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ChEMBL ligand: CHEMBL1551 (Actigall, Cholurso, Destolit, NSC-683769, Urdox, Urso, Urso 250, Ursodeoxycholate, Ursodeoxycholic acid, Ursodesoxycholic acid, Ursodiol, Ursofalk, Urso forte, Ursogal, Ursonorm) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]