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 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]