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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]