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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
Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR analysis
Binding affinity to C-terminal histidine tagged EED (unknown origin) expressed in Escherichia coli BL21(DE3) incubated for 15 mins by fluorescence polarization analysis
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to his tagged EED (1 to 441 residues) (unknown origin) incubated for 20 mins in presence of biotinylated H3K27me3 peptide (19 to 33 residues) by alphascreen competitive binding assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 5 Tested
Stabilization of EED (unknown origin) assessed as change in melting temperature by thermal shift assay
Displacement of H3K27me3 from EED (unknown origin) by competitive binding assay
Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR assay
Stabilization of EED (unknown origin) assessed as change in melting temperature at 50 to 500 uM by thermal shift assay
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
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