Compile Data Set for Download or QSAR
Report error Found 228 Enz. Inhib. hit(s) with all data for entry = 10857
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574927((R)-5-chloro-1-(1-(1-cyclopropylpiperidin-4-yl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574928(1-((R)-1-((R)-1-cyclopropyl-3,3-difluoropiperidin-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574925(1-((R)-1-(4-(2-methoxyethoxy)cyclohex-yl)ethyl)-2-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574926(7-((R)-1-(4-(3-fluoroazetidin-1-yl)cyclohexyl)ethy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574931(2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574932((R)-6-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574930(2-methyl-1-((R)-1-((2S,4S)-1-methyl-2-(trifluorome...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574935(2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574936(1-((R)-1-(4-(3-methoxyazetidin-1-yl)cyclohexyl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574933(2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574934(2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574939(1-((R)-1-(5-(3,3-dimethylazetidin-1-yl)-1,3-dioxan...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574938(7-((R)-1-(4-(3-methoxyazetidin-1-yl)cyclohexyl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574911((R)-1-(1-(1-cyclopropylpiperidin-4-yl)ethyl)-6-flu...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574912((R)-1-(1-(1-cyclopropylpiperidin-4-yl)ethyl)-5-flu...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574910(1-((R)-1-((3S,4R)-1-cyclopropyl-3-fluoropiperidin-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574915(US11459315, Example 60 (isomer 2))
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574916((R)-1-(1-(4-(tert-butylamino)cyclohexyl)eth-yl)-2-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574913((R)-1-(1-(1-(2,2-difluoroethyl)piperidin-4-yl)ethy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574914(1-((R)-1-(4-(difluoromethoxy)cyclohex-yl)ethyl)-2-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574919(6-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574920((R)-1-(1-(1-(3-fluorocyclobutyl)piperidin-4-yl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574917(2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dih...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574923((R)-1-(1-(1-(3-fluorocyclobutyl)piperidin-4-yl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574924(1-((R)-1-(4-(2-methoxyethoxy)cyclohex-yl)ethyl)-2-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574921(1-((R)-1-(1-(3-fluorocyclobutyl)piperidin-4-yl)eth...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574922(1-((R)-1-(4-(3-fluoroazetidin-1-yl)cyclohexyl)ethy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574959((R)-6-fluoro-2-methyl-N-((6-methyl-4-(methylthio)-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574960(N-((4-((fluoromethyl)thio)-6-methyl-2-oxo-1,2-dihy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574957(1-((R)-1-(4-(3-ethoxyazetidin-1-yl)cyclohexyl)ethy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574958(1-((R)-1-(4-(3-ethoxyazetidin-1-yl)cyclohexyl)ethy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574963(1-((R)-1-(4-(3,3-difluoropyrrolidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574964(1-((R)-1-(4-(3-(difluoromethyl)azetidin-1-yl)cyclo...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574961(5-fluoro-1-((R)-1-(4-(3-methoxyazetidin-1-yl)cyclo...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574967(N-((4-(cyclopropylthio)-6-methyl-2-oxo-1,2-dihydro...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574968(1-((R)-1-(4-(3-cyclopropoxyazetidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574966(5-chloro-1-((R)-1-(4-(3-fluoroazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574971(7-((R)-1-(4-(3-cyclopropoxyazetidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574972((R)-4-chloro-2-methyl-N-((6-methyl-4-(methylthio)-...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574970(7-((R)-1-(4-(3-cyclopropoxyazetidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574943(1-((R)-1-(4-(3-fluoro-3-methylazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574944((R)-1-(1-(1-(3,3-difluorocyclobutyl)piperidin-4-yl...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574941(1-((R)-1-(4-((R)-3-fluoropyrrolidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574942(1-((R)-1-(4-((R)-3-fluoropyrrolidin-1-yl)cyclohexy...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574947(5-fluoro-1-((R)-1-(4-(3-fluoroazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574948(5-fluoro-1-((R)-1-(4-(3-fluoroazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574945(7-fluoro-1-((R)-1-(4-(3-fluoroazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574946((R)-6-fluoro-1-(1-(4-(3-fluoroazetidin-1-yl)cycloh...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574949(1-((R)-1-(5-(3,3-difluoroazetidin-1-yl)-1,3-dioxan...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574955(1-((R)-1-(4-(3-methoxy-3-methylazetidin-1-yl)cyclo...)
Affinity DataIC50: 0.5nMAssay Description:Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM PRC2 containing wt EZH2 (pentame...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/7/2022
Entry Details
US Patent

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