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ChEMBL ligand: CHEMBL458603 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Constitutive androstane receptor/Nuclear receptor subfamily 1 group I member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5503] [GtoPdb: 607] [UniProtKB: Q14994] | ||||||||
ChEMBL | Agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 incubated for 23 hrs by luciferase reported gene assay | B | 6.21 | pEC50 | 620 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1039-1044 [PMID:31312405] |
ChEMBL | Agonist activity at human constitutive androstane receptor expressed in HepG2 cells co-expressing CYP2B6 incubated for 23 hrs by One-Glo luciferase reporter gene assay | B | 6.24 | pEC50 | 570 | nM | EC50 | Eur J Med Chem (2019) 179: 84-99 [PMID:31247375] |
ChEMBL | Agonist activity at human CAR3 expressed in African green monkey COS-1 cells cotransfected with RXRalpha after 24 hrs by CYP2B6-luciferase reporter gene assay | B | 6.29 | pEC50 | 510 | nM | EC50 | J Med Chem (2016) 59: 4601-4610 [PMID:27145071] |
ChEMBL | Agonist activity at human CAR expressed in HEK293 cells by luciferase reporter gene assay | B | 7.12 | pEC50 | 75 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
GtoPdb | - | - | 7.3 | pEC50 | - | - | - | J Biol Chem (2003) 278: 17277-83 [PMID:12611900] |
ChEMBL | Agonist activity at Polyhistidine-tagged human CAR LBD expressed in Escherichia coli by FRET-based assay | B | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
ChEMBL | Agonist activity at CAR LBD (108 to 348 residues) expressed in human HepG2 cells assessed as receptor binding to PGC1alpha by lanthascreenTR-FRET coactivator assay | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2016) 59: 4601-4610 [PMID:27145071] |
ChEMBL | Agonist activity at human CAR | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
ChEMBL | Agonist activity at human PXR transfected in human HepG2 cells cotransfected with CYP3A4 incubated for 23 hrs by luciferase reporter gene assay | B | 6 | pEC50 | 990 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1039-1044 [PMID:31312405] |
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]