ChEMBL ligand: CHEMBL1551 (Actigall, Cholurso, Destolit, NSC-683769, Urdox, Urso, Urso 250, Ursodeoxycholate, Ursodeoxycholic acid, Ursodesoxycholic acid, Ursodiol, Ursofalk, Urso forte, Ursogal, Ursonorm)
Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] There should be some charts here, you may need to enable JavaScript!
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] There should be some charts here, you may need to enable JavaScript!
CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] There should be some charts here, you may need to enable JavaScript!
GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6] There should be some charts here, you may need to enable JavaScript!
Sodium/bile acid and sulphated solute cotransporter 2/Ileal bile acid transporter in Human [ChEMBL: CHEMBL2778] [GtoPdb: 960] [UniProtKB: Q12908] There should be some charts here, you may need to enable JavaScript!
Vitamin D receptor in Human [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] There should be some charts here, you may need to enable JavaScript!

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	Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay	B	4	pEC50	>100000	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL	Agonist activity at human FXR expressed in COS1 cells by luciferase assay	F	4.3	pEC50	>50000	nM	EC50	J Med Chem (2008) 51: 1831-1841 [PMID:18307294]
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
GtoPdb	Inhibition of taurocholate uptake by HeLa cells expressing hSLC10A1/NTCP	-	5.44	pIC50	3600	nM	IC50	J Pharmacol Exp Ther (1999) 291: 1204-9 [PMID:10565843]
ChEMBL	TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells	F	5.44	pIC50	3600	nM	IC50	J Pharmacol Exp Ther (1999) 291: 1204-1209 [PMID:10565843]
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
ChEMBL	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis	B	5.95	pKi	1134	nM	Ki	Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
ChEMBL	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay	B	4.58	pIC50	26540	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
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 TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay	F	4	pEC50	>100000	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells by luciferase assay	F	4.44	pEC50	36400	nM	EC50	J Med Chem (2008) 51: 1831-1841 [PMID:18307294]
ChEMBL	Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay	F	5.62	pEC50	2390	nM	EC50	Bioorg Med Chem (2015) 23: 1613-1628 [PMID:25735208]
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	4.12	pKi	75000	nM	Ki	Am J Physiol (1998) 274: G157-G169 [PMID:9458785]
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473]
ChEMBL	Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay	B	4.3	pIC50	>50000	nM	IC50	Eur J Med Chem (2016) 109: 238-246 [PMID:26774929]

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]