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ChEMBL ligand: CHEMBL1551 (Actigall, Cholurso, Destolit, NSC-683769, Urdox, 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 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]