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Inhibition of PHF8 (unknown origin)
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
AlphaScreen Assay from Article 10.1016/j.chembiol.2017.02.006: "Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells."
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
KDM TR-FRET Assay from Article 10.1038/nchembio.2085: "An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells."
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
PHF8 Assay from US Patent US9896436: "Histone demethylase inhibitors"
Assay data:28 Active, 52 Activity ≤ 1 µM, 55 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
PHF8 Assay from US Patent US10071984: "Histone demethylase inhibitors"
Assay data:52 Active, 28 Activity ≤ 1 µM, 55 Tested
Inhibition of KDM7B (unknown origin) ARTKQTAR(KMe1)STGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of KDM7B (unknown origin)
Inhibition of human N-terminal FLAG-tagged KDM7B (2 to 525 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K9(Me2)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
Assay data:2 Tested
Inhibition of human N-terminal FLAG-tagged KDM7B (2 to 525 residues) expressed in baculovirus infected Sf9 insect cells at 25 uM using H3(1-21)K9(Me2)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay relative to control
Assay data:4 Tested
Inhibition of human N-terminal FLAG-tagged KDM7B (2 to 525 residues) expressed in baculovirus infected Sf9 insect cells at 50 uM using H3(1-21)K9(Me2)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay relative to control
Binding affinity to PHF8 (unknown origin) assessed as induction of thermal shifts at 20 uM measured for 25 mins by SYPRO orange dye thermal shift assay
Inhibition of Flag-tagged PHF8 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as formaldehyde release using core histone as substrate preincubated with enzyme for 10 mins followed by incubation with substrate for 1 hr measured following 2 hrs incubation with ammonium acetate/acetoacetanilide by fluorescence based analysis
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of KDM7B (PHD-JmjC) (unknown origin) demethylation activity at 100 uM preincubated for 10 mins followed by H3(1-15)K4me3K9me2 peptide substrate addition by MALDI-TOF-MS analysis
Assay data:7 Tested
Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7B (PHD-JmjC) (unknown origin) at 100 uM preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Assay data:3 Tested
Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7B (PHD-JmjC) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7B (PHD) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Assay data:1 Active, 15 Tested
Inhibition of recombinant human N-terminal FLAG-tagged KDM7B expressed in baculovirus infected Sf9 insect cells using H3K9me1 peptide as substrate after 30 to 45 mins by TR-FRET assay
Inhibition of recombinant human N-terminal FLAG-tagged PHF8 expressed in baculovirus infected Sf9 cells using H3K9mel-biotin labelled peptide as substrate measured after 15 mins by Lance TR-FRET assay
Assay data:49 Active, 52 Activity ≤ 1 µM, 55 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of PHF8 (unknown origin) using biotinylated H3K9me1 peptide and alpha-ketoglutarate as substrate measured after 20 mins by LANCE TR-FRET assay
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