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Inhibition of human WDR5 WIN site expressed in Escherichia coli
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
SummaryRelated BioAssays by Target
Competitive binding affinity to full length wild type MLL (unknown origin)
Assay data:5 Active, 1 Activity ≤ 1 µM, 7 Tested
Inhibition of human Menin to MLL protein-protein interaction
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of Menin to MLL (unknown origin) protein-protein interaction
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 4 Tested
Enzyme assay of inhibition against MLL1-WDR5 protein-protein interactions from US Patent US20230286948: "HALOALKYLPYRIDYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR"
Assay data:21 Active, 10 Activity ≤ 1 µM, 56 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Enzyme Assay of Inhibition Against MLL1-WDR5 Protein-Protein Interactions from US Patent US20230286925: "PHENYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR"
Assay data:33 Active, 32 Activity ≤ 1 µM, 33 Tested
Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b MLL
Assay data:1 Tested
Selectivity interaction (Methyltransferase panel) EUB0000196bCl MLL
Selectivity interaction (Reader proteins panel (DSF assay)) EUB0000034d WDR5
Selectivity interaction (Methyltransferase panel (radioactive enzyme assay)) EUB0000216b MLL
Selectivity interaction (HMT panel) EUB0000194b MLL
Selectivity interaction (Methyl-Lysine/Arginine panel (DSF assay)) EUB0000211b WDR5
Selectivity interaction (ITC) EUB0000211b WDR5
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Affinity Biochemical interaction (Biacore) EUB0000211b WDR5
Affinity Phenotypic Cellular interaction (Western Blot (effect on WDR5-MLL interaction in HEK293 cells)) EUB0000211b WDR5
Inhibition of MLL1 (unknown origin) using peptide substrate preincubated for 10 mins followed by substrate addition for 4 hrs by HTRF assay
SummaryPubMed CitationRelated BioAssays by Target
Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay
Assay data:36 Active, 34 Activity ≤ 1 nM, 39 Activity ≤ 1 µM, 39 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant incubated for 1 hr by TR-FRET assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of MLL1-WDR5 (unknown origin) interaction using 10mer-Thr-FAM as substrate by fluorescence polarization based competitive binding assay
Binding affinity to WDR5 (unknown origin) using 10mer-Thr-FAM as substrate incubated for 30 mins by fluorescence polarization based competitive binding assay
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