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 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]