sulfasalazine [Ligand Id: 4840] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL421 (Salazopyrin-en, Ucine, SAS-500, Salazopyrin e.c., Salazosulfapyridine, S.a.s., NSC-203730, Salazopyrin, Sulfasalazine, Azulfidine EN, Colizine, NSC-667219, Salicylazosulfapyridine, Sulphasalazine, S.a.s.-500, Azulfidine, Azulfidine en-tabs)
  • aldo-keto reductase family 1 member B/Aldose reductase in Rat [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
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  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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  • Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
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  • Proton-coupled folate transporter in Human [GtoPdb: 1213] [UniProtKB: Q96NT5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
ChEMBL DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) B 4.77 pIC50 17042 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.53 pKi 29301 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.36 pIC50 43951 nM IC50 DrugMatrix in vitro pharmacology data
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
ChEMBL 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 B 5.02 pIC50 9600 nM IC50 Bioorg Med Chem Lett (2019) 29: 126623-126623 [PMID:31439379]
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of human carbonic anhydrase 1 esterase activity by noncompetitive Lineweaver-Burke plot B 5.16 pKi 6870 nM Ki Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
ChEMBL Inhibition of human carbonic anhydrase 1 esterase activity by spectrophotometry B 5.52 pIC50 3040 nM IC50 Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of human carbonic anhydrase 2 esterase activity by non-competitive Lineweaver-Burke plot B 5.06 pKi 8720 nM Ki Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
ChEMBL Inhibition of human carbonic anhydrase 2 esterase activity by spectrophotometry B 5.35 pIC50 4490 nM IC50 Bioorg. Med. Chem. (2008) 16: 9101-9105 [PMID:18819808]
Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466]
ChEMBL DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC) B 4.54 pIC50 28812 nM IC50 DrugMatrix in vitro pharmacology data
Cystine/glutamate transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075149] [GtoPdb: 902] [UniProtKB: Q9UPY5]
ChEMBL 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 B 4.52 pIC50 30000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6184-6187 [PMID:21889337]
ChEMBL Inhibition of xCT-mediated cystein/glutamate transporter (unknown origin) assessed as reduction in L-[14C]cyctein uptake B 6.8 pIC50 160 nM IC50 Eur J Med Chem (2019) 163: 215-242 [PMID:30522056]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) B 5.2 pIC50 6332 nM IC50 DrugMatrix in vitro pharmacology data
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
ChEMBL DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) B 4.63 pIC50 23549 nM IC50 DrugMatrix in vitro pharmacology data
Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7]
ChEMBL Binding affinity to MERS-CoV papain-like protease by SPR analysis B 5.12 pKd 7600 nM Kd Bioorg Med Chem (2019) 27: 1981-1989 [PMID:30940566]
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 4.71 pIC50 19639 nM IC50 DrugMatrix in vitro pharmacology data
Proton-coupled folate transporter in Human [GtoPdb: 1213] [UniProtKB: Q96NT5]
GtoPdb - - 4.2 pIC50 60000 nM IC50 Cell (2006) 127: 917-28 [PMID:17129779]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]