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AlphaScreen Assay from US Patent US11919855: "Substituted pyrrolidones and piperidones as small molecule inhibitors of EZH2 and EED protein binding"
Assay data:30 Active, 9 Activity ≤ 1 µM, 103 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA immunodetection assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Induction of degradation of EZH2 degradation in human MDA-MB-453 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of EZH2 (unknown origin)
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Induction of degradation of EZH2 in human MV4-11 cells assessed as maximum degradation relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Induction of degradation of EZH2 in human MV4-11 cells
Induction of degradation of EZH2 in human EOL1 cells assessed as maximum degradation relative to control
Induction of degradation of EZH2 in human EOL1 cells
Inhibition of PRC2 complex of EZH2-EED-SUZ12 (unknown origin) using human nucleosome as substrate incubated for 70 mins in presence of [3H]SAM
Binding affinity to PRC2 complex of EZH2-EED-SUZ12 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry method
Stabilization of PRC2 complex of EZH2-EED-SUZ12 (unknown origin) assessed as thermal stability by measuring increase in melting temperature by thermal shift assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of EZH1 methyltransferase activity (unknown origin) assessed `transfer of [3H]methyl group from SAM to substrate by biochemical assay
Inhibition of EZH2 methyltransferase activity (unknown origin) assessed `transfer of [3H]methyl group from SAM to substrate by biochemical assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of PRC2 catalytic core EZH2 (unknown origin)
Inhibition of human EZH2 in human MCF-10A cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by In-cell western assay
Inhibition of EZH2 (unknown origin) in PRC2 complex using H3 (1 to 24 residues) and 3H-SAM as substrate incubated for 1 hrs by Scintillation proximity assay
Inhibition of EZH2-EED-SUZ12 (unknown origin) complex assessed as nucleosome methylation by radioactivity based assay
EZH2 Enzyme Activity Assay from US Patent US20230365541: "INHIBITOR OF ENHANCER OF ZESTE HOMOLOGUE 2, AND USE THEREOF"
Assay data:64 Active, 64 Activity ≤ 1 nM, 64 Activity ≤ 1 µM, 64 Tested
Enzyme Assay from US Patent US11642348: "Substituted benzene compounds"
Assay data:46 Active, 45 Activity ≤ 1 µM, 46 Tested
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