cilofexor [Ligand Id: 10644] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297613 (GS-9674, Gs-9674, PX-104, Cilofexor, PX104, GS 9674) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| hydroxysteroid 17-beta dehydrogenase 13/17-beta-hydroxysteroid dehydrogenase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5305042] [GtoPdb: 3222] [UniProtKB: Q7Z5P4] | ||||||||
| ChEMBL | Inhibition of HSD17B13 (unknown origin) using beta-estradiol and FAC-NAD+ as substrate incubated for 2 hrs by NAD(P)H-Glo detection reagent based luminescence assay | B | 5.02 | pIC50 | 9470 | nM | IC50 | J Med Chem (2025) 68: 6127-6148 [PMID:39851255] |
| Farnesoid X receptor/Bile acid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Agonist activity at FXR (unknown origin) | B | 7.24 | pEC50 | 58 | nM | EC50 | J Med Chem (2025) 68: 6127-6148 [PMID:39851255] |
| 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] |
| ChEMBL | Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0001168a NR1H4 | F | 7.4 | pEC50 | 40 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| 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] |
| EPH receptor A2 in Human [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| GtoPdb | Measuring inhibition of biotinylated ephrin-A1-Fc binding to immobilized EphA2 receptor | - | 5.07 | pKi | 8600 | nM | Ki | Biochem Pharmacol (2023) 209: 115452 [PMID:36792038] |
ChEMBL data shown on this page come from version 37:
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]
