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Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SETD8
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Methyltransferase panel) EUB0000196bCl SETD8
Selectivity interaction (Methyltransferase panel (radioactive enzyme assay)) EUB0000216b SETD8
Selectivity interaction (HMT panel) EUB0000194b SETD8
Selectivity interaction (Protein methyltransferase panel (activity assay)) EUB0000211b SETD8
Inhibition of human SET8 at 10 uM by radioisotope-based filter binding assay
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human his-tagged SETD8 (190 to 352 residues) at 1 to 10 uM incubated for 60 mins in presence of [3H]-SAM by hotspot assay
Inhibition of SETD8 (unknown origin) at 1 uM using 3H-SAM as a substrate relative to control
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr
Assay data:1 Active, 1 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates at 100 uM incubated for 1 hr relative to control
Assay data:6 Tested
Inhibition of human recombinant N-terminal his-tagged SET8 (190 to 352 residues) expressed in Escherichia coli at 50 uM in presence of [3H]-SAM by scintillation/filter plate assay relative to control
Inhibition of human recombinant N-terminal his-tagged SET8 (190 to 352 residues) expressed in Escherichia coli at 10 uM in presence of [3H]-SAM by scintillation/filter plate assay
Inhibition of SET8 (unknown origin) assessed as effect on H4K20 methylation incubated for 30 mins by Alphascreen assay
Inhibition of SETD8 (unknown origin) at 1 to 10 uM
Assay data:2 Tested
HMT Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of SET8 (unknown origin) at 10 uM using SAM as substrate measured up to 960 mins by AlphaScreen microplate reader assay relative to control
Inhibition of SET8 (unknown origin)-mediated H4K20 methylation using histone H4 and SAM as substrate incubated for 30 mins by AlphaScreen assay
Inhibition of recombinant human GST-tagged SETD8 (195 to 352 residues) expressed in Escherichia coli using nucleosome as substrate at 10 uM by radiometric HotSpot assay relative to control
Inhibition of wild type SETD8 catalytic domain (unknown origin) (234 to 380 residues) expressed in Escherichia coli assessed as compound-adduct dimer formation by measuring residual activity at 20 to 200 uM using varying levels of biotinylated H4 (1 to 24) peptide substrate measured after 1 hr in presence of [3H-SAM] by scintillation counting assay
Inhibition of wild type SETD8 catalytic domain (unknown origin) (234 to 380 residues) expressed in Escherichia coli assessed as compound-adduct monomer formation by measuring residual activity at 20 to 200 uM using varying levels of biotinylated H4 (1 to 24) peptide substrate measured after 1 hr in presence of [3H-SAM] by scintillation counting assay
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