ChEMBL ligand: CHEMBL458603
Pregnane X receptor/Nuclear receptor subfamily 1 group I member 2 in Human [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] There should be some charts here, you may need to enable JavaScript!
Constitutive androstane receptor/Nuclear receptor subfamily 1 group I member 3 in Human [ChEMBL: CHEMBL5503] [GtoPdb: 607] [UniProtKB: Q14994] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Pregnane X receptor/Nuclear receptor subfamily 1 group I member 2 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]
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 LBD in human HepG2 cells incubated for 24 hrs by firefly luciferase reporter assay	B	6.16	pEC50	690	nM	EC50	J Med Chem (2023) 66: 2422-2456 [PMID:36756805]
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 LBD (151 to 349 residues) expressed in HepG2 cells co-expressed with pGL5-luc luciferase assessed as increase in CAR activation measured after 1 to 4 hrs by LanthaScreen TR-FRET assay	B	7.89	pEC50	13	nM	EC50	Eur J Med Chem (2023) 259: 115631-115631 [PMID:37473690]
ChEMBL	Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assay	B	7.92	pEC50	12	nM	EC50	J Med Chem (2023) 66: 2422-2456 [PMID:36756805]
ChEMBL	Agonist activity at human CAR	B	8.3	pEC50	5	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]

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]