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 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]