Compile Data Set for Download or QSAR
Report error Found 373 of affinity data for UniProtKB/TrEMBL: Q8TEK3
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
Affinity DataKd:  0.0600nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataKd:  0.25nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50009672(AdoHcy | S-[1-(adenin-9-yl)-1,5-dideoxy-beta-D-rib...)
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50009672(AdoHcy | S-[1-(adenin-9-yl)-1,5-dideoxy-beta-D-rib...)
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
Affinity DataEC50:  9nMAssay Description:Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

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 Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataEC50:  9nMAssay Description:Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443022(CHEMBL3087499)
Affinity DataEC50:  9nMAssay Description:Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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 Depth
Date in BDB:
9/5/2020
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
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
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50235302(CHEMBL4099771)
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
In Depth
Date in BDB:
6/30/2019
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
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
In Depth
Date in BDB:
6/30/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50529550(CHEMBL4446126)
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
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50235301(CHEMBL4081752)
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
In Depth
Date in BDB:
6/30/2019
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50529551(CHEMBL4435508)
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
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50529554(CHEMBL4567485)
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
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
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
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50597863(CHEMBL5188291)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of DOT1L (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50597863(CHEMBL5188291)
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
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50597867(CHEMBL5176983)
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
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
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
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
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
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50536826(CHEMBL4590355)
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
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50536826(CHEMBL4590355)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of DOT1L (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM244792(US9446064, A5)
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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

LigandPNGBDBM244794(US9446064, A75)
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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM297391(US10112968, Compound A5 | (2R,3R,4S,5R)-2-(6-amino...)
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
In Depth
Date in BDB:
3/11/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50529544(CHEMBL4557484)
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
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM244795(US9446064, A86)
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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

LigandPNGBDBM244791(US9446064, A3)
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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM297390(US10112968, Compound A3 | (2R,3R,4S,5R)-2-(6-amino...)
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
In Depth
Date in BDB:
3/11/2019
Entry Details
Go to US Patent

LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM297389(US10112968, Compound A2 | (2R,3R,4S,5R)-2-(6-amino...)
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
In Depth
Date in BDB:
3/11/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
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
In Depth
Date in BDB:
3/30/2019
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
LigandPNGBDBM244796(US9446064, A87)
Affinity DataIC50: 0.800nMAssay 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
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

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