BDBM50193709 CHEMBL3911017

SMILES Cc1noc(C)c1-c1cc(Cl)c2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl

InChI Key InChIKey=PDKDOPJQPKXNCT-UHFFFAOYSA-N

Data  5 KI  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 11 hits for monomerid = 50193709   

TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 15nMAssay Description:Inhibition of EZH2 in human KARPAS422 cells assessed as reduction in H3K27Me3 levels after 72 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/4/2018
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 17nMAssay Description:Inhibition of EZH2 in human KARPAS422 cells assessed as reduction in H3K27me3 level after 72 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2019
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 17nMAssay Description:Inhibition of wild type EZH2 in human KARPAS-422 cells assessed as effect on H3K27Me3 levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 5nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 1nMAssay Description:Inhibition of EZH2 (unknown origin) using 3H-SAM as substrate incubated for 1 hour by filter binding methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataIC50: 16nMAssay Description:Inhibition of EZH2 in HEK293T cells assessed as H3K27me3 levels incubated for 48 hrs by flow cytometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  0.700nMAssay Description:Inhibition of wild-type EZH2 (unknown origin) expressed in baculovirus infected SF9 cells co-expressing SUZ12/EED/RbAp48 complex using HeLa cells der...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/4/2018
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  0.700nMAssay Description:Binding affinity to EZH2 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  1nMAssay Description:Inhibition of wild type EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  1.20nMAssay Description:Inhibition of EZH2 Y641N mutant (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)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  3nMAssay Description:Inhibition of wild type EZH2 Y641N mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed