BDBM50246942 CHEMBL4061264::US10570121, Example 163

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

InChI Key InChIKey=RSWZEDXOZHLOGZ-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 = 50246942   

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

US Patent
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataKi:  0.400nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataKi:  0.400nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataKi:  21nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataKi:  148nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  4nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  4nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  2.97E+3nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  47nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  1.10E+3nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  494nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  1.09E+3nMAssay 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
LigandPNGBDBM50246942(CHEMBL4061264 | US10570121, Example 163)
Affinity DataIC50:  86nMAssay 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