ChEMBL ligand: CHEMBL115097
Retinoid X receptor-α/Liver X receptor-α/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha in Human [ChEMBL: CHEMBL3430879] [GtoPdb: 610, 602] [UniProtKB: P19793, Q13133] There should be some charts here, you may need to enable JavaScript!
Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] There should be some charts here, you may need to enable JavaScript!
Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human [ChEMBL: CHEMBL2111394] [GtoPdb: 610, 595] [UniProtKB: P19793, P37231] 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
Retinoid X receptor-α/Liver X receptor-α/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430879] [GtoPdb: 610, 602] [UniProtKB: P19793, Q13133]
ChEMBL	Competitive antagonist activity at human LXR-alpha/RXRA expressed in African green monkey COS7 cells assessed as reduction in bexarotene-induced receptor activation by RXRE-dependent luciferase reporter gene assay	B	6.52	pKd	302	nM	Kd	J Med Chem (2021) 64: 430-439 [PMID:33356247]
GtoPdb	-	-	7.11	pA2	-	-	-	ACS Med Chem Lett (2011) 2: 896-900 [PMID:24900278]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL	Binding affinity to human RXR-alpha by ITC analysis	B	5.87	pKd	1350	nM	Kd	J Med Chem (2021) 64: 430-439 [PMID:33356247]
ChEMBL	Binding affinity to human RXR-alpha LBD incubated for 2 hrs by tryptophan fluorescence quenching assay	B	6.59	pKd	260	nM	Kd	J Med Chem (2021) 64: 430-439 [PMID:33356247]
ChEMBL	Antagonist activity at RXRalpha expressed in COS1 cells assessed as inhibition of NEt-TMN-induced luciferase activity after 18 hrs by reporter gene assay relative to LGD1069	F	7.11	pKd	77.62	nM	Kd	ACS Med Chem Lett (2011) 2: 896-900 [PMID:24900278]
ChEMBL	Competitive antagonist activity at human RXRA/RXRA expressed in African green monkey COS7 cells assessed as reduction in bexarotene-induced receptor activation by RXRE-dependent luciferase reporter gene assay	B	7.2	pKd	63.1	nM	Kd	J Med Chem (2021) 64: 430-439 [PMID:33356247]
ChEMBL	Displacement of [3H]-9-cis retinoic acid from recombinant human RXR-alpha LBD by liquid scintillation counting based competitive ligand binding assay	B	5.87	pKi	1340	nM	Ki	J Med Chem (2021) 64: 430-439 [PMID:33356247]
GtoPdb	-	-	7.11	pA2	-	-	-	ACS Med Chem Lett (2011) 2: 896-900 [PMID:24900278]
Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111394] [GtoPdb: 610, 595] [UniProtKB: P19793, P37231]
ChEMBL	Competitive antagonist activity at human PPAR-gamma/RXRA expressed in African green monkey COS7 cells assessed as reduction in bexarotene-induced receptor activation by RXRE-dependent luciferase reporter gene assay	B	8	pKd	10	nM	Kd	J Med Chem (2021) 64: 430-439 [PMID:33356247]
GtoPdb	-	-	7.11	pA2	-	-	-	ACS Med Chem Lett (2011) 2: 896-900 [PMID:24900278]

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]