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Found 5401 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EZH2'
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  467nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227458(US9333217, 75)
Affinity DataIC50:  7.18E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  283nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  380nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  4.80E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM139690(US8895245, 75)
Affinity DataIC50:  8.95E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM139690(US8895245, 75)
Affinity DataIC50:  2.50E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM139690(US8895245, 75)
Affinity DataIC50:  4.10E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM139690(US8895245, 75)
Affinity DataIC50:  7.18E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM139690(US8895245, 75)
Affinity DataIC50:  7.56E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  467nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2 [Y641H](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  263nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2 [Y641S](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  283nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2 [Y641N](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  380nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2 [Y641F](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  4.80E+3nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190225(US9175331, 75)
Affinity DataIC50:  8.95E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL , was plated in a 384 well microtiter plate. Positive control (100% inhib...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [Y641S](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190225(US9175331, 75)
Affinity DataIC50:  2.50E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL , was plated in a 384 well microtiter plate. Positive control (100% inhib...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [Y641N](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190225(US9175331, 75)
Affinity DataIC50:  4.10E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL , was plated in a 384 well microtiter plate. Positive control (100% inhib...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [Y641F](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190225(US9175331, 75)
Affinity DataIC50:  7.18E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL , was plated in a 384 well microtiter plate. Positive control (100% inhib...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [Y641H](Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190225(US9175331, 75)
Affinity DataIC50:  7.56E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL , was plated in a 384 well microtiter plate. Positive control (100% inhib...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  467nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  263nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  283nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  380nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  4.80E+3nMpH: 7.6Assay Description:S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive c...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227458(US9333217, 75)
Affinity DataIC50:  8.95E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227458(US9333217, 75)
Affinity DataIC50:  7.56E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227458(US9333217, 75)
Affinity DataIC50:  2.50E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227458(US9333217, 75)
Affinity DataIC50:  4.10E+3nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50009672(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Affinity DataIC50:  263nMpH: 7.6Assay Description:Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibit...More data for this Ligand-Target Pair
LigandPNGBDBM291926(N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-...)
Affinity DataIC50:  30nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291927(5-fluoro-4-(((8-(2-methylpyridin-3-yl)-[1,2,4]tria...)
Affinity DataIC50:  13.8nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291927(5-fluoro-4-(((8-(2-methylpyridin-3-yl)-[1,2,4]tria...)
Affinity DataIC50:  50nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291928(5-fluoro-4-(((8-(2-(hydroxymethyl)pyridin-3-yl)-[1...)
Affinity DataIC50:  15.4nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291928(5-fluoro-4-(((8-(2-(hydroxymethyl)pyridin-3-yl)-[1...)
Affinity DataIC50:  59nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291929(3-(5-(((5-fluoro-3-hydroxy-2,3-dihydrobenzofuran-4...)
Affinity DataIC50:  11.7nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291929(3-(5-(((5-fluoro-3-hydroxy-2,3-dihydrobenzofuran-4...)
Affinity DataIC50:  38.9nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291930(8-(1,2-dimethyl-1H-imidazol-5-yl)-N-((5-fluoro-2,3...)
Affinity DataIC50:  67.2nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291930(8-(1,2-dimethyl-1H-imidazol-5-yl)-N-((5-fluoro-2,3...)
Affinity DataIC50:  223nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227710( N-((2,6-dimethyl-4-oxo-1,4-dihydropyridin-3-yl)me...)
Affinity DataIC50:  316nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227711(US9556157, 2 | n-((2,6-dimethyl-4-oxo-1,4-dihydrop...)
Affinity DataIC50:  32nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227712(US9556157, 3 | n-((5-amino-2,6-dimethyl-4-oxo-1,4-...)
Affinity DataIC50:  32nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227713(2-bromo-n-((2,6-dimethyl-4-oxo-1,4-dihydropyridin-...)
Affinity DataIC50:  160nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227711(US9556157, 2 | n-((2,6-dimethyl-4-oxo-1,4-dihydrop...)
Affinity DataIC50:  100nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM227712(US9556157, 3 | n-((5-amino-2,6-dimethyl-4-oxo-1,4-...)
Affinity DataIC50:  16nMpH: 8.0 T: 2°CAssay Description:Compounds contained herein were evaluated for their ability to inhibit the methyltransferase activity of EZH2 within the PRC2 complex. Human PRC2 com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291894(N-(benzofuran-4-ylmethyl)-8-(4-(4-methylpiperazin-...)
Affinity DataIC50:  29nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291895(N-(benzofuran-4-ylmethyl)-8-(4-(1-(pyrrolidin-1-yl...)
Affinity DataIC50:  18.5nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291895(N-(benzofuran-4-ylmethyl)-8-(4-(1-(pyrrolidin-1-yl...)
Affinity DataIC50:  21.4nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291896(N-(benzofuran-4-ylmethyl)-8-(6-(4-methylpiperazin-...)
Affinity DataIC50:  32.2nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM291896(N-(benzofuran-4-ylmethyl)-8-(6-(4-methylpiperazin-...)
Affinity DataIC50:  28.8nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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