DY268 [Ligand Id: 14078] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3264644
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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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 Inhibition of GW4064-induced transactivation of FXR (unknown origin) expressed in HEK293T cells after 16 hrs by beta-lactamase reporter gene assay B 6.33 pIC50 468.5 nM IC50 Bioorg Med Chem (2014) 22: 2919-2938 [PMID:24775917]
GtoPdb - - 8.12 pIC50 7.5 nM IC50 Bioorg Med Chem (2014) 22: 2919-38 [PMID:24775917]
ChEMBL Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assay B 8.12 pIC50 7.5 nM IC50 Bioorg Med Chem (2014) 22: 2919-2938 [PMID:24775917]

ChEMBL data shown on this page come from version 35:

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]