BDBM50246927 CHEMBL4060447::US10570121, Example 127

SMILES COC(C1CCOC1)c1cc(Cl)c2CCN(Cc3c(OC)cc(C)[nH]c3=O)C(=O)c2c1Cl

InChI Key InChIKey=AZFROWZIMGUVBM-UHFFFAOYSA-N

Data  4 KI  8 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 12 hits for monomerid = 50246927   

TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataKi:  0.200nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataKi:  0.900nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataKi:  56nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataKi:  58nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [2-746,Y641N](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  2.20nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [2-746,Y641N](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  8nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2 [2-746,Y641N](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  165nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  16nMAssay 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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  110nMAssay 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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  391nMAssay 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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  391nMAssay 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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2 [2-746,Y641N](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM50246927(CHEMBL4060447 | US10570121, Example 127)
Affinity DataIC50:  892nMAssay Description:A. Compound preparation1. Prepare 10 mM stock solutions in 100% DMSO from solid material2. Serial dilute 10 mM compound stocks either 2 or 3-fold in ...More data for this Ligand-Target Pair
In DepthDetails US Patent