ChEMBL ligand: CHEMBL1961796
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!
Rev-Erb-β/Nuclear receptor subfamily 1 group D member 2 in Human [ChEMBL: CHEMBL1961784] [GtoPdb: 597] [UniProtKB: Q14995] 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	5.2	pIC50	6300	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]
ChEMBL	Dissociation constant for binding to REV-ERB-alpha by circular dichroism	B	6.1	pKd	800	nM	Kd	Nature (2012) 485: 62-68 [PMID:22460951]
ChEMBL	REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay	F	6.15	pIC50	710	nM	IC50	Nature (2012) 485: 62-68 [PMID:22460951]
GtoPdb	-	-	6.17	pIC50	670	nM	IC50	Nature (2012) 485: 62-8 [PMID:22460951]
ChEMBL	Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay	B	6.17	pIC50	670	nM	IC50	Nature (2012) 485: 62-68 [PMID:22460951]
ChEMBL	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay	B	6.17	pIC50	670	nM	IC50	Bioorg Med Chem Lett (2012) 22: 4413-4417 [PMID:22633688]
ChEMBL	Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment after 1 hr by FRET assay	B	4.3	pEC50	>50000	nM	EC50	J Med Chem (2013) 56: 4729-4737 [PMID:23656296]
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	6.15	pEC50	700	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	6.21	pEC50	620	nM	EC50	Bioorg Med Chem Lett (2020) 30: 127395-127395 [PMID:32738989]
Rev-Erb-β/Nuclear receptor subfamily 1 group D member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961784] [GtoPdb: 597] [UniProtKB: Q14995]
ChEMBL	Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay	B	6.1	pIC50	800	nM	IC50	Nature (2012) 485: 62-68 [PMID:22460951]
GtoPdb	-	-	6.1	pIC50	800	nM	IC50	Nature (2012) 485: 62-8 [PMID:22460951]

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]