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Assay Detail

CHEMBL1022202

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

Binding
Inhibition of rat microsomal DGAT1 by liquid scintillography
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6129)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.
Birch AM, Birtles S, Buckett LK, Kemmitt PD, Smith GJ, Smith TJ, Turnbull AV, Wang SJ.
J Med Chem (2009) 52 : 1558 -1568
PubMed 19256504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.89 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473384 1 8.05
CHEMBL473967 1 7.72
CHEMBL515415 1 -
CHEMBL513992 1 -
CHEMBL473385 1 -
CHEMBL473386 1 -
CHEMBL473982 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473384 IC50 = 9.0 nM 8.05
CHEMBL473967 IC50 = 19.0 nM 7.72
CHEMBL515415 IC50 - -
CHEMBL513992 IC50 - -
CHEMBL473385 IC50 - -
CHEMBL473386 IC50 - -
CHEMBL473982 IC50 - -