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Found 13 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EZH2' and Ligand = 'BDBM50075051'
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataKi:  24nMAssay Description:Competitive inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measure...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataKi:  24nMAssay Description:Competitive inhibition of wild type EZH2 in human PRC2 complex using S-adenosylmethionine as substrate by Michaelis-Menten plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  54nMAssay Description:Inhibition of EZH2 in human PRC2 complex preincubated for 30 mins followed by histone h3 peptide (21 to 44 residues) and S-adenosylmethionine and mea...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  54nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  54nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  54nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  80nMAssay Description:Inhibition of wild-type EZH2 in human OCI-LY19 cells assessed as reduction of H3K27me3 level after 96 hrs by ELISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  95nMAssay Description:Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50: <300nMAssay Description:Recombinant PRC2 Enzymes. Human PRC2 enzymes were purified as 4-component enzyme complexes co-expressed in Spodoptera frugiperda (sf9) cells using a ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50: <300nMAssay Description:eneral Procedure for Wild-Type PRC2 Enzyme Assay on Oligonucleosome Substrate. The assays was performed in a buffer consisting of 20 mM bicine (pH=7....More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  2.90E+3nMAssay Description:Inhibition of EZH2 in human OCILY19 cells assessed as reduction in H3K27me3 level treated for 96 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataIC50:  5.40E+4nMAssay Description:Inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measured after 90 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | EPZ005687 | US10273223, Compound C...)
Affinity DataEC50:  2.90E+3nMAssay Description:Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed