fexaramine [Ligand Id: 2744] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL192966 (Fexaramine)
  • 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 Agonist activity at human FXR transfected in CHO-K1 cells coexpressed with beta-galactosidase incubated for 3 to 16 hrs by PathHunter chemiluminescence based assay B 6.1 pEC50 800 nM EC50 J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
GtoPdb - - 6.6 pEC50 - - - Mol Cell (2003) 11: 1079-92 [PMID:12718892]
ChEMBL Effective concentration against farnesoid X receptor (FXR) B 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (2005) 15: 3119-3125 [PMID:15893927]
ChEMBL Effective concentration against farnesoid X receptor (FXR) B 7.6 pEC50 25 nM EC50 J Med Chem (2005) 48: 5613-5638 [PMID:16134928]
ChEMBL Effective concentration towards farnesoid X receptor (FXR) B 7.6 pEC50 25 nM EC50 J Med Chem (2005) 48: 5613-5638 [PMID:16134928]
ChEMBL Agonist activity at FXR F 7.6 pEC50 25 nM EC50 Nat Chem Biol (2005) 1: 74-84 [PMID:16408003]
ChEMBL Agonist activity at FXR F 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (2012) 22: 6848-6853 [PMID:23040732]

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]