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ChEMBL ligand: CHEMBL1961797 |
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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 | 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]