CITCO [Ligand Id: 2758] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
