BDBM50017293 CHEMBL3287735::US10647700, Compound GSK126

SMILES CC[C@H](C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCNCC1)C(=O)NCc1c(C)cc(C)[nH]c1=O

InChI Key InChIKey=FKSFKBQGSFSOSM-UHFFFAOYSA-N

Data  8 KI  13 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 21 hits for monomerid = 50017293   

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

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 1nMAssay Description:Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of wild type EZH2 (unknown origin) by AlphaLlSA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 3.30nMAssay Description:Inhibition of human EZH2 using SAM as substrate incubated for 1 hr by microplate luminescence based HMT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 9.90nMAssay Description:Inhibition of wild-type 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)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 9.90nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 10nMAssay 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)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 2.70nMAssay Description:Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated fo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 5.5nMAssay Description:Inhibition of EZH2 Y641F mutant (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader 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)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 13nMAssay Description:Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2 [Y641F](Human)
Tarapeutics Science

US Patent
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 121nMAssay Description:Enzymatic activity assay was conducted using EZH2(Y641F) TR-FRET assay KIT from Cisbio company on compounds that were shown to be active in primary s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2021
Entry Details
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 280nMAssay Description:Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Korea Research Institute of Chemical Technology

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 16nMAssay Description:Inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED protein complex (unknown origin) using histone H3 peptide/S-adenosylmethionin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataIC50: 2nMAssay Description:Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count ba...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 Y641C mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 Y641N mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 Y641H mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 Y641F mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 A677G mutant assessed as H3K27me1 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human EZH2 A677G mutant assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50017293(CHEMBL3287735 | US10647700, Compound GSK126)
Affinity DataKi:  0.5nMAssay Description:Inhibition of human wild-type EZH2 assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed