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Inhibition of KAT6B (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of KAT6A (unknown origin)
Genotoxicity in Salmonella typhimurium in absence of S9 fraction by Ames reverse mutation assay
Assay data:2 Tested
SummaryPubMed Citation
Genotoxicity in Salmonella typhimurium in presence of S9 fraction by Ames reverse mutation assay
Inhibition of recombinant KAT6A (unknown origin) expressed in C57BL/6 mouse embryonic fibroblasts assessed as reduction in cell proliferation supplemented with fresh medium containing compounds every 48 hrs after for 168 hrs under low oxygen condition
Assay data:8 Active, 6 Activity ≤ 1 µM, 9 Tested
Inhibition of N-terminal NusA-fused His6-tagged human KAT6A (507 to 778 residues) expressed in Escherichia coli BL21 (DE3) cells using 0.4 uM acetyl coenzyme A and N-terminal histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRKV-GGK-biotin) as substrate incubated for 60 mins by Alpha screen technology
Assay data:174 Active, 155 Activity ≤ 1 µM, 177 Tested
Half-life in human liver microsome measured over 60 mins in presence of NADPH-regenerating system by UPLC/MS analysis
Half-life in mouse liver microsome measured over 60 mins in presence of NADPH-regenerating system by UPLC/MS analysis
Apparent permeability across apical to basolateral side in human Caco2 cells measured over 90 mins by LC-MS/MS analysis
Kinetic solubility of the compound in phosphate buffer at pH 6.5 by nephelometry
Kinetic solubility of the compound in 0.01 M HCl at pH 2 by nephelometry
Protein binding in mouse plasma at 1000 ng/mL after 4.2 hrs by LC-MS analysis based ultracentrifugation assay
Assay data:1 Tested
Cysteine reactivity assessed as induction of confirmational change in 13C-methyl-labeled La antigen after 1 hr in absence of DTT by ALARM NMR assay
Cysteine reactivity assessed as induction of confirmational change in 13C-methyl-labeled La antigen after 1 hr in presence of excess DTT by ALARM NMR assay
Inhibition of N-terminal GST-tagged recombinant human KAT6B (431 to end residues) expressed in baculovirus infected Sf9 insect cells using acetyl coenzyme A and N-terminal histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRKV-GGK-biotin) as substrate incubated for 60 mins by Alpha screen technology
Inhibition of KAT6A in C57BL/6 mouse embryonic fibroblasts assessed as reduction in cell proliferation after 10 days
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Assay data:50 Active, 27 Activity ≤ 1 µM, 72 Tested
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