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Report error Found 13 Enz. Inhib. hit(s) for PDB: 4ER0
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataIC50:  14nMAssay Description:Inhibition of recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) using oligonucleosome as substrate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataIC50:  100nMAssay 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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataEC50:  9nMAssay Description:Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Baylor College of Medicine

Curated by ChEMBL
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
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)