BDBM50541920 Cpi-1205::Lirametostat

SMILES COc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)n([C@H](C)C2CCN(CC(F)(F)F)CC2)c2ccccc12

InChI Key InChIKey=HPODOLXTMDHLLC-QGZVFWFLSA-N

Data  6 IC50  2 EC50

  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 8 hits for monomerid = 50541920   

TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  3.10nMAssay Description:Inhibition of EZH2 Y641F mutant in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataEC50:  32nMAssay 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 DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  31nMAssay Description:Inhibition of wild-type EZH2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  2.13E+4nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of wild-type EZH2 in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins follow...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  22nMAssay Description:Inhibition of EZH2 Y641F mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistone-lysine N-methyltransferase EZH1(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50541920(Cpi-1205 | Lirametostat)
Affinity DataIC50:  52nMAssay Description:Inhibition of EZH1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed