ursodeoxycholic acid [Ligand Id: 7104] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1551 (Actigall, Cholurso, Ursodesoxycholic acid, Ursogal, Ursodeoxycholic acid, Urso, NSC-683769, Urso 250, Urdox, Ursofalk, Destolit, Ursodiol, Urso forte)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
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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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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 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]
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 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 B 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 28:

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