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Assay Detail

CHEMBL1768057

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

Binding
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using [14C]palmitic acid by TLC analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6009)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.
Qian Y, Wertheimer SJ, Ahmad M, Cheung AW, Firooznia F, Hamilton MM, Hayden S, Li S, Marcopulos N, McDermott L, Tan J, Yun W, Guo L, Pamidimukkala A, Chen Y, Huang KS, Ramsey GB, Whittard T, Conde-Knape K, Taub R, Rondinone CM, Tilley J, Bolin D.
J Med Chem (2011) 54 : 2433 -2446
PubMed 21413799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.18 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766813 1 6.18
CHEMBL1766806 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766813 EC50 = 660.0 nM 6.18
CHEMBL1766806 EC50 < 1000.0 nM -