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Assay Detail

CHEMBL2183210

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of plasma triacylglycerol excursion in 14 hrs fasted Han-Wistar rat at administered orally 2 hrs before bolus corn oil administration measured 1.5 hrs post corn oil challenge by oral lipid tolerance test relative to control
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Plasma
Confidence 1 — Organism
Curated By Autocuration

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

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 7.38 7.38
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297354 AZD-7687 1.0 2 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297354 AZD-7687 IC50 = 42.0 nM 7.38
CHEMBL4297354 AZD-7687 Inhibition - % -