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Selectivity interaction (Methyltransferase panel) EUB0000196bCl SETD2
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Methyltransferase panel) EUB0000034d SETD2
Inhibition of human GST-tagged SETD2 at 10 uM by radioisotope-based filter binding assay
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of SETD2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of SETD2 (unknown origin) at 1 uM using 3H-SAM as a substrate relative to control
Inhibition of SETD2 in human A549 cells assessed as reduction in H3K36me3 incubated for 3 days by in-cell western assay
Assay data:7 Active, 7 Activity ≤ 1 µM, 10 Tested
Inhibition of SETD2 (1434 to 1711 residues) (unknown origin) using SAM and biotin-Ahx-RKSAPATGGVKKPHR-NH2 as substrate preincubated for 30 mins followed by substrate addition by topcount scintillation counting method
Assay data:8 Active, 7 Activity ≤ 1 µM, 10 Tested
Inhibition of human recombinant N-terminal his-tagged SETD2 (1433 to 1711 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 SETD2 (1433 to 1711 residues) expressed in Escherichia coli at 10 uM in presence of [3H]-SAM by scintillation/filter plate assay
Inhibition of SETD2 in human A549 cells assessed as H3K36 trimethyl mark incubated for 3 days by in-cell western assay
Assay data:17 Active, 16 Activity ≤ 1 µM, 17 Tested
Binding affinity to SETD2 (unknown origin) by surface plasmon resonance
Inhibition of SETD2 (unknown origin) preincubated for 30 mins followed by SAM substrate addition measured after 2 hrs by plate reader method
Assay data:20 Active, 18 Activity ≤ 1 µM, 30 Tested
Inhibition of SETD2 (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."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of SETD2 (unknown origin) at 10 uM using SAM as substrate measured up to 960 mins by AlphaScreen microplate reader assay relative to control
Inhibition of SETD2 (unknown origin) using SAM as substrate preincubated for 10 mins followed by substrate addition measured after 4 hrs by AlphaLISA method
Inhibition of recombinant human N-terminal GST-tagged SETD2 (1433 to 1711 residues) expressed in Escherichia coli using nucleosome as substrate at 10 uM by radiometric HotSpot assay relative to control
Inhibition of N-terminal His6-tagged human SETD2 (1347 to 1711 residues) expressed in Escherichia coli Rosseta-2(DE3) cells assessed as residual activity at 50 uM using biotinylated-histone H3 (20 to 50 residues) as substrate in presence of [3H-Me]SAM by scintillation proximity assay relative to control
Assay data:24 Tested
Inhibition of SETD2 (unknown origin) at <5 uM using histone H3 peptide (21 to 44) as substrate in presence of co-factor SAM by LC-MS analysis
Inhibition of SETD2 (unknown origin) up to 50 uM
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