taurochenodeoxycholic acid [Ligand Id: 4747] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL185878 (Taurochenodeoxycholic acid) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Binding affinity for Farnesoid X Receptor (FXR) | B | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1865-1868 [PMID:12749886] |
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | TP_TRANSPORTER: competitive inhibition of Taurocholate uptake in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus | F | 4.55 | pKi | 28000 | nM | Ki | Gastroenterology (2002) 123: 1649-1658 [PMID:12404239] |
| 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 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay | F | 4.53 | pEC50 | 29570 | nM | EC50 | Eur J Med Chem (2015) 104: 57-72 [PMID:26435512] |
| ChEMBL | Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay | F | 5.64 | pEC50 | 2300 | nM | EC50 | Eur J Med Chem (2015) 104: 57-72 [PMID:26435512] |
| ChEMBL | Agonist activity at human TGR5 expressed in CHO cells by luciferase assay | F | 5.72 | pEC50 | 1920 | 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 | 5.21 | pKi | 6100 | nM | Ki | Am J Physiol (1998) 274: G157-G169 [PMID:9458785] |
| ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells | F | 4.26 | pIC50 | 55000 | nM | IC50 | Biochem J (2003) 371: 361-367 [PMID:12523936] |
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]
