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 33:
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]
