ChEMBL ligand: CHEMBL1961795 (GSK4112, SR6452)
Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] There should be some charts here, you may need to enable JavaScript!
Rev-Erb-α/Nuclear receptor subfamily 1 group D member 1 in Human [ChEMBL: CHEMBL1961783] [GtoPdb: 596] [UniProtKB: P20393] 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
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL	Binding affinity to LXRalpha (unknown origin) by radioligand displacement assay	B	5.3	pIC50	5000	nM	IC50	J Med Chem (2013) 56: 4729-4737 [PMID:23656296]
Rev-Erb-α/Nuclear receptor subfamily 1 group D member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961783] [GtoPdb: 596] [UniProtKB: P20393]
GtoPdb	-	-	5.64	pIC50	2300	nM	IC50	ACS Chem Biol (2011) 6: 131-4 [PMID:21043485]
ChEMBL	Agonist activity at Rev-erbalpha assessed as repression of transcription by luciferase-reporter gene assay	F	5.64	pEC50	2300	nM	EC50	Bioorg Med Chem Lett (2012) 22: 3739-3742 [PMID:22560469]
ChEMBL	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay	F	5.64	pEC50	2300	nM	EC50	Bioorg Med Chem Lett (2012) 22: 4413-4417 [PMID:22633688]
ChEMBL	Agonist activity at Rev-Erb alpha (unknown origin) by FRET assay	B	5.64	pEC50	2300	nM	EC50	Bioorg Med Chem Lett (2020) 30: 127395-127395 [PMID:32738989]
ChEMBL	Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment after 1 hr by FRET assay	B	6.3	pEC50	500	nM	EC50	J Med Chem (2013) 56: 4729-4737 [PMID:23656296]
ChEMBL	Agonist activity at Rev-erbalpha assessed as NCoR recruitment by FRET assay	F	6.4	pEC50	400	nM	EC50	Bioorg Med Chem Lett (2012) 22: 3739-3742 [PMID:22560469]
GtoPdb	-	-	6.4	pEC50	400	nM	EC50	ACS Chem Biol (2010) 5: 925-32 [PMID:20677822]

ChEMBL data shown on this page come from version 32:

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]