is divided into four distinct types: pleomorphic, predominantly in male adults; alveolar (RHABDOMYOSARCOMA, ALVEOLAR), mainly in adolescents and young adults; embryonal (RHABDOMYOSARCOMA, EMBRYONAL), predominantly in infants and children; and botryoidal, also in young children. It is one of the most frequently occurring soft tissue sarcomas and the most common in children under 15. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p2186; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, pp1647-9)		07.0610
Cardiomyopathy, Congestive
[description not available]		02.4620
Cardiomyopathy, Dilated
A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.		02.4620
Avian Flu
[description not available]		02.0610
Influenza in Birds
Infection of domestic and wild fowl and other BIRDS with INFLUENZA A VIRUS. Avian influenza usually does not sicken birds, but can be highly pathogenic and fatal in domestic POULTRY.		02.0610
Esophagitis, Reflux
[description not available]		02.4520
Esophagitis, Peptic
INFLAMMATION of the ESOPHAGUS that is caused by the reflux of GASTRIC JUICE with contents of the STOMACH and DUODENUM.		02.4520
Sore Throat
[description not available]		03.4511
Pharyngitis
Inflammation of the throat (PHARYNX).		15.4511
HIV Coinfection
[description not available]		03.8321
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		03.8321
Sinus Infections
[description not available]		03.8321
Nasal Diseases
[description not available]		03.4511
Sinusitis
Inflammation of the NASAL MUCOSA in one or more of the PARANASAL SINUSES.		08.8321
Aneurysm, Arteriovenous
[description not available]		02.0710
Colonic Inertia
Symptom characterized by the passage of stool once a week or less.		04.7521
Constipation
Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.		04.7521
Clinically Isolated CNS Demyelinating Syndrome
[description not available]		02.0710
Demyelinating Diseases
Diseases characterized by loss or dysfunction of myelin in the central or peripheral nervous system.		02.0710
Amyloid Angiopathy, Cerebral
[description not available]		02.9810
Cerebral Amyloid Angiopathy
A heterogeneous group of sporadic or familial disorders characterized by AMYLOID deposits in the walls of small and medium sized blood vessels of CEREBRAL CORTEX and MENINGES. Clinical features include multiple, small lobar CEREBRAL HEMORRHAGE; cerebral ischemia (BRAIN ISCHEMIA); and CEREBRAL INFARCTION. Cerebral amyloid angiopathy is unrelated to generalized AMYLOIDOSIS. Amyloidogenic peptides in this condition are nearly always the same ones found in ALZHEIMER DISEASE. (from Kumar: Robbins and Cotran: Pathologic Basis of Disease, 7th ed., 2005)		02.9810
Alveolar Soft Part Sarcoma
[description not available]		02.0610
Sarcoma, Alveolar Soft Part
A variety of rare sarcoma having a reticulated fibrous stroma enclosing groups of sarcoma cells, which resemble epithelial cells and are enclosed in alveoli walled with connective tissue. It is a rare tumor, usually occurring between 15 and 35 years of age. It appears in the muscles of the extremities in adults and most commonly in the head and neck regions of children. Though slow-growing, it commonly metastasizes to the lungs, brain, bones, and lymph nodes. (DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1365)		02.0610
Hematologic Malignancies
[description not available]		02.4420
Hematologic Neoplasms
Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.		02.4420
Ductal Carcinoma
[description not available]		02.0610
Carcinoma, Ductal
Malignant neoplasms involving the ductal systems of any of a number of organs, such as the MAMMARY GLANDS, the PANCREAS, the PROSTATE, or the LACRIMAL GLAND.		02.0610
Muscle Tissue Neoplasms
[description not available]		02.0710
Neoplasms, Bone Marrow
[description not available]		02.0610
Bone Marrow Neoplasms
Neoplasms located in the bone marrow. They are differentiated from neoplasms composed of bone marrow cells, such as MULTIPLE MYELOMA. Most bone marrow neoplasms are metastatic.		02.0610
Cardiac Rupture, Traumatic
[description not available]		02.0710
Hypermobility, Joint
[description not available]		02.0710
Peritoneal Diseases
Pathological processes involving the PERITONEUM.		02.4820
Pyrosis
[description not available]		03.4511
Heartburn
Substernal pain or burning sensation, usually associated with regurgitation of gastric juice into the esophagus.		03.4511
Serotonin Syndrome
An adverse drug interaction characterized by altered mental status, autonomic dysfunction, and neuromuscular abnormalities. It is most frequently caused by use of both serotonin reuptake inhibitors and monoamine oxidase inhibitors, leading to excess serotonin availability in the CNS at the serotonin 1A receptor.		02.9810
Chromosomal Instability
An increased tendency to acquire CHROMOSOME ABERRATIONS when various processes involved in chromosome replication, repair, or segregation are dysfunctional.		02.0710
Erythema Multiforme
A skin and mucous membrane disease characterized by an eruption of macules, papules, nodules, vesicles, and/or bullae with characteristic bull's-eye lesions usually occurring on the dorsal aspect of the hands and forearms.		03.3520
Female Genital Neoplasms
[description not available]		03.4611
Genital Neoplasms, Female
Tumor or cancer of the female reproductive tract (GENITALIA, FEMALE).		03.4611
Erosive Duodenitis
[description not available]		02.4420
Esophageal Varices
[description not available]		02.0710
Duodenitis
Inflammation of the DUODENUM section of the small intestine (INTESTINE, SMALL). Erosive duodenitis may cause bleeding in the UPPER GI TRACT and PEPTIC ULCER.		02.4420
Esophageal and Gastric Varices
Dilated blood vessels in the ESOPHAGUS or GASTRIC FUNDUS that shunt blood from the portal circulation (PORTAL SYSTEM) to the systemic venous circulation. Often they are observed in individuals with portal hypertension (HYPERTENSION, PORTAL).		02.0710
Leg Dermatoses
A nonspecific term used to denote any cutaneous lesion or group of lesions, or eruptions of any type on the leg. (From Stedman, 25th ed)		03.3520
Ascites, Gelatinous
[description not available]		02.0710
Pseudomyxoma Peritonei
A peritoneal adenocarcinoma characterized by build-up of MUCUS in the PERITONEAL CAVITY. Mucus secreting cells may attach to the peritoneal lining and continue to secrete mucus. The majority of cases represent tumor spread from a primary low-grade mucinous neoplasm of the APPENDIX (NCI Thesaurus).		02.0710
Abnormalities, Cardiovascular
[description not available]		04.9340
Cardiovascular Abnormalities
Congenital, inherited, or acquired anomalies of the CARDIOVASCULAR SYSTEM, including the HEART and BLOOD VESSELS.		04.9340
Cancer of Mediastinum
[description not available]		02.0710
Mediastinal Neoplasms
Tumors or cancer of the MEDIASTINUM.		02.0710
Leukoma
[description not available]		02.0710
Corneal Opacity
Disorder occurring in the central or peripheral area of the cornea. The usual degree of transparency becomes relatively opaque.		02.0710
Angor Pectoris
[description not available]		05.2543
Angina Pectoris
The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.		010.2543
Kidney, Polycystic
[description not available]		02.0710
Polycystic Kidney Diseases
Hereditary diseases that are characterized by the progressive expansion of a large number of tightly packed CYSTS within the KIDNEYS. They include diseases with autosomal dominant and autosomal recessive inheritance.		02.0710
Hepatorenal Syndrome
Functional KIDNEY FAILURE in patients with liver disease, usually LIVER CIRRHOSIS or portal hypertension (HYPERTENSION, PORTAL), and in the absence of intrinsic renal disease or kidney abnormality. It is characterized by intense renal vasculature constriction, reduced renal blood flow, OLIGURIA, and sodium retention.		07.0710
ADDH
[description not available]		04.7521
Attention Deficit Disorder with Hyperactivity
A behavior disorder originating in childhood in which the essential features are signs of developmentally inappropriate inattention, impulsivity, and hyperactivity. Although most individuals have symptoms of both inattention and hyperactivity-impulsivity, one or the other pattern may be predominant. The disorder is more frequent in males than females. Onset is in childhood. Symptoms often attenuate during late adolescence although a minority experience the full complement of symptoms into mid-adulthood. (From DSM-V)		04.7521
Mitral Incompetence
[description not available]		02.0710
Sicca Syndrome
[description not available]		07.7130
Mitral Valve Insufficiency
Backflow of blood from the LEFT VENTRICLE into the LEFT ATRIUM due to imperfect closure of the MITRAL VALVE. This can lead to mitral valve regurgitation.		02.0710
Sjogren's Syndrome
Chronic inflammatory and autoimmune disease in which the salivary and lacrimal glands undergo progressive destruction by lymphocytes and plasma cells resulting in decreased production of saliva and tears. The primary form, often called sicca syndrome, involves both KERATOCONJUNCTIVITIS SICCA and XEROSTOMIA. The secondary form includes, in addition, the presence of a connective tissue disease, usually rheumatoid arthritis.		02.7130
Endomyometritis
Inflammation of both the ENDOMETRIUM and the MYOMETRIUM, usually caused by infections after a CESAREAN SECTION.		02.0710
Premature Rupture of Fetal Membranes
[description not available]		02.0710
Endometritis
Inflammation of the ENDOMETRIUM, usually caused by intrauterine infections. Endometritis is the most common cause of postpartum fever.		02.0710
Fetal Membranes, Premature Rupture
Spontaneous tearing of the membranes surrounding the FETUS any time before the onset of OBSTETRIC LABOR. Preterm PROM is membrane rupture before 37 weeks of GESTATION.		02.0710
Dehiscence, Surgical Wound
[description not available]		02.0710
Fibrosis, Radiation
[description not available]		02.0810
Radiation Pneumonitis
Inflammation of the lung due to harmful effects of ionizing or non-ionizing radiation.		02.0810
Hyperpotassemia
[description not available]		03.8221
Hyperkalemia
Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)		08.8221
Autism
[description not available]		03.4711
Autistic Disorder
A disorder beginning in childhood. It is marked by the presence of markedly abnormal or impaired development in social interaction and communication and a markedly restricted repertoire of activity and interest. Manifestations of the disorder vary greatly depending on the developmental level and chronological age of the individual. (DSM-V)		08.4711
Bilateral Wilms Tumor
[description not available]		02.0710
Wilms Tumor
A malignant kidney tumor, caused by the uncontrolled multiplication of renal stem (blastemal), stromal (STROMAL CELLS), and epithelial (EPITHELIAL CELLS) elements. However, not all three are present in every case. Several genes or chromosomal areas have been associated with Wilms tumor which is usually found in childhood as a firm lump in a child's side or ABDOMEN.		02.0710
Intussusception
A form of intestinal obstruction caused by the PROLAPSE of a part of the intestine into the adjoining intestinal lumen. There are four types: colic, involving segments of the LARGE INTESTINE; enteric, involving only the SMALL INTESTINE; ileocecal, in which the ILEOCECAL VALVE prolapses into the CECUM, drawing the ILEUM along with it; and ileocolic, in which the ileum prolapses through the ileocecal valve into the COLON.		02.9910
Aortic Aneurysm, Ruptured
[description not available]		02.0710
Granuloma, Plasma Cell, Orbital
[description not available]		02.0810
Orbital Pseudotumor
A nonspecific tumor-like inflammatory lesion in the ORBIT of the eye. It is usually composed of mature LYMPHOCYTES; PLASMA CELLS; MACROPHAGES; LEUKOCYTES with varying degrees of FIBROSIS. Orbital pseudotumors are often associated with inflammation of the extraocular muscles (ORBITAL MYOSITIS) or inflammation of the lacrimal glands (DACRYOADENITIS).		02.0810
Gastritis, Atrophic
GASTRITIS with atrophy of the GASTRIC MUCOSA, the GASTRIC PARIETAL CELLS, and the mucosal glands leading to ACHLORHYDRIA. Atrophic gastritis usually progresses from chronic gastritis.		04.3911
Cicatrization
The formation of fibrous tissue in the place of normal tissue during the process of WOUND HEALING. It includes scar tissue formation occurring in healing internal organs as well as in the skin after surface injuries.		03.3620
Acquired Laryngeal Stenosis
[description not available]		02.0710
Cicatrix
The fibrous tissue that replaces normal tissue during the process of WOUND HEALING.		03.3620
Abdominal Neoplasms
New abnormal growth of tissue in the ABDOMEN.		02.0810
Benign Meningeal Neoplasms
[description not available]		02.7330
Angioblastic Meningioma
[description not available]		02.7330
Meningeal Neoplasms
Benign and malignant neoplastic processes that arise from or secondarily involve the meningeal coverings of the brain and spinal cord.		02.7330
Meningioma
A relatively common neoplasm of the CENTRAL NERVOUS SYSTEM that arises from arachnoidal cells. The majority are well differentiated vascular tumors which grow slowly and have a low potential to be invasive, although malignant subtypes occur. Meningiomas have a predilection to arise from the parasagittal region, cerebral convexity, sphenoidal ridge, olfactory groove, and SPINAL CANAL. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2056-7)		02.7330
Hepatoblastoma
A malignant neoplasm occurring in young children, primarily in the liver, composed of tissue resembling embryonal or fetal hepatic epithelium, or mixed epithelial and mesenchymal tissues. (Stedman, 25th ed)		02.0810
Intertrochanteric Fractures
[description not available]		013.73636
Hip Fractures
Fractures of the FEMUR HEAD; the FEMUR NECK; (FEMORAL NECK FRACTURES); the trochanters; or the inter- or subtrochanteric region. Excludes fractures of the acetabulum and fractures of the femoral shaft below the subtrochanteric region (FEMORAL FRACTURES).		013.73636
Diabetic Glomerulosclerosis
[description not available]		06.1843
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		06.1843
Arthritides, Bacterial
[description not available]		02.0810
Bile Duct Obstruction, Intrahepatic
[description not available]		03.1150
Cholestasis, Intrahepatic
Impairment of bile flow due to injury to the HEPATOCYTES; BILE CANALICULI; or the intrahepatic bile ducts (BILE DUCTS, INTRAHEPATIC).		03.1150
Intestinal Obstruction
Any impairment, arrest, or reversal of the normal flow of INTESTINAL CONTENTS toward the ANAL CANAL.		03.1250
Coronary Thrombosis
Coagulation of blood in any of the CORONARY VESSELS. The presence of a blood clot (THROMBUS) often leads to MYOCARDIAL INFARCTION.		05.2341
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		010.9433
Sprains
[description not available]		05.544
Ankle Injuries
Harm or hurt to the ankle or ankle joint usually inflicted by an external source.		05.544
Sprains and Strains
A collective term for muscle and ligament injuries without dislocation or fracture. A sprain is a joint injury in which some of the fibers of a supporting ligament are ruptured but the continuity of the ligament remains intact. A strain is an overstretching or overexertion of some part of the musculature.		05.544
Allergic Cutaneous Angiitis
[description not available]		04.0250
Cocarcinogenesis
The combination of two or more different factors in the production of cancer.		02.0110
Drug-Induced Stevens Johnson Syndrome
[description not available]		04.3270
Stevens-Johnson Syndrome
Rare cutaneous eruption characterized by extensive KERATINOCYTE apoptosis resulting in skin detachment with mucosal involvement. It is often provoked by the use of drugs (e.g., antibiotics and anticonvulsants) or associated with PNEUMONIA, MYCOPLASMA. It is considered a continuum of Toxic Epidermal Necrolysis.		04.3270
Diathesis
[description not available]		03.3420
Neoplasms, Otorhinolaryngologic
[description not available]		02.0110
Angioma, Cavernous
A tumor-like mass with large vascular space that is filled with blood or lymph.		02.0110
Disease, Pulmonary
[description not available]		02.9440
Lung Diseases
Pathological processes involving any part of the LUNG.		02.9440
Coronary Heart Disease
[description not available]		02.9340
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		02.9340
Hibernation, Myocardial
[description not available]		02.4120
Female Genital Diseases
[description not available]		02.9210
Heavy Menstrual Bleeding
[description not available]		02.9210
Polycystic Ovarian Syndrome
[description not available]		02.9210
Genital Diseases, Female
Pathological processes involving the female reproductive tract (GENITALIA, FEMALE).		02.9210
Menorrhagia
Excessive uterine bleeding during MENSTRUATION.		02.9210
Polycystic Ovary Syndrome
A complex disorder characterized by infertility, HIRSUTISM; OBESITY; and various menstrual disturbances such as OLIGOMENORRHEA; AMENORRHEA; ANOVULATION. Polycystic ovary syndrome is usually associated with bilateral enlarged ovaries studded with atretic follicles, not with cysts. The term, polycystic ovary, is misleading.		02.9210
Bilirubinemia
[description not available]		02.0110
Foot Dermatoses
Skin diseases of the foot, general or unspecified.		02.9210
Bile Duct Cysts
[description not available]		02.0110
Peripheral Nerve Diseases
[description not available]		04.7221
Peripheral Nervous System Diseases
Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.		04.7221
Kidney Papillary Necrosis
A complication of kidney diseases characterized by cell death involving KIDNEY PAPILLA in the KIDNEY MEDULLA. Damages to this area may hinder the kidney to concentrate urine resulting in POLYURIA. Sloughed off necrotic tissue may block KIDNEY PELVIS or URETER. Necrosis of multiple renal papillae can lead to KIDNEY FAILURE.		02.0110
Bright Disease
A historical classification which is no longer used. It described acute glomerulonephritis, acute nephritic syndrome, or acute nephritis. Named for Richard Bright.		02.7130
Glomerulonephritis
Inflammation of the renal glomeruli (KIDNEY GLOMERULUS) that can be classified by the type of glomerular injuries including antibody deposition, complement activation, cellular proliferation, and glomerulosclerosis. These structural and functional abnormalities usually lead to HEMATURIA; PROTEINURIA; HYPERTENSION; and RENAL INSUFFICIENCY.		02.7130
Odontalgia
[description not available]		04.550
Toothache
Pain in the adjacent areas of the teeth.		16.550
Psychoses
[description not available]		02.0110
Psychotic Disorders
Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994)		02.0110
Esophageal Stricture
[description not available]		02.0110
Epileptiform Neuralgia
[description not available]		02.4220
Esophageal Stenosis
A stricture of the ESOPHAGUS. Most are acquired but can be congenital.		02.0110
Esophagitis
INFLAMMATION, acute or chronic, of the ESOPHAGUS caused by BACTERIA, chemicals, or TRAUMA.		09.131
Trigeminal Neuralgia
A syndrome characterized by recurrent episodes of excruciating pain lasting several seconds or longer in the sensory distribution of the TRIGEMINAL NERVE. Pain may be initiated by stimulation of trigger points on the face, lips, or gums or by movement of facial muscles or chewing. Associated conditions include MULTIPLE SCLEROSIS, vascular anomalies, ANEURYSMS, and neoplasms. (Adams et al., Principles of Neurology, 6th ed, p187)		02.4220
Chronic Plantar Fasciitis
[description not available]		012.642626
Fasciitis, Plantar
Inflammation of the plantar fascia (APONEUROSIS) on the bottom of the foot causing heel pain. The etiology of plantar fasciitis remains controversial but is likely to involve a biomechanical imbalance. Though often presenting along with HEEL SPUR, they do not appear to be causally related.		012.642626
Brain Vascular Disorders
[description not available]		02.4220
Diseases, Peripheral Vascular
[description not available]		02.0110
Cerebrovascular Disorders
A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others.		02.4220
Peripheral Vascular Diseases
Pathological processes involving any one of the BLOOD VESSELS in the vasculature outside the HEART.		02.0110
Rhabdomyosarcoma, Embryonal
A form of RHABDOMYOSARCOMA arising primarily in the head and neck, especially the orbit, of children below the age of 10. The cells are smaller than those of other rhabdomyosarcomas and are of two basic cell types: spindle cells and round cells. This cancer is highly sensitive to chemotherapy and has a high cure rate with multi-modality therapy. (From Holland et al., Cancer Medicine, 3d ed, p2188)		02.0110
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		03.3420
Flaccid Quadriplegia
[description not available]		02.0110
Day Blindness
[description not available]		04.7970
Nephritis
Inflammation of any part of the KIDNEY.		02.4120
Ileal Diseases
Pathological development in the ILEUM including the ILEOCECAL VALVE.		02.0210
Microbial Superinvasion
[description not available]		03.411
Femoral Fractures
Fractures of the femur.		04.7321
Aseptic Meningitis
[description not available]		07.0210
Meningitis, Aseptic
A syndrome characterized by headache, neck stiffness, low grade fever, and CSF lymphocytic pleocytosis in the absence of an acute bacterial pathogen. Viral meningitis is the most frequent cause although MYCOPLASMA INFECTIONS; RICKETTSIA INFECTIONS; diagnostic or therapeutic procedures; NEOPLASTIC PROCESSES; septic perimeningeal foci; and other conditions may result in this syndrome. (From Adams et al., Principles of Neurology, 6th ed, p745)		02.0210
Diffuse Myofascial Pain Syndrome
[description not available]		02.0210
Fibromyalgia
A common nonarticular rheumatic syndrome characterized by myalgia and multiple points of focal muscle tenderness to palpation (trigger points). Muscle pain is typically aggravated by inactivity or exposure to cold. This condition is often associated with general symptoms, such as sleep disturbances, fatigue, stiffness, HEADACHES, and occasionally DEPRESSION. There is significant overlap between fibromyalgia and the chronic fatigue syndrome (FATIGUE SYNDROME, CHRONIC). Fibromyalgia may arise as a primary or secondary disease process. It is most frequent in females aged 20 to 50 years. (From Adams et al., Principles of Neurology, 6th ed, p1494-95)		02.0210
Salmonella Infections, Animal
Infections in animals with bacteria of the genus SALMONELLA.		02.0210
Foreign-Body Reaction
Chronic inflammation and granuloma formation around irritating foreign bodies.		03.411
Inflammation, Endodontic
[description not available]		02.4220
Pulpitis
Inflammation of the DENTAL PULP, usually due to bacterial infection in dental caries, tooth fracture, or other conditions causing exposure of the pulp to bacterial invasion. Chemical irritants, thermal factors, hyperemic changes, and other factors may also cause pulpitis.		02.4220
Cancer of Sigmoid
[description not available]		02.0210
Signet Ring Cell Carcinoma
[description not available]		02.0210
Pleural Effusion, Malignant
Presence of fluid in the PLEURAL CAVITY as a complication of malignant disease. Malignant pleural effusions often contain actual malignant cells.		02.0210
Carcinoma, Signet Ring Cell
A poorly differentiated adenocarcinoma in which the nucleus is pressed to one side by a cytoplasmic droplet of mucus. It usually arises in the gastrointestinal system.		02.0210
Shoulder Pain
Unilateral or bilateral pain of the shoulder. It is often caused by physical activities such as work or sports participation, but may also be pathologic in origin.		03.411
Edema, Pulmonary
[description not available]		02.0210
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.		07.0210
Gastritis, Familial Giant Hypertrophic
[description not available]		02.0210
Dermatitis, Contact, Photoallergic
[description not available]		02.0210
Amyotrophic Neuralgia
[description not available]		02.0210
Brachial Plexus Neuritis
A syndrome associated with inflammation of the BRACHIAL PLEXUS. Clinical features include severe pain in the shoulder region which may be accompanied by MUSCLE WEAKNESS and loss of sensation in the upper extremity. This condition may be associated with VIRUS DISEASES; IMMUNIZATION; SURGERY; heroin use (see HEROIN DEPENDENCE); and other conditions. The term brachial neuralgia generally refers to pain associated with brachial plexus injury. (From Adams et al., Principles of Neurology, 6th ed, pp1355-6)		02.0210
Arterial Obstructive Diseases
[description not available]		02.9310
Arterial Occlusive Diseases
Pathological processes which result in the partial or complete obstruction of ARTERIES. They are characterized by greatly reduced or absence of blood flow through these vessels. They are also known as arterial insufficiency.		02.9310
Brachial Plexopathy
[description not available]		02.0210
Brachial Plexus Neuropathies
Diseases of the cervical (and first thoracic) roots, nerve trunks, cords, and peripheral nerve components of the BRACHIAL PLEXUS. Clinical manifestations include regional pain, PARESTHESIA; MUSCLE WEAKNESS, and decreased sensation (HYPESTHESIA) in the upper extremity. These disorders may be associated with trauma (including BIRTH INJURIES); THORACIC OUTLET SYNDROME; NEOPLASMS; NEURITIS; RADIOTHERAPY; and other conditions. (From Adams et al., Principles of Neurology, 6th ed, pp1351-2)		02.0210
Bullous Dermatoses
[description not available]		02.4120
Methemoglobinemia
The presence of methemoglobin in the blood, resulting in cyanosis. A small amount of methemoglobin is present in the blood normally, but injury or toxic agents convert a larger proportion of hemoglobin into methemoglobin, which does not function reversibly as an oxygen carrier. Methemoglobinemia may be due to a defect in the enzyme NADH methemoglobin reductase (an autosomal recessive trait) or to an abnormality in hemoglobin M (an autosomal dominant trait). (Dorland, 27th ed)		07.0210
Rhinitis, Allergic, Nonseasonal
[description not available]		03.411
Rhinitis, Allergic, Perennial
Inflammation of the mucous membrane of the nose similar to that found in hay fever except that symptoms persist throughout the year. The causes are usually air-borne allergens, particularly dusts, feathers, molds, animal fur, etc.		03.411
B-Cell Chronic Lymphocytic Leukemia
[description not available]		02.0210
Leukemia, Lymphocytic, Chronic, B-Cell
A chronic leukemia characterized by abnormal B-lymphocytes and often generalized lymphadenopathy. In patients presenting predominately with blood and bone marrow involvement it is called chronic lymphocytic leukemia (CLL); in those predominately with enlarged lymph nodes it is called small lymphocytic lymphoma. These terms represent spectrums of the same disease.		02.0210
Arrhythmia
[description not available]		04.3341
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		04.3341
Amaurosis
[description not available]		02.9310
Scotoma
A localized defect in the visual field bordered by an area of normal vision. This occurs with a variety of EYE DISEASES (e.g., RETINAL DISEASES and GLAUCOMA); OPTIC NERVE DISEASES, and other conditions.		02.9310
Blindness
The inability to see or the loss or absence of perception of visual stimuli. This condition may be the result of EYE DISEASES; OPTIC NERVE DISEASES; OPTIC CHIASM diseases; or BRAIN DISEASES affecting the VISUAL PATHWAYS or OCCIPITAL LOBE.		02.9310
Chronic Motor and Vocal Tic Disorder
[description not available]		02.0210
Tourette Syndrome
A neuropsychological disorder related to alterations in DOPAMINE metabolism and neurotransmission involving frontal-subcortical neuronal circuits. Both multiple motor and one or more vocal tics need to be present with TICS occurring many times a day, nearly daily, over a period of more than one year. The onset is before age 18 and the disturbance is not due to direct physiological effects of a substance or another medical condition. The disturbance causes marked distress or significant impairment in social, occupational, or other important areas of functioning. (From DSM-IV, 1994; Neurol Clin 1997 May;15(2):357-79)		02.0210
Intraepithelial Prostatic Neoplasia
[description not available]		02.4320
Prostatic Intraepithelial Neoplasia
A premalignant change arising in the prostatic epithelium, regarded as the most important and most likely precursor of prostatic adenocarcinoma. The neoplasia takes the form of an intra-acinar or ductal proliferation of secretory cells with unequivocal nuclear anaplasia, which corresponds to nuclear grade 2 and 3 invasive prostate cancer.		02.4320
Eye Cancer, Retinoblastoma
[description not available]		02.4220
Retinoblastoma
A malignant tumor arising from the nuclear layer of the retina that is the most common primary tumor of the eye in children. The tumor tends to occur in early childhood or infancy and may be present at birth. The majority are sporadic, but the condition may be transmitted as an autosomal dominant trait. Histologic features include dense cellularity, small round polygonal cells, and areas of calcification and necrosis. An abnormal pupil reflex (leukokoria); NYSTAGMUS, PATHOLOGIC; STRABISMUS; and visual loss represent common clinical characteristics of this condition. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2104)		07.4220
Branch Vein Occlusion
[description not available]		02.4420
Retinal Vein Occlusion
Blockage of the RETINAL VEIN. Those at high risk for this condition include patients with HYPERTENSION; DIABETES MELLITUS; ATHEROSCLEROSIS; and other CARDIOVASCULAR DISEASES.		02.4420
Carcinoma, Adenosquamous
A mixed adenocarcinoma and squamous cell or epidermoid carcinoma.		06.4133
Experimental Leukemia
[description not available]		02.0210
Neoplasm Seeding
The local implantation of tumor cells by contamination of instruments and surgical equipment during and after surgical resection, resulting in local growth of the cells and tumor formation.		02.0210
Ascites
Accumulation or retention of free fluid within the peritoneal cavity.		08.8121
Gardner Syndrome
A variant of ADENOMATOUS POLYPOSIS COLI caused by mutation in the APC gene (GENES, APC) on CHROMOSOME 5. It is characterized by not only the presence of multiple colonic polyposis but also extracolonic ADENOMATOUS POLYPS in the UPPER GASTROINTESTINAL TRACT; the EYE; the SKIN; the SKULL; and the FACIAL BONES; as well as malignancy in organs other than the GI tract.		02.4320
Cocaine Abuse
[description not available]		03.4111
Cocaine-Related Disorders
Disorders related or resulting from use of cocaine.		03.4111
Erythema
Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes.		03.8121
Carotid Artery Narrowing
[description not available]		02.0210
Carotid Stenosis
Narrowing or stricture of any part of the CAROTID ARTERIES, most often due to atherosclerotic plaque formation. Ulcerations may form in atherosclerotic plaques and induce THROMBUS formation. Platelet or cholesterol emboli may arise from stenotic carotid lesions and induce a TRANSIENT ISCHEMIC ATTACK; CEREBROVASCULAR ACCIDENT; or temporary blindness (AMAUROSIS FUGAX). (From Adams et al., Principles of Neurology, 6th ed, pp 822-3)		02.0210
Brain Thrombosis
[description not available]		02.0210
Exertional Heat Illness
[description not available]		02.0210
Herpes Simplex Keratitis
[description not available]		02.0210
Keratitis, Herpetic
A superficial, epithelial Herpesvirus hominis infection of the cornea, characterized by the presence of small vesicles which may break down and coalesce to form dendritic ulcers (KERATITIS, DENDRITIC). (Dictionary of Visual Science, 3d ed)		02.0210
Atopic Hypersensitivity
[description not available]		05.5832
Nasal Catarrh
[description not available]		03.4111
Rhinitis
Inflammation of the NASAL MUCOSA, the mucous membrane lining the NASAL CAVITIES.		03.4111
Brain Damage, Chronic
A condition characterized by long-standing brain dysfunction or damage, usually of three months duration or longer. Potential etiologies include BRAIN INFARCTION; certain NEURODEGENERATIVE DISORDERS; CRANIOCEREBRAL TRAUMA; ANOXIA, BRAIN; ENCEPHALITIS; certain NEUROTOXICITY SYNDROMES; metabolic disorders (see BRAIN DISEASES, METABOLIC); and other conditions.		02.0210
Skin Diseases, Vascular
Skin diseases affecting or involving the cutaneous blood vessels and generally manifested as inflammation, swelling, erythema, or necrosis in the affected area.		03.4111
Infection
[description not available]		03.411
Infections
Invasion of the host organism by microorganisms or their toxins or by parasites that can cause pathological conditions or diseases.		03.411
Episcleritis
[description not available]		02.0210
Scleritis
Refers to any inflammation of the sclera including episcleritis, a benign condition affecting only the episclera, which is generally short-lived and easily treated. Classic scleritis, on the other hand, affects deeper tissue and is characterized by higher rates of visual acuity loss and even mortality, particularly in necrotizing form. Its characteristic symptom is severe and general head pain. Scleritis has also been associated with systemic collagen disease. Etiology is unknown but is thought to involve a local immune response. Treatment is difficult and includes administration of anti-inflammatory and immunosuppressive agents such as corticosteroids. Inflammation of the sclera may also be secondary to inflammation of adjacent tissues, such as the conjunctiva.		07.0210
Carcinoma, Bronchial
[description not available]		02.9410
Carcinoma, Bronchogenic
Malignant neoplasm arising from the epithelium of the BRONCHI. It represents a large group of epithelial lung malignancies which can be divided into two clinical groups: SMALL CELL LUNG CANCER and NON-SMALL-CELL LUNG CARCINOMA.		02.9410
Bronchial Hyperreactivity
Tendency of the smooth muscle of the tracheobronchial tree to contract more intensely in response to a given stimulus than it does in the response seen in normal individuals. This condition is present in virtually all symptomatic patients with asthma. The most prominent manifestation of this smooth muscle contraction is a decrease in airway caliber that can be readily measured in the pulmonary function laboratory.		02.0210
Kahler Disease
[description not available]		03.4111
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		110.4111
Duodenal Reflux
[description not available]		02.0210
Cancer of the Retina
[description not available]		02.0210
Acute Necrotizing Pancreatitis
[description not available]		07.4320
Alcohol Drinking
Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking.		03.4111
Respiratory Tract Neoplasms
New abnormal growth of tissue in the RESPIRATORY SYSTEM.		02.9410
Blood Diseases
[description not available]		03.4111
Hematologic Diseases
Disorders of the blood and blood forming tissues.		03.4111
Exposure, Dental Pulp
[description not available]		02.0210
Dental Pulp Exposure
The result of pathological changes in the hard tissue of a tooth caused by carious lesions, mechanical factors, or trauma, which render the pulp susceptible to bacterial invasion from the external environment.		02.0210
Bladder Neck Obstruction
[description not available]		02.0310
Urinary Calculi
Low-density crystals or stones in any part of the URINARY TRACT. Their chemical compositions often include CALCIUM OXALATE, magnesium ammonium phosphate (struvite), CYSTINE, or URIC ACID.		02.0210
Orbital Diseases
Diseases of the bony orbit and contents except the eyeball.		02.0310
Granulomatosis, Lipid
[description not available]		02.0310
Erdheim-Chester Disease
A rare form of non-Langerhans-cell histiocytosis (HISTIOCYTOSIS, NON-LANGERHANS-CELL) with onset in middle age. The systemic disease is characterized by infiltration of lipid-laden macrophages, multinucleated giant cells, an inflammatory infiltrate of lymphocytes and histiocytes in the bone marrow, and a generalized sclerosis of the long bones.		02.0310
Avian Diseases
[description not available]		02.0310
Benign Familial Infantile Convulsions
[description not available]		02.0310
Aneuploid
[description not available]		02.0310
Mouth Diseases
Diseases involving the MOUTH.		02.0310
Keratoderma Blennorrhagicum
[description not available]		02.0210
Papulosquamous Disorders
[description not available]		02.0210
Hand Dermatosis
[description not available]		02.0210
Hand Dermatoses
Skin diseases involving the HANDS.		02.0210
Keratosis
Any horny growth such as a wart or callus.		02.0210
Pink Eye
[description not available]		02.0310
Conjunctivitis
INFLAMMATION of the CONJUNCTIVA.		02.0310
Cancer of Gallbladder
[description not available]		02.0310
Gallbladder Neoplasms
Tumors or cancer of the gallbladder.		02.0310
Acute Autoimmune Neuropathy
[description not available]		02.0310
Porphyria
[description not available]		02.0310
Porphyrias
A diverse group of metabolic diseases characterized by errors in the biosynthetic pathway of HEME in the LIVER, the BONE MARROW, or both. They are classified by the deficiency of specific enzymes, the tissue site of enzyme defect, or the clinical features that include neurological (acute) or cutaneous (skin lesions). Porphyrias can be hereditary or acquired as a result of toxicity to the hepatic or erythropoietic marrow tissues.		02.0310
Guillain-Barre Syndrome
An acute inflammatory autoimmune neuritis caused by T cell- mediated cellular immune response directed towards peripheral myelin. Demyelination occurs in peripheral nerves and nerve roots. The process is often preceded by a viral or bacterial infection, surgery, immunization, lymphoma, or exposure to toxins. Common clinical manifestations include progressive weakness, loss of sensation, and loss of deep tendon reflexes. Weakness of respiratory muscles and autonomic dysfunction may occur. (From Adams et al., Principles of Neurology, 6th ed, pp1312-1314)		02.0310
Jaundice, Cholestatic
[description not available]		02.0210
Jaundice, Obstructive
Jaundice, the condition with yellowish staining of the skin and mucous membranes, that is due to impaired BILE flow in the BILIARY TRACT, such as INTRAHEPATIC CHOLESTASIS, or EXTRAHEPATIC CHOLESTASIS.		02.0210
Fractures, Ununited
A fracture in which union fails to occur, the ends of the bone becoming rounded and eburnated, and a false joint occurs. (Stedman, 25th ed)		02.0310
Entrapment Neuropathies
[description not available]		02.0310
Intestinal Perforation
Opening or penetration through the wall of the INTESTINES.		02.0310
Sigmoid Colon Diseases
[description not available]		02.0310
Growth Plate Fractures
[description not available]		02.0310
Leukemic Infiltration
A pathologic change in leukemia in which leukemic cells permeate various organs at any stage of the disease. All types of leukemia show various degrees of infiltration, depending upon the type of leukemia. The degree of infiltration may vary from site to site. The liver and spleen are common sites of infiltration, the greatest appearing in myelocytic leukemia, but infiltration is seen also in the granulocytic and lymphocytic types. The kidney is also a common site and of the gastrointestinal system, the stomach and ileum are commonly involved. In lymphocytic leukemia the skin is often infiltrated. The central nervous system too is a common site.		02.0310
Staphylococcal Pneumonia
[description not available]		02.0310
Pneumonia, Staphylococcal
Pneumonia caused by infections with bacteria of the genus STAPHYLOCOCCUS, usually with STAPHYLOCOCCUS AUREUS.		02.0310
Hyponatremia
Deficiency of sodium in the blood; salt depletion. (Dorland, 27th ed)		03.4111
Chronic Lymphocytic Thyroiditis
[description not available]		03.4111
Hashimoto Disease
Chronic autoimmune thyroiditis, characterized by the presence of high serum thyroid AUTOANTIBODIES; GOITER; and HYPOTHYROIDISM.		03.4111
Hypokalemia
Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed)		03.4211
Bronchial Diseases
Diseases involving the BRONCHI.		02.0310
Cystadenocarcinoma, Serous
A malignant cystic or semicystic neoplasm. It often occurs in the ovary and usually bilaterally. The external surface is usually covered with papillary excrescences. Microscopically, the papillary patterns are predominantly epithelial overgrowths with differentiated and undifferentiated papillary serous cystadenocarcinoma cells. Psammoma bodies may be present. The tumor generally adheres to surrounding structures and produces ascites. (From Hughes, Obstetric-Gynecologic Terminology, 1972, p185)		02.0310
Leukocytopenia
[description not available]		05.322
Rectovaginal Fistula
An abnormal anatomical passage between the RECTUM and the VAGINA.		03.4211
Leukopenia
A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000).		05.322
Acrodermatitis
Inflammation involving the skin of the extremities, especially the hands and feet. Several forms are known, some idiopathic and some hereditary. The infantile form is called Gianotti-Crosti syndrome.		02.0310
Basal Ganglia Diseases
Diseases of the BASAL GANGLIA including the PUTAMEN; GLOBUS PALLIDUS; claustrum; AMYGDALA; and CAUDATE NUCLEUS. DYSKINESIAS (most notably involuntary movements and alterations of the rate of movement) represent the primary clinical manifestations of these disorders. Common etiologies include CEREBROVASCULAR DISORDERS; NEURODEGENERATIVE DISEASES; and CRANIOCEREBRAL TRAUMA.		03.4211
Gastric Stasis
[description not available]		02.0310
Gastroparesis
Chronic delayed gastric emptying. Gastroparesis may be caused by motor dysfunction or paralysis of STOMACH muscles or may be associated with other systemic diseases such as DIABETES MELLITUS.		02.0310
Mucositis
An INFLAMMATION of the MUCOSA with burning or tingling sensation. It is characterized by atrophy of the squamous EPITHELIUM, vascular damage, inflammatory infiltration, and ulceration. It usually occurs at the mucous lining of the MOUTH, the GASTROINTESTINAL TRACT or the airway due to chemical irritations, CHEMOTHERAPY, or radiation therapy (RADIOTHERAPY).		03.4211
Fractures, Closed
Fractures in which the break in bone is not accompanied by an external wound.		02.0310
Brain Hemorrhage
[description not available]		02.0310
Intracranial Hemorrhages
Bleeding within the SKULL, including hemorrhages in the brain and the three membranes of MENINGES. The escape of blood often leads to the formation of HEMATOMA in the cranial epidural, subdural, and subarachnoid spaces.		02.0310
Low Bone Density
[description not available]		02.4420
Bone Diseases, Metabolic
Diseases that affect the METABOLIC PROCESSES of BONE TISSUE.		02.4420
Diffuse Cutaneous Systemic Sclerosis
[description not available]		02.0310
Basedow Disease
[description not available]		02.0310
Fasciitis
Inflammation of the fascia. There are three major types: 1, Eosinophilic fasciitis, an inflammatory reaction with eosinophilia, producing hard thickened skin with an orange-peel configuration suggestive of scleroderma and considered by some a variant of scleroderma; 2, Necrotizing fasciitis (FASCIITIS, NECROTIZING), a serious fulminating infection (usually by a beta hemolytic streptococcus) causing extensive necrosis of superficial fascia; 3, Nodular/Pseudosarcomatous /Proliferative fasciitis, characterized by a rapid growth of fibroblasts with mononuclear inflammatory cells and proliferating capillaries in soft tissue, often the forearm; it is not malignant but is sometimes mistaken for fibrosarcoma.		02.0310
Graves Disease
A common form of hyperthyroidism with a diffuse hyperplastic GOITER. It is an autoimmune disorder that produces antibodies against the THYROID STIMULATING HORMONE RECEPTOR. These autoantibodies activate the TSH receptor, thereby stimulating the THYROID GLAND and hypersecretion of THYROID HORMONES. These autoantibodies can also affect the eyes (GRAVES OPHTHALMOPATHY) and the skin (Graves dermopathy).		02.0310
Scleroderma, Diffuse
A rapid onset form of SYSTEMIC SCLERODERMA with progressive widespread SKIN thickening over the arms, the legs and the trunk, resulting in stiffness and disability.		02.0310
Meniscitis
[description not available]		02.0410
Hypersensitivity, Type III
[description not available]		02.0310
Cataract, Membranous
[description not available]		02.0310
Cataract
Partial or complete opacity on or in the lens or capsule of one or both eyes, impairing vision or causing blindness. The many kinds of cataract are classified by their morphology (size, shape, location) or etiology (cause and time of occurrence). (Dorland, 27th ed)		02.0310
Ulna Fractures
Fractures of the larger bone of the forearm.		02.0310
Bone Stress Reaction
[description not available]		02.0310
Acute Promyelocytic Leukemia
[description not available]		07.0310
Leukemia, Promyelocytic, Acute
An acute myeloid leukemia in which abnormal PROMYELOCYTES predominate. It is frequently associated with DISSEMINATED INTRAVASCULAR COAGULATION.		02.0310
Eye Hemorrhage
Intraocular hemorrhage from the vessels of various tissues of the eye.		02.0310
Birth Weight
The mass or quantity of heaviness of an individual at BIRTH. It is expressed by units of pounds or kilograms.		03.4211
Fibromatosis
[description not available]		02.0310
Hydronephrosis
Abnormal enlargement or swelling of a KIDNEY due to dilation of the KIDNEY CALICES and the KIDNEY PELVIS. It is often associated with obstruction of the URETER or chronic kidney diseases that prevents normal drainage of urine into the URINARY BLADDER.		02.0310
Fibroma
A benign tumor of fibrous or fully developed connective tissue.		02.0310
ATLL
[description not available]		02.0410
Leukemia-Lymphoma, Adult T-Cell
Aggressive T-Cell malignancy with adult onset, caused by HUMAN T-LYMPHOTROPIC VIRUS 1. It is endemic in Japan, the Caribbean basin, Southeastern United States, Hawaii, and parts of Central and South America and sub-Saharan Africa.		02.0410
Rhabdomyolysis
Necrosis or disintegration of skeletal muscle often followed by myoglobinuria.		02.0310
Acute Hepatic Failure
[description not available]		02.0310
Liver Failure, Acute
A form of rapid-onset LIVER FAILURE, also known as fulminant hepatic failure, caused by severe liver injury or massive loss of HEPATOCYTES. It is characterized by sudden development of liver dysfunction and JAUNDICE. Acute liver failure may progress to exhibit cerebral dysfunction even HEPATIC COMA depending on the etiology that includes hepatic ISCHEMIA, drug toxicity, malignant infiltration, and viral hepatitis such as post-transfusion HEPATITIS B and HEPATITIS C.		02.0310
Embolism, Pulmonary
[description not available]		04.3411
Endotoxin Shock
[description not available]		04.3411
Pulmonary Embolism
Blocking of the PULMONARY ARTERY or one of its branches by an EMBOLUS.		04.3411
Shock, Septic
Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.		04.3411
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		03.4311
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		03.4311
Pocket, Periodontal
[description not available]		03.4311
Periodontal Pocket
An abnormal extension of a gingival sulcus accompanied by the apical migration of the epithelial attachment and bone resorption.		03.4311
Lactic Acidosis
[description not available]		07.0410
Acidosis, Lactic
Acidosis caused by accumulation of lactic acid more rapidly than it can be metabolized. It may occur spontaneously or in association with diseases such as DIABETES MELLITUS; LEUKEMIA; or LIVER FAILURE.		02.0410
Rupture
Forcible or traumatic tear or break of an organ or other soft part of the body.		03.4311
Algodystrophic Syndrome
[description not available]		02.0410
Reflex Sympathetic Dystrophy
A syndrome characterized by severe burning pain in an extremity accompanied by sudomotor, vasomotor, and trophic changes in bone without an associated specific nerve injury. This condition is most often precipitated by trauma to soft tissue or nerve complexes. The skin over the affected region is usually erythematous and demonstrates hypersensitivity to tactile stimuli and erythema. (Adams et al., Principles of Neurology, 6th ed, p1360; Pain 1995 Oct;63(1):127-33)		02.0410
Left Ventricular Dysfunction
[description not available]		02.0410
Cardiomyopathy, Hypertrophic Obstructive
[description not available]		02.0410
Cardiomyopathy, Hypertrophic
A form of CARDIAC MUSCLE disease, characterized by left and/or right ventricular hypertrophy (HYPERTROPHY, LEFT VENTRICULAR; HYPERTROPHY, RIGHT VENTRICULAR), frequent asymmetrical involvement of the HEART SEPTUM, and normal or reduced left ventricular volume. Risk factors include HYPERTENSION; AORTIC STENOSIS; and gene MUTATION; (FAMILIAL HYPERTROPHIC CARDIOMYOPATHY).		02.0410
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		02.0410
Neurogenic Inflammation
Inflammation caused by an injurious stimulus of peripheral neurons and resulting in release of neuropeptides which affect vascular permeability and help initiate proinflammatory and immune reactions at the site of injury.		02.0410
Blood Pressure, Low
[description not available]		01.9910
Hypotension
Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.		01.9910
Infectious Diseases
[description not available]		0210
Communicable Diseases
An illness caused by an infectious agent or its toxins that occurs through the direct or indirect transmission of the infectious agent or its products from an infected individual or via an animal, vector or the inanimate environment to a susceptible animal or human host.		0210
Peptic Ulcer Perforation
Penetration of a PEPTIC ULCER through the wall of DUODENUM or STOMACH allowing the leakage of luminal contents into the PERITONEAL CAVITY.		02.420
Blunt Injuries
[description not available]		0210
Cutaneous T-Cell Lymphoma
[description not available]		0210
Lymphoma, T-Cell, Cutaneous
A group of lymphomas exhibiting clonal expansion of malignant T-lymphocytes arrested at varying stages of differentiation as well as malignant infiltration of the skin. MYCOSIS FUNGOIDES; SEZARY SYNDROME; LYMPHOMATOID PAPULOSIS; and PRIMARY CUTANEOUS ANAPLASTIC LARGE CELL LYMPHOMA are the best characterized of these disorders.		0210
Hallucination of Body Sensation
[description not available]		0210
Hallucinations
Subjectively experienced sensations in the absence of an appropriate stimulus, but which are regarded by the individual as real. They may be of organic origin or associated with MENTAL DISORDERS.		0710
Ecchymosis
Extravasation of blood into the skin, resulting in a nonelevated, rounded or irregular, blue or purplish patch, larger than a petechia.		0210
Connective Tissue Diseases
A heterogeneous group of disorders, some hereditary, others acquired, characterized by abnormal structure or function of one or more of the elements of connective tissue, i.e., collagen, elastin, or the mucopolysaccharides.		02.4120
Deficiency, Factor II
[description not available]		0210
Sunburn
An injury to the skin causing erythema, tenderness, and sometimes blistering and resulting from excessive exposure to the sun. The reaction is produced by the ultraviolet radiation in sunlight.		0210
Adamantiades-Behcet Disease
[description not available]		0210
Forestier-Certonciny Syndrome
[description not available]		0210
Aortic Arteritis, Giant Cell
[description not available]		0210
Anti-Phospholipid Antibody Syndrome
[description not available]		02.4120
Amyloidosis
A group of sporadic, familial and/or inherited, degenerative, and infectious disease processes, linked by the common theme of abnormal protein folding and deposition of AMYLOID. As the amyloid deposits enlarge they displace normal tissue structures, causing disruption of function. Various signs and symptoms depend on the location and size of the deposits.		0210
Behcet Syndrome
Rare chronic inflammatory disease involving the small blood vessels. It is of unknown etiology and characterized by mucocutaneous ulceration in the mouth and genital region and uveitis with hypopyon. The neuro-ocular form may cause blindness and death. SYNOVITIS; THROMBOPHLEBITIS; gastrointestinal ulcerations; RETINAL VASCULITIS; and OPTIC ATROPHY may occur as well.		0210
Polymyalgia Rheumatica
A syndrome in the elderly characterized by proximal joint and muscle pain, high erythrocyte sedimentation rate, and a self-limiting course. Pain is usually accompanied by evidence of an inflammatory reaction. Women are affected twice as commonly as men and Caucasians more frequently than other groups. The condition is frequently associated with GIANT CELL ARTERITIS and some theories pose the possibility that the two diseases arise from a single etiology or even that they are the same entity.		0210
Giant Cell Arteritis
A systemic autoimmune disorder that typically affects medium and large ARTERIES, usually leading to occlusive granulomatous vasculitis with transmural infiltrate containing multinucleated GIANT CELLS. The TEMPORAL ARTERY is commonly involved. This disorder appears primarily in people over the age of 50. Symptoms include FEVER; FATIGUE; HEADACHE; visual impairment; pain in the jaw and tongue; and aggravation of pain by cold temperatures. (From Adams et al., Principles of Neurology, 6th ed)		0210
Antiphospholipid Syndrome
The presence of antibodies directed against phospholipids (ANTIBODIES, ANTIPHOSPHOLIPID). The condition is associated with a variety of diseases, notably systemic lupus erythematosus and other connective tissue diseases, thrombopenia, and arterial or venous thromboses. In pregnancy it can cause abortion. Of the phospholipids, the cardiolipins show markedly elevated levels of anticardiolipin antibodies (ANTIBODIES, ANTICARDIOLIPIN). Present also are high levels of lupus anticoagulant (LUPUS COAGULATION INHIBITOR).		02.4120
Cough
A sudden, audible expulsion of air from the lungs through a partially closed glottis, preceded by inhalation. It is a protective response that serves to clear the trachea, bronchi, and/or lungs of irritants and secretions, or to prevent aspiration of foreign materials into the lungs.		08.3911
Cutis Laxa
A group of connective tissue diseases in which skin hangs in loose pendulous folds. It is believed to be associated with decreased elastic tissue formation as well as an abnormality in elastin formation. Cutis laxa is usually a genetic disease, but acquired cases have been reported. (From Dorland, 27th ed)		0210
Osteolysis
Dissolution of bone that particularly involves the removal or loss of calcium.		0210
Amnionitis
[description not available]		0210
Patency of the Ductus Arteriosus
[description not available]		0210
Chorioamnionitis
INFLAMMATION of the placental membranes (CHORION; AMNION) and connected tissues such as fetal BLOOD VESSELS and UMBILICAL CORD. It is often associated with intrauterine ascending infections during PREGNANCY.		0210
Ductus Arteriosus, Patent
A congenital heart defect characterized by the persistent opening of fetal DUCTUS ARTERIOSUS that connects the PULMONARY ARTERY to the descending aorta (AORTA, DESCENDING) allowing unoxygenated blood to bypass the lung and flow to the PLACENTA. Normally, the ductus is closed shortly after birth.		0210
Burns, Chemical
Burns caused by contact with or exposure to CAUSTICS or strong ACIDS.		0210
Pleural Effusion
Presence of fluid in the pleural cavity resulting from excessive transudation or exudation from the pleural surfaces. It is a sign of disease and not a diagnosis in itself.		0210
Delirium of Mixed Origin
[description not available]		0210
Delirium
A disorder characterized by CONFUSION; inattentiveness; disorientation; ILLUSIONS; HALLUCINATIONS; agitation; and in some instances autonomic nervous system overactivity. It may result from toxic/metabolic conditions or structural brain lesions. (From Adams et al., Principles of Neurology, 6th ed, pp411-2)		0710
Water-Electrolyte Imbalance
Disturbances in the body's WATER-ELECTROLYTE BALANCE.		0210
Oliguria
Decreased URINE output that is below the normal range. Oliguria can be defined as urine output of less than or equal to 0.5 or 1 ml/kg/hr depending on the age.		0210
Contact Dermatitis
[description not available]		02.0110
Mange, Sarcoptic
[description not available]		02.0110
Dermatitis, Contact
A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.		02.0110
Scabies
A contagious cutaneous inflammation caused by the bite of the mite SARCOPTES SCABIEI. It is characterized by pruritic papular eruptions and burrows and affects primarily the axillae, elbows, wrists, and genitalia, although it can spread to cover the entire body.		02.0110
Allergic Neuritis, Experimental
[description not available]		02.0110
Esophageal Diseases
Pathological processes in the ESOPHAGUS.		02.0110
Infections, Rhabdoviridae
[description not available]		02.0110
DDD MPGNII
[description not available]		02.0110
Glomerulonephritis, Membranoproliferative
Chronic glomerulonephritis characterized histologically by proliferation of MESANGIAL CELLS, increase in the MESANGIAL EXTRACELLULAR MATRIX, and a thickening of the glomerular capillary walls. This may appear as a primary disorder or secondary to other diseases including infections and autoimmune disease SYSTEMIC LUPUS ERYTHEMATOSUS. Various subtypes are classified by their abnormal ultrastructures and immune deposits. Hypocomplementemia is a characteristic feature of all types of MPGN.		02.0110
Acute Respiratory Distress Syndrome
[description not available]		02.0110
Respiratory Distress Syndrome
A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.		02.0110
Pouch Ileitis
[description not available]		02.0110
Pouchitis
Acute INFLAMMATION in the INTESTINAL MUCOSA of the continent ileal reservoir (or pouch) in patients who have undergone ILEOSTOMY and restorative proctocolectomy (PROCTOCOLECTOMY, RESTORATIVE).		02.0110
Brachial Paresis
[description not available]		02.0110