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Assay Detail

CHEMBL3294188

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

Binding
Inhibition of human DGAT1 expressed in Sf9 insect cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA substrate by scintillation counting analysis
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
Zhou G, Zorn N, Ting P, Aslanian R, Lin M, Cook J, Lachowicz J, Lin A, Smith M, Hwa J, van Heek M, Walker S.
ACS Med Chem Lett (2014) 5 : 544 -549
PubMed 24900877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.60 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287876 1 7.70
CHEMBL3287878 1 7.70
CHEMBL3287884 1 7.50
CHEMBL3287875 1 7.48
CHEMBL2036730 1 7.44
CHEMBL3233872 1 7.43
CHEMBL3287865 1 7.37
CHEMBL3287890 1 7.28
CHEMBL3287898 1 7.19
CHEMBL3233884 1 7.19
CHEMBL3287874 1 7.16
CHEMBL3287897 1 7.07
CHEMBL3287864 1 7.04
CHEMBL3287882 1 7.04
CHEMBL3287894 1 7.00
CHEMBL3287867 1 6.96
CHEMBL3287896 1 6.96
CHEMBL3287877 1 6.85
CHEMBL3287883 1 6.64
CHEMBL3287893 1 6.54
CHEMBL3287886 1 6.52
CHEMBL3287887 1 6.44
CHEMBL3287892 1 6.39
CHEMBL3287868 1 6.35
CHEMBL3287866 1 6.28
CHEMBL3286412 1 6.25
CHEMBL3287869 1 6.24
CHEMBL3287881 1 6.24
CHEMBL3287889 1 6.20
CHEMBL3287895 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287876 IC50 = 20.0 nM 7.70
CHEMBL3287878 IC50 = 20.0 nM 7.70
CHEMBL3287884 IC50 = 32.0 nM 7.50
CHEMBL3287875 IC50 = 33.0 nM 7.48
CHEMBL2036730 IC50 = 36.0 nM 7.44
CHEMBL3233872 IC50 = 37.0 nM 7.43
CHEMBL3287865 IC50 = 43.0 nM 7.37
CHEMBL3287890 IC50 = 52.0 nM 7.28
CHEMBL3287898 IC50 = 64.0 nM 7.19
CHEMBL3233884 IC50 = 65.0 nM 7.19
CHEMBL3287874 IC50 = 69.0 nM 7.16
CHEMBL3287897 IC50 = 85.0 nM 7.07
CHEMBL3287882 IC50 = 91.0 nM 7.04
CHEMBL3287864 IC50 = 91.0 nM 7.04
CHEMBL3287894 IC50 = 100.0 nM 7.00
CHEMBL3287867 IC50 = 110.0 nM 6.96
CHEMBL3287896 IC50 = 110.0 nM 6.96
CHEMBL3287877 IC50 = 140.0 nM 6.85
CHEMBL3287883 IC50 = 230.0 nM 6.64
CHEMBL3287893 IC50 = 290.0 nM 6.54
CHEMBL3287886 IC50 = 300.0 nM 6.52
CHEMBL3287887 IC50 = 360.0 nM 6.44
CHEMBL3287892 IC50 = 410.0 nM 6.39
CHEMBL3287868 IC50 = 450.0 nM 6.35
CHEMBL3287866 IC50 = 530.0 nM 6.28
CHEMBL3286412 IC50 = 560.0 nM 6.25
CHEMBL3287869 IC50 = 580.0 nM 6.24
CHEMBL3287881 IC50 = 580.0 nM 6.24
CHEMBL3287889 IC50 = 630.0 nM 6.20
CHEMBL3287895 IC50 = 640.0 nM 6.19
CHEMBL3287891 IC50 = 860.0 nM 6.07
CHEMBL3287885 IC50 = 950.0 nM 6.02
CHEMBL3287873 IC50 = 1700.0 nM 5.77
CHEMBL3287861 IC50 = 1900.0 nM 5.72
CHEMBL3288152 IC50 = 2900.0 nM 5.54
CHEMBL3287862 IC50 = 3100.0 nM 5.51
CHEMBL3287888 IC50 = 3100.0 nM 5.51
CHEMBL3287870 IC50 = 3700.0 nM 5.43
CHEMBL3287880 IC50 = 6100.0 nM 5.21
CHEMBL3287860 IC50 > 10000.0 nM -
CHEMBL3287879 IC50 > 10000.0 nM -
CHEMBL3287859 IC50 > 10000.0 nM -
CHEMBL3287858 IC50 > 10000.0 nM -
CHEMBL3287863 IC50 > 10000.0 nM -
CHEMBL3287871 IC50 > 10000.0 nM -
CHEMBL3287872 IC50 > 10000.0 nM -