fexaramine [Ligand Id: 2744] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL192966 |
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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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0000182b NR1H4 | F | 6.02 | pEC50 | 960 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 towards farnesoid X receptor (FXR) | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (2005) 48: 5613-5638 [PMID:16134928] |
| 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 | Agonist activity at FXR | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6848-6853 [PMID:23040732] |
| ChEMBL | Agonist activity at FXR | F | 7.6 | pEC50 | 25 | nM | EC50 | Nat Chem Biol (2005) 1: 74-84 [PMID:16408003] |
| 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 data shown on this page come from version 36:
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]
