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Found 6 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EZH2' and Ligand = 'BDBM50110355'
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataIC50: <1nMAssay Description:Inhibition of wild-type EZH2 in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins follow...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataIC50:  2nMAssay 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))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of EZH2 Y641F mutant in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataIC50:  3nMAssay 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))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataIC50:  80nMAssay 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))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50110355(CHEMBL3605457)
Affinity DataEC50:  80nMAssay Description:Inhibition of EZH2 in human HeLa cells assessed as inhibition of trimethylation of H3K27 after 72 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed