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Found 368 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase, H3 lysine-79 specific'
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM297395(US10112968, Compound D16)
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
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50443016(CHEMBL3087498)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM92649(EPZ004777)
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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM297394(US10112968, Compound C118)
Affinity DataKi:  13nM Kd:  1.70nM Kon:  0.0200M-1s-1 Koff:  1.20E+7s-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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  66nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM92642(SAH)
Affinity DataKi:  320nM Kd:  71nMAssay Description:Assay of DOT1L enzymatic activity were performed under balanced conditions using a radiometric assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM297392(US10112968, Compound SAH)
Affinity DataKi:  320nM Kd:  71nM Kon:  0.100M-1s-1 Koff:  1.40E+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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  73nMAssay Description:Competitive inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assa...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396979(CHEMBL2171170)
Affinity DataKd:  86nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  130nMAssay Description:Competitive inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assa...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataKd:  150nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396979(CHEMBL2171170)
Affinity DataKd:  150nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM297393(US10112968, Compound C94)
Affinity DataKi:  845nM Kd:  167nM Kon:  0.200M-1s-1 Koff:  1.20E+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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM92646(EPZ003647)
Affinity DataKi:  845nM Kd:  167nMAssay Description:Assay of DOT1L enzymatic activity were performed under balanced conditions using a radiometric assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  170nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  200nMAssay Description:Competitive inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assa...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  240nMAssay Description:Competitive inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assa...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataKd:  360nMAssay Description:Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataKd:  550nMAssay Description:Competitive inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assa...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50460739(CHEMBL4228892)
Affinity DataKd:  1.21E+3nMAssay Description:Binding affinity to recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) by surface plasmon resonance...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50460738(CHEMBL4225123)
Affinity DataKd:  4.78E+3nMAssay Description:Binding affinity to recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) by surface plasmon resonance...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50460742(CHEMBL4228634)
Affinity DataKd:  7.08E+3nMAssay Description:Binding affinity to recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) by surface plasmon resonance...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50460741(CHEMBL4229145)
Affinity DataKd:  7.40E+3nMAssay Description:Binding affinity to recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) by surface plasmon resonance...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50460740(CHEMBL4228404)
Affinity DataKd:  9.30E+3nMAssay Description:Binding affinity to recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) by surface plasmon resonance...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50501645(CHEMBL4084281)
Affinity DataKd:  1.73E+4nMAssay Description:Binding affinity to human N-terminal 6His-tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) after 150 secs by SPR-based bindin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50535041(CHEMBL1312860)
Affinity DataKd:  5.00E+4nMAssay Description:Binding affinity to biotinylated Avi tagged human DoT1L (2 to 416 residues) by SPR analysisMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50235302(CHEMBL4099771)
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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50075098(CHEMBL3414626 | US10143704, Compound A2 | US944606...)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50597868(CHEMBL5202438)
Affinity DataKi: <0.0700nMAssay Description:Binding affinity to DOT1L (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50075098(CHEMBL3414626 | US10143704, Compound A2 | US944606...)
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))
Epizyme

US Patent
LigandPNGBDBM50075098(CHEMBL3414626 | US10143704, Compound A2 | US944606...)
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))
Epizyme

US Patent
LigandPNGBDBM50536826(CHEMBL4590355)
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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396023(CHEMBL2169919)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50536819(CHEMBL4534250)
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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
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(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396980(CHEMBL2171169)
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
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396979(CHEMBL2171170)
Affinity DataKi:  0.760nMAssay 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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50396979(CHEMBL2171170)
Affinity DataKi:  0.800nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50443018(CHEMBL3087503)
Affinity DataKi:  1.10nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50443018(CHEMBL3087503)
Affinity DataKi:  1.10nMAssay Description:Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50443019(CHEMBL3087502)
Affinity DataKi:  1.30nMAssay Description:Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50443019(CHEMBL3087502)
Affinity DataKi:  1.30nMAssay Description:Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM92648(EPZ004450)
Affinity DataKi:  4nMAssay Description:Assay of DOT1L enzymatic activity were performed under balanced conditions using a radiometric assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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