Found 10 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase, H3 lysine-79 specific' and Ligand = 'BDBM50075098' TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.0120nMAssay Description:Competitive inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by...More data for this Ligand-Target Pair
3D Structure (crystal)TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.0800nMAssay Description:Inhibition of human DOT1-like Histone H3 Methyltransferase preincubated for 30 mins followed by 3H-SAM addition and measured after 120 minsMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.0800nMAssay Description:Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 min...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: <0.100nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.740nMAssay Description:Test compounds were serially diluted 3 fold in DMSO for 10 points and 1 μl was plated in a 384 well microtiter plate. Positive control (100% inh...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA methodMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISAMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 7.80nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged DOT1L (2 to 416 residues) expressed in Escherichia coli assessed as reduction in histone H3 lys...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 52nMAssay Description:Inhibition of DOT1L in human MOLM13 cells assessed as suppression of HoxA9 gene after 72 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
