Assay Detail

CHEMBL2183593

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Binding

Inhibition of DGAT1 in human liver microsomes

ChEMBL ↗

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Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6009) ↗

Open DB target context

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Diacylglycerol O-acyltransferase 1 (CHEMBL6009) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Diacylglycerol O-acyltransferase 1

CHEMBL6009

Anchored from Assay target.

Protein identity Diacylglycerol O-acyltransferase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Tissue	Liver
Subcellular	Microsome
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6009) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J.
J Med Chem (2012) 55 : 10610 -10629
PubMed 23116186 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.16	7.16

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4297354	AZD-7687	1.0	1	7.16

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4297354	AZD-7687	IC50	=	70.0	nM	7.16