SR9011 [Ligand Id: 8900] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1961797
  • 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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  • Rev-Erb-β/Nuclear receptor subfamily 1 group D member 2 in Human [ChEMBL: CHEMBL1961784] [GtoPdb: 597] [UniProtKB: Q14995]
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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 4.89 pIC50 13000 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 - - 6.1 pIC50 790 nM IC50 Nature (2012) 485: 62-8 [PMID:22460951]
ChEMBL Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay B 6.1 pIC50 790 nM IC50 Nature (2012) 485: 62-68 [PMID:22460951]
ChEMBL REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay F 6.21 pIC50 620 nM IC50 Nature (2012) 485: 62-68 [PMID:22460951]
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-Erb alpha (unknown origin) by FRET assay B 6.15 pEC50 710 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]
GtoPdb - - 6.25 pIC50 560 nM IC50 Nature (2012) 485: 62-8 [PMID:22460951]
ChEMBL Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay B 6.25 pIC50 560 nM IC50 Nature (2012) 485: 62-68 [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]