GSK4112 [Ligand Id: 2903] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1961795 (GSK4112, SR6452)
  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
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  • Rev-Erb-α/Nuclear receptor subfamily 1 group D member 1 in Human [ChEMBL: CHEMBL1961783] [GtoPdb: 596] [UniProtKB: P20393]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]