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TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335705(US9738630, Example 1 | 5-(Ethyl(tetrahydro-2H-pyra...)
Affinity DataEC50: <50nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335706(US9738630, Example 13 | 5-(Ethyl(tetrahydro-2H-pyr...)
Affinity DataEC50: <50nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335707(US9738630, Example 3 | N-((6,7-Dimethoxy-1-methyl-...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335708(US9738630, Example 4 | 5-(Ethyl(tetrahydro-2H-pyra...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335709(US9738630, Example 5 | 5-(Ethyl(tetrahydro-2H-pyra...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335711(US9738630, Example 6 | 5-(Ethyl(tetrahydro-2H-pyra...)
Affinity DataEC50: <50nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335712(US9738630, Example 7 | 5-(Ethyl(tetrahydro-2H-pyra...)
Affinity DataEC50: <500nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335713(US9738630, Example 8 | 4'-((1,1-Dioxidothiomorphol...)
Affinity DataEC50: <500nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335714(US9738630, Example 9 | tert-Butyl 4-(5-(1-(sec-but...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335715(US9738630, Example 10 | 1-(sec-Butyl)-3-methyl-N-(...)
Affinity DataEC50: <500nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335716(US9738630, Example 11 | N-((6,8-Difluoro-1-methyl-...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335717(US9738630, Example 12 | 5-(Ethyl(tetrahydro-2H-pyr...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335706(US9738630, Example 13 | 5-(Ethyl(tetrahydro-2H-pyr...)
Affinity DataEC50: <500nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335719(US9738630, Example 14 | 5-(Ethyl(tetrahydro-2H-pyr...)
Affinity DataEC50: <500nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335720(US9738630, Example 15 | 5-(Ethyl(tetrahydro-2H-pyr...)
Affinity DataEC50: <50nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335722(US9738630, Example 16 | N-((1,7-Dimethyl-3-oxo-2,3...)
Affinity DataEC50: <50nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335723(US9738630, Example 17 | 2,2-Dimethyl-N-((1-methyl-...)
Affinity DataEC50: <5.00E+3nMAssay Description:The effectiveness of compounds of the present invention as inhibitors of hitone methyl transferases can be readily tested by assays known to those sk...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataEC50:  1.05E+4nMAssay 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 Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50193657(CHEMBL3955994)
Affinity DataKd:  37nMAssay Description:Binding affinity to EZH2 (unknown origin) expressed in baculovirus infected SF9 cells co-expressing SUZ12/EED/RbAp48 complex by ITC analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/4/2018
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50149884(CHEMBL3770973)
Affinity DataEC50:  300nMAssay 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 Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541914(CHEMBL4635102)
Affinity DataEC50:  3.5nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataEC50:  200nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50563825(CHEMBL4794859)
Affinity DataEC50:  20nMAssay 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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50594130(CHEMBL5196227)
Affinity DataEC50: <1.00E+4nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50563827(CHEMBL4797333)
Affinity DataEC50:  39nMAssay 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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541917(CHEMBL4644363)
Affinity DataEC50: >1.00E+3nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541920(Lirametostat | Cpi-1205)
Affinity DataEC50:  28nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50574992(CHEMBL4850135)
Affinity DataKd:  0.0916nMAssay 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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM171998(US9090562, 2 | US10155002, Compound 2)
Affinity DataEC50:  700nMAssay 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 Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50546195(CHEMBL4777537)
Affinity DataKd:  116nMAssay Description:Binding affinity to EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50575222(CHEMBL4862681)
Affinity DataEC50:  21nMAssay 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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50149889(CHEMBL3769571)
Affinity DataEC50:  300nMAssay 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 Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50563826(CHEMBL4782143)
Affinity DataEC50:  38nMAssay 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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50574989(CHEMBL4856941)
Affinity DataKd:  32nMAssay 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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541902(CHEMBL4635809 | US11459315, Example 11)
Affinity DataEC50:  26nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50609427(CHEMBL5289464)
Affinity DataEC50:  140nMAssay Description:Induction of degradation of EZH2 degradation in human MDA-MB-453 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541911(CHEMBL4639983)
Affinity DataEC50:  1.80nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541910(CHEMBL4635863)
Affinity DataEC50:  3.5nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50563821(CHEMBL4780697)
Affinity DataEC50:  930nMAssay 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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50574994(CHEMBL4847620)
Affinity DataKd:  0.0693nMAssay 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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541897(CHEMBL4634390 | US11459315, Example 109)
Affinity DataEC50:  49nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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 Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50563820(CHEMBL4779123)
Affinity DataEC50:  110nMAssay 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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541908(CHEMBL4637958)
Affinity DataEC50:  1.80nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541913(CHEMBL4633923)
Affinity DataEC50:  6.30nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541905(CHEMBL4634677)
Affinity DataEC50:  6.70nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM50541906(CHEMBL4649131)
Affinity DataEC50:  2.40nMAssay 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 Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
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