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Assay Detail

CHEMBL3239091

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

Binding
Inhibition of human DGAT1
22
Total Activities
22
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 novel quinoline carboxylic acid series as DGAT1 inhibitors.
Zhou G, Ting PC, Wishart G, Zorn N, Aslanian RG, Lin M, Smith M, Walker SS, Cook J, Van Heek M, Lachowicz J.
Bioorg Med Chem Lett (2014) 24 : 1790 -1794
PubMed 24618302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.77 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233885 1 7.96
CHEMBL3233889 1 7.92
CHEMBL3233888 1 7.55
CHEMBL2036730 1 7.44
CHEMBL3233871 1 7.44
CHEMBL3233872 1 7.43
CHEMBL3233886 1 7.39
CHEMBL3233883 1 7.25
CHEMBL3233887 1 7.24
CHEMBL3233884 1 7.19
CHEMBL3233891 1 6.91
CHEMBL3233879 1 6.80
CHEMBL3233878 1 6.75
CHEMBL3233890 1 6.56
CHEMBL3233877 1 6.35
CHEMBL3233875 1 5.69
CHEMBL3233873 1 5.62
CHEMBL3233876 1 5.56
CHEMBL3233874 1 5.26
CHEMBL3233881 1 5.14
CHEMBL3233882 1 -
CHEMBL3233880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233885 IC50 = 11.0 nM 7.96
CHEMBL3233889 IC50 = 12.0 nM 7.92
CHEMBL3233888 IC50 = 28.0 nM 7.55
CHEMBL2036730 IC50 = 36.0 nM 7.44
CHEMBL3233871 IC50 = 36.0 nM 7.44
CHEMBL3233872 IC50 = 37.0 nM 7.43
CHEMBL3233886 IC50 = 41.0 nM 7.39
CHEMBL3233883 IC50 = 56.0 nM 7.25
CHEMBL3233887 IC50 = 58.0 nM 7.24
CHEMBL3233884 IC50 = 65.0 nM 7.19
CHEMBL3233891 IC50 = 122.0 nM 6.91
CHEMBL3233879 IC50 = 160.0 nM 6.80
CHEMBL3233878 IC50 = 180.0 nM 6.75
CHEMBL3233890 IC50 = 275.0 nM 6.56
CHEMBL3233877 IC50 = 448.0 nM 6.35
CHEMBL3233875 IC50 = 2030.0 nM 5.69
CHEMBL3233873 IC50 = 2393.0 nM 5.62
CHEMBL3233876 IC50 = 2735.0 nM 5.56
CHEMBL3233874 IC50 = 5548.0 nM 5.26
CHEMBL3233881 IC50 = 7257.0 nM 5.14
CHEMBL3233882 IC50 > 10000.0 nM -
CHEMBL3233880 IC50 > 10000.0 nM -