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Assay Detail

CHEMBL1767987

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

Binding
Inhibition of human DGAT1 expressed in baculovirus infected insect cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 26 6.90 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766884 1 7.80
CHEMBL1766887 1 7.55
CHEMBL1766807 1 7.46
CHEMBL1766813 1 7.42
CHEMBL1766888 1 7.39
CHEMBL1766816 1 7.32
CHEMBL1766811 1 7.24
CHEMBL1766886 1 7.23
CHEMBL1766882 1 7.17
CHEMBL1766805 1 7.17
CHEMBL1766889 1 7.15
CHEMBL1766810 1 7.11
CHEMBL1766812 1 7.09
CHEMBL1766806 1 7.08
CHEMBL1766891 1 7.08
CHEMBL473967 1 6.95
CHEMBL1766890 1 6.89
CHEMBL1766808 1 6.89
CHEMBL1766892 1 6.87
CHEMBL1766893 1 6.78
CHEMBL1766885 1 6.70
CHEMBL1766883 1 6.62
CHEMBL1766809 1 6.56
CHEMBL1766817 1 6.49
CHEMBL1766814 1 4.82
CHEMBL1766815 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766884 IC50 = 16.0 nM 7.80
CHEMBL1766887 IC50 = 28.0 nM 7.55
CHEMBL1766807 IC50 = 35.0 nM 7.46
CHEMBL1766813 IC50 = 38.0 nM 7.42
CHEMBL1766888 IC50 = 41.0 nM 7.39
CHEMBL1766816 IC50 = 48.0 nM 7.32
CHEMBL1766811 IC50 = 57.0 nM 7.24
CHEMBL1766886 IC50 = 59.0 nM 7.23
CHEMBL1766882 IC50 = 68.0 nM 7.17
CHEMBL1766805 IC50 = 67.0 nM 7.17
CHEMBL1766889 IC50 = 71.0 nM 7.15
CHEMBL1766810 IC50 = 77.0 nM 7.11
CHEMBL1766812 IC50 = 82.0 nM 7.09
CHEMBL1766806 IC50 = 84.0 nM 7.08
CHEMBL1766891 IC50 = 84.0 nM 7.08
CHEMBL473967 IC50 = 113.0 nM 6.95
CHEMBL1766890 IC50 = 128.0 nM 6.89
CHEMBL1766808 IC50 = 128.0 nM 6.89
CHEMBL1766892 IC50 = 136.0 nM 6.87
CHEMBL1766893 IC50 = 165.0 nM 6.78
CHEMBL1766885 IC50 = 202.0 nM 6.70
CHEMBL1766883 IC50 = 237.0 nM 6.62
CHEMBL1766809 IC50 = 277.0 nM 6.56
CHEMBL1766817 IC50 = 325.0 nM 6.49
CHEMBL1766814 IC50 = 15100.0 nM 4.82
CHEMBL1766815 IC50 = 24700.0 nM 4.61