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ChEMBL ligand: CHEMBL1961795 (GSK4112, SR6452) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]