Page last updated: 2024-11-04

meclofenamic acid

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Description

Meclofenamic acid is a non-steroidal anti-inflammatory drug (NSAID) that is used to treat pain and inflammation. It is available in both oral and topical forms. Meclofenamic acid is thought to work by inhibiting the production of prostaglandins, which are chemicals that cause pain and inflammation. The drug was first synthesized in 1964 and has been used to treat a variety of conditions, including rheumatoid arthritis, osteoarthritis, and menstrual cramps. Meclofenamic acid is a potent anti-inflammatory agent that is effective in reducing pain and inflammation associated with a variety of conditions. The drug is well-absorbed after oral administration and has a long duration of action. Meclofenamic acid is generally well-tolerated, but it can cause side effects such as gastrointestinal upset, headache, and dizziness. The drug is not recommended for use in people with a history of stomach ulcers or bleeding, or those who are allergic to aspirin or other NSAIDs. Meclofenamic acid is studied extensively as a potential treatment for a variety of diseases, including cancer, Alzheimer's disease, and Parkinson's disease.'

Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [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]

Cross-References

ID SourceID
PubMed CID4037
CHEMBL ID509
CHEBI ID6710
SCHEMBL ID106
MeSH IDM0013184

Synonyms (112)

Synonym
nsc 95309
acidum meclofenamicum [inn-latin]
einecs 211-419-5
benzoic acid, 2-((2,6-dichloro-3-methylphenyl)amino)-
ccris 5532
meclofenamic acid [usan:inn:ban]
acido meclofenamico [inn-spanish]
brn 2221428
acide meclofenamique [inn-french]
anthranilic acid, n-(2,6-dichloro-m-tolyl)-
2-((2,6-dichloro-3-methylphenyl)amino)benzoic acid
BRD-K50398167-323-03-3
BRD-K50398167-236-02-9
KBIO1_000504
DIVK1C_000504
bdbm22971
chembl509 ,
SPECTRUM_000893
SPECTRUM5_000942
UNM000001246303
BSPBIO_000191
inf 4668
n-(2,6-dichloro-m-tolyl)anthranilic acid
arquel
n-(3-methyl-2,6-dichlorophenyl)anthranilic acid
anthranilic acid,6-dichloro-m-tolyl)-
nsc95309
2-(2,6-dichloro-3-methylphenyl)aminobenzoic acid
meclophenamic acid
cl 583
ci-583 ,
benzoic acid,6-dichloro-3-methylphenyl)amino]-
meclomen (free acid)
inf-4668
nsc-95309
PRESTWICK3_000206
BPBIO1_000211
PRESTWICK2_000206
IDI1_000504
BSPBIO_001951
2-[(2,6-dichloro-3-methylphenyl)amino]benzoic acid
benzoic acid, 2-[(2,6-dichloro-3-methylphenyl)amino]-
inchi=1/c14h11cl2no2/c1-8-6-7-10(15)13(12(8)16)17-11-5-3-2-4-9(11)14(18)19/h2-7,17h,1h3,(h,18,19
644-62-2
C07117
meclofenamic acid
meclofenamate
DB00939
n-(2,6-dichloro-3-methylphenyl)anthranilic acid
meclofenamic acid (usan/inn)
D02341
LOPAC0_000727
KBIO3_001451
KBIO2_003941
KBIOSS_001373
KBIO2_006509
KBIOGR_000475
KBIO2_001373
SPBIO_002112
SPECTRUM2_001045
NINDS_000504
SPBIO_000970
PRESTWICK0_000206
SPECTRUM4_000038
SPECTRUM3_000486
PRESTWICK1_000206
NCGC00021132-01
chebi:6710 ,
cl-583
2-(2,6-dichloro-3-methylanilino)benzoic acid
AKOS012836983
JMS ,
2-[(2,6-dichloro-3-methyl-phenyl)amino]benzoic acid
acide meclofenamique
48i5lu4zwd ,
acido meclofenamico
unii-48i5lu4zwd
acidum meclofenamicum
FT-0610786
meclofenamic acid [green book]
meclofenamic acid [mi]
meclofenamic acid [vandf]
meclofenamic acid [usan]
meclofenamate [vandf]
meclofenamic acid [inn]
meclofenamic acid [mart.]
meclofenamic acid [who-dd]
gtpl7219
SCHEMBL106
DTXSID0048559 ,
2-[(2,6-dichloro-3-methylphenyl)amino]-benzoic acid
W-104838
SBI-0050705.P004
Q2823284
SDCCGSBI-0050705.P005
644-62-2 (free acid)
meclofenamic-acid
M-210
2-(2,6-dichloro-3-methylanilino)benzoic acid.
CS-0064844
HY-117275
2-((2,6-dichloro-3-methylphenyl)amino)benzoicacid
EN300-708777
arquel tablets
acidum meclofenamicum (inn-latin)
m02aa18
acide meclofenamique (inn-french)
meclofenamic acid (mart.)
dtxcid3028188
arquel granules
acido meclofenamico (inn-spanish)
m01ag04

Research Excerpts

Overview

Meclofenamic acid is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia) It has shown therapeutic potential for different types of cancers, including androgen-independent prostate neoplasms.

ExcerptReferenceRelevance
"Meclofenamic acid is a nonsteroidal anti-inflammatory drug that has shown therapeutic potential for different types of cancers, including androgen-independent prostate neoplasms. "( Histological changes caused by meclofenamic acid in androgen-independent prostate cancer tumors: evaluation in a mouse model.
Delgado-Enciso, I; Espinoza-Gómez, F; Galvan-Salazar, HR; Gonzalez-Alvarez, R; Guzman-Esquivel, J; Lara-Esqueda, A; Martinez-Martinez, R; Montes-Galindo, DA; Newton-Sanchez, OA; Rodriguez-Hernandez, A; Soriano-Hernández, AD; Valdez-Velazquez, LL,
)
1.86
"Meclofenamic acid was shown to be a potential antineoplastic agent for both androgen-dependent and androgen-independent prostate cancer."( Antitumor effect of meclofenamic acid on human androgen-independent prostate cancer: a preclinical evaluation.
Baltazar-Rodriguez, LM; Delgado-Enciso, I; Espinoza-Gómez, F; Galvan-Salazar, HR; Gonzalez-Alvarez, R; Guzman-Esquivel, J; Martinez-Martinez, R; Montes-Galindo, DA; Ortiz-Lopez, R; Rodriguez-Hernandez, A; Rojas-Martinez, A; Soriano-Hernández, AD; Valdez-Velazquez, LL, 2012
)
2.15
"Meclofenamic acid has proved to be a drug of choice in the treatment of slight to moderate musculo-skeletal pain syndromes."( [A comparative evaluation of the remission from acute lumbar-sciatic pain following treatment with meclofenamic acid and naproxen].
Fontanesi, G; Mele, C, 1993
)
1.22
"Meclofenamic acid is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). "( Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium.
Conroy, MC; Randinitis, EJ; Turner, JL, 1991
)
1.72
"Meclofenamic acid is an analgesic endowed with anti-inflammatory properties. "( Clinical experiences in the treatment of pain in rheumatology.
Pellegrini, P, 1991
)
1.72

Effects

Meclofenamic acid has been successfully used in several obstetrical and gynecological disorders sustained by a prostaglandin overproduction.

ExcerptReferenceRelevance
"Meclofenamic acid has proved to be a drug of choice in the treatment of slight to moderate musculo-skeletal pain syndromes."( [A comparative evaluation of the remission from acute lumbar-sciatic pain following treatment with meclofenamic acid and naproxen].
Fontanesi, G; Mele, C, 1993
)
1.22
"Meclofenamic acid has been successfully used in several obstetrical and gynecological disorders sustained by a prostaglandin overproduction. "( Use of meclofenamic acid in gynecology and obstetrics: effects on postsurgical stress.
De Pietri, R; Facchinetti, F; Genazzani, AR; Giunchi, M, 1991
)
2.18

Actions

ExcerptReferenceRelevance
"Meclofenamic acid was used to inhibit prostaglandin synthesis in lambs challenged with Ostertagia circumcincta. "( Effect of meclofenamic acid on the response of parasite-naive lambs and adult sheep to Ostertagia circumcincta.
Bogan, JA; McKellar, QA; Mitchell, ES, 1990
)
2.12

Treatment

Meclofenamic acid treatment in late pregnancy modified the normal initiation of lactation. High concentration of lactose and low concentrations of protein and Na+ in colostrum in treated sows compared to controls.

ExcerptReferenceRelevance
"Meclofenamic acid treatment in late pregnancy modified the normal initiation of lactation, as indicated by the high concentration of lactose and low concentrations of protein and Na+ in colostrum in treated sows compared to controls."( Influence of meclofenamic acid on the initiation of parturition and lactation in the sow.
Barker, I; Gooneratne, AD; Hartmann, PE, 1982
)
1.35
"Pretreatment with meclofenamic acid, resveratrol or paxilline before UVA irradiation was also performed."( Resveratrol protects against ultraviolet A-mediated inhibition of the phagocytic function of human retinal pigment epithelial cells via large-conductance calcium-activated potassium channels.
Sheu, SJ; Wu, TT, 2009
)
0.68
"Treatment with meclofenamic acid supported the establishment of pregnancy in recipient mares that ovulated before the donors. "( Meclofenamic acid extends donor-recipient asynchrony in equine embryo transfer.
Allen, WR; Kölling, M; Wilsher, S, 2006
)
2.13

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
" The rapid onset of activity of meclofenamic acid and its duration of action may be the result of its pharmacokinetic profile."( Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium.
Conroy, MC; Randinitis, EJ; Turner, JL, 1991
)
0.56

Compound-Compound Interactions

ExcerptReferenceRelevance
" Amongst the various NSAID compounds, Mefenamic acid (MEFE) and Meclofenamic acid (MECLO) showed considerable antiviral activity against viral replication individually or in combination with the common antiviral drug, Ribavirin (RIBA)."( Mefenamic acid in combination with ribavirin shows significant effects in reducing chikungunya virus infection in vitro and in vivo.
Abdulrahman, AY; Bahrani, H; Mohamed, Z; Othman, S; Rahman, NA; Rashid, NN; Rothan, HA; Teoh, TC; Yusof, R, 2016
)
0.67

Bioavailability

ExcerptReferenceRelevance
" More rapid and higher peak levels occurred following sodium meclofenamate than meclofenamic acid, although total bioavailability was similar."( The pharmacokinetics of meclofenamic acid in the horse.
Baxter, P; Snow, DH; Whiting, B, 1981
)
0.8
" The bioavailability was 48."( Comparison of the kinetics of sodium meclofenamate versus meclofenamic acid after oral administration to sheep.
Boggio, JC; de Vicente, ML; Encinas, T; Rodriguez, C; San Andres, MI; Vinagre, E, 1995
)
0.54
" The objectives of this study were to describe the pharmacokinetic behaviour of sodium meclofenamate after intravenous and oral administration to sheep and to determine the influence of closure of the reticular groove on the bioavailability of the drug."( Influence of closure of the reticular groove on the bioavailability and disposition kinetics of meclofenamate in sheep.
Boggio, JC; Encinas, T; Rodríguez, C; San Andrés, MD; San Andrés, MI; Vinagre, E, 1996
)
0.29
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" The orally bioavailable modulators of gap junctions meclofenamate and tonabersat break this paracrine loop, and we provide proof-of-principle that these drugs could be used to treat established brain metastasis."( Carcinoma-astrocyte gap junctions promote brain metastasis by cGAMP transfer.
Boire, A; Chen, Q; Cross, JR; Er, EE; Jacob, L; Jin, X; Lopez-Soto, A; Massagué, J; Patwa, R; Shah, H; Valiente, M; Xu, K, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
") shifted all the dose-response curves for PGF2 alpha (i."( Central cardiovascular and thermal effects of prostaglandin F2 alpha in rats.
Eskeli-Kaivosoja, A; Karppanen, H; Sirén, AL, 1979
)
0.26
" Sodium meclofenamate is completely bioavailable from capsules relative to an oral suspension dosage form."( Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium.
Conroy, MC; Randinitis, EJ; Turner, JL, 1991
)
0.28
" An initial 300 mg oral dose on day 1 was followed by a 100 mg every 8 h dosage regimen on study days 4 through 18."( A single and multiple dose pharmacokinetic and metabolism study of meclofenamate sodium.
Dyer, R; Kinkel, AW; Koup, JR; Sedman, AJ; Sharoky, M; Thomas, DJ; Tucker, E,
)
0.13
" The dose-response curve for vasopressin-sensitive Pf showed the Km to be 1 microU ml-1."( Modulation of vasopressin-induced water permeability of the cortical collecting tubule by endogenous and exogenous prostaglandins.
Stokes, JB, 1985
)
0.27
" BWA1433U induced a parallel shift of the adenosine dose-response curve to the right; however, it had no significant inhibitory effect on the decrease in lobar arterial pressure in response to ATP."( Adenosine does not mediate the pulmonary vasodilator response of adenosine 5'-triphosphate in the feline pulmonary vascular bed.
Hyman, AL; Kadowitz, PJ; Lippton, H; Neely, CF; Neiman, M, 1989
)
0.28
" LTB4 alone caused an increase in serum thromboxane B2 (TxB2) from 130 +/- 35 to 320 +/- 17 pg/ml 3 minutes after dosing but did not increase TxB2 following pre-treatment with meclofenamate."( Meclofenamate blocks the pulmonary arterial vasopressor effects of leukotriene B4 in awake sheep.
Lefferts, PL; Miller, RF; Purvis, AW; Snapper, JR, 1988
)
0.27
" Interestingly, in the absence of 1-methyl-3-isobutylxanthine (or an adenosine blocker), or in the presence of 1-methyl-3-isobutylxanthine (2 mM) and forskolin (30 microM), prostaglandin E1 (1 nM-100 microM) exhibited biphasic dose-response kinetics."( Interaction between prostaglandin E1 and forskolin in modulation of cyclic AMP levels in rat epididymal adipocytes.
Fatemi, SH, 1985
)
0.27
" Neither the hydrocortisone nor the meclofenamate sodium at the dosage used adversely affected osteoid formation."( Comparison of meclofenamate sodium and hydrocortisone for controlling the postsurgical inflammatory response in rats.
Hutton, CE; Kafrawy, AH; Potter, RH; Shieh, HL, 1988
)
0.27
" Three consecutive histamine dose-response curves were obtained in nine dogs pretreated with 5 mg/kg indomethacin; two of these nine were also pretreated with 10 mg/kg indomethacin."( Histamine tachyphylaxis in canine airways despite prostaglandin synthesis inhibition.
Antol, PJ; Gunst, SJ; Hyatt, RE, 1988
)
0.27
"In diabetes the sensitivity of isolated rat aortae to serotonin is greatly diminished and the dose-response curve is shifted to the right."( Experimental diabetes: reduction of serotonin-induced vasoconstriction by meclofenamic acid in vitro.
Hagen, AA; Shirasawa, Y; White, RP, 1985
)
0.5
" Dose-response relationships for inhibition of 45Ca uptake were identical with controls in mitochondria isolated from normal or essential fatty acid-deficient Long-Evans rats even though PGE synthesis in essential fatty acid-deficient was only 20% of that in normal rats."( Prostaglandin-independent inhibition of calcium transport by nonsteroidal anti-inflammatory drugs: differential effects of carboxylic acids and piroxicam.
Burch, RM; Halushka, PV; Wise, WC, 1983
)
0.27
" Meclofenamate sodium, even at these high dosage levels, was better tolerated than indometacin."( Meclofenamate sodium in the treatment of acute gout. Results of a double-blind study.
Dunky, A; Eberl, R, 1983
)
0.27
"1 X EC50) of NA were calculated from dose-response curves."( Effects of cyclooxygenase inhibitors and PGI2 on the adrenergic contractions of isolated rabbit arteries.
Hadházy, P; Magyar, K; Malomvölgyi, B, 1984
)
0.27
" The peptides produced dose-related increases in perfusion pressure, and dose-response curves to all six peptides were parallel."( Analysis of responses to angiotensin peptides in the hindquarters vascular bed of the cat.
Garrison, EA; Kadowitz, PJ; Osei, SY; Santiago, JA, 1995
)
0.29
" Meclofenamate and N omega-nitro-L-arginine methyl ester shifted the dose-response curve for ANG IV to the left in a manner similar to that observed with ANG II and ANG III."( Analysis of responses to ANG IV: effects of PD-123319 and DuP-753 in the pulmonary circulation of the rat.
Feng, CJ; Kadowitz, PJ; Kaye, AD; Nossaman, BD, 1995
)
0.29
" A positive dose-response was seen for both active drugs with meclofenamate 100 mg and ibuprofen 400 mg exhibiting the greatest efficacy for pain relief, pain reduction, time to remedication, and overall evaluation."( Single dose and multidose analgesic study of ibuprofen and meclofenamate sodium after third molar surgery.
Bergman, S; Betts, N; Cooper, S; Gaston, G; Henry, E; Hersh, EV; Lamp, C; MacAfee, K; Quinn, P; Wedell, D, 1993
)
0.29
") did not alter the dose-response curves."( Role of angiotensin II and prostaglandins in the regulation of uteroplacental blood flow.
Woods, LL, 1993
)
0.29
" Thirteen of the NSAIDs and the enantiomers of flurbiprofen were then tested in acute dosing studies in amyloid beta protein precursor (APP) transgenic mice, and plasma and brain levels of Abeta and the drug were evaluated."( NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo.
Das, P; Eriksen, JL; Golde, TE; Jessing, KW; Koo, EH; McLendon, DC; Ozols, VV; Sagi, SA; Smith, TE; Weggen, S; Zavitz, KH, 2003
)
0.32
" These studies propose for the first time a molecular basis for the observed often-unexpected, concentration-dependant changes in HPMC solution properties when co-formulated with different NSAIDs, and underline the importance of characterising such fundamental interactions that have the potential to influence drug release in solid HPMC-based dosage forms."( Solution interactions of diclofenac sodium and meclofenamic acid sodium with hydroxypropyl methylcellulose (HPMC).
Griffiths, PC; Melia, CD; Pygall, SR; Timmins, P; Wolf, B, 2011
)
0.63
" Cumulative radiation dosage of 8 Gy completely inhibited colony formation."( A dual-inhibition study on vascular smooth muscle cells with meclofenamic acid and β-irradiation for the prevention of restenosis.
Bantleon, R; Bayer, M; Claussen, CD; Dittmann, H; Kehlbach, R; Landers, A; Pritzkow, M; Sauter, A; Schmehl, J; Wiesinger, B, 2011
)
0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (8)

RoleDescription
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.
antirheumatic drugA drug used to treat rheumatoid arthritis.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
anticonvulsantA drug used to prevent seizures or reduce their severity.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitorA lipoxygenase inhibitor that interferes with the action of arachidonate 5-lipoxygenase (EC 1.13.11.34).
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitorA compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.
[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 (3)

ClassDescription
aminobenzoic acid
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)27.24000.11007.190310.0000AID1449628
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki0.31750.01501.24876.9200AID407366; AID407369
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)0.06750.00032.177410.0000AID162143; AID1798273
Fatty acid-binding protein, intestinalHomo sapiens (human)Ki8.90000.30005.48149.4000AID407368
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)24.00000.00462.018210.0000AID6867; AID7075
Aldo-keto reductase family 1 member C4Homo sapiens (human)IC50 (µMol)100.00002.30004.86338.2500AID703399; AID729956
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.21150.00021.557410.0000AID625243; AID729957
Mitogen-activated protein kinase 1Homo sapiens (human)IC50 (µMol)3.14400.00031.68789.2000AID625181
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.16180.00010.995010.0000AID162641; AID1798273; AID625244; AID729955
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)0.10000.00291.786810.0000AID161006; AID161023
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC50 (µMol)0.53070.05002.207010.0000AID1419335; AID703400; AID729959
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC50 (µMol)8.74000.37004.09519.2800AID703401; AID729958
Aldo-keto reductase family 1 member C1Homo sapiens (human)IC50 (µMol)2.35330.00603.12657.9000AID1419334; AID703402; AID729960
Prostaglandin G/H synthase 2Mus musculus (house mouse)IC50 (µMol)0.16400.00050.40086.2000AID160568; AID1798273; AID54719
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.10000.00291.823210.0000AID161006; AID161023
[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)
TransthyretinHomo sapiens (human)Kd0.48000.00301.348210.0000AID1239060
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (180)

Processvia Protein(s)Taxonomy
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)
signal transductionTransthyretinHomo sapiens (human)
purine nucleobase metabolic processTransthyretinHomo sapiens (human)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
fatty acid metabolic processFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein, intestinalHomo sapiens (human)
intestinal lipid absorptionFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid transportFatty acid-binding protein, intestinalHomo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid biosynthetic processAldo-keto reductase family 1 member C4Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
androgen metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid and bile salt transportAldo-keto reductase family 1 member C4Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C4Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C4Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C4Homo 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)
positive regulation of macrophage chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of macrophage proliferationMitogen-activated protein kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 1Homo sapiens (human)
protein phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 1Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
DNA damage responseMitogen-activated protein kinase 1Homo sapiens (human)
signal transductionMitogen-activated protein kinase 1Homo sapiens (human)
chemical synaptic transmissionMitogen-activated protein kinase 1Homo sapiens (human)
learning or memoryMitogen-activated protein kinase 1Homo sapiens (human)
insulin receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
Schwann cell developmentMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
cytosine metabolic processMitogen-activated protein kinase 1Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 1Homo sapiens (human)
androgen receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cellular pHMitogen-activated protein kinase 1Homo sapiens (human)
thyroid gland developmentMitogen-activated protein kinase 1Homo sapiens (human)
regulation of protein stabilityMitogen-activated protein kinase 1Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseMitogen-activated protein kinase 1Homo sapiens (human)
regulation of stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
mammary gland epithelial cell proliferationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to amino acid starvationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to reactive oxygen speciesMitogen-activated protein kinase 1Homo sapiens (human)
response to nicotineMitogen-activated protein kinase 1Homo sapiens (human)
ERBB signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
outer ear morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
myelinationMitogen-activated protein kinase 1Homo sapiens (human)
response to exogenous dsRNAMitogen-activated protein kinase 1Homo sapiens (human)
steroid hormone mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
negative regulation of cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
thymus developmentMitogen-activated protein kinase 1Homo sapiens (human)
progesterone receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
T cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
B cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cytoskeleton organizationMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomerase activityMitogen-activated protein kinase 1Homo sapiens (human)
Bergmann glial cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
long-term synaptic potentiationMitogen-activated protein kinase 1Homo sapiens (human)
face developmentMitogen-activated protein kinase 1Homo sapiens (human)
lung morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
trachea formationMitogen-activated protein kinase 1Homo sapiens (human)
labyrinthine layer blood vessel developmentMitogen-activated protein kinase 1Homo sapiens (human)
cardiac neural crest cell development involved in heart developmentMitogen-activated protein kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeMitogen-activated protein kinase 1Homo sapiens (human)
response to epidermal growth factorMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to cadmium ionMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 1Homo sapiens (human)
caveolin-mediated endocytosisMitogen-activated protein kinase 1Homo sapiens (human)
regulation of Golgi inheritanceMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere cappingMitogen-activated protein kinase 1Homo sapiens (human)
regulation of early endosome to late endosome transportMitogen-activated protein kinase 1Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 1Homo 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)
retinoid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
G protein-coupled receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
response to nutrientAldo-keto reductase family 1 member C3Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of cell population proliferationAldo-keto reductase family 1 member C3Homo sapiens (human)
male gonad developmentAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to starvationAldo-keto reductase family 1 member C3Homo sapiens (human)
farnesol catabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
cyclooxygenase pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
keratinocyte differentiationAldo-keto reductase family 1 member C3Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinal metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
macromolecule metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of retinoic acid receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
renal absorptionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to calcium ionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to corticosteroid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin D stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
negative regulation of retinoic acid biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of endothelial cell apoptotic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
G protein-coupled receptor signaling pathwayAldo-keto reductase family 1 member C2 Homo sapiens (human)
digestionAldo-keto reductase family 1 member C2 Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
positive regulation of cell population proliferationAldo-keto reductase family 1 member C2 Homo sapiens (human)
epithelial cell differentiationAldo-keto reductase family 1 member C2 Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C2 Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAldo-keto reductase family 1 member C2 Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C2 Homo sapiens (human)
cellular response to prostaglandin D stimulusAldo-keto reductase family 1 member C2 Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
xenobiotic metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
digestionAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid and bile salt transportAldo-keto reductase family 1 member C1Homo sapiens (human)
intestinal cholesterol absorptionAldo-keto reductase family 1 member C1Homo sapiens (human)
epithelial cell differentiationAldo-keto reductase family 1 member C1Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
retinal metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
cholesterol homeostasisAldo-keto reductase family 1 member C1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
response to organophosphorusAldo-keto reductase family 1 member C1Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C1Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (65)

Processvia Protein(s)Taxonomy
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)
hormone activityTransthyretinHomo sapiens (human)
protein bindingTransthyretinHomo sapiens (human)
identical protein bindingTransthyretinHomo sapiens (human)
thyroid hormone bindingTransthyretinHomo sapiens (human)
RNA-dependent RNA polymerase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
long-chain fatty acid transmembrane transporter activityFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
protein bindingFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C4Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid transmembrane transporter activityAldo-keto reductase family 1 member C4Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C4Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
chlordecone reductase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C4Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C4Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C4Homo 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)
phosphotyrosine residue bindingMitogen-activated protein kinase 1Homo sapiens (human)
DNA bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
phosphatase bindingMitogen-activated protein kinase 1Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 1Homo 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)
retinal dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C3Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin D2 11-ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
geranylgeranyl reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin-F synthase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
15-hydroxyprostaglandin-D dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
Delta4-3-oxosteroid 5beta-reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C3Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C2 Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
carboxylic acid bindingAldo-keto reductase family 1 member C2 Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C2 Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C2 Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C1Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C1Homo sapiens (human)
carboxylic acid bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C1Homo sapiens (human)
3beta-hydroxy-5beta-steroid dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
steroid dehydrogenase activity, acting on the CH-OH group of donors, NAD or NADP as acceptorAldo-keto reductase family 1 member C1Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
17-alpha,20-alpha-dihydroxypregn-4-en-3-one dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androsterone dehydrogenase (B-specific) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C1Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (43)

Processvia Protein(s)Taxonomy
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)
extracellular regionTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
azurophil granule lumenTransthyretinHomo sapiens (human)
extracellular exosomeTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
microvillusFatty acid-binding protein, intestinalHomo sapiens (human)
apical cortexFatty acid-binding protein, intestinalHomo sapiens (human)
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
nucleusFatty acid-binding protein, intestinalHomo sapiens (human)
cytoplasmAldo-keto reductase family 1 member C4Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C4Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C4Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C4Homo 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 regionMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 1Homo sapiens (human)
early endosomeMitogen-activated protein kinase 1Homo sapiens (human)
late endosomeMitogen-activated protein kinase 1Homo sapiens (human)
endoplasmic reticulum lumenMitogen-activated protein kinase 1Homo sapiens (human)
Golgi apparatusMitogen-activated protein kinase 1Homo sapiens (human)
centrosomeMitogen-activated protein kinase 1Homo sapiens (human)
cytosolMitogen-activated protein kinase 1Homo sapiens (human)
cytoskeletonMitogen-activated protein kinase 1Homo sapiens (human)
plasma membraneMitogen-activated protein kinase 1Homo sapiens (human)
caveolaMitogen-activated protein kinase 1Homo sapiens (human)
focal adhesionMitogen-activated protein kinase 1Homo sapiens (human)
pseudopodiumMitogen-activated protein kinase 1Homo sapiens (human)
azurophil granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
synapseMitogen-activated protein kinase 1Homo sapiens (human)
mitotic spindleMitogen-activated protein kinase 1Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo 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)
nucleusAldo-keto reductase family 1 member C3Homo sapiens (human)
cytoplasmAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C2 Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (118)

Assay IDTitleYearJournalArticle
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).
AID1849302Displacement of carboxyfluorescein-labelled bbc3-(G)14 from SARS-CoV-2 Mac3 by fluorescence polarization analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID681775TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Meclofenamate: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, May, Volume: 55, Issue:5
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.
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]
AID346025Binding affinity to beta cyclodextrin2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Convenient QSAR model for predicting the complexation of structurally diverse compounds with beta-cyclodextrins.
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]
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).
AID1676592Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1849298Binding affinity to 15N-labelled His6-tagged SARS-CoV Mac3 (527 to 652 residue) expressed in Escherichia coli Rosetta assessed as chemical shift perturbations at binding site 1 (1556, T559, M606, T612, S636, and S637 residues) by NMR HSQC spectral analysi2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID729960Inhibition of AKR1C1 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID162143Inhibition of the ovine Prostaglandin G/H synthase 1 was determined by thin-layer chromatography assay2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
AID232234Selectivity as ratio of IC50 against COX-1 to IC50 against COX-22002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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.
AID1849310Binding affinity to bbc3-(dG)14 quadruplex DNA (unknown origin) assessed as change in DNA melting temperature at 100 uM by CD melting based analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID1239060Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
AID1849292Binding affinity to 15N-labelled His6-tagged SARS-CoV-2 Mac3 (551 to 675 residues) V635I mutant expressed in Escherichia coli Rosetta by NMR HSQC spectral analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' 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
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1849306Binding affinity to bbc3-(dG)14 quadruplex DNA (unknown origin) at 100 uM by circular dichorism analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID729959Inhibition of AKR1C3 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
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).
AID1134012Antiinflammatory activity in depilated albino guinea pig assessed as suppression of UV radiation-induced skin erythema compound administered via gavage measured 2 hrs after UV irradiation exposure1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Antiinflammatory activity of isomeric phenylnaphthaleneacetic acids.
AID161023Inhibition of prostaglandin G/H synthase by measuring the reduction of prostaglandin F2-alpha in intact basophilic rat leukemia cells1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID703401Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID190003In vivo inflammatory activity measured on Gastric ulcerogenicity, (n= 10 rats per experimental group)1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID1755691Inhibition of Salmonella typhimurium LsrK expressed in Escherichia coli MET1158 in presence of DPD by kinase-glo max luminescent assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Tackling Antimicrobial Resistance with Small Molecules Targeting LsrK: Challenges and Opportunities.
AID703399Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
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).
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]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID26962Calculated partition coefficient (clogP)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Thyroid hormone uptake by hepatocytes: structure-activity relationships of phenylanthranilic acids with inhibitory activity.
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).
AID1676589Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1239061Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
AID1656360Half life in potassium phosphate buffer by liquid chromatography-tandem mass spectrometry2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Designing around Structural Alerts in Drug Discovery.
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.
AID1676590Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID54719Inhibition of the murine Arg120Ala mutant type COX-22002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-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]
AID703400Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
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).
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).
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).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1188962Aqueous solubility of the compound in H2O after 24 hrs incubation at 30 degC by LCMS analysis2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
An uncharged oxetanyl sulfoxide as a covalent modifier for improving aqueous solubility.
AID729957Inhibition of COX1 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
AID1419334Inhibition of recombinant human AKR1C1 expressed in Escherichia coli BL21 cells in presence of 9,10-phenanthrenequinone and NADPH by fluorescence assay2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Screening, synthesis, crystal structure, and molecular basis of 6-amino-4-phenyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles as novel AKR1C3 inhibitors.
AID162641Inhibition of the human Prostaglandin G/H synthase 2 was determined by thin-layer chromatography assay2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-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).
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID161006Inhibition of Prostaglandin G/H synthase mediated PGF2-alpha formation in rat basophilic leukemia (RBL-1) cells1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities.
AID1849301Displacement of carboxyfluorescein-labelled p53-(G)14 from SARS-CoV-2 Mac3 by fluorescence polarization analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID179443In vivo inflammatory activity measured on Mycobacterium foot-pad edema (MFE) model, peroral administration1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID407366Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1676593Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID78389Compound is evaluated for the inhibition of [125I]T3 uptake by H4 rat hepatoma cells at 0.1 mM1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Thyroid hormone uptake by hepatocytes: structure-activity relationships of phenylanthranilic acids with inhibitory activity.
AID6867Inhibition 5-lipoxygenase mediated LTB4 formation in rat basophilic leukemia (RBL-1) cells1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities.
AID1676599Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676597Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676595Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1849300Displacement of carboxyfluorescein-labelled bbc3-(dG)14 from SARS-CoV-2 Mac3 by fluorescence polarization analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
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).
AID1676588Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1849291Binding affinity to 15N-labelled His6-tagged SARS-CoV-2 Mac3 (551 to 675 residues) expressed in Escherichia coli Rosetta assessed as chemical shift perturbations at binding site I (M630, Y634, V635, T636, and S660 residues) at ligand to protein molar rati2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID407368Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1849309Binding affinity to p53-(dG)14 quadruplex DNA (unknown origin) assessed as change in DNA melting temperature at 100 uM by CD melting based analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID1849295Binding affinity to 15N-labelled MTSL-tagged SARS-CoV-2 Mac3 (551 to 675 residues) T583C mutant expressed in Escherichia coli Rosetta by transferred PRE analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID160568Inhibition of the murine wild type Prostaglandin G/H synthase 22002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID420788Ratio of IC50 for COX1 to IC50 for COX22009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1419335Inhibition of recombinant human AKR1C3 expressed in Escherichia coli BL21 cells in presence of 9,10-phenanthrenequinone and NADPH by fluorescence assay2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Screening, synthesis, crystal structure, and molecular basis of 6-amino-4-phenyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles as novel AKR1C3 inhibitors.
AID1676600Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1486519Binding affinity to transthyretin in human blood plasma assessed as plasma binding selectivity by measuring stoichiometry of small molecule bound to TTR incubated for 24 hrs at 37 degC by RP-HPLC2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID179441In vivo inflammatory activity measured on Carrageenan foot-pad edema (CFE) in rats, peroral administration1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID329525Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction at 50 uM after 2 hrs by fluorescence polarization assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41
A surface on the androgen receptor that allosterically regulates coactivator binding.
AID1676598Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID729955Inhibition of COX2 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
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).
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).
AID1486518Inhibition of acid-induced wild type transthyretin (unknown origin) aggregation expressed in Escherichia coli pre-incubated for 30 mins before acid addition and further incubated for 72 hrs at 37 degC under dark conditions by UV-Vis spectrophotometry2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID1676591Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID729958Inhibition of AKR1C2 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
AID7075Inhibition of 5-lipoxygenase measured by the reduction of leukotriene B4 (LTB4) in intact basophilic rat leukemia cells1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID1849299Displacement of carboxyfluorescein-labelled p53-(dG)14 from SARS-CoV-2 Mac3 by fluorescence polarization analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
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).
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]
AID1676601Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID407369Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID329528Activity at androgen receptor assessed as inhibition of dihydrotestosterone response by GAL4-MMTV luciferase reporter gene assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41
A surface on the androgen receptor that allosterically regulates coactivator binding.
AID1849289Binding affinity to 15N-labelled His6-tagged SARS-CoV-2 Mac3 (551 to 675 residues) expressed in Escherichia coli Rosetta assessed as chemical shift perturbations by NMR HSQC spectral analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID1676602Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1676594Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1849305Binding affinity to p53-(dG)14 quadruplex DNA (unknown origin) at 100 uM by circular dichorism analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID729956Inhibition of AKR1C4 (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID1849296Binding affinity to 15N-labelled His6-tagged SARS-CoV Mac3 (527 to 652 residue) expressed in Escherichia coli Rosetta assessed as chemical shift perturbations by NMR HSQC spectral analysis2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1676596Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID703402Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
AID1345284Human COX-1 (Cyclooxygenase)2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
AID1345206Human COX-2 (Cyclooxygenase)2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
AID1802654Fluorescence Polarization Assay from Article 10.1016/j.chembiol.2017.01.003: \\Small-Molecule Inhibitors of the SOX18 Transcription Factor.\\2017Cell chemical biology, Mar-16, Volume: 24, Issue:3
Small-Molecule Inhibitors of the SOX18 Transcription Factor.
AID1798273Time-Dependent Inhibition Assay from Article 10.1073/pnas.97.2.925: \\Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.\\2000Proceedings of the National Academy of Sciences of the United States of America, Jan-18, Volume: 97, Issue:2
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (969)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990555 (57.28)18.7374
1990's250 (25.80)18.2507
2000's85 (8.77)29.6817
2010's56 (5.78)24.3611
2020's23 (2.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 103.42

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 Index103.42 (24.57)
Research Supply Index6.96 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index189.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (103.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials55 (5.49%)5.53%
Reviews16 (1.60%)6.00%
Case Studies15 (1.50%)4.05%
Observational0 (0.00%)0.25%
Other915 (91.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pilot Open-label Trial of Pentosan Polysulfate Sodium and Meclofenamic Acid As Adjunctive Treatments in Patients With Psychotic Disorders [NCT02930005]Phase 28 participants (Actual)Interventional2015-08-07Completed
Pilot Study of Meclofenamate in Subjects With Recurrent or Progressive Brain Metastasis From Solid Tumor Primary [NCT02429570]30 participants (Actual)Interventional2015-04-22Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02930005 (2) [back to overview]Change in Cognitive Function as Assessed by the NIH Toolbox Cognitive Test Battery (NCTB) Composite Score
NCT02930005 (2) [back to overview]Change in Severity of Psychotic Symptoms as Assessed by Positive and Negative Syndrome Scale (PANSS)

Change in Cognitive Function as Assessed by the NIH Toolbox Cognitive Test Battery (NCTB) Composite Score

"A higher composite score on the NCTB indicates better cognitive performance. The NCTB consists of 7 tests and 8 sub-scores, and the NIH Toolbox software calculates total composite score by averaging the normalized scores of each subscale and then deriving scale scores. The NIH Toolbox Scoring and Interpretation Guide (found online) doesn't indicate a total composite score range (because the score ranges are infinite), but describes scoring as follows: To get a normalized composite score, the score of the test taker is compared to the scores in the NIH Toolbox nationally representative normative sample. The mean score is 100 and the standard deviation (SD) is 15. A score at or near 100 indicates average ability compared with others. Scores around 115 suggest above-average ability. Scores around 130 suggest superior ability (in the top 2 percent nationally). A score around 85 suggests below-average ability. A score in the range of 70 or below suggests significant impairment." (NCT02930005)
Timeframe: baseline, 8 weeks

Interventionscore (Number)
Meclofenamic Acid31.96
Pentosan Polysulfate Sodium0.96

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Change in Severity of Psychotic Symptoms as Assessed by Positive and Negative Syndrome Scale (PANSS)

Change in the Positive and Negative Syndrome Scale (PANSS) total score after 8 weeks. The range of scores on the PANSS is 30 to 210, with higher scores associated with better outcomes. (NCT02930005)
Timeframe: baseline, 8 weeks

Interventionscore (Number)
Meclofenamic Acid-11
Pentosan Polysulfate Sodium-22

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