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Selectivity interaction (Human bromodomain panel (DSF assay)) EUB0000233b MLL
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Methyltransferase screen (Scintillation proximity assays)) EUB0000255b MLL
Selectivity interaction (Methyltransferase screen (Scintillation proximity assays)) EUB0000230b MLL
Selectivity interaction (Methyltransferase screen (radiometric assays, panel of 8 PRMTs, 21 protein lysine methyltransferases, 3 DNA methyltransferases, and one RNA methyltransferase)) EUB0000272b MLL
Selectivity interaction (Methyltransferase screen (radiometric assays, panel of 8 PRMTs, 21 protein lysine methyltransferases, 3 DNA methyltransferases, and one RNA methyltransferase)) EUB0000271b MLL
Selectivity interaction (PWWP, WD40, and Tudor domain panel (DSLS measurements, literature)) EUB0000270b WDR5
Selectivity interaction (Bromodomain panel (DSF asssay)) EUB0000270b MLL
Selectivity interaction (Transferase panel (protein, RNA, and DNA methyltransferases. and EP300 (acetyltransferase))) EUB0000270b MLL
Inhibition of IncRNA-WDR5 complex in human MDA-MB-231 cells assessed as downregulation of HOTTIP expression measured after 3 days by RT-qPCR analysis
SummaryPubMed CitationRelated BioAssays by Target
Competitive inhibition of WDR5 (unknown origin) assessed as inhibition constant in presence of 5-[({2-[2-({[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S,2S)-1-{[(2S,5S,8S,14S)-8-{[(1S)-1-{[(1S)-1-carbamoyl-3-carboxypropyl]carbamoyl}-2-methylpropyl]carbamoyl}-3,6,12,15-tetraoxo-2,5-bis(propan-2-yl)-1,4,7,11-tetraazacyclopentadecan-14-yl]carbamoyl}-2-methylbutyl]carbamoyl}-3-carboxypropyl]carbamoyl}-3-carboxypropyl]carbamoyl}-3-carboxypropyl]carbamoyl}-2-carboxyethyl]carbamoyl}methoxy)ethoxy]ethyl}carbamothioyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid by fluorescence polarization assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Competitive inhibition of WDR5 (unknown origin) assessed as inhibition constant in presence of 5-{[(5S)-5-(6-{6-[(2S)-2-[(2S)-6-amino-2-[(2S)-5-carbamimidamido-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3R)-2-[(2S)-5-carbamimidamido-2-[(2S)-2-acetamidopropanamido]pentanamido]-3-hydroxybutanamido]-4-carboxybutanamido]-3-methylbutanamido]-3-(1H-imidazol-5-yl)propanamido]-4-methylpentanamido]pentanamido]hexanamido]-3-hydroxypropanamido]hexanamido}hexanamido)-5-carbamoylpentyl]carbamoyl}-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid by fluorescence polarization assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 4 Tested
Binding affinity of WDR5 F266A mutant (unknown origin) assessed as dissociation constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Binding affinity of WDR5 (unknown origin) assessed as dissociation constant
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay
Assay data:24 Active, 24 Activity ≤ 1 nM, 24 Activity ≤ 1 µM, 24 Tested
Induction of WDR5 degradation in human MV4-11 cells assessed as maximum degradation at 0.5 uM incubated for 18 hrs relative to control
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