TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.00200nMAssay 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
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nM Kd: 0.0100nM Kon: 0.000300M-1s-1 Koff: 3.00E+6s-1Assay Description:Unless otherwise indicated, assays of DOT1L enzymatic activity were performed under balanced conditions (all substrates present at concentrations equ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(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
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKd: 0.0600nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKd: 0.0600nMAssay Description:Binding affinity to recombinant N-terminal DOT1L (1 to 420 residues) (unknown origin) expressed in Escherichia coli (DE3) assessed as dissociation co...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: <0.0700nMAssay Description:Binding affinity to DOT1L (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(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(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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.0800nMAssay 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(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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nM Kd: 0.100nMAssay Description:Assay of DOT1L enzymatic activity were performed under balanced conditions using a radiometric assay.More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.110nMAssay Description:Inhibition of 0.05 nM DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosome as substrate and [3H]SAM as co-factor preincubated for...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.150nMAssay 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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.170nMAssay Description:Inhibition of 0.05 nM DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosome as substrate and [3H]SAM as co-factor preincubated for...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.190nMAssay Description:Inhibition of 0.05 nM DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosome as substrate and [3H]SAM as co-factor preincubated for...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKd: 0.25nMAssay Description:Binding affinity to recombinant N-terminal DOT1L (1 to 420 residues) (unknown origin) expressed in Escherichia coli (DE3) assessed as dissociation co...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKd: 0.25nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay 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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay Description:Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containingMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of DOT1L (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of DOT1L (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant DOT1L (unknown origin) using 3H-SAM/chicken erythrocyte nucleosomes as substrate preincubated for 30 mins followed by subst...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant DOT1L (unknown origin) using 3H-SAM/chicken erythrocyte nucleosomes as substrate preincubated for 30 mins followed by subst...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant N-terminal DOT1L (1 to 420 residues) (unknown origin) expressed in Escherichia coli (DE3) using [3H]-SAM as substrate prein...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay Description:Inhibition of human recombinant DOT1L (1 to 416 residues) using chicken erythrocyte oligonucleosomes as substrate and [3H]-SAM incubated for 120 mins...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay Description:Displacement of [3H]-SAM in recombinant human His-tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.300nMAssay Description:Binding affinity to human DOT1L after 120 minsMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.360nMAssay 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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay 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(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Competitive inhibition of human recombinant DOT1L (1 to 416 amino acid residues) using [3H]-SAM assessed as inhibition of nucleosome methylation incu...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of DOT1L (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 minsMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of recombinant human DOT1L (1 to 416) using [3H]-SAM, SAM and nucleosome as substrate assessed as incorporation of radioactivity into nucl...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.460nMAssay Description:Inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472) using [3H]-SAM after 30 mins by scintillation counterMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of recombinant N-terminal DOT1L (1 to 420 residues) (unknown origin) expressed in Escherichia coli (DE3) using [3H]-SAM as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 0.590nMAssay Description:An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or...More data for this Ligand-Target Pair
Affinity DataIC50: 0.590nMAssay Description:An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.590nMAssay Description:Inhibition of 0.05 nM DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosome as substrate and [3H]SAM as co-factor preincubated for...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.590nMAssay Description:Unless otherwise indicated, assays of DOT1L enzymatic activity were performed under balanced conditions (all substrates present at concentrations equ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.620nMAssay Description:An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataKi: 0.720nMAssay Description:Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containingMore data for this Ligand-Target Pair
Affinity DataIC50: 0.730nMAssay Description:An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.730nMAssay Description:Unless otherwise indicated, assays of DOT1L enzymatic activity were performed under balanced conditions (all substrates present at concentrations equ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(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
Affinity DataIC50: 0.740nMAssay Description:An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 0.740nMAssay Description:Unless otherwise indicated, assays of DOT1L enzymatic activity were performed under balanced conditions (all substrates present at concentrations equ...More data for this Ligand-Target Pair



3D Structure (crystal)



















