Compile Data Set for Download or QSAR
Report error Found 9 Enz. Inhib. hit(s) for PDB: 8ESM
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 4nMAssay Description:Inhibition of DGAT1 (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human liver flag-tagged DGAT1 expressed in baculovirus infected insect cells after 2 hrs by SPAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 15nMpH: 7.4 T: 2°CAssay Description:The assay mixture contains test compound, membrane protein, and 1,2 dioleoyl-sn-glycerol in a 96-deep well plate. The reaction was started by adding ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/5/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 16nMAssay Description:Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 72nMAssay Description:Inhibition of human DGAT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 72nMAssay Description:Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataIC50: 113nMAssay Description:Inhibition of human DGAT1 expressed in baculovirus infected insect cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDiacylglycerol O-acyltransferase 1(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM27947(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Affinity DataEC50:  1.44E+3nMAssay Description:Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)