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Inhibition of EZH1 methyltransferase activity (unknown origin) assessed `transfer of [3H]methyl group from SAM to substrate by biochemical assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibitory Activity Assay from US Patent US11535629: "Dioxoloisoquinolinone derivatives and use thereof"
Assay data:15 Active, 3 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b EZH1
SummaryRelated BioAssays by Target
Selectivity interaction (Methyltransferase panel) EUB0000196bCl EZH1
Selectivity interaction (Methyltransferase panel (HotSpot screen, Reaction Biology, radioisotope-based filter binding assays)) EUB0000215b EZH1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (Protein methyltransferase panel (activity assay)) EUB0000211b EZH1
Affinity Biochemical interaction (Radiometric kinase assay) EUB0000209b EZH1
Affinity Phenotypic Cellular interaction (Immunofluorescence in-cell Western (inhibition of H3K27 methylation in MCF10A cells)) EUB0000209b EZH1
Inhibition of N-terminal His-tagged full-length recombinant human EZH1 ( 2 to 747 residues) expressed in baculovirus expression system at 1 uM using 3H-SAM as a substrate relative to control
Inhibition of EZH1 (unknown origin) using dimethylated H3K27 as substrate in presence of SAM by biochemical assay
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]-SAM from EZH1 (unknown origin) using histone H3 as substrate incubated for 2 hrs by cell-free assay
Inhibition of EZH1 (unknown origin)
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of EZH1 (unknown origin) by AlphaLisa assay
Inhibition of wild-type EZH1 (unknown origin) by AlphaLisa assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of human recombinant N-terminal FLAG-tagged EZH1 (2 to 747 residues) expressed in insect cell/baculovirus expression system at 50 uM in presence of [3H]-SAM by scintillation/filter plate assay relative to control
Inhibition of human recombinant N-terminal FLAG-tagged EZH1 (2 to 747 residues) expressed in insect cell/baculovirus expression system at 10 uM in presence of [3H]-SAM by scintillation/filter plate assay
Inhibition of recombinant full length human N-terminal FLAG-tagged EZH1 in PRC2 complex expressed in baculovirus system using SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA immunodetection assay
HMT Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of EZH1 (unknown origin) at 10 uM using SAM as substrate measured up to 960 mins by AlphaScreen microplate reader assay relative to control
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