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Assay Detail

CHEMBL1767986

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 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
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 26 6.25 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766888 1 7.03
CHEMBL1766886 1 6.86
CHEMBL1766892 1 6.78
CHEMBL1766893 1 6.72
CHEMBL1766887 1 6.67
CHEMBL1766812 1 6.66
CHEMBL1766891 1 6.66
CHEMBL1766882 1 6.64
CHEMBL1766810 1 6.44
CHEMBL1766805 1 6.44
CHEMBL1766806 1 6.43
CHEMBL1766890 1 6.42
CHEMBL1766889 1 6.39
CHEMBL1766811 1 6.31
CHEMBL1766816 1 6.27
CHEMBL1766813 1 6.18
CHEMBL1766809 1 5.97
CHEMBL473967 1 5.84
CHEMBL1766807 1 5.75
CHEMBL1766817 1 5.74
CHEMBL1766808 1 5.63
CHEMBL1766883 1 5.25
CHEMBL1766884 1 4.60
CHEMBL1766885 1 -
CHEMBL1766815 1 -
CHEMBL1766814 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766888 EC50 = 93.0 nM 7.03
CHEMBL1766886 EC50 = 138.0 nM 6.86
CHEMBL1766892 EC50 = 165.0 nM 6.78
CHEMBL1766893 EC50 = 190.0 nM 6.72
CHEMBL1766887 EC50 = 216.0 nM 6.67
CHEMBL1766812 EC50 = 220.0 nM 6.66
CHEMBL1766891 EC50 = 219.0 nM 6.66
CHEMBL1766882 EC50 = 228.0 nM 6.64
CHEMBL1766810 EC50 = 365.0 nM 6.44
CHEMBL1766805 EC50 = 362.0 nM 6.44
CHEMBL1766806 EC50 = 371.0 nM 6.43
CHEMBL1766890 EC50 = 378.0 nM 6.42
CHEMBL1766889 EC50 = 410.0 nM 6.39
CHEMBL1766811 EC50 = 493.0 nM 6.31
CHEMBL1766816 EC50 = 534.0 nM 6.27
CHEMBL1766813 EC50 = 661.0 nM 6.18
CHEMBL1766809 EC50 = 1070.0 nM 5.97
CHEMBL473967 EC50 = 1436.0 nM 5.84
CHEMBL1766807 EC50 = 1764.0 nM 5.75
CHEMBL1766817 EC50 = 1803.0 nM 5.74
CHEMBL1766808 EC50 = 2363.0 nM 5.63
CHEMBL1766883 EC50 = 5660.0 nM 5.25
CHEMBL1766884 EC50 = 25000.0 nM 4.60
CHEMBL1766885 EC50 > 25000.0 nM -
CHEMBL1766815 EC50 > 25000.0 nM -
CHEMBL1766814 EC50 > 25000.0 nM -