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

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ChEMBL ligand: CHEMBL224867 (Cholic acid taurine conjugate, N-Choloyltaurine, Taurocholic acid, Cholaic 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]