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Found 1616 from Constellation Pharmaceuticals
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM424912(2-(6-(((1R,2S)-2-((E)-1-phenylbut-1-en-2-yl)cyclop...)
Affinity DataKi:  6.10nMAssay Description:Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataKi:  9.60nMAssay Description:Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542482(US11274095, Example 14-Enantiomer-1 | US11274095, ...)
Affinity DataIC50:  0.0370nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542469(US11274095, Example 4)
Affinity DataIC50:  0.0380nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542475(7-chloro-N-((4-chloro-6-methyl-2-oxo-1,2-dihydropy...)
Affinity DataIC50:  0.0390nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542486(7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-...)
Affinity DataIC50:  0.0430nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542476(US11274095, Example 9)
Affinity DataIC50:  0.0540nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542470(US11274095, Example 5)
Affinity DataIC50:  0.0540nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541911(CHEMBL4639983)
Affinity DataIC50:  0.0570nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541907(CHEMBL4640994)
Affinity DataIC50:  0.0590nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541915(CHEMBL4638754)
Affinity DataIC50:  0.0600nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541912(CHEMBL4637572)
Affinity DataIC50:  0.0630nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541902(CHEMBL4635809 | US11459315, Example 11)
Affinity DataIC50:  0.0670nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541910(CHEMBL4635863)
Affinity DataIC50:  0.0720nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542481(US11274095, Example 13)
Affinity DataIC50:  0.0840nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542466(US11274095, Example 1)
Affinity DataIC50:  0.0910nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542480(US11274095, Example 12)
Affinity DataIC50:  0.0920nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541914(CHEMBL4635102)
Affinity DataIC50:  0.0920nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541909(CHEMBL4639913)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541913(CHEMBL4633923)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542473(US11274095, Example 7-Enantiomer-1 | US11274095, E...)
Affinity DataIC50:  0.120nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541903(CHEMBL4633932 | US11459315, Example 133)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541905(CHEMBL4634677)
Affinity DataIC50:  0.130nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542478(US11274095, Example 11-isomer-1 | US11274095, Exam...)
Affinity DataIC50:  0.140nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542471(US11274095, Example 6-Enantiomer-1 | US11274095, E...)
Affinity DataIC50:  0.140nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541908(CHEMBL4637958)
Affinity DataIC50:  0.140nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541906(CHEMBL4649131)
Affinity DataIC50:  0.160nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541895(CHEMBL4639616 | US11459315, Example 12)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542478(US11274095, Example 11-isomer-1 | US11274095, Exam...)
Affinity DataIC50:  0.180nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541904(CHEMBL4639569)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541916(CHEMBL4633053)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541918(CHEMBL4641325)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541919(CHEMBL4632988)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541917(CHEMBL4644363)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542477(US11274095, Example 10)
Affinity DataIC50:  0.202nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542484(US11274095, Example 16-Enantiomer-1 | US11274095, ...)
Affinity DataIC50:  0.310nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM542468(US11274095, Example 3)
Affinity DataIC50:  0.370nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM50541897(CHEMBL4634390 | US11459315, Example 109)
Affinity DataIC50:  0.490nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone acetyltransferase p300(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50542055(CHEMBL4636118 | US11274090, Example 22 Isomer 2)
Affinity DataIC50: <0.5nMAssay Description:Binding affinity to recombinant full length EP300 (unknown origin) incubated for 30 mins followed by H3(1 to 21) addition and measured after 1 hr by ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetHistone acetyltransferase p300(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50542060(CHEMBL4641354 | US11274090, Example 33 Isomer 2)
Affinity DataIC50: <0.5nMAssay Description:Binding affinity to recombinant full length EP300 (unknown origin) incubated for 30 mins followed by H3(1 to 21) addition and measured after 1 hr by ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM575058(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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574745(US11459315, Example 1 (isomer 1))
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574801(US11459315, Example 1 (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574835(US11459315, Example 2 (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

US Patent
LigandPNGBDBM574836(US11459315, Example 3 (isomer 1))
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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