taurocholic acid [Ligand Id: 4547] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL224867 (Cholaic acid, Cholic acid taurine conjugate, N-Choloyltaurine, Taurocholic acid)
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Rat [ChEMBL: CHEMBL4847] [GtoPdb: 959] [UniProtKB: P26435]
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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  • Sodium/bile acid and sulphated solute cotransporter 2/Ileal bile acid transporter in Human [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908]
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells F 5.28 pIC50 5300 nM IC50 J Pharmacol Exp Ther (1999) 291: 1204-1209 [PMID:10565843]
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4847] [GtoPdb: 959] [UniProtKB: P26435]
ChEMBL Inhibition of [3H]taurocholate uptake in rat hepatocytes F 5.22 pIC50 6000 nM IC50 Bioorg Med Chem Lett (2004) 14: 4179-4183 [PMID:15261266]
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
ChEMBL Agonist activity at human TGR5 expressed in CHO cells by luciferase assay F 5.31 pEC50 4950 nM EC50 J Med Chem (2008) 51: 1831-1841 [PMID:18307294]
Sodium/bile acid and sulphated solute cotransporter 2/Ileal bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake in ASBT-expressing COS cells F 4.38 pKi 41500 nM Ki Am J Physiol (1998) 274: G157-G169 [PMID:9458785]
Multidrug resistance associated protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073669] [UniProtKB: Q96QA9]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.4 uM) in membrane vesicles from MRP3-expressing HEK cells F 4.4 pIC50 40000 nM IC50 Biochemistry (2003) 42: 9989-10000 [PMID:12924948]
Solute carrier organic anion transporter family member 1A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
ChEMBL TP_TRANSPORTER: inhibition of Enalapril uptake in Oatp1-expressing HeLa cells F 4.49 pKi 32000 nM Ki Hepatology (1998) 28: 1341-1346 [PMID:9794920]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing LLC-PK1 cells F 4.97 pKi 10800 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp2-expressing LLC-PK1 cells F 4.4 pKi 39400 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]