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ChEMBL ligand: CHEMBL4297613 (Cilofexor, Gs-9674, GS 9674, GS-9674, PX-104, PX104) |
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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 FXR (unknown origin) by cell based assay | B | 7.39 | pEC50 | 41 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
GtoPdb | EC50 determined as the ability of cilofexor to modulate the interaction between the purified bacterial expressed FXR ligand binding domain (LBD) and a synthetic biotinylated peptide based on residues 676-700 of SRC1, in a TR-FRET assay. | - | 7.6 | pEC50 | <25 | nM | EC50 | US10485795B2. FXR (NR1H4) binding and activity modulating compounds (2019) |
ChEMBL | Agonist activity at FXR (unknown origin) | B | 7.82 | pEC50 | 15 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
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]