sulfasalazine profile

Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

sulfasalazine is involved in 2 pathway(s), involving a total of 1 unique proteins and 49 unique compounds

ID Source	ID
PubMed CID	5339
CHEMBL ID	242373
CHEMBL ID	421
CHEMBL ID	100848
CHEMBL ID	1206016
CHEBI ID	9334
CHEBI ID	94500
SCHEMBL ID	18490
SCHEMBL ID	4515
SCHEMBL ID	4514
SCHEMBL ID	1079598
SCHEMBL ID	10289061
SCHEMBL ID	1229516
MeSH ID	M0019365

Synonym
BIDD:GT0161
AC-20497
HMS3393J21
AB00052101-06
BRD-K10670311-001-06-4
salazopyrin
azopyrin
azulfidine
5-[p-(2-pyridylsulfamoyl)phenylazo]salicylic acid
accucol
salazopyridin
nsc-203730
salazopiridazin
salisulf
sulcolon
colo-pleon
asulfidine
5-[[p-(2-pyridylsulfamoyl)phenyl]azo]salicylic acid
reupirin
azopyrine
s.a.s. 500
4-(pyridyl-2-amidosulfonyl)-3'-carboxy-4'-hydroxyazobenzene
w-t sasp oral
5-[p-(2-pyridylsulfamyl)phenylazo]salicylic acid
salazosulfapyridin
salicylic acid, 5-[[p-(2-pyridylsulfamoyl)phenyl]azo]-
benzosulfa
sulfasalazin
nsc203730
benzoic acid, 2-hydroxy-5-[[4-[(2-pyridinylamino)sulfonyl]phenyl]azo]-
wln: t6nj bswmr dnunr dq cvq
s.a.s.-500
DIVK1C_000860
KBIO1_000860
azulfidine en
2-hydroxy-5-[(e)-{4-[(pyridin-2-ylamino)sulfonyl]phenyl}diazenyl]benzoic acid
sulphasalazine, n-
einecs 209-974-3
sasp
ccris 4713
brn 0356241
sulfazalazine
nsc 203730
salazo-sulfapyridinum
salazosulfapiridina [inn-spanish]
azulfidine en-tabs
azosulfidin
sulfasalazina [inn-spanish]
sas-500
salicylic acid, 5-((p-(2-pyridylsulfamoyl)phenyl)azo)-
si-88
hsdb 3395
salazosulfapyridinum [inn-latin]
nsc 667219
2-hydroxy-5-[[4-[(2-pyridinylamino)sulfonyl]phenyl]azo]benzoic acid
sulfasalazinum [inn-latin]
nsc-667219
SPECTRUM_000998
PRESTWICK_848
cas-599-79-1
NCGC00016518-01
PRESTWICK2_000520
BSPBIO_002888
CMAP_000018
SMP2_000059
BSPBIO_000479
BPBIO1_000527
NCGC00090903-01
MLS001424109
sulfasalazine
salicylazosulfapyridine
C07316
salazosulfapyridine
599-79-1
2-hydroxy-5-[(e)-[4-(2-pyridylsulfamoyl)phenyl]azo]benzoic acid
sulphasalazine
benzoic acid, 2-hydroxy-5-((4-((2-pyridinylamino)sulfonyl)phenyl)azo)-
nsc667219
2-hydroxy-(5-([4-(2-pyridinylamino)sulfonyl]phenyl)azo)benzoic acid
SAS ,
MLS000759399
smr000059146
DB00795
13GS ,
5-(p-(2-pyridylsulfamyl)phenylazo)salicylic acid
2-hydroxy-5-[4-(pyridin-2-ylsulfamoyl)-phenylazo]-benzoic acid
5-(4-(2-pyridylsulfamoyl)phenylazo)-2-hydroxybenzoic acid
2-hydroxy-5-((4-((2-pyridinylamino)sulfonyl)phenyl)azo)benzoic acid
5-((p-(2-pyridylsulfamoyl)phenyl)azo)salicylic acid
azulfidine (tn)
sulfasalazine (usp/inn)
salazosulfapyridine (jp17)
D00448
PRESTWICK3_000520
5-[4-(2-pyridylsulfamoyl)phenylazo]salicylic acid
NCGC00090903-03
ssz
NCGC00090903-02
KBIO2_006614
KBIO3_002794
KBIO2_007450
KBIO2_004046
KBIOSS_001478
KBIOGR_002314
KBIO2_002314
KBIOGR_000753
KBIO2_001478
KBIOSS_002316
KBIO2_004882
KBIO3_002108
SPBIO_001032
SPECTRUM3_001364
NINDS_000860
SPECTRUM2_001216
SPBIO_002400
SPECTRUM4_000347
PRESTWICK1_000520
PRESTWICK0_000520
SPECTRUM1500552
SPECTRUM5_001443
IDI1_000860
NCGC00090903-04
NCGC00090903-05
HMS2051J21
HMS2092K07
HMS2090P13
S0580
CHEMBL242373
sulfasalazina
sulfasalazinum
CHEBI:9334 ,
salazosulfapiridina
2-hydroxy-5-{[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl}benzoic acid
(3z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid
salazosulfapyridinum
CHEMBL421
sulfasalazopyridine
HMS502K22
bdbm50097125
4-(pyridyl-2-amidosulfonyl)-3''-carboxy-4''-hydroxyazobenzene
HMS1921C05
HMS1569H21
AKOS002311709
A832559
5-(p-(2-pyridylsulfamoyl)phenylazo)salicylic acid
NCGC00186644-01
NCGC00090903-07
NCGC00090903-06
HMS2096H21
tox21_201239
NCGC00254313-01
tox21_300541
NCGC00258791-01
CHEMBL100848
nsc-757330
nsc757330
pharmakon1600-01500552
tox21_111037
dtxsid0021256 ,
dtxcid401256
HMS2232H07
CCG-39145
CCG-100987
unii-3xc8guz6cb
sulfasalazine [usan:usp:inn:ban]
3xc8guz6cb ,
5-22-08-00433 (beilstein handbook reference)
s.a.s.
FT-0603483
NCGC00090903-09
sulfasalazine [hsdb]
salazosulfapyridine [jan]
sulfasalazine [mi]
2-hydroxy-5-((4-((2-pyridinylamino)sulfonyl)phenyl)azo)benzoic acid [who-ip]
sulfasalazine [vandf]
sulfasalazine [usp-rs]
sulfasalazine [inn]
sulfasalazine [ep monograph]
sulfasalazine [orange book]
sulfasalazine [iarc]
sulfasalazine [usp monograph]
benzoic acid, 2-hydroxy-5-(2-(4-((2-pyridinylamino)sulfonyl)phenyl)diazenyl)-
sulfasalazinum [who-ip latin]
sulfasalazine [mart.]
sulfasalazine [usan]
sulfasalazine [who-dd]
sulfasalazine [who-ip]
EPITOPE ID:122672
S1576
2-hydroxy-5-[[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl]benzoic acid
HMS3370D16
gtpl4840
NCEXYHBECQHGNR-UHFFFAOYSA-N
AB00052101-04
DL-510
HY-14655
smr004703430
MLS006011702
NC00237
SCHEMBL18490
SCHEMBL4515
SCHEMBL4514
NCGC00090903-11
tox21_111037_1
HS-0062
SCHEMBL1079598
CHEMBL1206016
SCHEMBL10289061
SCHEMBL1229516
F2173-1125
737754-28-8
(e)-2-hydroxy-5-((4-(n-(pyridin-2-yl)sulfamoyl)phenyl)diazenyl)benzoic acid
sulphasalazine, antibiotic for culture media use only
Q-201769
5-[[4-(2-pyridylsulfamoyl)phenyl]azo]salicylic acid
NCEXYHBECQHGNR-QZQOTICOSA-N
2-hydroxy-5-((4-[(2-pyridinylamino)sulfonyl]phenyl)diazenyl)benzoic acid #
2-hydroxy-5-((4-(n-pyridin-2-ylsulfamoyl)phenyl)diazenyl)benzoic acid
AKOS025116975
AB00052101_07
AB00052101_08
bdbm50103596
mfcd00057363
AKOS026749974
SR-05000001721-3
sr-05000001721
sulfasalazine, united states pharmacopeia (usp) reference standard
CHEBI:94500
HMS3655G07
6-oxo-3-(2-[4-(n-pyridin-2-ylsulfamoyl)phenyl]hydrazono)cyclohexa-1,4-dienecarboxylic acid
6-oxo-3-((4-(pyridin-2-ylsulfamoyl)phenyl) hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid
OQANPHBRHBJGNZ-UHFFFAOYSA-N
SR-05000001721-1
SR-05000001721-2
sulfasalazine, european pharmacopoeia (ep) reference standard
sulfasalazine, analytical standard, >=98% (hplc)
SBI-0051526.P003
2-hydroxy-5-(2-{4-[(pyridin-2-yl)sulfamoyl]phenyl}diazen-1-yl)benzoic acid
HMS3713H21
SW196979-4
(e)-2-hydroxy-5-((4-(n-pyridin-2-ylsulfamoyl)phenyl)diazenyl)benzoic acid
2-hydroxy-5-{(e)-[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl}benzoic acid
NCGC00090903-08
FT-0674746
Q27166356
6-oxo-3-[[4-(2-pyridinylsulfamoyl)phenyl]hydrazinylidene]-1-cyclohexa-1,4-dienecarboxylic acid
sulfasalazine (azulfidine)
2-hydroxy-5-((4-(n-(pyridin-2-yl)sulfamoyl)phenyl)diazenyl)benzoic acid
iwata
OQANPHBRHBJGNZ-BKUYFWCQSA-N
BCP13311
Q63398427
Q420035
BRD-K10670311-001-08-0
HMS3871J13
HMS3884E21
5-{4-[(2-pyridylideneamino)sulfonyl]phenyldiazenyl}salicylic acid
SY052318
AKOS037515748
H10652
2-hydroxy-5-[(e)-2-{4-[(pyridin-2-yl)sulfamoyl]phenyl}diazen-1-yl]benzoic acid
EN300-119546
Z1521554012
PD087097

Excerpt	Reference
"Sulfasalazine (SAS) is an FDA-approved drug for the treatment of Crohn's disease, rheumatoid arthritis, and inflammatory bowel disease."	( Liu, J; Lou, C; Lv, H; Shang, P; Wang, Y; Zhen, C, 2022)
"Sulfasalazine is a safe option in chronic therapy of rheumatoid arthritis and spondyloarthritis. "	( David, R; Jayachandran, M; Koshy, V; Marwaha, V; Mithun, CB; Nair, AS; Padmanabhan, DS; Palatty, PL; Santhakumari, V; Singh, SK; Singhal, A; Suman, SK; Surendran, S; Tiwari, A; Yadav, P, 2022)
"Sulfasalazine (SAS) is a repurposed antitumor drug which inhibits the proliferation and survival of cancer cells by inhibiting the xCT cellular antioxidant system. "	( Bagherpoor, AJ; Kassie, F; Luo, X; Seelig, D; Shameem, M, 2023)
"Sulfasalazine (SAS) is a drug prescribed for pregnant and breastfeeding women with chronic inflammatory bowel diseases. "	( Aquino, ABO; Bilibio, JO; Borges, LI; Erthal, RP; Fernandes, GSA; Forcato, S; Gerardin, DCC; Guarnier, FA; Lens, HHM; Thomé, MLFL, 2023)
"Sulfasalazine is a recognized therapy for inflammatory bowel disease and is of paramount importance for maintaining intestinal barrier homeostasis. "	( Cao, Y; Chang, S, 2021)
"Sulfasalazine is an anti-inflammatory agent commonly used in the treatment of autoimmune conditions such as inflammatory bowel disease and rheumatoid arthritis. "	( Durando, M; Kim, JS; Tiu, H, 2017)
"Sulfasalazine is a commonly used drug for the treatment of rheumatoid arthritis and inflammatory bowel disease. "	( Abdoli, N; Asadi, B; Azarpira, N; Heidari, R; Khodaei, F; Mohammadzadeh, R; Najibi, A; Niknahad, H; Ommati, MM; Rasti, M; Saeedi, A; Shirazi Yeganeh, B; Taheri, V; Zarei, M, 2017)
"Sulfasalazine is an inhibitor of xCT that is known to increase cellular oxidative stress, giving it anti-tumor potential."	( Kanai, E; Maruo, T; Nagane, M; Shibata, Y; Shimizu, T; Yamashita, T; Yoshioka, C, 2018)
"Sulfasalazine (SSZ) is a well-known anti-inflammatory drug and also an inhibitor of the cystine-glutamate antiporter that is known to reduce intracellular glutathione (GSH) level and increase cellular oxidative stress, indicating its anti-tumor potential. "	( Fujiwara, K; Imaue, S; Jawaid, P; Kondo, T; Mitsuhashi, Y; Moniruzzaman, R; Noguchi, K; Noguchi, M; Ogawa, R; Rehman, MU; Saitoh, JI; Tomihara, K; Zhao, QL, 2018)
"Sulfasalazine is an anti-inflammatory and antioxidant medication used to treat autoimmune disease."	( Brownfoot, FC; Cannon, P; Hannan, NJ; Hastie, R; Kaitu'u-Lino, TJ; Nguyen, V; Parry, LJ; Senadheera, S; Tong, S; Tuohey, L, 2019)
"Sulfasalazine (SAS) is an US Food and Drug Administration (FDA)-approved drug for the treatment of Crohn disease that has been shown to inhibit the cystine/glutamate antiporter system xc- (SXC) and decrease tumor-associated seizures."	( Alcoreza, O; Bouslog, A; Campbell, SL; Savoia, A; Sontheimer, H; Tewari, BP, 2019)
"Sulfasalazine is a highly effective treatment for patients with antihistamine resistant CIU. "	( Orden, RA; Saini, SS; Timble, H, 2014)
"Sulfasalazine (SSZ) is an anti-inflammatory drug that has been used to treat inflammatory bowel disease and rheumatoid arthritis for decades. "	( Han, HY; Jeong, SH; Kim, H; Lim, DS; Ryu, MH, 2014)
"Sulfasalazine is a disease-modifying antirheumatic drug used in the treatment of AS."	( Chen, J; Lin, S; Liu, C, 2014)
"Sulfasalazine (SAS) is a classic inhibitor of NF-κB."	( Kang, J; Li, X; Li, Y; Liu, F; Su, J; Sun, L; Xia, M; Xu, Y, 2015)
"Sulfasalazine (SSZ) is an anti-inflammatory drug that has been demonstrated to induce apoptosis and tumor regression through inhibition of plasma membrane cystine transporter xc(-). "	( Chen, G; Hu, Y; Huang, P; Lu, WH; Ma, MZ; Song, M; Wang, P; Wen, S; Xu, RH; Yang, J; Zhu, CF, 2015)
"Sulfasalazine (SSZ) is a system XC- inhibitor; SSZ was applied intra-articularly to study the function of system XC- in the development of OA in rats subjected to anterior cruciate ligament transection and medial meniscectomy (ACLT + MMx)."	( Liu, CC; Tsai, RY; Tsai, WY; Wong, CS; Wu, JL, 2016)
"Sulfasalazine is an anti-inflammatory and immune-modulating drug that is used in rheumatology and inflammatory bowel disease."	( Chang, KY; Cho, SC; Ha, YW; Kim, S; Lee, DW; Lee, YI; Na, JE; Park, HC; Park, SC; Rhyu, IJ, 2015)
"Sulfasalazine (SSA) is a common medication used for treatment of patients with AS."	( Huang, HB; Huang, HL; Huang, KY; Lai, NS; Liu, SQ; Lu, MC; Yu, HC, 2015)
"Sulfasalazine (SSZ) is an inhibitor of xCT and was shown to suppress the survival of CD44v-positive stem-like cancer cells both in vitro and in vivo."	( Doi, T; Einaga, Y; Fukutani, M; Hasegawa, H; Hironaka, S; Imamura, CK; Ishii, Y; Kuwata, T; Nagano, O; Nakajima, TE; Nomura, S; Ohtsu, A; Ozeki, T; Sato, A; Saya, H; Shitara, K; Takahashi, S; Tsuchihashi, K, 2017)
"Sulfasalazine (SASP) is a drug commonly used in the treatment of inflammatory bowel diseases (IBD). "	( Albina, ML; Alonso, V; Bellés, M; Domingo, JL; Linares, V; Sánchez, DJ; Sirvent, JJ, 2009)
"Sulfasalazine (SAZ) is a widely used drug in inflammatory bowel disease patients but its mechanism of action is incompletely understood. "	( González, R; López-Posadas, R; Martínez-Augustin, O; Sánchez de Medina, F; Suárez, MD; Zarzuelo, A, 2009)
"Sulfasalazine is a combination of sulfapyridine and 5-aminosalicylic acid and is used as a first-line treatment in inflammatory bowel disease."	( Alivanis, P; Aperis, G; Arvanitis, A; Karvouniaris, N; Lambrianou, F; Paliouras, C; Zervos, A, 2010)
"Sulfasalazine is a prodrug composed by a molecule of 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), linked by an azo bond, which has been shown to be effective in the therapy of inflammatory bowel diseases (IBD) such as ulcerative colitis and Crohn's disease, as well as of rheumatic diseases, such as rheumatoid arthritis and ankylosing spondylitis. "	( Couto, D; Fernandes, E; Freitas, M; Gomes, A; Lima, JL; Ribeiro, D, 2010)
"Sulfasalazine (SASP) is a drug commonly used in the treatment of inflammatory bowel diseases (IBD) such as ulcerative colitis and Crohn's disease (CD) and rheumatoid arthritis (RA). "	( Alonso, V; Domingo, JL; Linares, V, 2011)
"Sulfasalazine (SLZ) is a synthetic nonsteroidal anti-inflammatory drug used mainly for the treatment of an inflammatory bowel and other diseases. "	( Castro, GR; Costas, L; López, AG; Mechetti, M; Pera, LM, 2012)
"Sulfasalazine (SSZ) is a drug used in inflammatory bowel disease, whose precise mechanism of action remains to be clarified. "	( Assi, K; Gómez-Muñoz, A; Huang, S; O'Brien, L; Salh, B; Steinbrecher, U, 2002)
"Sulfasalazine (SASP) is a novel, potent inhibitor of cellular cystine uptake mediated by the x(c)- cystine/glutamate antiporter. "	( Gout, PW; Robertson, MC; Simms, CR, 2003)
"Sulfasalazine is a successful therapeutic option for cutaneous LP, constituting an alternative to corticosteroids and retinoids."	( Bauzá, A; España, A; Gil, P; Lloret, P; Vázquez Doval, FJ, 2005)
"Sulfasalazine (SFZ) is a synthetic anti-inflammatory comprising an aminosalicylate, 5-amino salicylic acid (5-ASA), linked to an antibiotic, sulfapyridine (SPY)."	( Ganesan, A; Habens, F; Mann, DA; Oakley, F; Packham, G; Srinivasan, N, 2005)
"Sulfasalazine is a potent inhibitor of GCDCA induced hepatocyte apoptosis in vitro and in the intact liver."	( Bauchmuller, K; Bernt, C; Beuers, U; Fickert, P; Fuchsbichler, A; Rust, C; Vennegeerts, T, 2006)
"Sulfasalazine is an antibiotic used in the treatment of inflammatory bowel diseases. "	( Gallego-Iglesias, E; Maquieira, A; Pastor-Navarro, N; Puchades, R, 2007)
"Sulfasalazine is a well established disease-modifying anti-rheumatic drug commonly used in the treatment of rheumatic disorders and inflammatory bowel disease. "	( Biasi, D; Cantarini, L; Fioravanti, A; Galeazzi, M; Tinazzi, I, 2007)
"Sulfasalazine is a potent antiinflammatory drug used in the treatment of ulcerative colitis. "	( Lobos, E; Stenson, WF, 1983)
"Sulfasalazine is an effective treatment for rheumatoid arthritis (RA), producing improvements in disease parameters similar to those seen with penicillamine, hydroxychloroquine or oral or parenteral gold in comparative clinical trials."	( Faulds, D; Noble, S; Rains, CP, 1995)
"Sulfasalazine is an efficient treatment for rheumatoid arthritis (RA), but its mode of action is not known. "	( Anaya, JM; Bologna, C; Jorgensen, C; Reme, T; Sany, J, 1993)
"Sulfasalazine is an effective treatment in some inflammatory diseases that exhibit mast cell (MC) hyperplasia. "	( Befus, AD; Bissonnette, EY; Enciso, JA, 1996)
"Sulfasalazine is a prodrug which is enzymatically split in the bowel to form sulfapyridine (the principal active metabolite) and 5-aminosalicylic acid."	( Furst, DE; Gardner, G, 1995)
"Sulfasalazine is an effective agent for chronic discoid lupus erythematosus (CDLE) but the response to treatment is considerably variable between patients and is also unpredictable. "	( Broly, F; Delaporte, E; Lo-Guidice, JM; Marez, D; Piette, F; Sabbagh, N, 1997)
"Sulfasalazine (SSZ) is a commonly used drug in the treatment of inflammatory diseases such as rheumatoid arthritis and Crohn's disease. "	( Ganga, A; Rodenburg, RJ; van de Putte, LB; van Lent, PL; van Venrooij, WJ, 2000)
"Sulfasalazine is a widely used anti-inflammatory agent in the treatment of inflammatory bowel disease and several rheumatological disorders. "	( Fontana, RJ; Greenson, J; Haftel, HM; Quallich, LG, 2001)
"Sulfasalazine has proven to be an effective agent in the therapy of inflammatory bowel disease (IBD). "	( Charland, C; Field, CE; Thayer, WR, 1979)
"Sulfasalazine is an important therapeutic agent in the management of chronic inflammatory bowel disease (CIBD). "	( Tolia, V, 1992)
"Sulfasalazine appears to be an effective second line agent for the treatment of psoriatic arthritis."	( Harrington, TM; Newman, ED; Perruquet, JL, 1991)
"Sulfasalazine continues to be a common treatment for active Crohn's disease. "	( Hanauer, SB, 1990)
"Sulfasalazine is a safe and effective drug in the short term treatment of AS."	( Atra, E; Ferraz, MB; Goldsmith, CH; Tugwell, P, 1990)
"Sulfasalazine is a potent inhibitor of superoxide production and granule enzyme release by stimulated neutrophils, and modulation of these responses may contribute to its anti-inflammatory properties. "	( Neal, TM; Vissers, MC; Winterbourn, CC, 1987)
"Sulfasalazine is an effective drug for maintaining remission in ulcerative colitis, but its use may be precluded by side effects. "	( Greenberg, GR; Habal, FM, 1988)

Excerpt	Reference
"Sulfasalazine (SSZ), which has an arylamine sulfonamide structure, is an anti-inflammatory drug used in the treatment of many rheumatic diseases. "	( Cildag, S; Senturk, T, 2017)
"Sulfasalazine has a relatively short lag time until its onset of action and is often considered to be among the more efficacious traditional DMARDs."	( Croom, KF; Plosker, GL, 2005)
"Sulfasalazine has a fairly rapid onset of clinical effects and modulates immune function."	( Brooks, P; Conaghan, PG, 1993)
"Sulfasalazine, which has an effect in the acute exacerbations of ankylosing spondylitis, is probably also effective in chronic reactive arthritis."	( Leirisalo-Repo, M, 1993)
"Sulfasalazine has a beneficial effect on articular activity by controlling gut inflammation, but it cannot prevent evolution to overt IBD."	( Cuvelier, C; De Vos, M; Elewaut, A; Mielants, H; Veys, E, 1996)
"Sulfasalazine (SASP) has evident anti-inflammatory effects and pharmacological functions on autoimmune disease."	( Bai, Y; Chen, C; Gao, Z; Jiang, X; Meng, Y; Zhang, X; Zheng, C, 2022)
"Sulfasalazine has been widely used in treatment of rheumatoid arthritis and spondyloarthritis. "	( David, R; Jayachandran, M; Koshy, V; Marwaha, V; Mithun, CB; Nair, AS; Padmanabhan, DS; Palatty, PL; Santhakumari, V; Singh, SK; Singhal, A; Suman, SK; Surendran, S; Tiwari, A; Yadav, P, 2022)
"Sulfasalazine has been identified as a candidate molecule to be investigated as an intervention to treat preterm pre-eclampsia during pregnancy. "	( Brownfoot, F; Cluver, C; Decloedt, E; Kellermann, T; Louw, V, 2023)
"Sulfasalazine has potential to treat or prevent preeclampsia and warrants investigation in clinical trials."	( Brownfoot, FC; Cannon, P; Hannan, NJ; Hastie, R; Kaitu'u-Lino, TJ; Nguyen, V; Parry, LJ; Senadheera, S; Tong, S; Tuohey, L, 2019)
"Sulfasalazine (SASP) has been shown to inhibit NF-κB and reduce lipopolysaccharide-induced cytokine concentrations in fetal membrane explants and reduce the rate of Escherichia coli-induced preterm labour in mice."	( Bennett, PR; Boyce, EJ; Lee, YS; MacIntyre, DA; Rasheed, ZB; Sykes, L; Teoh, TG; Thomson, KR, 2015)
"Sulfasalazine has long been used for the treatment of rheumatoid arthritis and is often chosen as a first-line treatment. "	( Carlucci, F; Narayan, N; Rigby, S, 2017)
"Sulfasalazine has proved effective in acute pouchitis therapy."	( Bazzoli, F; Belluzzi, A; Digby, RJ; Festi, D; Liverani, E; Poggioli, G; Rosati, G; Sartini, A; Scaioli, E; Ugolini, G, 2017)
"Sulfasalazine (SSZ), which has an arylamine sulfonamide structure, is an anti-inflammatory drug used in the treatment of many rheumatic diseases. "	( Cildag, S; Senturk, T, 2017)
"Sulfasalazine has been reported to show success in the treatment of persistent cases of alopecia areata."	( Mahd, AA; Rashidi, T, 2008)
"Oral sulfasalazine has been reported to be effective in patients with idiopathic cutaneous lichen planus (LP)."	( Ayoobi, A; Cheraghian, B; Feily, A; Mapar, MA; Omidian, M, 2010)
"Sulfasalazine has modest efficacy compared to placebo and is inferior to corticosteroids for the treatment of mild to moderately active Crohn's disease. "	( Hanauer, S; Lim, WC, 2010)
"Sulfasalazine has demonstrated modest efficacy when Crohn's disease is confined to the colon."	( Feagan, BG; Sandborn, WJ, 2003)
"Sulfasalazine (SASP) has been reported to depress the fertility in men and experimental male animals, but the fundamental mechanisms of infertility caused by SASP are still unknown. "	( Adachi, T; Fukushima, T; Hamada, Y; Horii, I; Horimoto, M; Kato, M; Komiyama, M; Mori, C, 2005)
"Sulfasalazine has a relatively short lag time until its onset of action and is often considered to be among the more efficacious traditional DMARDs."	( Croom, KF; Plosker, GL, 2005)
"Sulfasalazine has more frequent side effects than olsalazine, balsalazide, and mesalamine formulations."	( Sandborn, WJ, 2006)
"Oral sulfasalazine has been found useful in treating this condition and is often used for prolonged therapy to prevent relapses."	( Jacknowitz, AI, 1980)
"Sulfasalazine, which has been used for treatment of ulcerative colitis in man, caused a dose-dependent and reversible reduction in fertility of the male rat. "	( Pholpramool, C; Srikhao, A, 1983)
"Sulfasalazine has a fairly rapid onset of clinical effects and modulates immune function."	( Brooks, P; Conaghan, PG, 1993)
"Sulfasalazine, which has an effect in the acute exacerbations of ankylosing spondylitis, is probably also effective in chronic reactive arthritis."	( Leirisalo-Repo, M, 1993)
"Sulfasalazine has recently gained wide acceptance in the treatment of rheumatoid arthritis, and beneficial effects have also been noted in ankylosing spondylitis and reactive arthritis."	( Ellis, CN; Grober, JS; Gupta, AK; Hamilton, TA; McCune, WJ; Siegel, MT; Voorhees, JJ, 1995)
"Sulfasalazine has a beneficial effect on articular activity by controlling gut inflammation, but it cannot prevent evolution to overt IBD."	( Cuvelier, C; De Vos, M; Elewaut, A; Mielants, H; Veys, E, 1996)
"Sulfasalazine has proven to be effective in such cases, leading to improvement in clinical and laboratory indices of disease activity."	( Toussirot, E; Wendling, D, 1998)
"Sulfasalazine (SSZ) has regulatory approval for treatment of inflammatory bowel disease in children and adults, and for use as a slow acting agent in adult rheumatoid arthritis (RA). "	( Brooks, CD, 2001)
"4). Sulfasalazine has been known to suppress certain inflammatory responses of the immune system, including the production of cytokines such as tumor necrosis factor and interleukins 1 and 2; and to be a scavenger of superoxide radicals thought to provoke HIV by affecting the long terminal repeat of the virus."	( Smith, D, 1995)
"Sulfasalazine has no clinically relevant benefit in patients with ankylosing spondylitis. "	( Droste, U; Gromnica-Ihle, E; Milleck, D; Schmidt, WA; Wierth, S, 2002)
"Sulfasalazine (SSZ) has recently been shown to be effective for the management of juvenile rheumatoid arthritis (JRA). "	( Chen, CC; Chiang, BL; Lin, YT; Yang, YH, 2002)
"Sulfasalazine, therefore, has certain properties of an antifolate drug."	( Dhar, GJ; Rosenberg, IH; Selhub, J, 1978)
"Sulfasalazine has proven to be an effective agent in the therapy of inflammatory bowel disease (IBD). "	( Charland, C; Field, CE; Thayer, WR, 1979)
"Sulfasalazine has been used for many years in the management of ulcerative colitis. "	( Fitzgerald, JM; Marsh, TD, 1991)
"Sulfasalazine has been evaluated by several groups of investigators in ankylosing spondylitis and psoriatic arthritis."	( Kozin, F, 1991)
"Sulfasalazine therapy has been shown effective in rheumatoid arthritis and ankylosing spondylitis. "	( Harrington, TM; Newman, ED; Perruquet, JL, 1991)
"Sulfasalazine has been widely used in the treatment of inflammatory bowel disease. "	( Barwick, KW; DeLuca, VA; Dobuler, K; Moseley, RH, 1985)
"Sulfasalazine has been associated with bronchopulmonary complications of inflammatory bowel disease (IBD) in adults. "	( Fechner, RE; Sutphen, JL; Teague, WG, 1985)
"Sulfasalazine has been reported to induce pulmonary eosinophilia and hypersensitivity with symptoms of dyspnea and fever. "	( Pauwels, R; Valcke, Y; Van der Straeten, M, 1987)
"Sulfasalazine has been used for a decade in the United Kingdom for treating rheumatoid arthritis. "	( Dacre, JE; Scott, DL, 1988)
"Sulfasalazine (SASP) has been used for many years as a disease-modifying agent in inflammatory bowel disease and in rheumatoid arthritis. "	( Gerdin, B; Tufveson, G; Wanders, A, 1988)

Excerpt	Reference
"Sulfasalazine can cause analytical interference in some assays for urinary normetanephrine and result in spuriously elevated levels, leading to misdiagnosis of phaeochromocytoma."	( Balasubramanian, S; Debono, M; Rab, E; Zuling, ET, 2023)
"Sulfasalazine (SF) promotes remyelination and improves the outcome of multiple sclerosis (MS) patients. "	( Chen, H; Chen, X; Duan, C; Li, Y; Liu, X; Liu, Y; Yang, J; Yue, J; Zhou, X, 2018)
"Sulfasalazine is known to inhibit nuclear factor kappa-light-chain-enhancer of activated B cells (NFkB) and upregulate heme-oxygenase 1 (HO-1) thus we explored the effect of these transcription factors on sFlt-1 secretion from human cytotrophoblasts."	( Brownfoot, FC; Cannon, P; Hannan, NJ; Hastie, R; Kaitu'u-Lino, TJ; Nguyen, V; Parry, LJ; Senadheera, S; Tong, S; Tuohey, L, 2019)
"Sulfasalazine was used to inhibit the nuclear factor-kappaB (NFkappaB) pathway and SP600125, a chemical inhibitor of the c-Jun N-terminal kinase, was used as an inhibitor of the activator protein-1 (AP-1) pathway."	( Boelen, A; Kwakkel, J; Wiersinga, WM, 2006)
"Sulfasalazine may enhance the inhibitory proliferation and apoptosis effect on BxPC-3 cells induced by 5-FU, which is closely related to synergistically the cell cycle arrested in G0/G1-phase."	( Guo, KJ; Guo, RX; He, SG; Huang, Z, 2007)
"Sulfasalazine was used because of its inhibitory effect on B cells."	( Dohi, Y; Imai, F; Ishibashi, T; Ohno, S; Suzuki, T; Tanaka, M, 1994)
"Sulfasalazine appears to inhibit binding of NKCF to the target cell whereas sulfapyridine predominantly inhibits early post-binding events."	( Kane, MG; MacDermott, RP; Niederlehner, A; Shanahan, F; Stenson, WF; Targan, S, 1986)
"Sulfasalazine may cause reversible male infertility, but it is entirely safe for use during pregnancy and lactation."	( Sachar, DB, 1988)

Excerpt	Reference
"Sulfasalazine treatment significantly decreased intracellular glutathione levels and induced apoptosis when combined with cisplatin in USC cell lines."	( Nagase, S; Ohta, T; Seino, M; Sendo, K, 2022)
"Sulfasalazine-treated wild-type mice and xCT knockout mice were analyzed."	( Choi, E; Engevik, AC; Goldenring, JR; Massion, PP; Meyer, AR; Mills, JC; Willet, SG; Williams, JA; Zou, Y, 2019)
"Sulfasalazine treatment also increased inosine levels in sciatic nerves of diabetic rats."	( Berti-Mattera, LN; Kern, TS; Mitchell, R; Nemet, I; Siegel, RE, 2008)
"Sulfasalazine and FTY720 treatment did not prevent body weight loss or reduce clinical scores of diarrhea or intestinal gross pathology, when compared with vehicle treatment. "	( Benson, EL; Heuvelman, DM; Masferrer, JL; Radi, ZA, 2011)
"Sulfasalazine treatment was not found effective on enthesal abnormalities of IRD patients."	( Duyur Cakit, B; Erdem, HR; Genc, H; Kacar, M; Nacir, B; Saracoglu, M, 2007)
"Sulfasalazine treated patients also showed significant improvements in cutaneous involvement."	( Ellis, CN; Grober, JS; Gupta, AK; Hamilton, TA; McCune, WJ; Siegel, MT; Voorhees, JJ, 1995)
"Sulfasalazine treatment decreased ICAM-1 and VCAM-1 protein expression."	( Feeley, BT; Hoyt, EG; Park, AK; Robbins, RC, 1999)
"Sulfasalazine treatment showed no significant protective effect on the development of colorectal dysplasia or cancer in patients with ulcerative colitis."	( Broomé, U; Lindberg, BU; Persson, B, 2001)
"The sulfasalazine-treated guinea pigs showed a significantly better clinical outcome, as well as a significantly lower histological inflammation score compared with 19 controls."	( Hoffmann, G; Neu, I; Prosiegel, M; Ruhenstroth-Bauer, G; Vogl, S; Wildfeuer, A, 1990)
"Treatment with sulfasalazine, etanercept, adalimumab, infliximab, and methotrexate gave no long-lasting remission."	( Haq, SA; Momen Majumder, MS; Rasker, JJ, 2023)
"Treatment with sulfasalazine, low dose of natrexone or their combination resulted in significant improvement of all measured parameters compared with enteritis group."	( Abdel-Salam, LO; Kamel, MM; Khattab, A; Osman, AS; Tawfik, DI; Tolba, HM, 2016)
"Treatment with sulfasalazine, doxantrazole, quercetin, or nedocromil did not increase the histamine concentration or the mast cell number in the colon on day 26, thereby showing absence of degranulation of these cells."	( de Oliveira, DM; Di Stasi, LC; Gomes, JC; Luchini, AC; Pellizzon, CH, 2009)
"Cotreatment with sulfasalazine, which inhibited nuclear translocation of NF-kappaB p65, had a rapid and marked inhibitory effect on the rate of cytokine accumulation in the maternal compartment, with lesser but significant effects observed in the fetal compartment."	( Keelan, JA; Khan, S; Mitchell, MD; Yosaatmadja, F, 2009)
"Treatment with Sulfasalazine with and without methotrexate produced good response in 71.4 % and 12.5% respectively."	( Ganu, AS; Ganu, MA, 2011)
"Treatment with sulfasalazine correlated positively with BMD at 3 of the 5 measured bone sites."	( Hafström, I; Tengstrand, B, 2002)
"Treatment with sulfasalazine normalized these alterations."	( Brandtzaeg, P; Feltelius, N; Hällgren, R; Hvatum, M; Knutson, L, 1994)
"Treatment with sulfasalazine and prednisone resulted in a clinical remission after seven weeks."	( Hoppen, T; Keller, KM; Rister, M; Stolte, M, 1993)
"Treatment with sulfasalazine markedly decreased the number of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch."	( Buckley, MT; Carlin, G; Cronstein, BN; Gadangi, P; Levin, RI; Longaker, M; Montesinos, MC; Naime, D; Recht, PA, 1996)
"Treatment with sulfasalazine prior to LPS also decreased reperfusion injury compared to LPS and saline groups."	( Feeley, BT; Hoyt, EG; Park, AK; Robbins, RC, 1999)
"Treatment with sulfasalazine is an effective method to decrease reperfusion injury and prolong allograft survival in a rat cardiac transplantation model."	( Feeley, BT; Hoyt, EG; Park, AK; Robbins, RC, 1999)
"Drug treatment with sulfasalazine or 5-aminosalicylic acid improved enteritis score."	( Selve, N, 1992)

Pathway	Proteins	Compounds
Amino acid metabolism in triple-negative breast cancer cells	0	16
Ferroptosis	1	33

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Luciferase	Photinus pyralis (common eastern firefly)	Potency	63.8254	0.0072	15.7588	89.3584	AID1224835
acetylcholinesterase	Homo sapiens (human)	Potency	49.3080	0.0025	41.7960	15,848.9004	AID1347397; AID1347398; AID1347399
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	13.3332	0.0060	38.0041	19,952.5996	AID1159521
ATAD5 protein, partial	Homo sapiens (human)	Potency	2.2297	0.0041	10.8903	31.5287	AID624249
USP1 protein, partial	Homo sapiens (human)	Potency	50.1187	0.0316	37.5844	354.8130	AID504865
Microtubule-associated protein tau	Homo sapiens (human)	Potency	12.5893	0.1800	13.5574	39.8107	AID1460
AR protein	Homo sapiens (human)	Potency	21.9554	0.0002	21.2231	8,912.5098	AID743063
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	39.8107	0.0112	12.4002	100.0000	AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	0.2239	0.0013	7.7625	44.6684	AID2120
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	1.5849	0.0013	18.0743	39.8107	AID926; AID938
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	61.3171	0.0010	22.6508	76.6163	AID1224838; AID1224893
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	47.8991	0.0030	41.6115	22,387.1992	AID1159552; AID1159555
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	28.4204	0.0008	17.5051	59.3239	AID1159527; AID1159531
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	6.8799	0.0015	30.6073	15,848.9004	AID1224841; AID1259401
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	13.3322	0.3758	27.4851	61.6524	AID743220
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	46.3637	0.0002	29.3054	16,493.5996	AID743069; AID743080
G	Vesicular stomatitis virus	Potency	12.3018	0.0123	8.9648	39.8107	AID1645842
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	50.1187	0.0010	19.4141	70.9645	AID588537
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	68.5896	0.0016	28.0151	77.1139	AID1259385
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	41.9315	0.0391	47.5451	146.8240	AID1224845
cytochrome P450 2C9 precursor	Homo sapiens (human)	Potency	7.9433	0.0063	6.9043	39.8107	AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1	Homo sapiens (human)	Potency	14.1879	0.0018	15.6638	39.8107	AID894
histone deacetylase 9 isoform 3	Homo sapiens (human)	Potency	29.2663	0.0376	17.0823	61.1927	AID1259364; AID1259388
ubiquitin carboxyl-terminal hydrolase 2 isoform a	Homo sapiens (human)	Potency	6.3096	0.6561	9.4520	25.1189	AID927
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	40.2364	0.0006	27.2152	1,122.0200	AID651741; AID743202
lamin isoform A-delta10	Homo sapiens (human)	Potency	0.0316	0.8913	12.0676	28.1838	AID1487
Interferon beta	Homo sapiens (human)	Potency	12.3018	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	12.3018	0.0123	8.9648	39.8107	AID1645842
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	7.9433	0.0063	8.2350	39.8107	AID883
Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)	Potency	6.3096	1.5849	13.0043	25.1189	AID927
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	12.3018	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	12.3018	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Glutathione S-transferase	Homo sapiens (human)	Ki	24.0000	24.0000	24.0000	24.0000	AID977610
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	14.6000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	1.5000	0.2000	5.6774	10.0000	AID1473741
Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)	IC50 (µMol)	3.0000	0.5500	3.7083	6.1000	AID699544
Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)	Ki	3.0000	0.5300	4.1157	8.4800	AID699544
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	134.0000	0.1100	7.1903	10.0000	AID1443980; AID1473738
Carbonic anhydrase 1	Homo sapiens (human)	IC50 (µMol)	3.0400	0.0058	2.1410	7.9000	AID349140
Carbonic anhydrase 1	Homo sapiens (human)	Ki	6.8700	0.0000	1.3726	10.0000	AID349142
Carbonic anhydrase 2	Homo sapiens (human)	IC50 (µMol)	4.4900	0.0002	1.1060	8.3000	AID349141
Carbonic anhydrase 2	Homo sapiens (human)	Ki	8.7200	0.0000	0.7236	9.9200	AID349145
Interstitial collagenase	Homo sapiens (human)	IC50 (µMol)	23.5490	0.0002	0.8502	10.0000	AID625177
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0000	2.8005	10.0000	AID1210069
Androgen receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	43.9510	0.0010	1.9794	14.1600	AID625228
Androgen receptor	Rattus norvegicus (Norway rat)	Ki	29.3010	0.0003	1.2185	8.9270	AID625228
Thromboxane-A synthase	Homo sapiens (human)	IC50 (µMol)	19.6390	0.0009	1.2304	10.0000	AID625229
Mitogen-activated protein kinase 1	Homo sapiens (human)	IC50 (µMol)	6.3320	0.0003	1.6878	9.2000	AID625181
Caspase-1	Homo sapiens (human)	IC50 (µMol)	28.8120	0.0020	1.7013	8.8000	AID625174
Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)	Ki	22.0000	0.4000	0.6400	0.8800	AID1660992
Cytochrome P450 2J2	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0120	2.5312	9.4700	AID1210069
Sodium/bile acid cotransporter	Homo sapiens (human)	IC50 (µMol)	6.7333	1.0000	5.9267	9.6000	AID1600822; AID1896148; AID1896149
Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)	IC50 (µMol)	12.0000	0.1047	2.7195	7.0795	AID699543
Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)	Ki	11.0000	0.0800	2.4688	9.8000	AID699543
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	0.4600	0.0040	1.9666	10.0000	AID1873197
Cystine/glutamate transporter	Homo sapiens (human)	IC50 (µMol)	235.0400	0.1400	1.1400	5.0000	AID1534336; AID1534337; AID1534338; AID622159
Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)	IC50 (µMol)	0.5600	0.0500	2.3797	9.7000	AID699542
Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)	Ki	0.5300	0.0440	1.3630	5.0000	AID699542
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Replicase polyprotein 1ab	Betacoronavirus England 1	Kd	7.6000	7.6000	7.6000	7.6000	AID1594519
Tumor necrosis factor	Homo sapiens (human)	Kd	9.0000	0.0027	4.2926	9.7700	AID1802828
Fibroblast growth factor 1	Homo sapiens (human)	Kd	609.0000	0.0080	0.1240	0.2400	AID73456
ATP-dependent translocase ABCB1	Homo sapiens (human)	EC50 (µMol)	0.9160	0.0160	0.6786	3.1000	AID1690379
Flavin reductase (NADPH)	Homo sapiens (human)	Kd	0.4383	0.0700	0.7968	1.7100	AID1815675
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
monoatomic ion transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
organic anion transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
prostaglandin transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
heme catabolic process	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
transmembrane transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
bile acid and bile salt transport	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 1	Homo sapiens (human)
morphogenesis of an epithelium	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of cellular pH reduction	Carbonic anhydrase 2	Homo sapiens (human)
angiotensin-activated signaling pathway	Carbonic anhydrase 2	Homo sapiens (human)
regulation of monoatomic anion transport	Carbonic anhydrase 2	Homo sapiens (human)
secretion	Carbonic anhydrase 2	Homo sapiens (human)
regulation of intracellular pH	Carbonic anhydrase 2	Homo sapiens (human)
neuron cellular homeostasis	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of dipeptide transmembrane transport	Carbonic anhydrase 2	Homo sapiens (human)
regulation of chloride transport	Carbonic anhydrase 2	Homo sapiens (human)
carbon dioxide transport	Carbonic anhydrase 2	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
negative regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
positive regulation of MAP kinase activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of MAPK cascade	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-33 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory response	Tumor necrosis factor	Homo sapiens (human)
negative regulation of miRNA transcription	Tumor necrosis factor	Homo sapiens (human)
positive regulation of miRNA transcription	Tumor necrosis factor	Homo sapiens (human)
negative regulation of signaling receptor activity	Tumor necrosis factor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Tumor necrosis factor	Homo sapiens (human)
positive regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
negative regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-8 production	Tumor necrosis factor	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Tumor necrosis factor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascade	Tumor necrosis factor	Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory response	Tumor necrosis factor	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Tumor necrosis factor	Homo sapiens (human)
positive regulation of synoviocyte proliferation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of I-kappaB phosphorylation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of apoptotic signaling pathway	Tumor necrosis factor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Tumor necrosis factor	Homo sapiens (human)
response to hypoxia	Tumor necrosis factor	Homo sapiens (human)
microglial cell activation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of cytokine production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein phosphorylation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of endothelial cell proliferation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of L-glutamate import across plasma membrane	Tumor necrosis factor	Homo sapiens (human)
macrophage activation involved in immune response	Tumor necrosis factor	Homo sapiens (human)
chronic inflammatory response to antigenic stimulus	Tumor necrosis factor	Homo sapiens (human)
leukocyte migration involved in inflammatory response	Tumor necrosis factor	Homo sapiens (human)
regulation of immunoglobulin production	Tumor necrosis factor	Homo sapiens (human)
negative regulation of cytokine production involved in immune response	Tumor necrosis factor	Homo sapiens (human)
positive regulation of chronic inflammatory response to antigenic stimulus	Tumor necrosis factor	Homo sapiens (human)
positive regulation of humoral immune response mediated by circulating immunoglobulin	Tumor necrosis factor	Homo sapiens (human)
skeletal muscle contraction	Tumor necrosis factor	Homo sapiens (human)
negative regulation of systemic arterial blood pressure	Tumor necrosis factor	Homo sapiens (human)
glucose metabolic process	Tumor necrosis factor	Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process	Tumor necrosis factor	Homo sapiens (human)
inflammatory response	Tumor necrosis factor	Homo sapiens (human)
humoral immune response	Tumor necrosis factor	Homo sapiens (human)
JNK cascade	Tumor necrosis factor	Homo sapiens (human)
circadian rhythm	Tumor necrosis factor	Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptors	Tumor necrosis factor	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage	Tumor necrosis factor	Homo sapiens (human)
response to xenobiotic stimulus	Tumor necrosis factor	Homo sapiens (human)
response to virus	Tumor necrosis factor	Homo sapiens (human)
response to salt stress	Tumor necrosis factor	Homo sapiens (human)
response to fructose	Tumor necrosis factor	Homo sapiens (human)
negative regulation of heart rate	Tumor necrosis factor	Homo sapiens (human)
vascular endothelial growth factor production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
negative regulation of gene expression	Tumor necrosis factor	Homo sapiens (human)
negative regulation of lipid storage	Tumor necrosis factor	Homo sapiens (human)
response to activity	Tumor necrosis factor	Homo sapiens (human)
regulation of metabolic process	Tumor necrosis factor	Homo sapiens (human)
calcium-mediated signaling	Tumor necrosis factor	Homo sapiens (human)
extracellular matrix organization	Tumor necrosis factor	Homo sapiens (human)
osteoclast differentiation	Tumor necrosis factor	Homo sapiens (human)
sequestering of triglyceride	Tumor necrosis factor	Homo sapiens (human)
cortical actin cytoskeleton organization	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein-containing complex assembly	Tumor necrosis factor	Homo sapiens (human)
positive regulation of fever generation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of myelination	Tumor necrosis factor	Homo sapiens (human)
response to nutrient levels	Tumor necrosis factor	Homo sapiens (human)
negative regulation of interleukin-6 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of chemokine production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of fractalkine production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of type II interferon production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-1 beta production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-18 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-6 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of interleukin-8 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Tumor necrosis factor	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Tumor necrosis factor	Homo sapiens (human)
positive regulation of heterotypic cell-cell adhesion	Tumor necrosis factor	Homo sapiens (human)
toll-like receptor 3 signaling pathway	Tumor necrosis factor	Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activity	Tumor necrosis factor	Homo sapiens (human)
response to isolation stress	Tumor necrosis factor	Homo sapiens (human)
response to macrophage colony-stimulating factor	Tumor necrosis factor	Homo sapiens (human)
vasodilation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT protein	Tumor necrosis factor	Homo sapiens (human)
positive regulation of apoptotic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of programmed cell death	Tumor necrosis factor	Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction	Tumor necrosis factor	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Tumor necrosis factor	Homo sapiens (human)
negative regulation of protein-containing complex disassembly	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein-containing complex disassembly	Tumor necrosis factor	Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of MAP kinase activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of MAPK cascade	Tumor necrosis factor	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	Tumor necrosis factor	Homo sapiens (human)
positive regulation of JUN kinase activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of neuron apoptotic process	Tumor necrosis factor	Homo sapiens (human)
negative regulation of blood vessel endothelial cell migration	Tumor necrosis factor	Homo sapiens (human)
negative regulation of viral genome replication	Tumor necrosis factor	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	Tumor necrosis factor	Homo sapiens (human)
response to ethanol	Tumor necrosis factor	Homo sapiens (human)
regulation of fat cell differentiation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of fat cell differentiation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of myoblast differentiation	Tumor necrosis factor	Homo sapiens (human)
negative regulation of osteoblast differentiation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of osteoclast differentiation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein catabolic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of action potential	Tumor necrosis factor	Homo sapiens (human)
positive regulation of cell adhesion	Tumor necrosis factor	Homo sapiens (human)
positive regulation of mitotic nuclear division	Tumor necrosis factor	Homo sapiens (human)
negative regulation of DNA-templated transcription	Tumor necrosis factor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Tumor necrosis factor	Homo sapiens (human)
negative regulation of mitotic cell cycle	Tumor necrosis factor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Tumor necrosis factor	Homo sapiens (human)
positive regulation of translational initiation by iron	Tumor necrosis factor	Homo sapiens (human)
negative regulation of glucose import	Tumor necrosis factor	Homo sapiens (human)
positive regulation of JNK cascade	Tumor necrosis factor	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Tumor necrosis factor	Homo sapiens (human)
astrocyte activation	Tumor necrosis factor	Homo sapiens (human)
embryonic digestive tract development	Tumor necrosis factor	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of inflammatory response	Tumor necrosis factor	Homo sapiens (human)
negative regulation of neurogenesis	Tumor necrosis factor	Homo sapiens (human)
regulation of insulin secretion	Tumor necrosis factor	Homo sapiens (human)
positive regulation of synaptic transmission	Tumor necrosis factor	Homo sapiens (human)
regulation of synapse organization	Tumor necrosis factor	Homo sapiens (human)
defense response to Gram-positive bacterium	Tumor necrosis factor	Homo sapiens (human)
cognition	Tumor necrosis factor	Homo sapiens (human)
leukocyte tethering or rolling	Tumor necrosis factor	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	Tumor necrosis factor	Homo sapiens (human)
negative regulation of lipid catabolic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of membrane protein ectodomain proteolysis	Tumor necrosis factor	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein transport	Tumor necrosis factor	Homo sapiens (human)
response to glucocorticoid	Tumor necrosis factor	Homo sapiens (human)
positive regulation of hair follicle development	Tumor necrosis factor	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Tumor necrosis factor	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Tumor necrosis factor	Homo sapiens (human)
positive regulation of glial cell proliferation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of vitamin D biosynthetic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of calcidiol 1-monooxygenase activity	Tumor necrosis factor	Homo sapiens (human)
epithelial cell proliferation involved in salivary gland morphogenesis	Tumor necrosis factor	Homo sapiens (human)
regulation of branching involved in salivary gland morphogenesis	Tumor necrosis factor	Homo sapiens (human)
negative regulation of vascular wound healing	Tumor necrosis factor	Homo sapiens (human)
negative regulation of branching involved in lung morphogenesis	Tumor necrosis factor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Tumor necrosis factor	Homo sapiens (human)
cellular response to lipopolysaccharide	Tumor necrosis factor	Homo sapiens (human)
cellular response to amino acid stimulus	Tumor necrosis factor	Homo sapiens (human)
cellular response to retinoic acid	Tumor necrosis factor	Homo sapiens (human)
cellular response to nicotine	Tumor necrosis factor	Homo sapiens (human)
cellular response to type II interferon	Tumor necrosis factor	Homo sapiens (human)
cellular response to ionizing radiation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of mononuclear cell migration	Tumor necrosis factor	Homo sapiens (human)
positive regulation of podosome assembly	Tumor necrosis factor	Homo sapiens (human)
endothelial cell apoptotic process	Tumor necrosis factor	Homo sapiens (human)
protein localization to plasma membrane	Tumor necrosis factor	Homo sapiens (human)
negative regulation of oxidative phosphorylation	Tumor necrosis factor	Homo sapiens (human)
inflammatory response to wounding	Tumor necrosis factor	Homo sapiens (human)
extrinsic apoptotic signaling pathway	Tumor necrosis factor	Homo sapiens (human)
cellular response to toxic substance	Tumor necrosis factor	Homo sapiens (human)
liver regeneration	Tumor necrosis factor	Homo sapiens (human)
necroptotic signaling pathway	Tumor necrosis factor	Homo sapiens (human)
negative regulation of bile acid secretion	Tumor necrosis factor	Homo sapiens (human)
antiviral innate immune response	Tumor necrosis factor	Homo sapiens (human)
response to Gram-negative bacterium	Tumor necrosis factor	Homo sapiens (human)
positive regulation of neuroinflammatory response	Tumor necrosis factor	Homo sapiens (human)
negative regulation of amyloid-beta clearance	Tumor necrosis factor	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Tumor necrosis factor	Homo sapiens (human)
positive regulation of amyloid-beta formation	Tumor necrosis factor	Homo sapiens (human)
response to L-glutamate	Tumor necrosis factor	Homo sapiens (human)
positive regulation of neutrophil activation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	Tumor necrosis factor	Homo sapiens (human)
regulation of establishment of endothelial barrier	Tumor necrosis factor	Homo sapiens (human)
negative regulation of bicellular tight junction assembly	Tumor necrosis factor	Homo sapiens (human)
cellular response to amyloid-beta	Tumor necrosis factor	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cell	Tumor necrosis factor	Homo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cell	Tumor necrosis factor	Homo sapiens (human)
regulation of membrane lipid metabolic process	Tumor necrosis factor	Homo sapiens (human)
response to 3,3',5-triiodo-L-thyronine	Tumor necrosis factor	Homo sapiens (human)
response to gold nanoparticle	Tumor necrosis factor	Homo sapiens (human)
positive regulation of protein localization to cell surface	Tumor necrosis factor	Homo sapiens (human)
positive regulation of blood microparticle formation	Tumor necrosis factor	Homo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 2 production	Tumor necrosis factor	Homo sapiens (human)
positive regulation of hepatocyte proliferation	Tumor necrosis factor	Homo sapiens (human)
regulation of endothelial cell apoptotic process	Tumor necrosis factor	Homo sapiens (human)
regulation of reactive oxygen species metabolic process	Tumor necrosis factor	Homo sapiens (human)
positive regulation of DNA biosynthetic process	Tumor necrosis factor	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligand	Tumor necrosis factor	Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathway	Tumor necrosis factor	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
proteolysis	Interstitial collagenase	Homo sapiens (human)
protein metabolic process	Interstitial collagenase	Homo sapiens (human)
extracellular matrix disassembly	Interstitial collagenase	Homo sapiens (human)
collagen catabolic process	Interstitial collagenase	Homo sapiens (human)
positive regulation of protein-containing complex assembly	Interstitial collagenase	Homo sapiens (human)
cellular response to UV-A	Interstitial collagenase	Homo sapiens (human)
extracellular matrix organization	Interstitial collagenase	Homo sapiens (human)
positive regulation of cell population proliferation	Fibroblast growth factor 1	Homo sapiens (human)
fibroblast growth factor receptor signaling pathway	Fibroblast growth factor 1	Homo sapiens (human)
angiogenesis	Fibroblast growth factor 1	Homo sapiens (human)
organ induction	Fibroblast growth factor 1	Homo sapiens (human)
signal transduction	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of cell population proliferation	Fibroblast growth factor 1	Homo sapiens (human)
fibroblast growth factor receptor signaling pathway	Fibroblast growth factor 1	Homo sapiens (human)
anatomical structure morphogenesis	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of endothelial cell migration	Fibroblast growth factor 1	Homo sapiens (human)
lung development	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of cell migration	Fibroblast growth factor 1	Homo sapiens (human)
activation of protein kinase B activity	Fibroblast growth factor 1	Homo sapiens (human)
cellular response to heat	Fibroblast growth factor 1	Homo sapiens (human)
wound healing	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of MAP kinase activity	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of cholesterol biosynthetic process	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of angiogenesis	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Fibroblast growth factor 1	Homo sapiens (human)
epithelial cell proliferation	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of cell division	Fibroblast growth factor 1	Homo sapiens (human)
branch elongation involved in ureteric bud branching	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Fibroblast growth factor 1	Homo sapiens (human)
mesonephric epithelium development	Fibroblast growth factor 1	Homo sapiens (human)
regulation of endothelial tube morphogenesis	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of intracellular signal transduction	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of sprouting angiogenesis	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of hepatocyte proliferation	Fibroblast growth factor 1	Homo sapiens (human)
regulation of endothelial cell chemotaxis to fibroblast growth factor	Fibroblast growth factor 1	Homo sapiens (human)
cell differentiation	Fibroblast growth factor 1	Homo sapiens (human)
positive regulation of gene expression	Fibroblast growth factor 1	Homo sapiens (human)
animal organ morphogenesis	Fibroblast growth factor 1	Homo sapiens (human)
regulation of cell migration	Fibroblast growth factor 1	Homo sapiens (human)
G2/M transition of mitotic cell cycle	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic metabolic process	ATP-dependent translocase ABCB1	Homo sapiens (human)
response to xenobiotic stimulus	ATP-dependent translocase ABCB1	Homo sapiens (human)
phospholipid translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
terpenoid transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of response to osmotic stress	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
transepithelial transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
stem cell proliferation	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
export across plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
positive regulation of anion channel activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of chloride transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
prostaglandin biosynthetic process	Thromboxane-A synthase	Homo sapiens (human)
icosanoid metabolic process	Thromboxane-A synthase	Homo sapiens (human)
cyclooxygenase pathway	Thromboxane-A synthase	Homo sapiens (human)
intracellular chloride ion homeostasis	Thromboxane-A synthase	Homo sapiens (human)
response to ethanol	Thromboxane-A synthase	Homo sapiens (human)
positive regulation of vasoconstriction	Thromboxane-A synthase	Homo sapiens (human)
response to fatty acid	Thromboxane-A synthase	Homo sapiens (human)
positive regulation of macrophage chemotaxis	Mitogen-activated protein kinase 1	Homo sapiens (human)
positive regulation of macrophage proliferation	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Mitogen-activated protein kinase 1	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase 1	Homo sapiens (human)
apoptotic process	Mitogen-activated protein kinase 1	Homo sapiens (human)
chemotaxis	Mitogen-activated protein kinase 1	Homo sapiens (human)
DNA damage response	Mitogen-activated protein kinase 1	Homo sapiens (human)
signal transduction	Mitogen-activated protein kinase 1	Homo sapiens (human)
chemical synaptic transmission	Mitogen-activated protein kinase 1	Homo sapiens (human)
learning or memory	Mitogen-activated protein kinase 1	Homo sapiens (human)
insulin receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylation	Mitogen-activated protein kinase 1	Homo sapiens (human)
Schwann cell development	Mitogen-activated protein kinase 1	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase 1	Homo sapiens (human)
peptidyl-threonine phosphorylation	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytosine metabolic process	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of ossification	Mitogen-activated protein kinase 1	Homo sapiens (human)
androgen receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of cellular pH	Mitogen-activated protein kinase 1	Homo sapiens (human)
thyroid gland development	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of protein stability	Mitogen-activated protein kinase 1	Homo sapiens (human)
lipopolysaccharide-mediated signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
positive regulation of telomere maintenance via telomerase	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of stress-activated MAPK cascade	Mitogen-activated protein kinase 1	Homo sapiens (human)
mammary gland epithelial cell proliferation	Mitogen-activated protein kinase 1	Homo sapiens (human)
cellular response to amino acid starvation	Mitogen-activated protein kinase 1	Homo sapiens (human)
cellular response to reactive oxygen species	Mitogen-activated protein kinase 1	Homo sapiens (human)
response to nicotine	Mitogen-activated protein kinase 1	Homo sapiens (human)
ERBB signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
ERBB2-ERBB3 signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
outer ear morphogenesis	Mitogen-activated protein kinase 1	Homo sapiens (human)
myelination	Mitogen-activated protein kinase 1	Homo sapiens (human)
response to exogenous dsRNA	Mitogen-activated protein kinase 1	Homo sapiens (human)
steroid hormone mediated signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
negative regulation of cell differentiation	Mitogen-activated protein kinase 1	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
thymus development	Mitogen-activated protein kinase 1	Homo sapiens (human)
progesterone receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
T cell receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
B cell receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of cytoskeleton organization	Mitogen-activated protein kinase 1	Homo sapiens (human)
positive regulation of telomerase activity	Mitogen-activated protein kinase 1	Homo sapiens (human)
Bergmann glial cell differentiation	Mitogen-activated protein kinase 1	Homo sapiens (human)
long-term synaptic potentiation	Mitogen-activated protein kinase 1	Homo sapiens (human)
face development	Mitogen-activated protein kinase 1	Homo sapiens (human)
lung morphogenesis	Mitogen-activated protein kinase 1	Homo sapiens (human)
trachea formation	Mitogen-activated protein kinase 1	Homo sapiens (human)
labyrinthine layer blood vessel development	Mitogen-activated protein kinase 1	Homo sapiens (human)
cardiac neural crest cell development involved in heart development	Mitogen-activated protein kinase 1	Homo sapiens (human)
ERK1 and ERK2 cascade	Mitogen-activated protein kinase 1	Homo sapiens (human)
response to epidermal growth factor	Mitogen-activated protein kinase 1	Homo sapiens (human)
cellular response to cadmium ion	Mitogen-activated protein kinase 1	Homo sapiens (human)
cellular response to tumor necrosis factor	Mitogen-activated protein kinase 1	Homo sapiens (human)
caveolin-mediated endocytosis	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of Golgi inheritance	Mitogen-activated protein kinase 1	Homo sapiens (human)
positive regulation of telomere capping	Mitogen-activated protein kinase 1	Homo sapiens (human)
regulation of early endosome to late endosome transport	Mitogen-activated protein kinase 1	Homo sapiens (human)
cell surface receptor signaling pathway	Mitogen-activated protein kinase 1	Homo sapiens (human)
intracellular signal transduction	Mitogen-activated protein kinase 1	Homo sapiens (human)
cellular response to organic substance	Caspase-1	Homo sapiens (human)
pattern recognition receptor signaling pathway	Caspase-1	Homo sapiens (human)
proteolysis	Caspase-1	Homo sapiens (human)
apoptotic process	Caspase-1	Homo sapiens (human)
signal transduction	Caspase-1	Homo sapiens (human)
osmosensory signaling pathway	Caspase-1	Homo sapiens (human)
protein autoprocessing	Caspase-1	Homo sapiens (human)
positive regulation of interleukin-1 beta production	Caspase-1	Homo sapiens (human)
positive regulation of interleukin-18 production	Caspase-1	Homo sapiens (human)
defense response to bacterium	Caspase-1	Homo sapiens (human)
regulation of apoptotic process	Caspase-1	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Caspase-1	Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process	Caspase-1	Homo sapiens (human)
icosanoid biosynthetic process	Caspase-1	Homo sapiens (human)
regulation of inflammatory response	Caspase-1	Homo sapiens (human)
positive regulation of inflammatory response	Caspase-1	Homo sapiens (human)
protein maturation	Caspase-1	Homo sapiens (human)
defense response to virus	Caspase-1	Homo sapiens (human)
pyroptosis	Caspase-1	Homo sapiens (human)
cellular response to lipopolysaccharide	Caspase-1	Homo sapiens (human)
cellular response to mechanical stimulus	Caspase-1	Homo sapiens (human)
cellular response to type II interferon	Caspase-1	Homo sapiens (human)
cytokine precursor processing	Caspase-1	Homo sapiens (human)
signaling receptor ligand precursor processing	Caspase-1	Homo sapiens (human)
AIM2 inflammasome complex assembly	Caspase-1	Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathway	Caspase-1	Homo sapiens (human)
megakaryocyte differentiation	Flavin reductase (NADPH)	Homo sapiens (human)
heme catabolic process	Flavin reductase (NADPH)	Homo sapiens (human)
negative regulation of insulin receptor signaling pathway	Flavin reductase (NADPH)	Homo sapiens (human)
brainstem development	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
nucleobase-containing compound metabolic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
GMP biosynthetic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
'de novo' IMP biosynthetic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
response to inorganic substance	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
cerebellum development	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
cerebral cortex development	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
animal organ regeneration	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
'de novo' AMP biosynthetic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
dihydrofolate metabolic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
tetrahydrofolate biosynthetic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
'de novo' XMP biosynthetic process	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
cellular response to interleukin-7	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
fatty acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
icosanoid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
regulation of heart contraction	Cytochrome P450 2J2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
organic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathway	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
response to hypoxia	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
neutrophil mediated immunity	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
germinal center formation	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
positive regulation of leukocyte chemotaxis	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
proteolysis	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
membrane protein ectodomain proteolysis	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
cell adhesion	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
Notch receptor processing	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
positive regulation of cell population proliferation	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
response to xenobiotic stimulus	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)

Process	via Protein(s)	Taxonomy
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
transmembrane transporter activity	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
arylesterase activity	Carbonic anhydrase 1	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 1	Homo sapiens (human)
protein binding	Carbonic anhydrase 1	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 1	Homo sapiens (human)
hydro-lyase activity	Carbonic anhydrase 1	Homo sapiens (human)
cyanamide hydratase activity	Carbonic anhydrase 1	Homo sapiens (human)
arylesterase activity	Carbonic anhydrase 2	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
protein binding	Carbonic anhydrase 2	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 2	Homo sapiens (human)
cyanamide hydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
transcription cis-regulatory region binding	Tumor necrosis factor	Homo sapiens (human)
protease binding	Tumor necrosis factor	Homo sapiens (human)
cytokine activity	Tumor necrosis factor	Homo sapiens (human)
tumor necrosis factor receptor binding	Tumor necrosis factor	Homo sapiens (human)
protein binding	Tumor necrosis factor	Homo sapiens (human)
death receptor agonist activity	Tumor necrosis factor	Homo sapiens (human)
identical protein binding	Tumor necrosis factor	Homo sapiens (human)
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endopeptidase activity	Interstitial collagenase	Homo sapiens (human)
metalloendopeptidase activity	Interstitial collagenase	Homo sapiens (human)
serine-type endopeptidase activity	Interstitial collagenase	Homo sapiens (human)
peptidase activity	Interstitial collagenase	Homo sapiens (human)
zinc ion binding	Interstitial collagenase	Homo sapiens (human)
fibroblast growth factor receptor binding	Fibroblast growth factor 1	Homo sapiens (human)
integrin binding	Fibroblast growth factor 1	Homo sapiens (human)
protein binding	Fibroblast growth factor 1	Homo sapiens (human)
growth factor activity	Fibroblast growth factor 1	Homo sapiens (human)
heparin binding	Fibroblast growth factor 1	Homo sapiens (human)
Hsp70 protein binding	Fibroblast growth factor 1	Homo sapiens (human)
S100 protein binding	Fibroblast growth factor 1	Homo sapiens (human)
protein binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
efflux transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP hydrolysis activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ubiquitin protein ligase binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylcholine floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylethanolamine flippase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
monooxygenase activity	Thromboxane-A synthase	Homo sapiens (human)
thromboxane-A synthase activity	Thromboxane-A synthase	Homo sapiens (human)
iron ion binding	Thromboxane-A synthase	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	Thromboxane-A synthase	Homo sapiens (human)
heme binding	Thromboxane-A synthase	Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activity	Thromboxane-A synthase	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Thromboxane-A synthase	Homo sapiens (human)
phosphotyrosine residue binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
DNA binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 1	Homo sapiens (human)
MAP kinase activity	Mitogen-activated protein kinase 1	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activity	Mitogen-activated protein kinase 1	Homo sapiens (human)
phosphatase binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
identical protein binding	Mitogen-activated protein kinase 1	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 1	Homo sapiens (human)
endopeptidase activity	Caspase-1	Homo sapiens (human)
cysteine-type endopeptidase activity	Caspase-1	Homo sapiens (human)
protein binding	Caspase-1	Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic process	Caspase-1	Homo sapiens (human)
kinase binding	Caspase-1	Homo sapiens (human)
cytokine binding	Caspase-1	Homo sapiens (human)
identical protein binding	Caspase-1	Homo sapiens (human)
CARD domain binding	Caspase-1	Homo sapiens (human)
caspase binding	Caspase-1	Homo sapiens (human)
biliverdin reductase (NAD(P)H) activity	Flavin reductase (NADPH)	Homo sapiens (human)
protein binding	Flavin reductase (NADPH)	Homo sapiens (human)
FMN reductase (NAD(P)H) activity	Flavin reductase (NADPH)	Homo sapiens (human)
peptidyl-cysteine S-nitrosylase activity	Flavin reductase (NADPH)	Homo sapiens (human)
riboflavin reductase (NADPH) activity	Flavin reductase (NADPH)	Homo sapiens (human)
FMN reductase (NADPH) activity	Flavin reductase (NADPH)	Homo sapiens (human)
FMN reductase (NADH) activity	Flavin reductase (NADPH)	Homo sapiens (human)
biliberdin reductase NAD+ activity	Flavin reductase (NADPH)	Homo sapiens (human)
biliverdin reductase (NADPH) activity	Flavin reductase (NADPH)	Homo sapiens (human)
IMP cyclohydrolase activity	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
protein homodimerization activity	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
cadherin binding	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
phosphoribosylaminoimidazolecarboxamide formyltransferase activity	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
iron ion binding	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
heme binding	Cytochrome P450 2J2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2J2	Homo sapiens (human)
endopeptidase activity	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
metalloendopeptidase activity	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
Notch binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
interleukin-6 receptor binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
integrin binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
protein binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
peptidase activity	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
metallopeptidase activity	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
SH3 domain binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
cytokine binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
PDZ domain binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
tumor necrosis factor binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
metal ion binding	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic process	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
virus receptor activity	Sodium/bile acid cotransporter	Homo sapiens (human)
protein binding	Sodium/bile acid cotransporter	Homo sapiens (human)
bile acid:sodium symporter activity	Sodium/bile acid cotransporter	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
efflux transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP hydrolysis activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
identical protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein homodimerization activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein binding	Cystine/glutamate transporter	Homo sapiens (human)
cystine:glutamate antiporter activity	Cystine/glutamate transporter	Homo sapiens (human)
L-kynurenine transmembrane transporter activity	Cystine/glutamate transporter	Homo sapiens (human)
L-amino acid transmembrane transporter activity	Cystine/glutamate transporter	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
thyroid hormone transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
apical plasma membrane	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
apical plasma membrane	Solute carrier organic anion transporter family member 2B1	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
cytosol	Carbonic anhydrase 1	Homo sapiens (human)
extracellular exosome	Carbonic anhydrase 1	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
cytosol	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
myelin sheath	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
extracellular exosome	Carbonic anhydrase 2	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
extracellular space	Tumor necrosis factor	Homo sapiens (human)
phagocytic cup	Tumor necrosis factor	Homo sapiens (human)
extracellular region	Tumor necrosis factor	Homo sapiens (human)
extracellular space	Tumor necrosis factor	Homo sapiens (human)
plasma membrane	Tumor necrosis factor	Homo sapiens (human)
external side of plasma membrane	Tumor necrosis factor	Homo sapiens (human)
cell surface	Tumor necrosis factor	Homo sapiens (human)
neuronal cell body	Tumor necrosis factor	Homo sapiens (human)
membrane raft	Tumor necrosis factor	Homo sapiens (human)
recycling endosome	Tumor necrosis factor	Homo sapiens (human)
cell surface	Tumor necrosis factor	Homo sapiens (human)
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular region	Interstitial collagenase	Homo sapiens (human)
extracellular matrix	Interstitial collagenase	Homo sapiens (human)
extracellular space	Interstitial collagenase	Homo sapiens (human)
extracellular region	Fibroblast growth factor 1	Homo sapiens (human)
extracellular space	Fibroblast growth factor 1	Homo sapiens (human)
nucleoplasm	Fibroblast growth factor 1	Homo sapiens (human)
cytosol	Fibroblast growth factor 1	Homo sapiens (human)
cell cortex	Fibroblast growth factor 1	Homo sapiens (human)
extracellular matrix	Fibroblast growth factor 1	Homo sapiens (human)
cytoplasm	Fibroblast growth factor 1	Homo sapiens (human)
extracellular space	Fibroblast growth factor 1	Homo sapiens (human)
nucleus	Fibroblast growth factor 1	Homo sapiens (human)
cytoplasm	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cell surface	ATP-dependent translocase ABCB1	Homo sapiens (human)
membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
extracellular exosome	ATP-dependent translocase ABCB1	Homo sapiens (human)
external side of apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum	Thromboxane-A synthase	Homo sapiens (human)
endoplasmic reticulum membrane	Thromboxane-A synthase	Homo sapiens (human)
cytosol	Thromboxane-A synthase	Homo sapiens (human)
extracellular region	Mitogen-activated protein kinase 1	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 1	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 1	Homo sapiens (human)
mitochondrion	Mitogen-activated protein kinase 1	Homo sapiens (human)
early endosome	Mitogen-activated protein kinase 1	Homo sapiens (human)
late endosome	Mitogen-activated protein kinase 1	Homo sapiens (human)
endoplasmic reticulum lumen	Mitogen-activated protein kinase 1	Homo sapiens (human)
Golgi apparatus	Mitogen-activated protein kinase 1	Homo sapiens (human)
centrosome	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytoskeleton	Mitogen-activated protein kinase 1	Homo sapiens (human)
plasma membrane	Mitogen-activated protein kinase 1	Homo sapiens (human)
caveola	Mitogen-activated protein kinase 1	Homo sapiens (human)
focal adhesion	Mitogen-activated protein kinase 1	Homo sapiens (human)
pseudopodium	Mitogen-activated protein kinase 1	Homo sapiens (human)
azurophil granule lumen	Mitogen-activated protein kinase 1	Homo sapiens (human)
synapse	Mitogen-activated protein kinase 1	Homo sapiens (human)
mitotic spindle	Mitogen-activated protein kinase 1	Homo sapiens (human)
ficolin-1-rich granule lumen	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 1	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 1	Homo sapiens (human)
cytoplasm	Caspase-1	Homo sapiens (human)
cytosol	Caspase-1	Homo sapiens (human)
nucleolus	Caspase-1	Homo sapiens (human)
cytoplasm	Caspase-1	Homo sapiens (human)
cytosol	Caspase-1	Homo sapiens (human)
microtubule	Caspase-1	Homo sapiens (human)
plasma membrane	Caspase-1	Homo sapiens (human)
canonical inflammasome complex	Caspase-1	Homo sapiens (human)
NLRP1 inflammasome complex	Caspase-1	Homo sapiens (human)
NLRP3 inflammasome complex	Caspase-1	Homo sapiens (human)
AIM2 inflammasome complex	Caspase-1	Homo sapiens (human)
protein-containing complex	Caspase-1	Homo sapiens (human)
IPAF inflammasome complex	Caspase-1	Homo sapiens (human)
protease inhibitor complex	Caspase-1	Homo sapiens (human)
cytoplasm	Flavin reductase (NADPH)	Homo sapiens (human)
nucleoplasm	Flavin reductase (NADPH)	Homo sapiens (human)
cytosol	Flavin reductase (NADPH)	Homo sapiens (human)
plasma membrane	Flavin reductase (NADPH)	Homo sapiens (human)
intracellular membrane-bounded organelle	Flavin reductase (NADPH)	Homo sapiens (human)
extracellular exosome	Flavin reductase (NADPH)	Homo sapiens (human)
cytosol	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
plasma membrane	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
membrane	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
extracellular exosome	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
cytosol	Bifunctional purine biosynthesis protein ATIC	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2J2	Homo sapiens (human)
extracellular exosome	Cytochrome P450 2J2	Homo sapiens (human)
cytoplasm	Cytochrome P450 2J2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2J2	Homo sapiens (human)
cell-cell junction	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
focal adhesion	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
ruffle membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
Golgi membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
cytoplasm	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
endoplasmic reticulum lumen	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
cytosol	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
plasma membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
cell surface	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
actin cytoskeleton	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
apical plasma membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
membrane raft	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
plasma membrane	Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)
plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
basolateral plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
nucleoplasm	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
brush border membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
mitochondrial membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
membrane raft	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
external side of apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Cystine/glutamate transporter	Homo sapiens (human)
cell surface	Cystine/glutamate transporter	Homo sapiens (human)
membrane	Cystine/glutamate transporter	Homo sapiens (human)
brush border membrane	Cystine/glutamate transporter	Homo sapiens (human)
microvillus membrane	Cystine/glutamate transporter	Homo sapiens (human)
apical part of cell	Cystine/glutamate transporter	Homo sapiens (human)
astrocyte projection	Cystine/glutamate transporter	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (472)

Assay ID	Title	Year	Journal	Article
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID977610	Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB	1999	Journal of molecular biology, Aug-27, Volume: 291, Issue:4	The ligandin (non-substrate) binding site of human Pi class glutathione transferase is located in the electrophile binding site (H-site).
AID1811	Experimentally measured binding affinity data derived from PDB	1999	Journal of molecular biology, Aug-27, Volume: 291, Issue:4	The ligandin (non-substrate) binding site of human Pi class glutathione transferase is located in the electrophile binding site (H-site).
AID1347161	Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347149	Furin counterscreen qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347169	Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347157	Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588519	A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities	2011	Antiviral research, Sep, Volume: 91, Issue:3	High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299	A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis	2010	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21	Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID686947	qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen	2013	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15	Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID622159	Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Inhibition of xc⁻ transporter-mediated cystine uptake by sulfasalazine analogs.
AID231333	Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer)	2001	Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12	Experimental and computational screening models for the prediction of intestinal drug absorption.
AID444055	Fraction absorbed in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1211093	Tmax in wild-type Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID386623	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy	2008	Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19	Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1211023	Clearance in BCRP knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1129361	Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis	2014	Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7	A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID156203	Binding to POPC/GMI liposomes using biosensor system	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID436239	Antiinflammatory activity against trinitrobenzenesulfonic acid-induced colitis in Wistar rat assessed as decrease in colonic myeloperoxidase activity at 100 mg/kg, po measured 24 hrs after last dose on day 11 by spectrometry	2009	European journal of medicinal chemistry, Oct, Volume: 44, Issue:10	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1757483	Anti-colitis activity against DSS-induced BALB/c mouse model of subchronic relapsing colitis assessed as effect on colon length at 100 mg/kg/day, po administered for 7 days in second week during 2 weeks DSS challenge and measured at the end of 2nd week	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	6-(methylsulfinyl)hexyl isothiocyanate (6-MITC) from Wasabia japonica alleviates inflammatory bowel disease (IBD) by potential inhibition of glycogen synthase kinase 3 beta (GSK-3β).
AID1211167	Tmax in BCRP knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211146	Volume of distribution at steady state in MRP2-deficient Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211148	Half life in MRP2-deficient Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current 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.
AID1211158	AUC (infinity) in MDR1A knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1413411	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in ICAM1 expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by Western blot analysi	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1245316	Anti-ulcerative colitis activity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as improvement in number of visible colitis lesions at 300 mg/kg, po qd measured on day 8	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID1272121	Antiulcerative colitis activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in severity of inflammation at 300 mg/kg qd for 6 consecutive days measured on 7th day	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Synthesis, colon-targeted studies and pharmacological evaluation of an anti-ulcerative colitis drug 4-Aminosalicylic acid-β-O-glucoside.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1757471	Anti-colitis activity against DSS-induced BALB/c mouse model of subchronic relapsing colitis assessed as increase in body weight at 100 mg/kg/day, po administered for 7 days in second week during 2 weeks DSS challenge and measured at the end of 2nd week	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	6-(methylsulfinyl)hexyl isothiocyanate (6-MITC) from Wasabia japonica alleviates inflammatory bowel disease (IBD) by potential inhibition of glycogen synthase kinase 3 beta (GSK-3β).
AID509500	Antibacterial activity agaisnt Staphylococcus aureus MTCC 3160 by agar diffusion method	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID1209582	Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1824207	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as fold decrease in disease activity index at 50 mg/kg, po administered via gavage twice daily for 10 days relative to control	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID236916	Percentage of mass balance in hexadecane membranes model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID1245298	Toxicity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as change in body weight at 300 mg/kg, po qd (Rvb = -15.3%)	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID1221977	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID699543	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1824877	Anti-colitis activity against DSS-induced BALB/c mouse model assessed as increase in body weight at 100 mg/kg, po administered for 5 to 14 days	2022	Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1	Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID296197	Antiinflammatory activity against dextran sodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as rectal prolaps	2007	European journal of medicinal chemistry, Aug, Volume: 42, Issue:8	Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
AID604025	Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID156089	Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1221980	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID453204	Permeability in human skin after 48 hrs by Franz cell permeability assay	2010	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1	Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1594519	Binding affinity to MERS-CoV papain-like protease by SPR analysis	2019	Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10	Identification and design of novel small molecule inhibitors against MERS-CoV papain-like protease via high-throughput screening and molecular modeling.
AID1824213	Anti-colitis activity against DSS-induced C57BL/6 mouse model of colitis assessed as fold change in disease activity index at 25 to 100 mg/kg, po administered via gavage twice a day for 10 days relative to SASP	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID194538	Tested for peak serum concentration in rat 6	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211024	Clearance in MRP2 knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID699544	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current 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.
AID1815672	Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as change in enthalpy by isothermal titration calorimetry	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target.
AID73470	Binding affinity for Fibroblast growth factor 2 (No data)	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Validation of molecular docking calculations involving FGF-1 and FGF-2.
AID1221969	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1413403	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as myeloperoxidase level at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by ELISA (Rvb = 456.67 +/- 41.	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID696364	Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay	2012	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21	Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-κB activation and PPAR transcriptional activity.
AID1221958	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1404016	Permeability of the compound by PAMPA	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID1676588	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1896148	Inhibition of preS1-peptide binding to human HA-tagged NTCP in U2OS expresseing NTCP in incubated for 24 hrs using Myrcludex B as substrate by competitive binding assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1272123	Antiulcerative colitis activity in TNBS-induced Sprague-Dawley rat colitis model assessed as myeloperoxidase activity at 300 mg/kg, qd for 6 consecutive days by spectrophotometry (Rvb = 1.44 +/- 0.041 U/g)	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Synthesis, colon-targeted studies and pharmacological evaluation of an anti-ulcerative colitis drug 4-Aminosalicylic acid-β-O-glucoside.
AID170015	Effect of compound on myeloperoxidase activity was evaluated in rat	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID1211151	Volume of distribution at steady state in BCRP knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1690379	Activation of ABCB1 ATPase activity (unknown origin) expressed in baculovirus infected Sf9 insect cells using ATP as substrate measured after 1 hr by colorimetric assay	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).
AID1392402	Inhibition of DSS-induced acute ulcerative colitis C57BL/6J mouse model at 500 mg/kg, po qd administered for 7 days relative to control	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9	Syntheses and structure-activity relationships on antibacterial and anti-ulcerative colitis properties of quaternary 13-substituted palmatines and 8-oxo-13-substituted dihydropalmatines.
AID614828	Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:5 by DSC technique	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
AID678721	Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current 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.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current 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.
AID444054	Oral bioavailability in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current 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.
AID604021	Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1074029	Apparent permeability in pig LLC-PK1 cells by LC-MS/MS analysis	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
AID509501	Antibacterial activity agaisnt Bacillus subtilis MTCC 1456 by agar diffusion method	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678714	Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID152782	Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells	2001	Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4	Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID1211165	Tmax in wild-type Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID509504	Antiulcerogenic activity against acetic acid-induced ulcerative colitis in albino rat assessed as ulcer area at 12.5 mmol/kg, po	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID194533	Tested for peak serum concentration in rat	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211149	AUC (infinity) in wild-type Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1676598	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1413402	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as recovery in colon weight at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1221974	Fold activity change at MRP2 ATPase (unknown origin) relative to control	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug 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.
AID1211152	Volume of distribution at steady state in MRP2 knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID179007	Fecal recovery in colostomized rats at 2 hr intervals for 48 h	1993	Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26	Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid.
AID1676593	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID699542	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1676599	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID152781	Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS	2001	Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4	Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID1061076	Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	New anti-inflammatory cembranoid diterpenoids from the Vietnamese soft coral Lobophytum crassum.
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current 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.
AID1470760	Trypanocidal activity against bloodstream form of Trypanosoma cruzi NINOA infected in NIH mouse assessed as reduction in parasitemia at 100 mg/kg, po measured at 2 to 4 hrs post dose by microscopic method	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1473739	Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1211157	AUC (infinity) in wild-type Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1824215	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as decrease in MPO level in colon at 50 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID19419	Partition coefficient (logD7.4)	1998	Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7	Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID1211098	Oral bioavailability in MRP2-deficient Wistar rat at 5 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1761236	Permeability of compound at pH 7.4 measured after 6 hrs by PAMPA assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.
AID1634677	Antiinflammatory activity in DSS-induced C57BL/6 mouse acute colitis model assessed as lowering of IL-6 level at 300 mg/kg administered by oral gavage from day 5 to day 12 measured on day 13	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Anti-inflammatory Actions of (+)-3'α-Angeloxy-4'-keto-3',4'-dihydroseselin (Pd-Ib) against Dextran Sulfate Sodium-Induced Colitis in C57BL/6 Mice.
AID1757485	Anti-colitis activity against DSS-induced BALB/c mouse model of subchronic relapsing colitis assessed as decrease in colon weight to length ratio at 100 mg/kg/day, po administered for 7 days in second week during 2 weeks DSS challenge and measured at the	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	6-(methylsulfinyl)hexyl isothiocyanate (6-MITC) from Wasabia japonica alleviates inflammatory bowel disease (IBD) by potential inhibition of glycogen synthase kinase 3 beta (GSK-3β).
AID425628	Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as effect on average time to detection of growth at >10'2 CFU of inoculum by MGIT 960 susceptibility test	2008	Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2	Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1824209	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as increase in colon length at 50 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1211097	Oral bioavailability in wild-type Wistar rat at 5 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1221964	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1221965	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID299084	Ulcerogenic activity in Wistar rat assessed as ulcer index at 2290 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid with D-phenylalanine for colon specific drug delivery in inflammatory bowel disease.
AID1221978	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID678722	Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1209591	Drug uptake in Sprague-Dawley rat brain slices at 100 nM after 5 hrs in presence of 10 uM of fumitremorgin-C and 20 uM of MK-571	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID622107	Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Oleanane-type triterpene saponins from the bark of Aralia elata and their NF-κB inhibition and PPAR activation signal pathway.
AID1473835	Stimulation of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID415827	Half life in TNBS-induced po dosed Wistar rat colitis model assessed as assessed as release of 5-aminosalicylic acid	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats.
AID1221970	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID173949	Tested for peak serum concentration in urine after oral administered dose in rat 5	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1470761	Trypanocidal activity against bloodstream form of Trypanosoma cruzi NINOA infected in NIH mouse assessed as reduction in parasitemia at 100 mg/kg, po measured at 6 hrs post dose by microscopic method	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID80567	Tested for weight loss in guinea pig at 60 umol concentration of compound	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211026	Volume of distribution at steady state in MDR1A knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1470753	Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1413414	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in IL-6 expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by Western blot analysis	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID678717	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID395170	Antiinflammatory activity against dextrane disodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as diseased animal with rectal prolapse at 250 mg/kg administered 1 hr before dextrane disodium sulfate challenge	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis.
AID91481	Binding constant against human serum albumin (HSA)	2001	Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25	Cheminformatic models to predict binding affinities to human serum albumin.
AID173943	Tested for peak serum concentration in feces after oral administered dose in rat 6	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1676601	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1211160	AUC (infinity) in MRP2 knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID509502	Antibacterial activity agaisnt Escherichia coli MTCC 8739 by agar diffusion method	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID395169	Antiinflammatory activity against dextrane disodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as diseased animal with stool consistency at 250 mg/kg administered 1 hr before dextrane disodium sulfate challenge	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis.
AID1576578	Fraction absorbed of the compound by PAMPA	2019	MedChemComm, Dec-01, Volume: 10, Issue:12	Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID1542240	Permeability of the compound at 30 to 50 uM at pH 7.4 measured up to 6 hrs by PAMPA-BBB assay method	2019	European journal of medicinal chemistry, Apr-01, Volume: 167	Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID1221976	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1230165	Anti-colitis activity in Wistar rat assessed as suppression of TNBS-induced body weight reduction at 300 mg/kg, po qd administered for 1 week starting 48 hrs post TNBS induction	2015	Journal of natural products, Jun-26, Volume: 78, Issue:6	Bacteria-Derived Compatible Solutes Ectoine and 5α-Hydroxyectoine Act as Intestinal Barrier Stabilizers to Ameliorate Experimental Inflammatory Bowel Disease.
AID173944	Tested for peak serum concentration in urine after mean oral administered dose in rat	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211164	Cmax in MRP2 knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1763266	Anti-colitis activity against TNBS-induced rat model of colitis assessed as increase in body weight at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID1211019	AUC (infinity) in BCRP knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1079936	Choleostatic 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]
AID1211095	Half life in wild-type Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1676591	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID209811	Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells	2001	Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4	Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID433903	Hepatotoxicity in mouse assessed as carcinogenic potency	2009	European journal of medicinal chemistry, Sep, Volume: 44, Issue:9	Development of QSAR models for predicting hepatocarcinogenic toxicity of chemicals.
AID1392398	Antiulcerogenic activity in DSS-induced acute ulcerative colitis C57BL/6J mouse model assessed as decrease in body weight at 500 mg/kg, po qd administered for 7 days (Rvb = 23.96%)	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9	Syntheses and structure-activity relationships on antibacterial and anti-ulcerative colitis properties of quaternary 13-substituted palmatines and 8-oxo-13-substituted dihydropalmatines.
AID655417	Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis	2012	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7	Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.
AID1211120	Oral bioavailability in MRP2 knockout Sprague-Dawley rat at 20 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID78212	Tested for mean score after quantitative histological evaluation result in guinea pig	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID417730	Ulcerogenic effect in rat colon assessed as ulcer index at 3000 mg/kg by Rainsford's cold stress method	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats.
AID1824210	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as reduction colonic damage at 50 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1824219	Antiinflammatory activity in DSS-induced C57BL/6 mouse model of colitis assessed as decrease in TNF-gamma level 25 to 100 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1824218	Antiinflammatory activity in DSS-induced C57BL/6 mouse model of colitis assessed as decrease in IL-1beta level 25 to 100 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1660992	Inhibition of AICAR transformylase (unknown origin)	2020	Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15	The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.
AID1211159	AUC (infinity) in BCRP knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1824921	Anti-colitis activity against DSS-induced BALB/c mouse model assessed as reduction in disease activity index at 100 mg/kg, po administered for 5 to 14 days	2022	Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1	Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
AID1392406	Antiulcerogenic activity in DSS-induced acute ulcerative colitis C57BL/6J mouse model assessed as disappearance of inflammatory edema at 500 mg/kg, po qd administered for 7 days by microscopic analysis	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9	Syntheses and structure-activity relationships on antibacterial and anti-ulcerative colitis properties of quaternary 13-substituted palmatines and 8-oxo-13-substituted dihydropalmatines.
AID1211020	AUC (infinity) in MRP2 knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID349141	Inhibition of human carbonic anhydrase 2 esterase activity by spectrophotometry	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
AID444051	Total clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID604022	Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID1321649	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as inhibition of myeloperoxidase level in colon at 300 mg/kg/day, po administered for 5 days post 1 day of TNBS-challenge by colorimetric method relative to control	2016	Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19	In vitro and in vivo inhibitory activity of 6-amino-2,4,5-trimethylpyridin-3-ols against inflammatory bowel disease.
AID1824220	Antiinflammatory activity in DSS-induced C57BL/6 mouse model of colitis assessed as increase in IL-10 level 25 to 100 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID190858	Urinary recovery in colostomized rats at 2 hr intervals for 48 h	1993	Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26	Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid.
AID1221971	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID425632	Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as minimum drug level resulting in no detectable growth at 10'6 CFU of inoculum after 56 days by MGIT 960 susceptibility test	2008	Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2	Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1221961	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1896149	Inhibition of human NTCP mediated TCA uptake in U2OS expresseing HA-tagged NTCP cells preincubated for 10 mins followed by substrate addition and measured after 2 mins using [3H]-taurocholate as substrate by liquid scintillation counter analysis	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1470762	Trypanocidal activity against bloodstream form of Trypanosoma cruzi NINOA infected in NIH mouse assessed as reduction in parasitemia at 100 mg/kg, po measured at 4 hrs post dose by microscopic method relative to control	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1815674	Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as change in gibbs free energy by isothermal titration calorimetry	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target.
AID455986	Permeability across human Caco-2 cells	2009	Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19	Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID588210	Human drug-induced liver injury (DILI) modelling dataset from Ekins et al	2010	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12	A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1600822	Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method	2019	Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19	Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.
AID1211116	Half life in MRP2 knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1221960	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1534338	Inhibition of cystine/glutamate antiporter system xc- in human Calu1 cells assessed as reduction in L-[3,3'-14C]-cystine uptake in presence of Na+ free uptake buffer by scintillation counting assay	2019	European journal of medicinal chemistry, Feb-01, Volume: 163	Discovery and development of small molecule modulators targeting glutamine metabolism.
AID1211051	Oral bioavailability in BCRP knockout mouse at 20 mg/kg	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID444056	Fraction escaping gut-wall elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID173942	Tested for peak serum concentration in feces after oral administered dose in rat 5	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211094	Tmax in MRP2-deficient Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1245306	Anti-ulcerative colitis activity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as colon macroscopic damage index at 300 mg/kg, po qd measured on day 8 (Rvb = 5.69 +/- 1.12 No_unit)	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID1470755	Inhibition of Trypanosoma cruzi trans-sialidase at 1 mM using N-acetyllactosamine as substrate in presence of 3'-sialyllactose measured after 15 mins by HPAEC-PAD relative to control	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID349142	Inhibition of human carbonic anhydrase 1 esterase activity by noncompetitive Lineweaver-Burke plot	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
AID143586	Tested in vivo for the ability to inhibit myeloperoxidase (MPO) activity in the colon of the TNB/ethanol-induced chronic colitis rats at the dosage of 500 mg/kg/day	1994	Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19	Novel dual inhibitors of 5-lipoxygenase and thromboxane A2 synthetase: synthesis and structure-activity relationships of 3-pyridylmethyl-substituted 2-amino-6-hydroxybenzothiazole derivatives.
AID1211145	Volume of distribution at steady state in wild-type Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1211161	Cmax in wild-type Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1763270	Anti-colitis activity against TNBS-induced rat model of colitis assessed as increase in colon length at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID1676590	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1079935	Cytolytic 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]
AID1221982	Fraction absorbed in human	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1499312	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as recovery of colon tissue edematous inflammation at 300 mg/kg, po qd administered for 5 days measured on day 6	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease.
AID977599	Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM	2013	Molecular pharmacology, Jun, Volume: 83, Issue:6	Structure-based identification of OATP1B1/3 inhibitors.
AID296200	Antiinflammatory activity against dextran sodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as weight loss after 6 days	2007	European journal of medicinal chemistry, Aug, Volume: 42, Issue:8	Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
AID1211143	Clearance in wild-type Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID509505	Antiulcerogenic activity against acetic acid-induced ulcerative colitis in albino rat assessed as ratio of wet weight and length at 12.5 mmol/kg, po	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID1221957	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1230183	Toxicity in Wistar rat assessed as decrease in Hsp70 level at 300 mg/kg, po qd administered for 1 week starting 48 hrs post TNBS induction by ELISA	2015	Journal of natural products, Jun-26, Volume: 78, Issue:6	Bacteria-Derived Compatible Solutes Ectoine and 5α-Hydroxyectoine Act as Intestinal Barrier Stabilizers to Ameliorate Experimental Inflammatory Bowel Disease.
AID1413412	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in TNFalpha expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by Western blot anal	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1576577	Effective permeability of compound incubated for 8 hrs by PAMPA	2019	MedChemComm, Dec-01, Volume: 10, Issue:12	Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID444053	Renal clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1634664	Antiinflammatory activity in DSS-induced C57BL/6 mouse acute colitis model assessed as lowering of disease activity index at 300 mg/kg administered by oral gavage from day 5 to day 12 measured on day 13 relative to DSS-treated control	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Anti-inflammatory Actions of (+)-3'α-Angeloxy-4'-keto-3',4'-dihydroseselin (Pd-Ib) against Dextran Sulfate Sodium-Induced Colitis in C57BL/6 Mice.
AID1498652	In vivo of inhibition of TNBS-induced decrease in body weight in TNBS-induced colitis Sprague-Dawley rat model at 300 mg/kg/day, po administered on day of TNBS administration and on four consecutive days measured on day 6	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.
AID28399	Cellular permeability (Pc) (Caco-2 cell monolayer)	2001	Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12	Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1413410	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in MCP1 expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by ELISA	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1763267	Anti-colitis activity against TNBS-induced rat model of colitis assessed as decrease in congestion at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID1815675	Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1321643	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as colon weight recovery at 300 mg/kg/day, po administered for 5 days post 1 day of TNBS-challenge relative to control	2016	Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19	In vitro and in vivo inhibitory activity of 6-amino-2,4,5-trimethylpyridin-3-ols against inflammatory bowel disease.
AID417722	Antiinflammatory activity against TNBS-induced Wistar rat colitis model assessed as decrease in severity of inflammation treated rectally 3 days after TNBS induction measured on day 7	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats.
AID1703908	Permeability of the compound by PAMPA-TGI assay	2020	European journal of medicinal chemistry, Oct-15, Volume: 204	Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID190239	% of rats exhibiting diarrhea	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID781326	pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X	2014	Pharmaceutical research, Apr, Volume: 31, Issue:4	Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID28925	Highest effective permeability across hexadecane membrane (pH 4-8)	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID1221979	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID678713	Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID453203	Lipophilicity, log D of the compound	2010	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1	Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1534336	Inhibition of xCT-mediated cystein/glutamate transporter (unknown origin) assessed as reduction in L-[14C]cyctein uptake	2019	European journal of medicinal chemistry, Feb-01, Volume: 163	Discovery and development of small molecule modulators targeting glutamine metabolism.
AID1211155	Half life in BCRP knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678716	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID476929	Human intestinal absorption in po dosed human	2010	European journal of medicinal chemistry, Mar, Volume: 45, Issue:3	Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1824212	Anti-colitis activity against DSS-induced C57BL/6 mouse model of colitis assessed as fold change in colon length at 25 to 100 mg/kg, po administered via gavage twice a day for 10 days relative to SASP	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID173950	Tested for peak serum concentration in urine after oral administered dose in rat 6	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID509503	Antibacterial activity agaisnt Candida albicans MTCC 3541 by agar diffusion method	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID1634676	Antiinflammatory activity in DSS-induced C57BL/6 mouse acute colitis model assessed as lowering of IL-17A level at 300 mg/kg administered by oral gavage from day 5 to day 12 measured on day 13	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Anti-inflammatory Actions of (+)-3'α-Angeloxy-4'-keto-3',4'-dihydroseselin (Pd-Ib) against Dextran Sulfate Sodium-Induced Colitis in C57BL/6 Mice.
AID237585	Tested for fraction of oral dose absorbed orally in humans	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID1824203	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as increase in colon length at 25 mg/kg, po administered via gavage twice daily for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID614829	Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:100 by DSC technique	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
AID173937	Tested for peak serum concentration in feces after mean oral administered dose in rat	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1676594	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID77141	Tested for cecal ulceration in diarrhea at 60 umol concentration of compound	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID444057	Fraction escaping hepatic elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079933	Acute 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
AID1221968	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID188198	Effect of compound on LTB4 production was measured in rat	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID293918	Antiinflammatory activity in Wistar rat colon assessed as myeloperoxidase activity per 100 mg tissue	2007	European journal of medicinal chemistry, Jun, Volume: 42, Issue:6	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1824202	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as assessed as recovery of body weight at 25 mg/kg, po administered via gavage twice daily for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1211118	Oral bioavailability in MDR1A knockout Sprague-Dawley rat at 20 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID444052	Hepatic clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1221963	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1824217	Antiinflammatory activity in DSS-induced C57BL/6 mouse model of colitis assessed as decrease in TNF-alpha level 25 to 100 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1211022	Clearance in MDR1A knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211153	Half life in wild-type Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID977602	Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM	2013	Molecular pharmacology, Jun, Volume: 83, Issue:6	Structure-based identification of OATP1B1/3 inhibitors.
AID1074028	Efflux ratio of permeability in pig LLC-PK1 cells transfected with human MDR1 at 1 uM by LC-MS/MS analysis	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
AID425631	Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as lowest drug level producing inhibition at 10'6 CFU of inoculum by agar counting method	2008	Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2	Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1499313	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as recovery in body weight decrease at 300 mg/kg, po qd administered for 5 days measured on day 6	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease.
AID1221966	Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1221962	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID175772	Damage to the colon observed after 48 hr after colitis induction in rats	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID293919	Antiarthritic activity in Freund's adjuvant-induced arthritis Wistar rat model after 13 days	2007	European journal of medicinal chemistry, Jun, Volume: 42, Issue:6	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1763269	Anti-colitis activity against TNBS-induced rat model of colitis assessed as increase in colon weight at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID77142	Tested for cecal ulceration in necropsy at 60 umol concentration of compound	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211117	Oral bioavailability in wild-type Sprague-Dawley rat at 20 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1824211	Anti-colitis activity against DSS-induced C57BL/6 mouse model of colitis assessed as fold change in body weight recovery at 25 to 100 mg/kg, po administered via gavage twice a day for 10 days relative to SASP	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID1676592	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID436235	Antiinflammatory activity against trinitrobenzenesulfonic acid-induced colitis in Wistar rat at 100 mg/kg, administered rectally	2009	European journal of medicinal chemistry, Oct, Volume: 44, Issue:10	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID194536	Tested for peak serum concentration in rat 4	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1230173	Anti-colitis activity in Wistar rat assessed as suppression of TNBS-induced reduction of colonic GSH level at 300 mg/kg, po qd administered for 1 week starting 48 hrs post TNBS induction by spectrophotometric analysis	2015	Journal of natural products, Jun-26, Volume: 78, Issue:6	Bacteria-Derived Compatible Solutes Ectoine and 5α-Hydroxyectoine Act as Intestinal Barrier Stabilizers to Ameliorate Experimental Inflammatory Bowel Disease.
AID1873197	Inhibition of ABCG2 (unknown origin) expressed in human HEK cells membrane vesicle assessed as inhibition of BCRP- mediated transport of [3H]-E3S using [3H]-oestrone 3-sulfate as radiolabeled substrate by liquid scintillation counter analysis	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID1634667	Antiinflammatory activity in DSS-induced C57BL/6 mouse acute colitis model assessed as protection against mucosal injury at 300 mg/kg administered by oral gavage from day 5 to day 12 measured on day 13 by hematoxylin/eosin staining-based microscopic analy	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Anti-inflammatory Actions of (+)-3'α-Angeloxy-4'-keto-3',4'-dihydroseselin (Pd-Ib) against Dextran Sulfate Sodium-Induced Colitis in C57BL/6 Mice.
AID1230169	Anti-colitis activity in Wistar rat assessed as reduction of TNBS-induced colon mass index at 300 mg/kg, po qd administered for 1 week starting 48 hrs post TNBS induction	2015	Journal of natural products, Jun-26, Volume: 78, Issue:6	Bacteria-Derived Compatible Solutes Ectoine and 5α-Hydroxyectoine Act as Intestinal Barrier Stabilizers to Ameliorate Experimental Inflammatory Bowel Disease.
AID349140	Inhibition of human carbonic anhydrase 1 esterase activity by spectrophotometry	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
AID395173	Antiinflammatory activity against dextrane disodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as length of colon at 250 mg/kg administered 1 hr before dextrane disodium sulfate challenge	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis.
AID1534337	Inhibition of cystine/glutamate antiporter system xc- in human HT1080 cells assessed as reduction in L-[3,3'-14C]-cystine uptake in presence of Na+ free uptake buffer by scintillation counting assay	2019	European journal of medicinal chemistry, Feb-01, Volume: 163	Discovery and development of small molecule modulators targeting glutamine metabolism.
AID1209589	Drug uptake in Sprague-Dawley rat brain slices at 100 nM after 5 hrs in presence of 10 uM of fumitremorgin-C	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID73467	Dissociation constant for Fibroblast growth factor 2 (None Observed)	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Validation of molecular docking calculations involving FGF-1 and FGF-2.
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID299088	Ulcerogenic activity in Wistar rat assessed as ulcer index at 3000 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid with D-phenylalanine for colon specific drug delivery in inflammatory bowel disease.
AID1211154	Half life in MDR1A knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID395171	Antiinflammatory activity against dextrane disodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as diseased animal with small intestine bleeding at 250 mg/kg administered 1 hr before dextrane disodium sulfate challenge	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis.
AID299841	Effect on TNBS-induced experimental colitis in po dosed Sprague-Dawely rat assessed as colon to body weight ratio after 5 days relative to control	2007	Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14	Colon-specific, mutual azo prodrug of 5-aminosalicylic acid with L-tryptophan: synthesis, kinetic studies and evaluation of its mitigating effect in trinitrobenzenesulfonic acid-induced colitis in rats.
AID1763268	Anti-colitis activity against TNBS-induced rat model of colitis assessed as decrease in adhesion at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID1392404	Antiulcerogenic activity in DSS-induced acute ulcerative colitis C57BL/6J mouse model assessed as colon macroscopic damage index at 500 mg/kg, po qd administered for 7 days (Rvb = 4.13 +/- 0.78 No_unit)	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9	Syntheses and structure-activity relationships on antibacterial and anti-ulcerative colitis properties of quaternary 13-substituted palmatines and 8-oxo-13-substituted dihydropalmatines.
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1211017	AUC (infinity) in wild-type Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID296198	Antiinflammatory activity against dextran sodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as small intestinal bleeding	2007	European journal of medicinal chemistry, Aug, Volume: 42, Issue:8	Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1413413	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as decrease in IL1beta expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by Western blot analy	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1470763	Solubility of the compound in water	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1703889	Permeability of the compound incubated for 8 hrs by PAMPA-TGI assay	2020	European journal of medicinal chemistry, Oct-15, Volume: 204	Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID436237	Antiarthritic activity against Freund's adjuvant-induced arthritis in Wistar rat assessed as reduction in paw volume administered 13 days after Freund's adjuvant challenge measured on day 21	2009	European journal of medicinal chemistry, Oct, Volume: 44, Issue:10	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1245317	Anti-ulcerative colitis activity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as recovery of each muscle layer structure at 300 mg/kg, po qd measured on day 8	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1824208	Anti-colitis activity against DSS-induced colitis in C57BL/6 mouse model assessed as body weight recovery at 50 mg/kg, po administered via gavage twice a day for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID293916	Ulcerogenic effect in Wistar rat at 3000 mg/kg, po by Rainsford's cold stress method relative to contro	2007	European journal of medicinal chemistry, Jun, Volume: 42, Issue:6	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1211114	Cmax in wild-type Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211018	AUC (infinity) in MDR1A knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1676589	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID173959	Tested for peak serum concentration in feces after oral administered dose in rat 6	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211162	Cmax in MDR1A knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211141	AUC (infinity) in wild-type Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211169	Half life in wild-type Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1079931	Moderate 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]
AID604020	Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID436234	Antiinflammatory activity against trinitrobenzenesulfonic acid-induced colitis in Wistar rat assessed as decrease in colon to body weight ratio at 100 mg/kg, po measured 24 hrs after last dose on day 11	2009	European journal of medicinal chemistry, Oct, Volume: 44, Issue:10	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID236912	Permeability Coefficient in 2/4/A1 cell model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID28392	Apparent permeability coefficient (Papp) (Caco-2 cell monolayer)	2001	Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12	Experimental and computational screening models for the prediction of intestinal drug absorption.
AID173109	Colonic weight was measured in rats	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID1209583	Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID296201	Antiinflammatory activity against dextran sodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as colon length	2007	European journal of medicinal chemistry, Aug, Volume: 42, Issue:8	Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
AID1211156	Half life in MRP2 knockout Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID404304	Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1221975	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID29844	Fraction absorbed after oral administration in humans	2001	Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12	Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1404017	Permeability of the compound at 500 uM after 8 hrs by PAMPA	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID626970	Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay	2011	Journal of natural products, Sep-23, Volume: 74, Issue:9	Anti-inflammatory triterpenoid saponins from the stem bark of Kalopanax pictus.
AID236268	Fraction absorbed in human intestine after oral administration compound was measured	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID1676595	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID173948	Tested for peak serum concentration in urine after oral administered dose in rat 4	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID425630	Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as lowest drug level producing inhibition at 10'6 CFU of inoculum by MGIT 960 susceptibility test	2008	Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2	Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1221956	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID409954	Inhibition of mouse brain MAOA	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID299838	Ulcerogenic activity in Wistar rat at 3000 mg/kg, po by cold stress method relative to control	2007	Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14	Colon-specific, mutual azo prodrug of 5-aminosalicylic acid with L-tryptophan: synthesis, kinetic studies and evaluation of its mitigating effect in trinitrobenzenesulfonic acid-induced colitis in rats.
AID293920	Antiarthritic activity in Freund's adjuvant-induced arthritis Wistar rat model after 21 days	2007	European journal of medicinal chemistry, Jun, Volume: 42, Issue:6	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID77143	Tested for cecal ulceration with mortality at 60 umol concentration of compound	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211147	Half life in wild-type Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID18849	Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology.	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans.
AID1211144	Clearance in MRP2-deficient Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1676596	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID173941	Tested for peak serum concentration in feces after oral administered dose in rat 4	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID236913	Permeability Coefficient in Caco-2 cell culture model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID1211115	Half life in BCRP knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1703888	Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay	2020	European journal of medicinal chemistry, Oct-15, Volume: 204	Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1676602	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211092	Cmax in MRP2-deficient Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1757479	Anti-colitis activity against DSS-induced BALB/c mouse model of subchronic relapsing colitis assessed as increase in softening of feces at 100 mg/kg/day, po administered for 7 days in second week during 2 weeks DSS challenge and measured at the end of 2nd	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	6-(methylsulfinyl)hexyl isothiocyanate (6-MITC) from Wasabia japonica alleviates inflammatory bowel disease (IBD) by potential inhibition of glycogen synthase kinase 3 beta (GSK-3β).
AID316228	Inhibition of SGK1 at 33 uM	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	Kinase-likeness and kinase-privileged fragments: toward virtual polypharmacology.
AID1211142	AUC (infinity) in MRP2-deficient Wistar rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1209581	Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID20050	Human absorption A (%)	1998	Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7	Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID1470754	Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood after 24 hrs by optical microscopic method	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1392400	Antiulcerogenic activity in DSS-induced acute ulcerative colitis C57BL/6J mouse model assessed as colon contracture at 500 mg/kg, po qd administered for 7 days (Rvb = 41.87%)	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9	Syntheses and structure-activity relationships on antibacterial and anti-ulcerative colitis properties of quaternary 13-substituted palmatines and 8-oxo-13-substituted dihydropalmatines.
AID1498653	In vivo of inhibition of TNBS-induced increase in colon weight in TNBS-induced colitis Sprague-Dawley rat model at 300 mg/kg/day, po administered on day of TNBS administration and on four consecutive days measured on day 6	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.
AID1211170	Half life in MDR1A knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1245312	Anti-ulcerative colitis activity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as improvement in colon contracture at 300 mg/kg, po qd measured on day 8 (Rvb = 41.8%)	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID417725	Antiinflammatory activity against TNBS-induced po dosed Wistar rat colitis model assessed as inhibition of MPO activity in neutrophils per 100 mg of tissue	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats.
AID1209592	Dissociation constant, pKa of the basic compound by capillary electrophoresis-mass spectrometry analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1757475	Anti-colitis activity against DSS-induced BALB/c mouse model of subchronic relapsing colitis assessed as reduction in fecal blood at 100 mg/kg/day, po administered for 7 days in second week during 2 weeks DSS challenge and measured at the end of 2nd week	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	6-(methylsulfinyl)hexyl isothiocyanate (6-MITC) from Wasabia japonica alleviates inflammatory bowel disease (IBD) by potential inhibition of glycogen synthase kinase 3 beta (GSK-3β).
AID28679	Partition coefficient (logD6.8)	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID73458	Binding affinity for Fibroblast growth factor 1	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Validation of molecular docking calculations involving FGF-1 and FGF-2.
AID395172	Antiinflammatory activity against dextrane disodium sulfate-induced ulcerative colitis in BALB/c mouse assessed as diseased animal with large intestine bleeding at 250 mg/kg administered 1 hr before dextrane disodium sulfate challenge	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis.
AID349145	Inhibition of human carbonic anhydrase 2 esterase activity by non-competitive Lineweaver-Burke plot	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
AID28234	% absorbed in human GI-tract	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID249179	Permeability Coefficient in hexadecane membranes model	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Exploring the role of different drug transport routes in permeability screening.
AID678715	Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID616223	Binding affinity to multilamellar vesicles assessed as apparent binding constant after 2 hrs by double reciprocal plot	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
AID1676597	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1211025	Volume of distribution at steady state in wild-type Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1824205	Anti-colitis activity against DSS-induced C57BL/6 mouse model of colitis assessed as assessed as body weight recovery at 50 mg/kg, po administered via gavage DSS stimulation for 5 days followed by compound addition once daily for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID167806	Concentration required to inhibit PAF-induced maximum aggregation by 50%	2001	Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18	Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID1245302	Anti-ulcerative colitis activity in DSS-induced acute C57Bl/6J mouse ulcerative colitis model assessed as inhibition rate of disease activity index at 300 mg/kg, po qd measured on day 8 relative to control	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
AID588209	Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset	2010	Chemical research in toxicology, Jul-19, Volume: 23, Issue:7	Developing structure-activity relationships for the prediction of hepatotoxicity.
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID436229	Gastrointestinal toxicity in Wistar rat assessed as ulcer index at 3000 mg/kg, po by Rainsford's cold stress method	2009	European journal of medicinal chemistry, Oct, Volume: 44, Issue:10	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
AID1470752	Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood after 24 hrs by optical microscopic method	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID299085	Decrease in inflammation in TNBS-induced Wistar rat colitis model after 24 to 48 hrs	2007	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7	Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid with D-phenylalanine for colon specific drug delivery in inflammatory bowel disease.
AID1211166	Tmax in MDR1A knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID179008	Fecal recovery in non-colostomized rats at 2 hr intervals for 48 h	1993	Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26	Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid.
AID1498655	In vivo of inhibition of TNBS-induced increase in myeloperoxidase level in TNBS-induced colitis Sprague-Dawley rat model colon tissue at 300 mg/kg/day, po administered on day of TNBS administration and on four consecutive days measured on day 6	2018	Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14	Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.
AID73456	Dissociation constant for Fibroblast growth factor 1	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Validation of molecular docking calculations involving FGF-1 and FGF-2.
AID1211119	Oral bioavailability in BCRP knockout Sprague-Dawley rat at 20 mg/kg by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID28924	Effective permeability (Pe) across a hexadecane membrane (pH 6.8)	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug 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.
AID604023	Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1413415	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as increase in IL-10 expression at 300 mg/kg, po administered once daily via gavage for 5 days starting 1 day post TNBS induction measured on day 7 by Western blot analysi	2018	MedChemComm, Aug-01, Volume: 9, Issue:8	Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
AID1321638	Antiinflammatory activity in TNBS-induced Sprague-Dawley rat colitis model assessed as body weight recovery at 300 mg/kg/day, po administered for 5 days post 1 day of TNBS-challenge measured daily during compound dosing relative to control	2016	Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19	In vitro and in vivo inhibitory activity of 6-amino-2,4,5-trimethylpyridin-3-ols against inflammatory bowel disease.
AID184773	Tested for the ability to decrease lesion area in the colon of the TNB/ethanol-induced chronic colitis rats at the dosage of 500 mg/kg/day	1994	Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19	Novel dual inhibitors of 5-lipoxygenase and thromboxane A2 synthetase: synthesis and structure-activity relationships of 3-pyridylmethyl-substituted 2-amino-6-hydroxybenzothiazole derivatives.
AID194537	Tested for peak serum concentration in rat 5	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1211021	Clearance in wild-type Sprague-Dawley rat at 5 mg/kg, iv by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1209590	Drug uptake in Sprague-Dawley rat brain slices at 100 nM after 5 hrs in presence of 20 uM of MK-571	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1211096	Half life in MRP2-deficient Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1211168	Tmax in MRP2 knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID678712	Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1824206	Anti-colitis activity against DSS-induced C57BL/6 mouse model of colitis assessed as increase in colon length at 50 mg/kg, po administered via gavage DSS stimulation for 5 days followed by compound addition once daily for 10 days	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
AID190859	Urinary recovery in non-colostomized rats at 2 hr intervals for 48 h	1993	Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26	Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid.
AID18847	Percent of drug absorbed by human intestine after oral administration	2000	Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20	Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
AID1576576	Effective permeability of compound by PAMPA	2019	MedChemComm, Dec-01, Volume: 10, Issue:12	Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID1824922	Anti-colitis activity against DSS-induced colitis BALB/c mouse model assessed as effect on colon length at 100 mg/kg, po measured after 14 days	2022	Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1	Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
AID425629	Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as effect on average time to detection of growth at 10'5 CFU of inoculum by MGIT 960 susceptibility test	2008	Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2	Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1210069	Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1211163	Cmax in BCRP knockout Sprague-Dawley rat at 20 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1676600	Binding 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 chromatography	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID592681	Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis	2011	Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8	QSAR-based permeability model for drug-like compounds.
AID515780	Intrinsic solubility of the compound in water	2010	Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19	QSAR-based solubility model for drug-like compounds.
AID15120	Percent of the drug absorbed after administration to humans was determined	1999	Journal of medicinal chemistry, May-20, Volume: 42, Issue:10	Molecular hashkeys: a novel method for molecular characterization and its application for predicting important pharmaceutical properties of molecules.
AID1221973	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID442514	Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation	2010	European journal of medicinal chemistry, Feb, Volume: 45, Issue:2	Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID442515	Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation at 50 uM	2010	European journal of medicinal chemistry, Feb, Volume: 45, Issue:2	Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID614827	Binding affinity to dipalmitoyl phosphatidyl choline lipid bilayer assessed as decrease in pre-transition temperature at compound to lipid molar ratio of 1:1 by DSC technique	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
AID173957	Tested for total administered dose in rat 5	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1079938	Chronic 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]
AID1763277	Anti-colitis activity against TNBS-induced rat model of colitis assessed as decrease in MPO level in colon at 300 mg/kg, po administered for 5 days and measured on day 5	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Synthesis and activity of N-(5-hydroxy-3,4,6-trimethylpyridin-2-yl)acetamide analogues as anticolitis agents via dual inhibition of TNF-α- and IL-6-induced cell adhesions.
AID1211150	AUC (infinity) in MRP2-deficient Wistar rat at 5 mg/kg, po by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9	Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
AID1221972	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1470751	Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control	2017	European journal of medicinal chemistry, May-26, Volume: 132	An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID509498	Antiulcerogenic activity against acetic acid-induced ulcerative colitis in albino rat assessed as ulcer index at 12.5 mmol/kg, po	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Design, synthesis and anti-ulcerogenic effect of some of furo-salicylic acid derivatives on acetic acid-induced ulcerative colitis.
AID616228	Antifertility effect in goat epididymis spermatozoa assessed as decrease in lactate production at 1.25 mm after 2 hrs by NMR analysis	2011	European journal of medicinal chemistry, Sep, Volume: 46, Issue:9	In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
AID173956	Tested for total administered dose in rat 4	1983	Journal of medicinal chemistry, Sep, Volume: 26, Issue:9	A polymeric drug for treatment of inflammatory bowel disease.
AID1815673	Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as change in entropy by isothermal titration calorimetry	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic Target.
AID417721	Antiinflammatory activity against TNBS-induced Wistar rat colitis model assessed as decrease in severity of inflammation treated po 3 days after TNBS induction measured on day 7	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347163	384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347158	ZIKV-mCherry secondary qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347164	384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347156	DAPI mCherry counterscreen qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1634957	Antiulcerative activity in DSS-induced C57BL/6J mouse model of acute ulcerative colitis assessed as partial disappearance of inflammatory edema at 200 mg/kg, po measured over 7 days by microscopic analysis	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
AID1634949	Antiulcerative activity in DSS-induced C57BL/6J mouse model of acute ulcerative colitis assessed as body weight loss at 300 mg/kg, po measured over 7 days (Rvb = 18%)	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
AID1634951	Antiulcerative activity in DSS-induced C57BL/6J mouse model of acute ulcerative colitis assessed as colon contracture at 300 mg/kg, po measured over 7 days (Rvb = 37 %)	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
AID1634955	Antiulcerative activity in DSS-induced C57BL/6J mouse model of acute ulcerative colitis assessed as colon macroscopic damage index at 300 mg/kg, po measured over 7 days (Rvb = 4.63 +/- 0.52 No_unit)	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
AID1634953	Antiulcerative activity in DSS-induced C57BL/6J mouse model of acute ulcerative colitis assessed as inhibition of disease activity index at 300 mg/kg, po measured over 7 days relative to control	2016	Journal of natural products, Apr-22, Volume: 79, Issue:4	Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
AID1345155	Human Proton-coupled folate transporter (SLC46 family of folate transporters)	2006	Cell, Dec-01, Volume: 127, Issue:5	Identification of an intestinal folate transporter and the molecular basis for hereditary folate malabsorption.
AID1159550	Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening	2015	Nature cell biology, Nov, Volume: 17, Issue:11	6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1802828	Surface Plasmon Resonance (SPR) Assay from Article 10.1074/jbc.M113.521708: \\A novel small-molecule tumor necrosis factor a inhibitor attenuates inflammation in a hepatitis mouse model.\\	2014	The Journal of biological chemistry, May-02, Volume: 289, Issue:18	A novel small-molecule tumor necrosis factor α inhibitor attenuates inflammation in a hepatitis mouse model.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1388 (33.44)	18.7374
1990's	927 (22.33)	18.2507
2000's	808 (19.47)	29.6817
2010's	777 (18.72)	24.3611
2020's	251 (6.05)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	585 (13.18%)	5.53%
Reviews	631 (14.22%)	6.00%
Case Studies	932 (21.01%)	4.05%
Observational	24 (0.54%)	0.25%
Other	2,265 (51.05%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (67)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
The Effect of Sulfasalazine on CRH Levels in Pregnant Women With a History of Pre-Term Birth: A Randomized Controlled Trial[NCT05703425]	Phase 2	50 participants (Anticipated)	Interventional	2023-03-01	Recruiting
IL-7 and IL-7R Expression in Peripheral Blood Mononuclear Cells, Peripheral Blood Monocytes or Differentiated Macrophages of Rheumatoid Arthritis Patients With Active vs. Inactive Disease Treated With DMARD and/or CIMZIA[NCT02451748]	Phase 4	32 participants (Actual)	Interventional	2015-08-31	Completed
A Prospective, Single-centre, Randomised Study Evaluating the Clinical, Imaging and Immunological Depth of Remission Achieved by Very Early Versus Delayed Etanercept in Patients With Rheumatoid Arthritis[NCT02433184]	Phase 4	120 participants (Actual)	Interventional	2011-07-31	Completed
Comparison of Sulfasalazine Versus Leflunomide Based Combination Disease Modifying Anti-rheumatic Drug Therapy (DMARD) in Patients With Rheumatoid Arthritis Failing Methotrexate Monotherapy : A Randomized Control Trial[NCT02930343]	Phase 3	136 participants (Actual)	Interventional	2016-09-30	Terminated(stopped due to Due to time constraints, the study was halted prematurely)
Gastrointestinal Nutrient Transit and Enteroendocrine Function After Upper Gastrointestinal Surgery[NCT03734627]		40 participants (Actual)	Observational	2016-07-01	Completed
On the Impact of Therapeutic Tumor Necrosis Factor-alpha Inhibition on Anogenital Human Papillomavirus Infection[NCT02376478]		222 participants (Actual)	Observational	2009-12-31	Completed
Targeted Treatment Early With Etanercept Plus Methotrexate Versus T2T Care for DMARD-naïve Early RA Patients. A Prospective, Longitudinal Cohort Study With Embedded Pilot Randomised Controlled Trial to Assess Treatment Rationalisation Based on naïve T-cel[NCT03813771]	Phase 4	106 participants (Anticipated)	Interventional	2019-03-31	Not yet recruiting
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics[NCT02099240]	Early Phase 1	11 participants (Actual)	Interventional	2014-03-06	Terminated(stopped due to Not enough patient enrollment and lack of staffing)
CSP #551 - Rheumatoid Arthritis: Comparison of Active Therapies in Patients With Active Disease Despite Methotrexate Therapy[NCT00405275]		353 participants (Actual)	Interventional	2007-07-31	Completed
Effect of Sarilumab on Patient-reported Outcomes in Patients With Moderately to Severely Active Rheumatoid Arthritis and With Inadequate Response or Intolerance to Current Conventional Synthetic DMARDs or Tumor Necrosis Factor Inhibitors[NCT03449758]	Phase 4	84 participants (Actual)	Interventional	2018-03-05	Completed
A Prospective, Randomized, Controlled, Open Label, Assessor-blinded, Parallel-group Phase III Clinical Trial to Evaluate the Impact of Tapering Systemic Immunosuppressive Therapy in a Treat-to-target Approach on Maintaining Minimal Disease Activity in Adu[NCT04610476]	Phase 3	270 participants (Anticipated)	Interventional	2020-10-19	Recruiting
A Phase Ib/II Randomized, Open Label Drug Repurposing Trial of Glutamate Signaling Inhibitors in Combination With Chemoradiotherapy in Patients With Newly Diagnosed Glioblastoma[NCT05664464]	Phase 1/Phase 2	120 participants (Anticipated)	Interventional	2023-01-01	Recruiting
Clinical Effectiveness of Standard Step up Care (Methotrexate) Compared to Early Combination DMARD Therapy With Standard Step up Care Compared to Early Use of TNF Inhibitors With Standard Step up Care for the Treatment of Moderate to Severe Psoriatic Arth[NCT03739853]	Phase 4	315 participants (Anticipated)	Interventional	2019-05-14	Recruiting
An Open Label, Randomised Study to Compare the Efficacy of Certolizumab Pegol (CZP) Plus a Dynamic or Fixed Dose Treatment Strategy in Patients With Rheumatoid Arthritis, a Phase II Study[NCT02293590]	Phase 2	43 participants (Actual)	Interventional	2013-11-30	Completed
Treatment of Early Aggressive Rheumatoid Arthritis (TEAR)[NCT00259610]	Phase 4	755 participants (Actual)	Interventional	2004-05-31	Completed
Phase I/II Clinical Trial Assessing the Combination of Sulfasalazine With Standard of Care Induction Therapy in Newly Diagnosed Acute Myeloid Leukemias (AML) Patients 60 Years or Older- the SALMA Study[NCT05580861]	Phase 1/Phase 2	64 participants (Anticipated)	Interventional	2023-05-17	Recruiting
Treatment of Rheumatoid Arthritis With DMARDs: Predictors of Response[NCT03414502]	Phase 3	400 participants (Anticipated)	Interventional	2007-12-10	Recruiting
A Prospective Randomized, Open, Multi-Center Trial Comparing TNF-Blockade + MTX to MTX+SSZ+HCQ in Patients With Early RA With an Inadequate Response to MTX[NCT00764725]	Phase 4	487 participants (Actual)	Interventional	2002-12-31	Completed
Double Blind Trial Investigating the Role of Sulfasalazine in Decreasing Opioids Requirements in Breast Cancer Patients[NCT03847311]	Phase 2	40 participants (Anticipated)	Interventional	2021-05-03	Recruiting
A Randomized, Double-blind, Multicenter Study Evaluating the Safety and Efficacy of Sarilumab Added to Non-MTX DMARDs or as Monotherapy in Japanese Patients With Active Rheumatoid Arthritis[NCT02373202]	Phase 3	91 participants (Actual)	Interventional	2015-02-28	Completed
Clinical Study Evaluating the Efficacy and Safety of Sulfasalazine in Patients With Metastatic Colorectal Cancer[NCT06134388]	Phase 3	50 participants (Anticipated)	Interventional	2023-09-01	Recruiting
Use of TNF-blocking Therapy in Combination With DMARDs in Patients With Early Rheumatoid Arthritis[NCT00908089]	Phase 4	100 participants (Actual)	Interventional	2003-03-31	Active, not recruiting
Efficacy and Safety of Etanercept Dose Reduction in Patients With Ankylosing Spondylitis[NCT02638896]	Phase 4	100 participants (Anticipated)	Interventional	2016-01-31	Not yet recruiting
Longitudinal Observational Study on Rheumatoid Arthritis Patients: Effects of Antirheumatic Treatment on Serum Levels of Survivin[NCT03440892]		2,500 participants (Anticipated)	Observational	2017-11-01	Recruiting
Treat-to-target Strategy in Ankylosing Spondylitis Using Etanercept and Conventional Synthetic DMARDs, a Prospective Randomized Controlled Study[NCT04077957]	Phase 4	100 participants (Anticipated)	Interventional	2019-10-07	Not yet recruiting
Triple III Comparison of Leflunomide Alone Versus Two DMARD Combinations (Leflunomide-Hydroxychloroquine-Sulfasalazine or Methotrexate-Hydroxychloroquine-Sulfasalazine) in the Treatment of Rheumatoid Arthritis[NCT00579878]	Phase 3	69 participants (Actual)	Interventional	2001-03-27	Completed
A Randomized, Open-Label Study in the Asia-Pacific Region Comparing the Safety and Efficacy of Etanercept With Usual DMARD Therapy in Subjects With Rheumatoid Arthritis[NCT00422227]	Phase 4	300 participants (Actual)	Interventional	2007-06-30	Completed
Randomized Controlled Clinical Trial Evaluating Methotrexate or Leflunomide + Targeted Therapy Versus Methotrexate or Leflunomide + Sulfasalazine + Hydroxychloroquine in Patients With Rheumatoid Arthritis and Insufficient Response to Methotrexate or Leflu[NCT02714634]	Phase 4	286 participants (Anticipated)	Interventional	2016-03-30	Recruiting
Phase I Trial Combining Sulfasalazine and Gamma Knife Radiosurgery for Recurrent Glioblastoma[NCT04205357]	Phase 1	24 participants (Actual)	Interventional	2020-03-01	Completed
A Phase 1, Open-label Study in Healthy Adult Subjects to Evaluate Effects of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of CC-99677 and the Effects of CC-99677 on the Pharmacokinetics of Digoxin, Metformin, Methotrexate, Midazolam, R[NCT04268394]	Phase 1	48 participants (Actual)	Interventional	2020-03-13	Completed
CHronic Nonbacterial Osteomyelitis International Registry (CHOIR)[NCT04725422]		2,000 participants (Anticipated)	Observational	2018-08-01	Recruiting
Comparison of Anti-TNF Therapy Plus Methotrexate, Combination Therapy of DMARDs, and Methotrexate Alone in Very Early Polyarticular Juvenile Idiopathic Arthritis. A National Randomized Multicenter Clinical Trial.[NCT01015547]	Phase 3	60 participants (Actual)	Interventional	2003-05-31	Completed
Pilot Study of the Safety and Efficacy of Sulfasalazine in Pulmonary Arterial Hypertension[NCT04528056]	Phase 1/Phase 2	80 participants (Anticipated)	Interventional	2020-08-01	Recruiting
Phase III, Randomized, Study of Sulfasalazine Versus Placebo in the Prevention of Acute Diarrhea in Patients Receiving Pelvic Radiation Therapy[NCT01198145]	Phase 3	87 participants (Actual)	Interventional	2011-04-30	Completed
A 2 Year Prospective Multicentre Randomised Controlled Trial Comparing Effectiveness in Daily Practice of Different Treatment Strategies for Early Rheumatoid Arthritis.[NCT01172639]	Phase 4	400 participants (Actual)	Interventional	2009-02-28	Completed
Randomized Controlled 12 Months Trial With Etanercept (Enbrel ®) vs. Sulfasalazine in Early Axial Spondyloarthritis With Focus on Improvement of Acute Inflammatory Lesions as Detected by MRI. Amendment 4: 1-Year Extension of Study[NCT00844142]	Phase 2	80 participants (Anticipated)	Interventional	2005-11-30	Recruiting
Clinical Study of Tripterygium Capsule to Treat Early Ankylosing Spondylitis: a 12-Week, Multiple Centers, Randomized Double-Blind, Positive Drug and Placebo Controlled Clinical Trial[NCT00889694]	Phase 2/Phase 3	80 participants (Anticipated)	Interventional	2008-10-31	Enrolling by invitation
Effect of Sulfasalazine on Endothelial Function[NCT00554203]		60 participants (Anticipated)	Interventional	2003-07-31	Completed
Comparison of Three Different Treatment Regimes in Early Rheumatoid Arthritis: A Randomized Open-labelled Trial[NCT01870128]	Phase 3	60 participants (Actual)	Interventional	2009-08-31	Completed
A Randomized, Double-Blind Study Evaluating the Safety and Efficacy of Etanercept and Sulphasalazine in Subjects With Ankylosing Spondylitis[NCT00247962]	Phase 4	566 participants (Actual)	Interventional	2005-12-31	Completed
A Phase 1, Fixed Sequence, Open-label, Drug-drug Interaction Study to Evaluate the Effect of GLPG3970 on the Pharmacokinetics of Sulfasalazine in Adult, Healthy Subjects[NCT04720183]	Phase 1	8 participants (Actual)	Interventional	2021-01-11	Completed
Effects of Sulfasalazine on BOLD Response to Alcohol Cues[NCT01312129]		23 participants (Actual)	Interventional	2010-03-31	Completed
Leflunomide Versus Sulfasalazine/Methotrexate in Rheumatoid Arthritis Patients With Active Disease Despite Methotrexate: an Ultrasound and Magnetic Resonance Imaging Study[NCT01659242]	Phase 4	1 participants (Actual)	Interventional	2012-07-31	Terminated
A Phase 1, Three-Part, Open-label Study in Healthy Adult Volunteers to Assess Vadadustat as a Perpetrator in Drug-Drug Interactions With Rosuvastatin, Sulfasalazine, Pravastatin, Atorvastatin and Simvastatin[NCT03801733]	Phase 1	134 participants (Actual)	Interventional	2018-06-17	Completed
A Single-center, Randomized, Double-blind Clinical Study to Evaluate the Effect of Sulfasalazine on Painful Neuropathy[NCT01667029]	Phase 2	8 participants (Actual)	Interventional	2013-05-31	Terminated(stopped due to poor enrollment)
A Pilot Study to Determine the Effect of Sulfasalazine on Glutamate Levels Detected by Magnetic Resonance Spectroscopy(MRS) in Patients With Glioma[NCT01577966]		9 participants (Actual)	Interventional	2012-01-31	Completed
An Open Label, Single Dose, Three Part Study to Assess the Effects of Rolapitant (1.8 mg/mL Rolapitant IV Solution) on the Pharmacokinetics of Digoxin (P-gp); Sulfasalazine (BCRP); and the Cooperstown Cocktail (Midazolam [CYP3A4], Omeprazole [CYP2C19], Wa[NCT02434861]	Phase 1	102 participants (Actual)	Interventional	2015-05-31	Completed
A Randomized, Double-Blind, Double-Dummy Study Assessing The Safety and Tolerability of Sarilumab and Tocilizumab In Patients With Rheumatoid Arthritis Who Are Inadequate Responders to or Intolerant of TNF Antagonists[NCT01768572]	Phase 3	202 participants (Actual)	Interventional	2013-03-31	Completed
Pharmacokinetics of Sulfasalazine, Paracetamol, Fexofenadine and Valsartan After Oral Administration Using 240 ml Non-caloric Water, a Carbohydrate Enriched Drink and Grapefruit Juice in Correlation to the Intestinal Availability of Water as Quantified by[NCT03012763]	Phase 1	9 participants (Actual)	Interventional	2016-04-30	Completed
Clinical Effectiveness of Symptomatic Therapy Compared to Standard Step up Care for the Treatment of Low Impact Psoriatic Oligoarthritis: a 2 Arm Parallel Group Feasibility Study[NCT03797872]	Phase 4	1 participants (Actual)	Interventional	2019-04-17	Completed
Effects of Extended Release Methylnaltrexone Bromide (150 mg b.i.d.) in Comparison to Extended Release Naloxone Hydrochloride (20 mg b.i.d.) on Loperamide-induced Delay of the Oro-cecal, Whole-gut and Colon Transit Time in Healthy Subjects.[NCT01596764]	Phase 1	16 participants (Actual)	Interventional	2011-05-31	Completed
Effects of 500 mg Immediate Release and Extended Release Methylnaltrexone on Loperamide-induced Delay of the Oro-cecal and Whole-gut Transit Time in Healthy Subjects[NCT01596777]	Phase 1	15 participants (Actual)	Interventional	2010-01-31	Completed
Sequential Application of Yisaipu® and Disease Modifying Anti-Rheumatic Drugs (DMARDs) in Treating Mild-to-Moderate Ankylosing Spondylitis: the Mid-term Follow-up Result[NCT03411798]	Phase 4	76 participants (Actual)	Interventional	2017-12-15	Completed
Induction of Remission in RA Patients at Low Disease Activity by Additional Infliximab-therapy[NCT00521924]	Phase 3	8 participants (Actual)	Interventional	2007-06-30	Terminated(stopped due to Slow Enrollment)
Treatments Against RA and Effect on FDG-PET/CT (The TARGET Trial)[NCT02374021]	Phase 4	159 participants (Actual)	Interventional	2016-07-31	Completed
A Multicenter, Randomized, Open-Label, Parallel-Group Usability Study Of The Sarilumab Auto-Injector Device And A Prefilled Syringe In Patients With Moderate To Severe Active Rheumatoid Arthritis Who Are Candidates For Anti-IL6R Therapy[NCT02057250]	Phase 3	217 participants (Actual)	Interventional	2014-03-31	Completed
A Multicenter, Randomized, Open-label, Blinded-assessor, Follow-up, Phase 4 Study in Patients With Rheumatoid Arthritis Who Have Completed the Initial Treatment Part in the NORD-STAR Study and Have Reached Stable Low Disease Activity[NCT02466581]	Phase 4	25 participants (Actual)	Interventional	2015-02-03	Active, not recruiting
A Phase 1, Two-part, Open-label, Drug-drug Interaction Study in Healthy Male Adult Participants to Evaluate the Effects of BMS-986371 on the Pharmacokinetics of Methotrexate in the Presence and Absence of Sulfasalazine[NCT05445440]	Phase 1	30 participants (Actual)	Interventional	2022-09-06	Completed
A Randomized, Placebo-controlled Pilot Study of Sulfasalazine for the Treatment of Primary Sclerosing Cholangitis (PSC)[NCT03561584]	Phase 2	42 participants (Anticipated)	Interventional	2018-07-01	Recruiting
Anti-Tumor Necrosis Factor Therapy In Patients With Ankylosing Spondylitis-A Registry Project[NCT02456363]	Phase 2	300 participants (Anticipated)	Interventional	2009-11-30	Recruiting
Adjunctive Effect of Topical Sulfasalazine for Oral Lichen Planus Management: A Randomized Clinical Trial[NCT06060301]	Phase 3	46 participants (Actual)	Interventional	2023-03-01	Active, not recruiting
An Open Label Non-randomized Study To Characterize The Steady State Pharmacokinetics Of Sulfasalazine Delayed Release Tablets In Children With Juvenile Idiopathic Arthritis[NCT00637780]	Phase 4	2 participants (Actual)	Interventional	2010-06-30	Terminated(stopped due to Study terminated on 13 April 2016 for business reasons. No safety and/or efficacy concerns contributed to the termination of the study)
Multicenter, Open Label, Phase IIIb Study to Evaluate the Safety and Tolerability of Subcutaneous Tocilizumab as Monotherapy and/or in Combination With Methotrexate or Other Non-Biologic Disease-Modifying Antirheumatic Drugs in Patients With Rheumatoid Ar[NCT01941095]	Phase 3	100 participants (Actual)	Interventional	2013-11-20	Completed
Methotrexate, Blood Pressure and Arterial Function in Rheumatoid Arthritis[NCT03254589]	Phase 4	124 participants (Anticipated)	Interventional	2017-10-01	Recruiting
Anti-TNF Therapy and Nerve Conduction Studies in Patients With Ankylosing Spondylitis[NCT04943237]		60 participants (Actual)	Observational	2019-07-01	Completed
Comparison of Infliximab With Sulfasalazine/Hydroxychloroquine Initiated After Methotrexate by Rheumatoid Arthritis Patients Treated in Clinical Practice (Real-World Emulation of SWEFOT Trial)[NCT05051137]		509 participants (Actual)	Observational	2006-01-12	Completed
A Randomized, Double-blind, Parallel, Placebo-controlled Study Assessing the Efficacy and Safety of Sarilumab Added to Non-biologic DMARD Therapy in Patients With Rheumatoid Arthritis Who Are Inadequate Responders to or Intolerant of TNF-α Antagonists[NCT01709578]	Phase 3	546 participants (Actual)	Interventional	2012-10-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Disease Activity as Per Ultrasound-7 (US-7) Score

Ultrasound 7 score (US-7) Calculates ultrasound score in 7 joints using greyscale and power doppler to evaluate for disease activity (synovitis, tenosynovitis) and damage (erosions) Score minimum value= 0 Maximum value = 108 Higher score indicates worse disease (NCT02930343)
Timeframe: 12 weeks

Intervention	units on a scale (Median)
Group 1- MTX+LEF+HCQ	3.5
Group 2- MTX+SSZ+HCQ	4

Indian Health Assessment Questionnaire (iHAQ)

Indian version of Health assessment Questionnaire (iHAQ) Comprises of 12 questions relating to functional activity iHAQ score ranges from 0 to 3 (minimum 0, maximum 3) Higher scores indicate more disability (NCT02930343)
Timeframe: 12 weeks

Intervention	score on a scale (Median)
Group 1- MTX+LEF+HCQ	0.7
Group 2- MTX+SSZ+HCQ	0.5

Number of Patients Achieving Good EULAR Response at the End of 12 Weeks

"EULAR response criteria for Rheumatoid arthritis includes- estimation of DAS 28 ESR, that includes-~Tender joint count 28~Swollen joint count 28~ESR~Patient global assessment of health" (NCT02930343)
Timeframe: 12 weeks

Intervention	participants (Number)
Group 1- MTX+LEF+HCQ	40
Group 2- MTX+SSZ+HCQ	37

Number of Participants With Adverse Drug Reactions

Infections, transaminitis, nausea, vomiting, derranged renal function tests etc (NCT02930343)
Timeframe: 24 weeks

Intervention	Participants (Count of Participants)
	Total number of any adverse events	Serious adverse events	Any gastrointestinal adverse reaction	Nausea	Diarrhea	Switch to parenteral Methotrexate	Raised liver enzymes > 2 times upper limit normal	Herpes labialis	upper respiratory tract infection	urinary tract infection	Hypertension	hairfall	Cytopenia
Group 1- MTX+LEF+HCQ	15	0	11	4	1	5	1	0	5	1	1	2	0
Group 2- MTX+SSZ+HCQ	21	0	16	6	1	14	1	2	5	0	0	2	0

Mean 48-week Change in DAS28

"Average difference between 48-week and Baseline DAS28.~The Disease Activity Score for 28 Joints (DAS28) is a well-validated composite outcome measure ranging from 2-10 (higher scores indicating more disease) that incorporates a tender and swollen joint count of 28 joints, a laboratory measure of systemic inflammation (ESR) and a patient-reported general assessment of health on a visual analog scale (ranging from 0-10cm) all into one measure.~Low disease activity is defined as DAS28 ≤ 3.2 units." (NCT00405275)
Timeframe: 48 weeks after baseline assessment

Intervention	units on a scale (Mean)
Triple	-2.12
Etanercept	-2.29

Change From Baseline in Rheumatoid Arthritis Impact of Disease Total Score at Week 24

RAID was a participant reported outcome measure used to evaluate the impact of RA on participant's quality of life which comprised 7 domains: • pain, • function, • fatigue, • physical and psychological well-being, • sleep disturbance, and • coping. Each domain was a single question scored on a 0 to 10 continuous NRS. The values for each of these domains were weighed by participant assessment of relative importance and combined in a single value. Total RAID score range was 0 (not affected, very good) to 10 (most affected), where higher value indicated worse status. (NCT03449758)
Timeframe: Baseline, Week 24

Intervention	score on a scale (Mean)
Sarilumab	-2.4

Change From Baseline in Clinical Disease Activity Index Total Score at Weeks 4, 12, and 24

CDAI was a composite index constructed to measure clinical remission in RA that does not include a laboratory test, and is a numerical summation of 4 components: SJC (28 joints), TJC (28 joints), participant's global disease activity (in cm), and physician's global assessment of disease (in cm). CDAI total score ranges from 0 to 76 with a lower score indicating less disease activity. A CDAI score of <=2.8 represents clinical remission and a score of <=10.0 represents LDA. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-9.8	-12.2	-14.6

Change From Baseline in Disease Activity Score-28 for Rheumatoid Arthritis With Erythrocyte Sedimentation Rate at Weeks 4, 12, and 24

DAS28-ESR was a composite score that included 4 variables: TJC (based on 28 joints); SJC (based on 28 joints); participant's global assessment of health activity using 100 mm VAS: range 0 (no pain) to 100 (maximum pain imaginable); marker of inflammation assessed by ESR in mm/h. DAS28-ESR total score ranged from 0-10, higher score indicated more disease activity. The DAS28-ESR score provided a number indicating the current disease activity of the RA. A DAS28-ESR score above 5.1 indicated high disease activity, DAS28-ESR score <= 3.2 indicated LDA, > 3.2 to <=5.1 implied moderate disease activity and DAS28-ESR score below 2.6 indicated disease remission. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-1.8	-2.3	-2.7

Change From Baseline in Duration of Morning Stiffness at Weeks 4, 12, and 24

Duration of morning stiffness was defined as the time elapsed (in minutes) between the time of usual awakening (even if not in the morning) and the time the participant was able to resume normal activities without stiffness. At each specified time point, duration of morning stiffness was reported by the participant during the visit. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	minutes (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-39.9	-47.9	-52.8

Change From Baseline in Erythrocyte Sedimentation Rate at Weeks 4, 12, and 24

ESR was a laboratory test to provide non-specific measure of inflammation in the body. The test assessed the rate at which red blood cells fell in a test tube and was measured in mm/h. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	mm/h (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-18.1	-19.5	-22.0

Change From Baseline in Functional Assessment of Chronic Illness Therapy - Fatigue Total Scores at Weeks 4, 12 and 24

FACIT-F was a 13-item questionnaire that assess fatigue in participants under chronic illness therapy. Participants scored each item on a 5-point Likert scale ranged from 0 to 4 (0 = not at all; 1 = a little bit; 2 = somewhat; 3 = quite a bit; 4 = very much). The scores of each item were reversed during score calculations, so that higher score values indicated more favorable conditions. Total score was the sum of score from each item and resulted in a score range from 0 to 52, with higher score indicated better participant health status (lower level of fatigue). (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-4.8	-6.4	-7.6

Change From Baseline in Hospital Anxiety and Depression Scale: Anxiety (HADS-A) and Depression (HADS-D) Subscale Scores at Weeks 4, 12 and 24

HADS questionnaire measures the presence and severity of anxiety and depression in both hospital and community settings. The questionnaire comprised of 14 items divided into 2 subscales: 7 items for anxiety subscale (HADS-A) and 7 items for depression subscale (HADS-D). Each item was scored on a 0 to 3 rating scale. The anxiety and depression subscales each ranged from 0 to 21 (0-7: normal, 8-10: borderline abnormal and 11-21: abnormal), where higher scores indicated greater severity of anxiety/depression. The subscales were independent for each result of depression and anxiety. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	HADS-A: Week 4	HADS-A: Week 12	HADS-A: Week 24	HADS-D: Week 4	HADS-D: Week 12	HADS-D: Week 24
Sarilumab	-1.0	-2.1	-1.9	-0.4	-1.2	-1.7

Change From Baseline in International Physical Activity Questionnaire Total Score at Weeks 4, 12 and 24

IPAQ was a 27-item self-reported questionnaire designed to measure physical activity of participant. The score was reported in MET minutes per week. MET minutes represented the amount of energy expended to carry out physical activity. For IPAQ total score, the minimum value is zero and there is no maximum. Higher scores mean better levels of physical activity. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	MET minutes per week (Mean)
	Week 4	Week 12	Week 24
Sarilumab	175.6	533.4	382.0

Change From Baseline in Multidimensional Assessment of Thymic States Scale Total Score at Weeks 4, 12 and 24

MAThyS was a multi-dimensional self-administered questionnaire comprised of five dimensions (emotional reactivity, cognition speed, psychomotor function, motivation and sensory perception) divided into 20 items relating to individual states as perceived by participants for the preceding week (at each specified Week). Each item was measured on a VAS (in cm) ranging from 0 (inhibition of the state evaluated by the item) to 10 (excitation for the evaluated state). Total MAThyS score was sum of the 20 items and that might vary from score range 0 to 200 with lower scores indicated general inhibition and higher scores indicated general excitation. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	cm (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-0.2	2.9	-1.1

Change From Baseline in Number of Swelling Joints at Weeks 4, 12, and 24

Number of joints with swelling are reported. Joints which were assessed included 28 joints (which included shoulders, elbows, wrists, knees and 2 joints in each finger and thumb). (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	joints (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-3.9	-4.1	-4.7

Change From Baseline in Number of Tender Joints at Weeks 4, 12, and 24

Number of joints with tenderness are reported. Joints which were assessed included 28 joints (which included shoulders, elbows, wrists, knees and 2 joints in each finger and thumb). (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	joints (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-2.5	-3.7	-4.8

Change From Baseline in Patient Global Assessment of Disease Activity Score by Visual Analog Scale at Weeks 4, 12, and 24

PtGA of disease activity was measured using a 100 mm horizontal VAS ranged from 0=no pain to 100=maximum pain imaginable, where higher score indicated more disease activity. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	mm (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-17.2	-24.3	-26.7

Change From Baseline in Rheumatoid Arthritis Impact of Disease Total Score at Weeks 4 and 12

RAID was a participant reported outcome measure used to evaluate the impact of RA on participant's quality of life which comprised 7 domains: • pain, • function, • fatigue, • physical and psychological wellbeing, • sleep disturbance, and • coping. Each domain was a single question scored on a 0 to 10 continuous NRS. The values for each of these domains were weighed by participant assessment of relative importance and combined in a single value. Total RAID score range was 0 (not affected, very good) to 10 (most affected), where higher value indicated worse status. (NCT03449758)
Timeframe: Baseline, Weeks 4 and 12

Intervention	score on a scale (Mean)
	Week 4	Week 12
Sarilumab	-1.2	-1.8

Change From Baseline in Stanford Health Assessment Questionnaire Disability Index Total Score at Weeks 4, 12 and 24

HAQ-DI was a participant-oriented questionnaire developed specifically to assess the extent of a RA participant's functional ability. It consisted of at least 2 or 3 questions per category, participant reported assessment of ability to perform tasks in 8 categories of daily living activities: dress/groom; arise; eat; walk; reach; grip; hygiene; and common activities over past week (at each specified visit) rated on a 4-point scale where 0 = no difficulty; 1 = some difficulty; 2 = much difficulty; 3 = unable to do. Overall score was computed as the sum of category scores and divided by the number of categories answered, and ranged from 0 to 3, where 0 = no disability and 3 = completely disabled, higher score indicated more disability. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Week 4	Week 12	Week 24
Sarilumab	-0.2	-0.4	-0.5

Clinical Disease Activity Index (CDAI) Total Score at Baseline, Weeks 4, 12, and 24

Intervention	score on a scale (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	22.5	12.6	9.9	8.1

Disease Activity Score-28 for Rheumatoid Arthritis With Erythrocyte Sedimentation Rate (DAS28-ESR) at Baseline, Weeks 4, 12, and 24

DAS28-ESR was a composite score that included 4 variables: tender joint count (TJC) (based on 28 joints); swollen joint count (SJC) (based on 28 joints); participant's global assessment of health activity using 100 mm VAS: range 0 (no pain) to 100 (maximum pain imaginable); marker of inflammation assessed by ESR in mm/h. DAS28-ESR total score ranged from 0-10, higher score indicated more disease activity. The DAS28-ESR score provided a number indicating the current disease activity of the RA. A DAS28-ESR score above 5.1 indicated high disease activity, DAS28-ESR score less than or equal to (<=) 3.2 indicated low disease activity (LDA), greater than (>) 3.2 to <=5.1 implied moderate disease activity and DAS28-ESR score below 2.6 indicated disease remission. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	5.0	3.1	2.6	2.3

Duration of Morning Stiffness at Baseline, Weeks 4, 12, and 24

Intervention	minutes (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	72.3	34.7	28.9	21.3

Erythrocyte Sedimentation Rate (ESR) at Baseline, Weeks 4, 12, and 24

ESR was a laboratory test to provide non-specific measure of inflammation in the body. The test assessed the rate at which red blood cells fell in a test tube and was measured in millimeter per hour (mm/h). (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	mm/h (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	28.8	10.5	9.2	8.4

Functional Assessment of Chronic Illness Therapy - Fatigue (FACIT-F) Total Scores at Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	25.5	21.0	18.8	17.9

Hospital Anxiety and Depression Scale (HADS): Anxiety (HADS-A) and Depression (HADS-D) Subscale Scores at Baseline, Weeks 4, 12, and 24

Intervention	score on a scale (Mean)
	HADS-A: Baseline	HADS-A: Week 4	HADS-A: Week 12	HADS-A: Week 24	HADS-D: Baseline	HADS-D: Week 4	HADS-D: Week 12	HADS-D: Week 24
Sarilumab	8.1	7.2	6.1	6.6	7.0	6.6	5.7	5.5

International Physical Activity Questionnaire (IPAQ) Total Score at Baseline, Weeks 4, 12 and 24

IPAQ was a 27-item self-reported questionnaire designed to measure physical activity of participant. The score was reported in metabolic equivalent (MET)-minutes per week. MET minutes represented the amount of energy expended to carry out physical activity. For IPAQ total score, the minimum value is zero and there is no maximum. Higher scores mean better levels of physical activity. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	MET minutes per week (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	1759.9	1881.1	2061.0	2089.5

Multidimensional Assessment of Thymic States (MAThyS) Scale Total Score at Baseline, Weeks 4, 12 and 24

MAThyS was a multi-dimensional self-administered questionnaire comprised of five dimensions (emotional reactivity, cognition speed, psychomotor function, motivation and sensory perception) divided into 20 items relating to individual states as perceived by participants for the preceding week (at each specified Week). Each item was measured on a visual analog scale (VAS; in centimeters [cm]) ranged from 0 (inhibition of the state evaluated by the item) to 10 (excitation for the evaluated state). Total MAThyS score was sum of the 20 items and that might vary from score range 0 to 200 with lower scores indicated general inhibition and higher scores indicated general excitation. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	cm (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	88.4	89.6	94.8	90.9

Number of Participants Achieving Clinical Disease Activity Index: Low Disease Activity (CDAI Score <=10.0) and Remission (CDAI Score <=2.8) Weeks 12, and 24

CDAI was a composite index constructed to measure clinical remission in RA that does not included a laboratory test, and is a numerical summation of 4 components: SJC (28 joints), TJC (28 joints), participant's global disease activity (in cm), and physician's global assessment (in cm). Total score ranged from 0 to 76 with a lower score indicated less disease activity. A CDAI score of <=2.8 represents clinical remission and a score of <=10.0 represents LDA. (NCT03449758)
Timeframe: Weeks 12 and 24

Intervention	Participants (Count of Participants)
	LDA: Week 12	LDA: Week 24	Remission: Week 12	Remission: Week 24
Sarilumab	29	29	18	20

Number of Participants Achieving Low Disease Activity (DAS28 ESR Score <=3.2) and Remission (DAS28 ESR Score <2.6) at Weeks 12, and 24

DAS28-ESR was a composite score that included 4 variables: TJC (based on 28 joints); SJC (based on 28 joints); participant's global assessment of health activity using 100 mm VAS: range 0 (no pain) to 100 (maximum pain imaginable) marker of inflammation assessed by ESR in mm/h. DAS28-ESR total score ranged from 0-10, higher score indicated more disease activity. The DAS28-ESR score provided a number indicating the current disease activity of the RA. A DAS28-ESR score above 5.1 indicated high disease activity, DAS28-ESR score <= 3.2 indicated LDA, > 3.2 to <=5.1 implied moderate disease activity and DAS28-ESR score below 2.6 indicated disease remission. (NCT03449758)
Timeframe: Weeks 12 and 24

Intervention	Participants (Count of Participants)
	LDA: Week 12	LDA: Week 24	Remission: Week 12	Remission: Week 24
Sarilumab	12	4	40	45

Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant who received study drug and did not necessarily had a causal relationship with the study treatment. SAE: Any untoward medical occurrence that resulted in any of the following outcomes: death, life-threatening, required initial or prolonged in-patient hospitalization, persistent or significant disability/incapacity, congenital anomaly/birth defect, or considered as medically important event. TEAEs were defined as AEs that occurred in the time from the first injection of study drug up to 39.7 weeks. (NCT03449758)
Timeframe: Baseline up to end of study (up to 39.7 weeks)

Intervention	Participants (Count of Participants)
	SAE	TEAE	AE leading to death
Sarilumab	10	76	0

Number of Swollen Joints at Baseline, Weeks 4, 12, and 24

Intervention	joints (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	6.3	2.5	1.9	1.6

Number of Tender Joints at Baseline, Weeks 4, 12, and 24

Intervention	joints (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	7.3	4.7	3.5	2.5

Patient Global Assessment (PtGA) of Disease Activity Score by Visual Analog Scale (VAS) at Baseline, Weeks 4, 12 and 24

PtGA of disease activity was measured using a 100 millimeters (mm) horizontal VAS ranged from 0=no pain to 100=maximum pain imaginable, where higher score indicated more disease activity. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	mm (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	61.1	44.1	36.6	34.6

Rheumatoid Arthritis Impact of Disease Total Score at Baseline, Weeks 4, 12 and 24

RAID was a participant reported outcome measure used to evaluate the impact of RA on participant's quality of life which comprised 7 domains: • pain, • function, • fatigue, • physical and psychological well-being, • sleep disturbances, and • coping. Each domain was a single question scored on a 0 to 10 continuous NRS. The values for each of these domains were weighed by participant assessment of relative importance and combined in a single value. Total RAID score range was 0 (not affected, very good) to 10 (most affected), where higher value indicated worse status. (NCT03449758)
Timeframe: Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Week 4	Week 12	Week 24
Sarilumab	4.6	3.9	3.3

Stanford Health Assessment Questionnaire Disability Index (HAQ-DI) Total Score at Baseline, Weeks 4, 12 and 24

Intervention	score on a scale (Mean)
	Baseline	Week 4	Week 12	Week 24
Sarilumab	1.3	1.1	0.8	0.8

Disease Activity Score Erythrocyte Sedimentation Rate(DAS28-ESR)

"Outcome measured was the observed-group analysis of the DAS28-ESR between weeks 48 and 102. DAS28 is a calculated scale using a formula that includes the number of tender joints and swollen joints (28 joints maximum). The following is the calculation: DAS28 = 0.56 * sqrt(tender28) + 0.28 * sqrt(swollen28) + 0.70 * ln(ESR) + 0.014 * GH. The ESR is the rate at which red blood cells sediment in a period of one hour.~The total range for the DAS28ESR goes from 0.0 to 9.2; this indicates the current activity of the rheumatoid arthritis of a subject. A DAS28 above 5.1 means high disease activity whereas a DAS28 below 3.2 indicates low disease activity." (NCT00259610)
Timeframe: Change of the Mean of DAS28-ESR between weeks 48 - 102.

Intervention	Scores on a scale (Mean)
MTX + Immediate Etanercept	3.0
MTX+ Immediate SSZ +HCQ	2.9
MTX + Step-up Etanercept	3.1
MTX + Step-up SSZ + HCQ(ST)	2.8

Radiographic Disease Progression Between Baseline and Week 102 as Assessed by Van Der Heijde Modified Sharp Scores.

Changes in disease progression between treatment groups will be described by the mean score at two years as assessed after adjustment for the baseline radiographic score. Radiographs were observed of hands, wrists, and feet. The range of scores available for the modified Sharp Score is 0 to 448. The erosion score per joint of the hands can range from 0 to 5. The maximal erosion score for each hand is thus 80, considering the 16 areas for erosions per hand. Joint space narrowing and joint subluxation or luxation are combined in a single score with a range of 0 to 4 with a max score of 60. The erosion score per joint can range from 0 to 10, with each side of the joint independently scored from 0 to 5. The maximal erosion score per foot is thus 60. The joint space narrowing and joint (sub)luxation are combined in a single score with a range of 0 to 4. The maximal narrowing/(sub)luxation score per foot is thus 24. (NCT00259610)
Timeframe: Year 2, Week 102

Intervention	Scores on a scale (Mean)
MTX + Immediate Etanercept	7.0
MTX+ Immediate SSZ +HCQ	7.3
MTX + Step-up Etanercept	4.8
MTX + Step-up SSZ + HCQ(ST)	6.2

Change From Baseline at Week 52 in Disease Activity Score for 28 Joints Based on C-Reactive Protein (DAS28-CRP)

DAS28-CRP is a composite score that contains 4 variables: TJC (based on 28 joints), SJC (based on 28 joints), participant's assessment of general health on VAS (range 0 [very well] to 100 mm [extremely bad]) and CRP (mg/L). DAS28-CRP total score ranges from 2-10 with a lower score indicating less disease activity. A DAS28-CRP above 5.1 indicates high disease activity, whereas below 3.2 indicates low disease activity and below 2.6 as disease remission. (NCT02373202)
Timeframe: Baseline, Week 52

Intervention	units on a scale (Mean)
Sarilumab 150 mg q2w + DMARDs	-2.90
Sarilumab 200 mg q2w + DMARDs	-2.47
Sarilumab 150 mg q2w	-2.62
Sarilumab 200 mg q2w	-2.64

Change From Baseline in Health Assessment Questionnaire-Disability Index (HAQ-DI) Score at Week 52

HAQ-DI assessed the degree of difficulty participants experienced in 8 daily living activity domains during a week: dressing/grooming, arising, eating, walking, hygiene, reach, grip, and other activities. Each activity category consisted of 2-3 items. Each items's difficulty was scored from 0-3 (0=no difficulty, 1=some difficulty, 2=much difficulty, 3=unable to do). Overall HAQ-DI score was computed as the sum of domain scores divided by the number of domains answered, providing a score from 0-3. Low scores denoted improvement of disability/lower degree of domain difficulty. (NCT02373202)
Timeframe: Baseline, Week 52

Intervention	units on a scale (Mean)
Sarilumab 150 mg q2w + DMARDs	-0.52
Sarilumab 200 mg q2w + DMARDs	-0.34
Sarilumab 150 mg q2w	-0.48
Sarilumab 200 mg q2w	-0.38

Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Abnormalities

"Criteria for potentially clinically significant ECG abnormalities:~PR Interval: >200 milliseconds (ms); >200 ms and IFB >=25%; >220 ms; >220 ms and IFB >=25%; >240 ms; >240 ms and IFB >=25%~QRS Interval: >110 ms; >110 ms and IFB >=25%; >120 ms; >120 ms and IFB >=25%~QT Interval: >500 ms~QTc Bazett (QTc B): >450 ms; >480 ms; >500 ms; IFB >30 and <=60 ms, IFB >60 ms~QTc Fridericia (QTc F): >450 ms; >480 ms; >500 ms; IFB >30 and <=60 ms; IFB >60 ms" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	PR >200 ms	PR >200 ms and IFB >=25%	PR >220 ms	PR >220 ms and IFB >=25%	PR >240 ms	PR >240 ms and IFB >=25%	QRS >110 ms	QRS >110 ms and IFB >=25%	QRS >120 ms	QRS >120 ms and IFB >=25%	QT >500 ms	QTc B >450 ms	QTc B >480 ms	QTc B >500 ms	QTc B IFB >30 and <=60 ms	QTc B IFB >60 ms	QTc F >450 ms	QTc F >480 ms	QTc F >500 ms	QTc F IFB >30 and <=60 ms	QTc F IFB >60 ms
Sarilumab 150 mg q2w	0	0	0	0	0	0	0	0	0	0	0	6	0	0	2	0	2	0	0	0	0
Sarilumab 150 mg q2w + DMARDs	0	0	0	0	0	0	0	0	0	0	0	2	0	0	0	0	2	0	0	0	0
Sarilumab 200 mg q2w	1	0	1	0	0	0	1	0	0	0	1	10	1	0	1	0	6	1	0	0	0
Sarilumab 200 mg q2w + DMARDs	0	0	0	0	0	0	2	0	2	0	0	1	1	0	1	0	1	0	0	0	0

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Electrolytes

"Criteria for potentially clinically significant abnormalities:~Sodium: <=129 mmol/L; >=160 mmol/L~Potassium: <3 mmol/L; >=5.5 mmol/L~Chloride: <80 mmol/L; >115 mmol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	Sodium <=129 mmol/L	Sodium >=160 mmol/L	Potassium <3 mmol/L	Potassium >=5.5 mmol/L	Chloride <80 mmol/L	Chloride >115 mmol/L
Sarilumab 150 mg q2w	0	0	0	0	0	0
Sarilumab 150 mg q2w + DMARDs	0	0	0	0	0	0
Sarilumab 200 mg q2w	0	0	0	0	0	0
Sarilumab 200 mg q2w + DMARDs	0	0	0	0	0	0

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Hematological Parameters

"Criteria for potentially clinically significant abnormalities:~Hemoglobin: <=115 g/L (Male[M]) or <=95 g/L (Female[F]); >=185 g/L (M) or >=165 g/L (F); DFB >=20 g/L~Hematocrit: <=0.37 v/v (M) or <=0.32 v/v (F); >=0.55 v/v (M) or >=0.5 v/v (F)~Red blood cells (RBC): >=6 Tera/L~Platelets: <50 Giga/L; >=50 and <100 Giga/L; >=700 Giga/L~White blood cells (WBC): <3.0 Giga/L (Non-Black [NB]) or <2.0 Giga/L (Black [B]); >=16.0 Giga/L~Neutrophils: <1.5 Giga/L (NB) or <1.0 Giga/L (B); <1.0 Giga/L~Lymphocytes: <0.5 Giga/L; >=0.5 Giga/L and 4.0 Giga/L~Monocytes: >0.7 Giga/L~Basophils: >0.1 Giga/L~Eosinophils: >0.5 Giga/L or >upper limit of normal (ULN) (if ULN >=0.5 Giga/L)" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	Hemoglobin <=115 g/L (M) or <=95 g/L (F)	Hemoglobin >=185 g/L (M) or >=165 g/L (F)	Hemoglobin DFB >=20 g/L	Hematocrit <=0.37 v/v (M) or <=0.32 v/v (F)	Hematocrit >0.55 v/v (M) or >=0.5 v/v (F)	RBC >=6 Tera/L	Platelets <50 Giga/L	Platelets >=50 and <100 Giga/L	Platelets >=700 Giga/L	WBC <3.0 Giga/L (NB) or <2.0 Giga/L (B)	WBC >=16.0 Giga/L	Neutrophils <1.5 Giga/L (NB) or <1.0 Giga/L (B)	Neutrophils <1.0 Giga/L	Lymphocytes <0.5 Giga/L	Lymphocytes >=0.5 Giga/L and	Lymphocytes >4.0 Giga/L	Monocytes >0.7 Giga/L	Basophils >0.1 Giga/L	Eosinophils >0.5 Giga/L or >ULN (ULN >=0.5 Giga/L)
Sarilumab 150 mg q2w	1	0	0	2	0	0	0	1	0	7	0	8	2	0	3	0	3	0	2
Sarilumab 150 mg q2w + DMARDs	0	0	0	0	0	0	0	1	0	6	0	8	5	0	3	0	1	1	0
Sarilumab 200 mg q2w	3	0	2	6	0	0	0	0	0	9	0	13	4	1	8	0	2	5	2
Sarilumab 200 mg q2w + DMARDs	1	0	0	3	0	0	0	1	0	9	0	11	3	0	4	1	0	0	0

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Liver Function Parameters

"Criteria for potentially clinically significant abnormalities:~Alanine Aminotransferase (ALT): >1 ULN and <=1.5 ULN; >1.5 ULN and <=3 ULN; >3 ULN and <=5 ULN; >5 ULN and <=10 ULN; >10 ULN and <=20 ULN; >20 ULN~Aspartate aminotransferase (AST): >1 ULN and <=1.5 ULN; >1.5 ULN and <=3 ULN; >3 ULN and <=5 ULN; >5 ULN and <=10 ULN; >10 ULN and <=20 ULN; >20 ULN~Alkaline phosphatase: >1.5 ULN~Total bilirubin (TBILI): >1.5 ULN; >2 ULN~Conjugated bilirubin(CBILI): >1.5 ULN~Unconjugated bilirubin: >1.5 ULN~ALT >3 ULN and TBILI >2 ULN~CBILI >35% TBILI and TBILI >1.5 ULN~Albumin: <=25 g/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	ALT >1 ULN and <=1.5 ULN	ALT >1.5 ULN and <=3 ULN	ALT >3 ULN and <=5 ULN	ALT >5 ULN and <=10 ULN	ALT >10 ULN and <=20 ULN	ALT >20 ULN	AST >1 ULN and <=1.5 ULN	AST >1.5 ULN and <=3 ULN	AST >3 ULN and <=5 ULN	AST >5 ULN and <=10 ULN	AST >10 ULN and <=20 ULN	AST >20 ULN	Alkaline Phosphatase >1.5 ULN	TBILI >1.5 ULN	TBILI >2 ULN	CBILI >1.5 ULN	Unconjugated Bilirubin >1.5 ULN	ALT> 3 ULN and TBILI >2ULN	CBILI >35% TBILI and TBILI >1.5 ULN	Albumin <=25 g/L
Sarilumab 150 mg q2w	7	3	1	0	0	0	8	2	0	0	0	0	0	0	0	0	0	0	0	0
Sarilumab 150 mg q2w + DMARDs	3	2	1	1	0	0	6	1	1	0	0	0	0	1	0	0	0	0	0	0
Sarilumab 200 mg q2w	6	2	4	0	0	0	4	3	1	0	0	0	0	0	0	0	0	0	0	0
Sarilumab 200 mg q2w + DMARDs	4	1	0	0	0	0	5	0	0	0	0	0	0	1	0	0	0	0	0	0

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Metabolic Parameters

"Criteria for potentially clinically significant abnormalities:~Glucose: <=3.9 mmol/L and =11.1 mmol/L (unfasted [unfas]) or >=7 mmol/L (fasted [fas])~Hemoglobin A1c (HbA1c): >8%~Total cholesterol: >=6.2 mmol/L; >=7.74 mmol/L~LDL cholesterol: >=4.1 mmol/L; >=4.9 mmol/L~Triglycerides: >=4.6 mmol/L; >=5.6 mmol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	Glucose <=3.9 mmol/L and	Glucose >=11.1 mmol/L (unfas) or >=7 mmol/L (fas)	HbA1c >8%	Total Cholesterol >=6.2 mmol/L	Total Cholesterol >=7.74 mmol/L	LDL Cholesterol >=4.1 mmol/L	LDL Cholesterol >=4.9 mmol/L	Triglycerides >=4.6 mmol/L	Triglycerides >=5.6 mmol/L
Sarilumab 150 mg q2w	1	0	0	12	1	6	2	0	0
Sarilumab 150 mg q2w + DMARDs	0	0	0	6	1	1	0	0	0
Sarilumab 200 mg q2w	1	2	1	13	2	3	1	1	1
Sarilumab 200 mg q2w + DMARDs	0	1	0	7	1	3	1	0	0

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Renal Function Parameters

"Criteria for potentially clinically significant abnormalities:~Creatinine: >=150 micromol/L (adults); >=30% change from baseline, >=100% change from baseline~Creatinine clearance: <15 mL/min; >=15 to <30 mL/min; >=30 to <60 mL/min; >=60 to <90 mL/min~Blood urea nitrogen: >=17 mmol/L~Uric acid: <120 micromol/L; >408 micromol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	Creatinine >=150 micromol/L (Adults)	Creatinine >=30% change from baseline	Creatinine >=100% change from baseline	Creatinine Clearance <15 mL/min	Creatinine clearance >=15 to <30 mL/min	Creatinine clearance >=30 to <60 mL/min	Creatinine clearance >=60 to <90 mL/min	Blood Urea Nitrogen >=17 mmol/L	Uric acid <120 micromol/L	Uric acid >408 micromol/L
Sarilumab 150 mg q2w	0	6	0	0	0	6	15	0	0	2
Sarilumab 150 mg q2w + DMARDs	0	3	0	0	0	6	8	0	0	1
Sarilumab 200 mg q2w	1	5	0	0	0	5	17	0	0	4
Sarilumab 200 mg q2w + DMARDs	0	3	0	0	0	6	7	0	1	1

Number of Participants With Potentially Clinically Significant Vital Signs Abnormalities

"Criteria for potentially clinically significant vital sign abnormalities:~Systolic blood pressure (SBP) supine: <=95 mmHg and decrease from baseline (DFB) >=20 mmHg; >=160 mmHg and increase from baseline (IFB) >=20 mmHg~Diastolic blood pressure (DBP) supine: <=45 mmHg and DFB >=10 mmHg; >=110 mmHg and IFB ≥10 mmHg~SBP (Orthostatic): <=-20 mmHg~DBP (Orthostatic): <=-10 mmHg~Heart rate (HR) supine: <=50 beats per minute (bpm) and DFB >=20 bpm; >=120 bpm and IFB >=20 bpm~Weight: >=5% DFB; >=5% IFB" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	SBP (supine) <=95 mmHg and DFB >=20 mmHg	SBP (supine) >=160 mmHg and IFB >=20 mmHg	DBP (supine) <=45 mmHg and DFB >=10 mmHg	DBP (supine) >=110 mmHg and IFB >=10 mmHg	SBP (orthostatic) <=-20 mmHg	DBP (orthostatic) <=-10 mmHg	HR (supine) <=50 bpm and DFB >= 20 bpm	HR (supine) >=120 bpm and IFB >=20 bpm	Weight >=5% DFB	Weight >=5% IFB
Sarilumab 150 mg q2w	0	1	0	0	5	5	1	0	2	12
Sarilumab 150 mg q2w + DMARDs	0	1	0	0	8	3	0	0	1	3
Sarilumab 200 mg q2w	0	1	0	0	9	10	1	0	0	7
Sarilumab 200 mg q2w + DMARDs	0	1	0	0	5	3	0	0	1	2

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

Adverse event (AE) was defined as any untoward medical occurrence in a participant who received IMP and did not necessary have to had a causal relationship with treatment. All AEs that occurred from the first dose of the IMP administration up to 6 weeks after last dose of treatment (up to Week 58) were considered as TEAEs. SAEs were AEs resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly or a medically important event. TEAEs included both SAEs and non-SAEs. (NCT02373202)
Timeframe: Baseline up to Week 58

,,,

Intervention	participants (Number)
	Any TEAE	SAE
Sarilumab 150 mg q2w	25	1
Sarilumab 150 mg q2w + DMARDs	14	0
Sarilumab 200 mg q2w	28	2
Sarilumab 200 mg q2w + DMARDs	13	3

Percentage of Participants Achieving American College of Rheumatology (ACR) 20, 50 and 70 Responses at Week 52

ACR response is a composite rating scale that includes 7 variables: tender joints count (TJC [68 joints]); swollen joints count (SJC [66 joints]); levels of an acute phase reactant (high sensitivity C-reactive protein [hs-CRP level]); participant's assessment of pain (measured on 0 [no pain]-100 mm [worst pain] visual analog scale [VAS]); participant's global assessment of disease activity (measured on 0 [no arthritis activity]-100 mm [maximal arthritis activity] VAS); physician's global assessment of disease activity (measured on 0 [no arthritis activity]-100 mm [maximal arthritis activity] VAS); participant's assessment of physical function (measured by Health Assessment Question-Disability Index [HAQ-DI], with scoring range of 0 [better health] - 3 [worst health]). ACR20/50/70 response is defined as at least 20/50/70% improvement in both TJC and SJC, and at least 20/50/70% improvement in at least 3 of the 5 other assessments, respectively. (NCT02373202)
Timeframe: Week 52

,,,

Intervention	percentage of participants (Number)
	ACR20	ACR50	ACR70
Sarilumab 150 mg q2w	76.7	56.7	26.7
Sarilumab 150 mg q2w + DMARDs	73.3	60.0	53.3
Sarilumab 200 mg q2w	74.2	54.8	25.8
Sarilumab 200 mg q2w + DMARDs	40.0	33.3	26.7

Measuring the Safety and Efficacy of a New DMARD, Leflunomide Alone or in Combination With Traditional DMARD's. Participants Reaching ACR 20 Response. at 48 Weeks

"The combination of Methotrexate-Sulfasalazine-Hydroxychloroquine has been shown to be more effective than Methotrexate alone or the double combination of Methotrexate-Hydroxychloroquine. Primary outcome is ACR 20 response at 48 weeks.~An ACR 20 Response is a measure of at least 20% improvement in the number of tender and swollen joints. and a 20% improvement in at least 3 of the following:~the patient's global assessment of disease status; the patient's assessment of pain; the patient's assessment of function; the physician's global assessment of disease status; serum C-reactive protein levels." (NCT00579878)
Timeframe: 48 weeks

Intervention	Participants (Count of Participants)
1 Leflunomide Alone vs Combination Therapy	8
Methotrexate-Sulfasalazine-Hydroxychloroquine	20
Leflunomide-Sulfasalazine-Hydroxychloroquine	12

Change From Baseline in Adjusted Mean of American College of Rheumatology Response (ACR-N) Area Under Curve (AUC) Over 16 Weeks

"ACR-N = the lowest of 3 values (percent change in the number of swollen joints, percent change in the number of tender joints, and median of the other 5 measures in the ACR core data set). Negative numbers indicate worsening.~The ACR-N AUC was calculated using the trapezoidal rule as the ACR-N multiplied by the duration of the assessment period (in weeks) and was presented as %-weeks." (NCT00422227)
Timeframe: 16 weeks

Intervention	Units on a scale (Mean)
ETN/MTX	434.83
DMARD/MTX	289.54

Percent Change From Baseline in DAS28 at Week 16

Disease Activity Score 28 based on 28 Joints (DAS28) is the calculation of DAS28: DAS28 = 0.56 sqrt (28 painful joint count) + 0.28 sqrt (28 swollen joint count) + 0.70 (ln erythrocyte sedimentation rate (ESR)) + 0.014 (General Health) (GH). GH = Subject general health visual analog scale (0-10 mm). (NCT00422227)
Timeframe: Week 16

Intervention	Percent change (Number)
ETN/MTX	38.32
DMARD/MTX	27.46

Percentage of Participants Achieving European League Against Rheumatism (EULAR) Moderate or Good Response

EULAR Response Criteria DAS28) improvement at week 16. Good response was defined as >1.2 improvement in DAS from Baseline and DAS attained during follow-up of ≤2.4. Non-responders were participants with improvement of ≤0.6 or participants with improvement of >0.6 but ≤1.2 and DAS attained during follow-up of >3.7. Remaining participants were classified as moderate. Scores of good and moderate were considered to have therapeutic response. (NCT00422227)
Timeframe: Week 16

Intervention	Percentage of Participants (Number)
ETN/MTX	87.82
DMARD/MTX	73.79

Percent Change From Baseline in Duration (Minutes) of Morning Stiffness

The duration of morning stiffness on the day of examination should be determined by asking the following two questions: When did you awaken this morning? When were you able to resume your normal activities without stiffness? Duration of morning stiffness is equal to the time elapsed between the above two times in minutes; If none is present enter 0, If morning stiffness is still continuing, please indicate average of duration of stiffness over the past 3 days. If stiffness persists the entire day 1440 minutes (24h x 60 minutes) should be recorded. (NCT00422227)
Timeframe: Week 2, 4, 8, 12, 16

Intervention	Percent change (Number)
	Week 2	Week 4	Week 8	Week 12	Week 16
DMARD/MTX	16.43	33.22	37.35	52.76	46.77
ETN/MTX	54.92	63.85	73.41	79.76	80.55

Percent Change From Baseline in General Health, Pain, and Fatigue, Visual Analog Scales

"VAS, participant indicates by marking a vertical line at an appropriate position through a horizontal line. The length of the line measures from left (in mm) and the value (in mm) is recorded. General Health VAS, in general how would you rate your heath over the last 2-3 weeks, 0mm equals very well and 100mm equals extremely bad. Pain VAS: indicate the amount of pain experienced during the last 2-3 days, 0 mm equals no pain and 100 mm equals pain as bad as it can be. Fatigue VAS: how fatigued or tired have you been over the last week, range =No Fatigue - Extremely Fatigued." (NCT00422227)
Timeframe: Week 2, 4, 8, 12, 16

Intervention	Percent change (Number)
	General Health - Week 2	General Health - Week 4	General Health - Week 8	General Health - Week 12	General Health - Week 16	Pain - Week 2	Pain - Week 4	Pain - Week 8	Pain - Week 12	Pain - Week 16	Fatigue - Week 2	Fatigue - Week 4	Fatigue - Week 8	Fatigue - Week 12	Fatigue - Week 16
DMARD/MTX	8.88	22.78	27.86	30.26	33.89	9.99	22.98	29.14	33.97	36.45	6.63	19.00	21.82	28.65	30.04
ETN/MTX	21.14	30.61	38.57	42.10	50.49	27.59	34.73	42.97	48.46	54.42	20.90	30.87	35.92	39.65	46.92

Percent Change From Baseline in Painful and Swollen Joint Counts

Participant's assessment of pain - A horizontal pain visual analog scale (VAS) (0-100 mm) is used to assess the participants current level of pain; 0 = no pain and 100 = worst pain. Swollen joint count - ACR swollen joint count, an assessment of 28 joints. Joints are classified as either swollen or not swollen. (NCT00422227)
Timeframe: Week 2, 4, 8, 12, 16

Intervention	Percent change (Number)
	Painful Joints - Week 2	Painful Joints - Week 4	Painful Joints - Week 8	Painful Joints - Week 12	Painful Joints - Week 16	Swollen Joints - Week 2	Swollen Joints - Week 4	Swollen Joints - Week 8	Swollen Joints - Week 12	Swollen Joints - Week 16
DMARD/MTX	27.68	36.71	49.71	55.55	57.31	21.32	27.72	44.19	50.48	56.32
ETN/MTX	34.17	46.11	55.48	65.65	68.99	38.59	49.33	59.91	67.97	73.83

Percent Change From Baseline in Physician And Subject Global Assessments

The Physician Global Assessment of Disease Activity: The participant's disease activity is estimated over the last two - three days by the physician; A zero (0) means no disease activity and a ten (10) means extreme disease activity. The Subject Global Assessment of Disease Activity: The participant assesses overall arthritis activity. A zero (0) means no disease activity and a ten (10) means extreme disease activity. (NCT00422227)
Timeframe: Week 2, 4, 8, 12, 16

Intervention	Percent change (Number)
	Physician Global Assessment - Week 2	Physician Global Assessment - Week 4	Physician Global Assessment - Week 8	Physician Global Assessment - Week 12	Physician Global Assessment - Week 16	Subject Global Assessment - Week 2	Subject Global Assessment - Week 4	Subject Global Assessment - Week 8	Subject Global Assessment - Week 12	Subject Global Assessment - Week 16
DMARD/MTX	11.83	22.81	35.41	38.67	45.04	7.24	19.22	26.08	30.10	30.55
ETN/MTX	30.40	39.58	45.86	55.00	62.05	21.84	28.94	34.92	43.18	50.76

Percentage of Participants Achieving ACR 20, 50, and 70 Responses

Response includes improvement in tender or swollen joints as well as 20 percent improvement in three of the other five criteria. Required: ≥ 20%, 50% or 70% improvement in tender joint count ≥ 20% , 50% or 70% improvement in swollen joint count and at least 20%, 50%, 70% improvement in 3 of the following 5:Patient pain assessment , Patient global assessment ,Physician global assessment, Patient self-assessed disability. (NCT00422227)
Timeframe: Week 16

Intervention	Percentage of Participants (Number)
	ACR 20	ACR 50	ACR 70
DMARD/MTX	58.16	34.69	7.14
ETN/MTX	78.87	56.70	19.07

Percentage of Participants Achieving DAS28 <3.2 (Low Disease Activity) and <2.6 (Remission)

Intervention	Percentage of Participants (Number)
	Low Disease (DAS28 <3.2)	Remission (DAS28 <2.6)
DMARD/MTX	18.45	7.77
ETN/MTX	39.09	15.74

Percentage of Participants With DAS28 Improvement of ≥0.6 and ≥1.2

Disease Activity Score 28 based on 28 Joints (DAS28) is the calculation of DAS28: DAS28 = 0.56 sqrt (28 painful joint count) + 0.28 sqrt (28 swollen joint count) + 0.70 (ln erythrocyte sedimentation rate (ESR) + 0.014 (General Health) (GH). GH = Subject general health visual analog scale (0-10 mm). (NCT00422227)
Timeframe: Week 16

Intervention	Percentage of Participants (Number)
	≥0.6	≥1.2
DMARD/MTX	78.64	66.02
ETN/MTX	91.37	82.74

Percentage of Patients in Each Arm That Require Any Type of Antidiarrheal Medications.

The number of patients reporting the use of anti-diarrheal medications divided by the number of patients evaluated for this endpoint. (NCT01198145)
Timeframe: Up to 24 months post radiotherapy

Intervention	percentage of participants (Number)
Arm I: Sulfasalazine	48.7
Arm II: Placebo	28.6

"Percent of Patients in Each Arm That Recorded Yes to Each of Questions 2-10 on the Bowel Function Questionnaire"

"Questions that were used in this analysis:~2. Have you had a problem causing you to get up at night to have a bowel movement? 3. Have you had a problem causing you to lose control of your bowel movements? 4. Have you had a problem causing you to have a bowel movement within 30 minutes of a prior bowel movement? 5. Have you had to wear protective clothing or a pad in case you lost control of a bowel movement? 6. Have you had a problem causing you to be unable to tell the difference between stool and gas? 7. Have you had a problem causing you to have stools that are liquid? 1=yes 2=no q08 8. Have you found that once you feel the urge to have a bowel movement, you must do so within 15 minutes to avoid an accident? 9. Have you had cramping with a bowel movement? 10. Have you had blood in your bowel movement?" (NCT01198145)
Timeframe: Up to 6 weeks post radiation therapy

Intervention	percentage of participants (Number)
	During RT : Q2	During RT : Q3	During RT : Q4	During RT : Q5	During RT : Q6	During RT : Q7	During RT : Q8	During RT : Q9	During RT : Q10	After RT : Q2	After RT : Q3	After RT : Q4	After RT : Q5	After RT : Q6	After RT : Q7	After RT : Q8	After RT : Q9	After RT : Q10
Arm I: Sulfasalazine	19	11	33	7	26	11	44	4	7	39	24	55	18	37	37	70	34	50
Arm II: Placebo	10	10	33	0	23	20	43	17	7	27	22	56	12	46	37	61	34	29

Area Under the Curve That Combines the Individual Severity of Diarrhea Toxicity as Measured by the CTCAE v4.0 During and After RT

For each patient, an Area Under the Curve (AUC) summary statistic will be calculated taking into account the individual severity of diarrhea toxicity over time. Severity of diarrhea was graded using the terminology and grading categories defined in the NCI's Common Toxicity Criteria (CTCAE), Version 4.0. Grade 0 = None; 1=Mild; Grade 2=Moderate, Grade 3=Severe, Grade 4=Life-threatening. The curve was constructed using weekly assessments during and after RT. A separate analysis was done during the course of RT and every week for 6 weeks following RT. (NCT01198145)
Timeframe: During radiation therapy and up to 6 weeks post radiation therapy

Intervention	grade*week (Mean)
	During RT	After RT
Arm I: Sulfasalazine	4.0	1.2
Arm II: Placebo	3.3	1.3

Average Graded Severity for Tenesmus, Abdominal Pain, Constipation, Diarrhea and Hemorrhage During and After RT as Graded by CTCAE v4.0

Tenesmus, Abdominal pain, constipation, diarrhea and hemorrhaging were assessed during RT and up to 6 weeks after RT. Severity of these events were graded using the terminology and grading categories defined in the NCI's Common Toxicity Criteria (CTCAE), Version 4.0. Grade 0 = None; 1=Mild; Grade 2=Moderate, Grade 3=Severe, Grade 4=Life-threatening. For each patient, an average score for each outcome variable during and after RT calculated as follows: The sum of all severity scores for that variable divided by the number of severity scores for that variable recorded for the patient during the course of RT and for 6 weeks following RT. (NCT01198145)
Timeframe: During radiation therapy and up to 6 weeks post radiation therapy

Intervention	Average Grade of Event (Mean)
	Tenesmus during RT	Tenesmus after RT	Abdominal pain during RT	Abdominal pain after RT	Constipation during RT	Constipation after RT	Diarrhea during RT	Diarrhea after RT	Rectal bleeding during RT	Rectal bleeding after RT
Arm I: Sulfasalazine	0.2	0.1	0.3	0.2	0.2	0.1	0.8	0.3	0.2	0.1
Arm II: Placebo	0.1	0.1	0.2	0.2	0.2	0.1	0.6	0.3	0.2	0.1

Maximum Severity of Diarrhea Toxicity as Measured by the CTCAE v4.0 During and After Radiotherapy (RT)

"The primary endpoint for this study is the maximal severity of diarrhea toxicity. Severity of diarrhea was graded using the terminology and grading categories defined in the NCI's Common Toxicity Criteria (CTCAE), Version 4.0. Grade 0 = None; 1=Mild; Grade 2=Moderate, Grade 3=Severe, Grade 4=Life-threatening as measured by the CTCAE version 4.0. Assessments were recorded during the course of RT and for 6 weeks following RT. The table below represents the worst graded diarrhea for each patient.~A two-sided Wilcoxon rank-sum test will be used to test the equality of the distributions of maximum diarrhea severity grades between the two treatment arms." (NCT01198145)
Timeframe: During radiation therapy and up to 6 weeks post radiation therapy

Intervention	Participants (Count of Participants)
	Grade 0	Grade 1	Grade 2	Grade 3	Grade 4
Arm I: Sulfasalazine	10	13	8	10	1
Arm II: Placebo	10	15	13	4	0

Percentage of Patients in Each Arm That Experience Clinically Significant Deficits in Overall Quality of Life and Fatigue

For each arm, the percentage of patients experience clinically significant deficits in overall QOL and fatigue as indicated by a score of 5 or lower on the 0-10 scale. The analysis was done using the questionnaire that was completed during the first week of radiotherapy (RT) and 6 weeks after RT. (NCT01198145)
Timeframe: Up to 6 weeks post radiotherapy

Intervention	percentage of participants (Number)
	During RT	After RT
Arm I: Sulfasalazine	17.9	26.9
Arm II: Placebo	7.5	27.6

Percentage of Patients in Each Arm That Experience Tenesmus, Abdominal Pain, Constipation, Diarrhea and Rectal Bleeding During and After RT

The number of patients that reported any grade 1 or higher adverse event was divided by the total number of patients evaluated. The analysis was done separately for each of the 5 outcomes and separately during RT and after RT. (NCT01198145)
Timeframe: During radiation therapy and up to 6 weeks post radiation therapy

Intervention	percentage of participants (Number)
	Tenesmus during RT	Tenesmus after RT	Abdominal pain during RT	Abdominal pain after RT	Constipation during RT	Constipation after RT	Diarrhea during RT	Diarrhea after RT	Rectal bleeding during RT	Rectal bleeding after RT
Arm I: Sulfasalazine	35.7	11.9	47.6	19.1	38.1	14.3	76.2	33.3	38.1	11.9
Arm II: Placebo	28.6	19.1	38.1	11.9	35.7	16.7	73.8	35.7	47.6	4.8

Maximum Severity of Each Outcome Variable (Rectal Bleeding, Abdominal Cramping, Tenesmus, Constipation, and Diarrhea) Measured During and After RT

"The maximal severity of each of 5 different adverse even types (Tenesmus, Abdominal Pain, Constipation, Diarrhea, and Rectal Bleeding) were collected as a secondary endpoint. Severity of the events was graded using the terminology and grading categories defined in the NCI's Common Toxicity Criteria (CTCAE), Version 4.0. Grade 0 = None; 1=Mild; Grade 2=Moderate, Grade 3=Severe, Grade 4=Life-threatening. Adverse events were assessed during the course of RT and for 6 weeks following RT. The table below represents the worst grade for each patient for each type.~Two-sided chi-square tests will be used to compare each percentage variable between treatment arms for each event type." (NCT01198145)
Timeframe: During radiation therapy and up to 6 weeks post radiation therapy

Intervention	Participants (Count of Participants)
	Tenesmus during RT72333267					Tenesmus during RT72333269	Tenesmus after RT72333267	Tenesmus after RT72333269	Abdominal pain during RT72333267	Abdominal pain during RT72333269	Abdominal pain after RT72333269	Abdominal pain after RT72333267	Constipation during RT72333267	Constipation during RT72333269	Constipation after RT72333269	Constipation after RT72333267	Diarrhea during RT72333267	Diarrhea during RT72333269	Diarrhea after RT72333269	Diarrhea after RT72333267	Rectal bleeding during RT72333267	Rectal bleeding during RT72333269	Rectal bleeding after RT72333267	Rectal bleeding after RT72333269
	Grade 0	Grade 1	Grade 4	Grade 2	Grade 3
Arm I: Sulfasalazine	27
Arm II: Placebo	30
Arm II: Placebo	9
Arm I: Sulfasalazine	7
Arm I: Sulfasalazine	18
Arm II: Placebo	21
Arm I: Sulfasalazine	5
Arm II: Placebo	7
Arm II: Placebo	1
Arm I: Sulfasalazine	0
Arm I: Sulfasalazine	22
Arm II: Placebo	26
Arm I: Sulfasalazine	14
Arm II: Placebo	12
Arm II: Placebo	4
Arm I: Sulfasalazine	3
Arm II: Placebo	0
Arm I: Sulfasalazine	17
Arm II: Placebo	24
Arm I: Sulfasalazine	8
Arm II: Placebo	2
Arm II: Placebo	3
Arm I: Sulfasalazine	12
Arm I: Sulfasalazine	4
Arm I: Sulfasalazine	19
Arm II: Placebo	22
Arm I: Sulfasalazine	6
Arm II: Placebo	6
Arm I: Sulfasalazine	10
Arm II: Placebo	11
Arm I: Sulfasalazine	13
Arm II: Placebo	14
Arm I: Sulfasalazine	9
Arm II: Placebo	13
Arm I: Sulfasalazine	1
Arm I: Sulfasalazine	11
Arm II: Placebo	10
Arm I: Sulfasalazine	2
Arm I: Sulfasalazine	26
Arm I: Sulfasalazine	16
Arm II: Placebo	20
Arm I: Sulfasalazine	20
Arm II: Placebo	27

Clinically Significant Change in HAQ Score

"Number of patients with a change of > 0.22 in the Health Assessment Questionnaire (HAQ) score over the period between baseline and week 104.~A change of > 0.22 in this score is considered as clinical relevant for rheumatoid arthritis patients." (NCT01172639)
Timeframe: Baseline-week104

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	71
CoBRA Slim High Risk Group	62
CoBRA Avant-garde High Risk Group	64
CoBRA Slim Low Risk Group	25
Tight Step Up Low Risk Group	26

Remission According to DAS28-CRP at Week 104

"Number of patients in remission according to DAS28-CRP (Disease Activity Score based on 28 joint count and C-reactive Protein) at week 104. (co-primary endpoints)~DAS28-CRP is calculated with the following formula : 0.56*SQRT TJC28+0.28*SQRT SJC28+0.36*ln (CRP+1)+0.014*GH+0.96 in which TJC is the tender joint count, SJC the Swollen Joint Count and GH the general health estimated by the patient on a Visual Analogue Scale (VAS).~A value below 2.6 is indicating remission, below or equal to 3.2 low disease activity, between 3.2 and 5.1 moderate disease activity and above 5.1 high disease activity." (NCT01172639)
Timeframe: week 104

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	64
CoBRA Slim High Risk Group	71
CoBRA Avant-garde High Risk Group	69
CoBRA Slim Low Risk Group	29
Tight Step Up Low Risk Group	34

Remission According to DAS28-CRP at Week 16

"Number of patients in remission according to DAS28-CRP (Disease Activity Score based on 28 joint count and C-reactive Protein) at week 16.~DAS28-CRP is calculated with the following formula : 0.56*SQRT TJC28+0.28*SQRT SJC28+0.36*ln (CRP+1)+0.014*GH+0.96 in which TJC is the tender joint count, SJC the Swollen Joint Count and GH the general health estimated by the patient on a Visual Analogue Scale (VAS).~A value below 2.6 is indicating remission, below or equal to 3.2 low disease activity, between 3.2 and 5.1 moderate disease activity and above 5.1 high disease activity." (NCT01172639)
Timeframe: week 16

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	69
CoBRA Slim High Risk Group	72
CoBRA Avant-garde High Risk Group	61
CoBRA Slim Low Risk Group	25
Tight Step Up Low Risk Group	23

Remission According to DAS28-CRP at Week 52

"Number of patients in remission according to DAS28-CRP (Disease Activity Score based on 28 joint count and C-reactive Protein) at week 52. (co-primary end point)~DAS28-CRP is calculated with the following formula : 0.56*SQRT TJC28+0.28*SQRT SJC28+0.36*ln (CRP+1)+0.014*GH+0.96 in which TJC is the tender joint count, SJC the Swollen Joint Count and GH the general health estimated by the patient on a Visual Analogue Scale (VAS).~A value below 2.6 is indicating remission, below or equal to 3.2 low disease activity, between 3.2 and 5.1 moderate disease activity and above 5.1 high disease activity." (NCT01172639)
Timeframe: week 52

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	63
CoBRA Slim High Risk Group	57
CoBRA Avant-garde High Risk Group	57
CoBRA Slim Low Risk Group	29
Tight Step Up Low Risk Group	29

Remission According to SDAI (Simple Disease Activity Index) at Week 16

"Number of patients in remission according to SDAI (Simplified Disease Activity Index) at week 16.~SDAI is calculated with the following formula : TJC28+SJC28+GH+GA ph in which TJC is the number of tender joints, SJC the number of Swollen Joint and GH the general health assessed by the patient on a Visual Analogue Scale (VAS) and GA ph the general assessment of the physician on a VAS.~A value below 3.3 is indicating remission, between 3.4 and 11.0 low disease activity, between 11.1 and 26.0 moderate disease activity and above 26.0 high disease activity." (NCT01172639)
Timeframe: week 16

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	42
CoBRA Slim High Risk Group	33
CoBRA Avant-garde High Risk Group	44
CoBRA Slim Low Risk Group	12
Tight Step Up Low Risk Group	12

Remission According to SDAI at Week 104

"Number of patients in remission according to SDAI (Simplified Disease Activity Index) at week 104.~SDAI is calculated with the following formula : TJC28+SJC28+GH+GA ph in which TJC is the number of tender joints, SJC the number of Swollen Joint and GH the general health assessed by the patient on a Visual Analogue Scale (VAS) and GA ph the general assessment of the physician on a VAS.~A value below 3.3 is indicating remission, between 3.4 and 11.0 low disease activity, between 11.1 and 26.0 moderate disease activity and above 26.0 high disease activity." (NCT01172639)
Timeframe: week 104

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	31
CoBRA Slim High Risk Group	28
CoBRA Avant-garde High Risk Group	41
CoBRA Slim Low Risk Group	20
Tight Step Up Low Risk Group	13

Remission According to SDAI at Week 52

"Number of patients in remission according to SDAI (Simplified Disease Activity Index) at week 52.~SDAI is calculated with the following formula : TJC28+SJC28+GH+GA ph in which TJC is the number of tender joints, SJC the number of Swollen Joint and GH the general health assessed by the patient on a Visual Analogue Scale (VAS) and GA ph the general assessment of the physician on a VAS.~A value below 3.3 is indicating remission, between 3.4 and 11.0 low disease activity, between 11.1 and 26.0 moderate disease activity and above 26.0 high disease activity." (NCT01172639)
Timeframe: week 52

Intervention	Participants (Count of Participants)
CoBRA Classic High Risk Group	36
CoBRA Slim High Risk Group	27
CoBRA Avant-garde High Risk Group	39
CoBRA Slim Low Risk Group	20
Tight Step Up Low Risk Group	15

Number of Patients Achieving Assessment in Ankylosing Spondylitis (ASAS 20)

ASAS measures symptomatic improvement in Ankylosing Spondylitis (AS) participants ASAS = 4 domains: participant global assessment of disease activity, pain, function, inflammation. ASAS 20 = 20% improvement from baseline and an improvement ≥ 10 units on a 0-100 scale (0=no disease activity; 100=high disease activity) for ≥ 3 domains, and no worsening in remaining domain. (NCT00247962)
Timeframe: 16 weeks

Intervention	participants (Number)
Etanercept	287
Sulphasalazine	99

Ankylosing Spondylitis Quality of Life (ASQoL) Total Score Change From Baseline

"ASQoL is a questionnaire to assess disease specific quality of life. It consists of 18 statements that are relevant to the physical and mental conditions for a patient with Ankylosing Spondylitis (AS). Each statement is answered by the patients as a Yes (scored as 1) or No (scored as 0). All item scores are summed to give a total score. Scores can range from 0 (good QoL) to 18 (poor QoL)." (NCT00247962)
Timeframe: Baseline and 16 Weeks

Intervention	units on a scale (Mean)
	Baseline	Week 16
Etanercept	11.03	6.21
Sulphasalazine	11.32	9.06

% BOLD Response Increase Above Baseline

Test whether Sulfasalazine, as compared to placebo, diminishes blood-oxygen-level dependent (BOLD) response to alcohol cues in the striatum and prefrontal cortex (PFC). BOLD response refers to brain activation in response to the presence of oxygen in a particular part of the brain. To test the hypothesis, we will compare Sulfasalazine treatment with placebo treatment. During the fMRI scan session, participants will be presented with the alcohol cue task. We will compare the difference in BOLD response during the presence of alcohol vs. a novel substance during the alcohol cue task. Outcome data collected during the alcohol cue task will provide us with BOLD response data for each intervention period. We will analyze the outcome data using FSL (Oxford Centre for Functional MRI of the Brain (FMRIB) Software - a collection of functional and structural brain image analysis tools). (NCT01312129)
Timeframe: Over two weeks

Intervention	% BOLD Response increase above baseline (Mean)
	Control Cue	Alcohol Cue
Placebo	.106	.074
Sulfasalazine	.082	.097

Breakthrough Treatment (First Treatment Period Only)

Number of days breakthrough pain medication was taken (NCT01667029)
Timeframe: Assessed during two week treatment period

Intervention	days (Mean)
Sulfasalazine	0.75
Placebo	2.00

Breakthrough Treatment (Using the Crossover Comparison Structure of the Study)

Number of days breakthrough pain medication was taken (NCT01667029)
Timeframe: Assessed during two week treatment period

Intervention	days (Mean)
Sulfasalazine	1.29
Placebo	1.14

Emotional Functioning (First Treatment Period Only)

Will be assessed by the Beck Depression Inventory (BDI) total score. The BDI has 21 items, each scored 0-3. Higher values are worse. The total score is the sum of the 21 items and ranges from 0-63. (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	units on a scale (Mean)
Sulfasalazine	8.25
Placebo	10.50

Emotional Functioning (Using the Crossover Comparison Structure of the Study)

Intervention	units on a scale (Mean)
Sulfasalazine	7.29
Placebo	8.29

Missed Medication Dose (First Treatment Period Only)

Number of missed medication doses (NCT01667029)
Timeframe: Assessed during two week treatment period

Intervention	dose (Mean)
Sulfasalazine	0
Placebo	0

Missed Medication Doses (Using the Crossover Comparison Structure of the Study)

Number of missed medication doses (NCT01667029)
Timeframe: Assessed during two week treatment period

Intervention	doses (Mean)
Sulfasalazine	0.43
Placebo	0

Number of Patients With >=50% Pain Reduction (First Treatment Period)

Average pain score will be the average of daily pain scores (0-10) recorded by the subject in a pain diary at baseline and during the second week of the two week treatment period. Higher scores are worse (0=no pain, 10=pain as bad as you can imagine). Percent pain reduction will be calculated from BL to end of treatment period 1 (2 weeks), based on average pain scores at each time point. (NCT01667029)
Timeframe: second week of two week treatment period

Intervention	Participants (Count of Participants)
Sulfasalazine	0
Placebo	0

Number of Patients With >=50% Pain Reduction (Using the Crossover Comparison Structure of the Study)

Average pain score will be the average of daily pain scores (0-10) recorded by the subject in a pain diary during baseline and the second week of each of the two week treatment periods. Higher scores are worse (0=no pain, 10=pain as bad as you can imagine). Percent pain reduction will be calculated from BL to end of treatment period 1 (2 weeks) and from end of treatment period 1 to end of treatment period 2 (2 weeks), based on average pain scores at each time point. (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	Participants (Count of Participants)
Sulfasalazine	0
Placebo	1

Pain Score (First Treatment Period)

Average pain score will be the average of daily pain scores (0-10) recorded by the subject in a pain diary during the second week of the two week treatment period. Higher scores are worse (0=no pain, 10=pain as bad as you can imagine). (NCT01667029)
Timeframe: second week of two week treatment period

Intervention	units on a scale (Mean)
Sulfasalazine	5.60
Placebo	4.20

Pain Score (Using the Crossover Comparison Structure of the Study)

Intervention	units on a scale (Mean)
Sulfasalazine	4.91
Placebo	3.93

Categorical Rating of Pain Intensity (First Treatment Period Only)

Assessed using number of days rated as none, mild, moderate, or severe in pain diary (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	days (Mean)
	"None rating"	"Mild rating"	"Moderate rating"	"Severe rating"
Placebo	0	1.75	5.25	0
Sulfasalazine	0	1.67	4.33	1.00

Categorical Rating of Pain Intensity (Using the Crossover Comparison Structure of the Study)

Assessed using number of days rated as none, mild, moderate, or severe in pain diary (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	days (Mean)
	"None rating"	"Mild rating"	"Moderate rating"	"Severe rating"
Placebo	1.17	1.83	3.83	0.17
Sulfasalazine	0	2.00	4.33	0.67

Overall Improvement (First Treatment Period Only)

The Patient Global Impression of Change (PGIC) reflects a patient's belief about the efficacy of treatment. Item 1 is as follows: Since beginning treatment at this clinic, how would you describe the change (if any) in ACTIVITY LIMITATIONS, SYMPTOMS, EMOTIONS, and OVERALL QUALITY OF LIFE, related to your painful condition? (tick ONE box) (1=No change (or condition has gotten worse), 2=Almost the same, hardly any change at all, 3=A little better, but no noticeable change, 4=Somewhat better, but the change has not made any real difference, 5=Moderately better, and a slight but noticeable change, 6=Better, and a definite improvement that has made a real and worthwhile difference, 7=A great deal better, and a considerable improvement that has made all the difference). Item 2 is as follows: In a similar way, please circle the number below that matches your degree of change since beginning care at this clinic (0-10 scale): 0= Much better, 5= No change, 10= Much worse. (NCT01667029)
Timeframe: Will be assessed at end of two week treatment period

Intervention	units on a scale (Mean)
	PGIC Item 1	PGIC Item 2
Placebo	1.75	4.50
Sulfasalazine	1.50	5.00

Overall Improvement (Using the Crossover Comparison Structure of the Study)

Intervention	units on a scale (Mean)
	PGIC item 1	PGIC item 2
Placebo	3.00	3.56
Sulfasalazine	2.80	4.00

Physical Functioning Score Assessed Using the Brief Pain Inventory (BPI) Interference Scale (First Treatment Period Only)

The BPI interference items are general activity, mood, walking ability, normal work (including housework), relations with other people, sleep, and enjoyment of life. The seven items are rated from 0 (pain does not interfere) to 10 (pain completely interferes). (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	units on a scale (Mean)
	General activity	Mood	Walking ability	Normal work	Relations with other people	Sleep	Enjoyment of life
Placebo	4.00	5.00	5.50	4.75	3.75	5.25	4.75
Sulfasalazine	5.25	3.75	4.50	5.25	1.25	5.00	5.75

Physical Functioning Score Assessed Using the Brief Pain Inventory (BPI) Interference Scale (Using the Crossover Comparison Structure of the Study)

Intervention	units on a scale (Mean)
	General activity	Mood	Walking ability	Normal work	Relations with other people	Sleep	Enjoyment of life
Placebo	3.71	4.00	4.57	4.14	2.57	4.43	4.00
Sulfasalazine	4.00	3.57	3.57	4.14	1.43	4.86	4.57

Physical Functioning Score Assessed Using the Euroquality of Life (EQ-5D) (Using the Crossover Comparison Structure of the Study)

The EQ-5D physical functioning items are mobility self-care, and usual activities. These three items are rated from 1 (no problems) to 5 (unable). (NCT01667029)
Timeframe: Assessed at end of two week treatment period

Intervention	Participants (Count of Participants)
	EQ-5D mobility72173110					EQ-5D mobility72173111	EQ-5D self-care72173111	EQ-5D self-care72173110	EQ-5D usual activities72173110	EQ-5D usual activities72173111
	4	1	2	3	5
Sulfasalazine	4
Sulfasalazine	1
Placebo	1
Sulfasalazine	5
Placebo	7
Sulfasalazine	2
Placebo	0
Sulfasalazine	0
Placebo	2
Placebo	3

Physical Functioning Score Assessed Using the Euroquality of Life (EQ-5D) Metrics (First Treatment Period Only)

Intervention	Participants (Count of Participants)
	EQ-5D mobility72173110					EQ-5D mobility72173111	EQ-5D self-care72173110	EQ-5D self-care72173111	EQ-5D usual activities72173110	EQ-5D usual activities72173111
	1	2	3	4	5
Sulfasalazine	3
Placebo	4
Sulfasalazine	1
Sulfasalazine	0
Placebo	0
Sulfasalazine	2
Placebo	1
Placebo	2

Percent Decrease in Central Nervous System Bioavailability of Sulfasalazine

To determine the ability of sulfasalazine to alter glioma glutamate levels. These levels will be measured by Magnetic Resonance Spectroscopy (MRS). The percent change is noted per subject. The measure is a % decrease of glioma glutamate levels (NCT01577966)
Timeframe: up to 2 years post baseline

Intervention	percentage of change (Number)
	GBM Pt 2	GBM Pt 1	GBM Pt 4	Astro Pt 3	Astro Pt 9	Astro Pt 5	Oligo Pt 8	Oligo Pt 6	Oligo Pt 7
Sulfasalazine	17	23	28	5	55	58	12	18	42

Number of Participants With Treatment Emergent Adverse Events (TEAEs)

Adverse event (AE) was defined as any untoward medical occurrence in a participant who received study drug and does not necessary have to have a causal relationship with treatment. All adverse events that occurred from the first dose of the study drug administration up to 60 days after the end of treatment visit were considered as TEAEs. Serious AE (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly or a medically important event. A summary of SAEs, all other non-serious AEs, regardless of causality, are reported in AE section. (NCT01768572)
Timeframe: Up to 211 days

Intervention	participants (Number)
	Any TEAE	Any treatment-emergent SAE	Any TEAE leading to death	Any TEAE leading to discontinuation
Sarilumab 150 mg q2w	33	1	0	6
Sarilumab 200 mg q2w	36	3	0	8
Tocilizumab q4w	68	7	1	4

Number of Participants Who Are Eligible, Consent, and Complete the 48 Weeks Study

To establish acceptability of this treatment approach assessing proportion of patients who are eligible, consent and complete the 48 week study. We will examine how many patients in the MONITOR cohort are eligible per year. All eligible patients in the MONITOR cohort will be approached and invited to join the study. We will then review how many patients complete the 48 week study period attending all visits from baseline to 48 weeks (0, 12, 24, 36 and 48). (NCT03797872)
Timeframe: 48 weeks

Intervention	Participants (Count of Participants)
Standard Care	0

Change From Baseline in the Average TBR of the Aorta

"The outcome was the change in the target to background ratio (TBR) of the aorta as measured by FDG-PET/CT scans conducted at baseline and after 24 weeks of randomized treatment allocation (MDS meanmaxTBR). Higher values indicate greater vascular inflammation.~FDG uptake measurement: PET-CT images were batch-analyzed by an investigator blinded to the patients' clinical information. FDG uptake was evaluated within the wall of the ascending aorta and bilateral carotid arteries (as maximum and mean standardized FDG uptake value [SUVmax and SUVmean, respectively]) approximately every 5 mm on axial images. Subsequently, the target-to-background ratio (TBR) was reported (ratio of the average arterial to blood axial slice SUVmax) to correct for the blood compartment contribution." (NCT02374021)
Timeframe: 0, 6 months

Intervention	Ratio (Mean)
Triple Therapy (MTX+SSZ+HCQ)	-0.06
TNF Inhibitor (Etanercept or Adalimumab)	-0.02

Change From Baseline in the Average TBR of the Bilateral Carotids

"The outcome was the change in the target to background ratio (TBR) of the average of the left and right carotids as measured by FDG-PET/CT scans conducted at baseline and after 24 weeks of randomized treatment allocation (MDS meanmaxTBR). The baseline values of the left and right carotids were averaged and then the follow-up values of the left and right carotids were averaged resulting in one value at each time point. Higher values indicate greater vascular inflammation.~FDG uptake measurement: PET-CT images were batch-analyzed by an investigator blinded to the patients' clinical information. FDG uptake was evaluated within the wall of the ascending aorta and bilateral carotid arteries (as maximum and mean standardized FDG uptake value [SUVmax and SUVmean, respectively]) approximately every 5 mm on axial images. Subsequently, the target-to-background ratio (TBR) was reported (ratio of the average arterial to blood axial slice SUVmax) to correct for the blood compartment contribution. (NCT02374021)
Timeframe: 0, 6 months

Intervention	Ratio (Mean)
Triple Therapy (MTX+SSZ+HCQ)	-0.10
TNF Inhibitor (Etanercept or Adalimumab)	-0.06

Change From Baseline in the Average TBR of the Index Vessel

"The outcome was the change in the target to background ratio (TBR) in the index vessel as measured by FDG-PET/CT scans conducted at baseline and after 24 weeks of randomized treatment allocation (MDS meanmaxTBR). Higher values indicate greater vascular inflammation.~FDG uptake measurement: PET-CT images were batch-analyzed by an investigator blinded to the patients' clinical information. FDG uptake was evaluated within the wall of the ascending aorta and bilateral carotid arteries (as maximum and mean standardized FDG uptake value [SUVmax and SUVmean, respectively]) approximately every 5 mm on axial images. Subsequently, the target-to-background ratio (TBR) was reported (ratio of the average arterial to blood axial slice SUVmax) to correct for the blood compartment contribution." (NCT02374021)
Timeframe: 0, 6 months

Intervention	Ratio (Mean)
Triple Therapy (MTX+SSZ+HCQ)	-0.07
TNF Inhibitor (Etanercept or Adalimumab)	-0.09

Change From Baseline in the MDS of the Aorta

"The outcome was the change in the mean of the maximum of the target to background ratio (TBR) in the most diseased segment (MDS) of the aorta as measured by FDG-PET/CT scans conducted at baseline and after 24 weeks of randomized treatment allocation (MDS meanmaxTBR). Higher values indicate greater vascular inflammation.~FDG uptake measurement: PET-CT images were batch-analyzed by an investigator blinded to the patients' clinical information. FDG uptake was evaluated within the wall of the ascending aorta and bilateral carotid arteries (as maximum and mean standardized FDG uptake value [SUVmax and SUVmean, respectively]) approximately every 5 mm on axial images. Subsequently, the target-to-background ratio (TBR) was reported (ratio of the average arterial to blood axial slice SUVmax) to correct for the blood compartment contribution." (NCT02374021)
Timeframe: 0, 6 months

Intervention	Ratio (Mean)
Triple Therapy (MTX+SSZ+HCQ)	-0.17
TNF Inhibitor (Etanercept or Adalimumab)	-0.17

Change From Baseline in Vascular Inflammation as Measured by FDG-PET/CT at 6 Months

"The primary outcome was the change in the mean of the maximum of the target to background ratio (TBR) in the most diseased segment (MDS) of of the index vessel as measured by FDG-PET/CT scans conducted at baseline and after 24 weeks of randomized treatment allocation (MDS meanmaxTBR). The index vessel is the vessel (either aorta, left carotid, or right carotid) with the highest meanmaxTBR at baseline. Higher values indicate greater vascular inflammation.~FDG uptake measurement: PET-CT images were batch-analyzed by an investigator blinded to the patients' clinical information. FDG uptake was evaluated within the wall of the ascending aorta and bilateral carotid arteries (as maximum and mean standardized FDG uptake value [SUVmax and SUVmean, respectively]) approximately every 5 mm on axial images. Subsequently, the target-to-background ratio (TBR) was reported (ratio of the average arterial to blood axial slice SUVmax) to correct for the blood compartment contribution." (NCT02374021)
Timeframe: 0, 6 months

Intervention	ratio (Mean)
Triple Therapy (MTX+SSZ+HCQ)	-0.19
TNF Inhibitor (Etanercept or Adalimumab)	-0.24

Number of Validated AID Associated Product Technical Failures (PTFs)

"A PTF was defined as any product technical complaint (PTC) related to the use of the AID that had a validated technical cause. Each participant was given a diary having questions related to participant's ability to remove the cap, to start the injection, to complete the injection and regarding confirmation of completing the injection. Participants were asked to answer the questions each time they self-inject the sarilumab. If the response was no to any of the first 3 questions, this was considered as a PTC. The used AID, for which PTC was reported, was sent to sponsor, examined and evaluated for the occurrence of a PTF." (NCT02057250)
Timeframe: Baseline up to Week 12

Intervention	PTFs (Number)
Sarilumab 150 mg by AID (AID Assessment Phase)	0
Sarilumab 200 mg by AID (AID Assessment Phase)	0

Area Under the Serum Concentration Versus Time Curve Calculated Using the Trapezoidal Method During a Dose Interval (AUC[0-tau]) for Sarilumab

AUC(0-tau) is defined as area under the serum concentration versus time curve calculated using the trapezoidal method during a dose interval, where dose interval was 2 weeks. Serum concentrations of sarilumab were analyzed using validated enzyme linked immunosorbent assay (ELISA). (NCT02057250)
Timeframe: Week 0-2: pre-dose on Day 1, anytime post-dose on Day 3, Day 5, Day 8, Day 12, Day 15; Week 10-12: pre-dose on Day 71, anytime post-dose on Day 73, Day 75, Day 78, Day 82, Day 85

,,,

Intervention	mg*day/L (Mean)
	Week 0-2	Week 10-12
Sarilumab 150 mg by AID (AID Assessment Phase)	131	205
Sarilumab 150 mg by PFS (AID Assessment Phase)	152	220
Sarilumab 200 mg by AID (AID Assessment Phase)	235	455
Sarilumab 200 mg by PFS (AID Assessment Phase)	227	405

Number of Participants With Laboratory Test Abnormalities

Number of participants with laboratory test abnormalities without regard to baseline abnormality. Laboratory test parameters included hematology, coagulation, liver function, renal function, electrolytes,clinical chemistry, and urinalysis (dipstick and microscopy). (NCT00637780)
Timeframe: Screening, Day 0, and Day 7

Intervention	participants (Number)
Sulfasalazine in Juvenile Idiopathic Arthritis	1

Number of Participants With Vital Signs Values Meeting Categorical Summarization Criteria

Vital sign values which met categorical summarization criteria included: supine/sitting pulse rate less than (<) 40 or more than (>) 120 beats per minute (bpm); erect pulse rate <40 or >140 bpm; changes from baseline in same posture of systolic blood pressure (SBP) more than or equal to (>=) 30 millimeters of mercury (mm Hg) or diastolic blood pressure (DBP) >=20 mm Hg; SBP <90 mm Hg; and DBP <50 mm Hg. (NCT00637780)
Timeframe: Screening, Day 0, and Day 7

Intervention	participants (Number)
Sulfasalazine in Juvenile Idiopathic Arthritis	0