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Found 33 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EZH2' and Ligand = 'BDBM172038'
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataKi:  2.5nMAssay Description:Inhibition of wild-type human EZH2 by flash plate 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  0.340nMAssay Description:Inhibition of wild type EZH2 (unknown origin) by AlphaLISA 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  1nMAssay Description:Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count ba...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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  1nMAssay Description:Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based methodMore 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  2.45nMAssay Description:The inhibitory activity of the synthesized compounds above against EZH1 or EZH2 methyltransferase was measured. The experiments were consigned to Rea...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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  3.19nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  3.19nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  3.19nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated fo...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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  4nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH2(Rattus norvegicus)
Northwestern University

Curated by ChEMBL
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  4nMAssay Description:Inhibition of rat EZH2 using H3K27 peptides as substrateMore 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  11nMAssay Description:Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  11.1nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  13.0nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  13.0nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  13nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  13nMAssay Description:Inhibition of EZH2 (unknown origin) using H3K27me0 peptide substrate incubated for 3 hrs by HMT 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  13nMAssay 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  20nMAssay Description:Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA methodMore 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  20nMAssay 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  150nMAssay Description:Inhibition of EZH2 (unknown origin) using H3-derivede peptide (21 to 44) as substrate incubated for 60 min in presence of SAM by MTase-Glo assayMore 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataIC50:  200nMAssay Description:Inhibition of EZH2 (unknown origin) assessed as reduction in H3K27me3 level treated for 4 days by cellular assay based 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  64nMAssay Description:Inhibition of EZH2 Y641N mutant in human KARPAS-422 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  62nMAssay Description:Inhibition of EZH2 Y641N mutant in human SU-DHL-6 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  64nMAssay Description:Inhibition of EZH2 Y641S mutant in human SU-DHL-4 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataKd:  0.0935nMAssay Description:Inhibition of recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant using H3K27me0 peptide substrate incubated for 3 hrs b...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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  200nMAssay 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
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataKd:  12nMAssay Description:Inhibition of recombinant PRC2 complex (unknown origin) assessed as kd/ka using H3K27me0 peptide substrate incubated for 3 hrs by HMT 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  5nMAssay Description:Inhibition of EZH2 Y641F mutant in human WSUDLCL2 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  6nMAssay Description:Inhibition of EZH2 A677G mutant in human Pfeiffer cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  51nMAssay Description:Inhibition of EZH2 in human Daudi cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  46nMAssay Description:Inhibition of EZH2 in human U2932 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot 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
LigandPNGBDBM172038(US10155002, Compound 44 | US10647700, Compound EPZ...)
Affinity DataEC50:  46nMAssay Description:Inhibition of EZH2 in human Raji cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed