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Assay Detail

CHEMBL2343709

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

Binding
Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
35
Total Activities
35
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

Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
Ting PC, Lee JF, Zorn N, Kim HM, Aslanian RG, Lin M, Smith M, Walker SS, Cook J, Van Heek M, Lachowicz J.
Bioorg Med Chem Lett (2013) 23 : 985 -988
PubMed 23317570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.97 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2334097 1 7.62
CHEMBL2334088 1 7.60
CHEMBL2334082 1 7.54
CHEMBL2334075 1 7.48
CHEMBL1766813 1 7.42
CHEMBL2334093 1 7.41
CHEMBL2334092 1 7.40
CHEMBL2334085 1 7.39
CHEMBL2334095 1 7.38
CHEMBL2334094 1 7.29
CHEMBL2334100 1 7.28
CHEMBL2334081 1 7.27
CHEMBL2334089 1 7.26
CHEMBL2334091 1 7.22
CHEMBL2334098 1 7.16
CHEMBL2334078 1 7.10
CHEMBL2334096 1 6.99
CHEMBL2334079 1 6.94
CHEMBL2334070 1 6.92
CHEMBL2334071 1 6.92
CHEMBL2334068 1 6.90
CHEMBL2334090 1 6.84
CHEMBL2334084 1 6.83
CHEMBL2334069 1 6.82
CHEMBL2334087 1 6.72
CHEMBL2334077 1 6.71
CHEMBL2334072 1 6.62
CHEMBL2334101 1 6.55
CHEMBL2334099 1 6.51
CHEMBL2334076 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2334097 IC50 = 24.0 nM 7.62
CHEMBL2334088 IC50 = 25.0 nM 7.60
CHEMBL2334082 IC50 = 29.0 nM 7.54
CHEMBL2334075 IC50 = 33.0 nM 7.48
CHEMBL1766813 IC50 = 38.0 nM 7.42
CHEMBL2334093 IC50 = 39.0 nM 7.41
CHEMBL2334092 IC50 = 40.0 nM 7.40
CHEMBL2334085 IC50 = 41.0 nM 7.39
CHEMBL2334095 IC50 = 42.0 nM 7.38
CHEMBL2334094 IC50 = 51.0 nM 7.29
CHEMBL2334100 IC50 = 52.0 nM 7.28
CHEMBL2334081 IC50 = 54.0 nM 7.27
CHEMBL2334089 IC50 = 55.0 nM 7.26
CHEMBL2334091 IC50 = 60.0 nM 7.22
CHEMBL2334098 IC50 = 70.0 nM 7.16
CHEMBL2334078 IC50 = 79.0 nM 7.10
CHEMBL2334096 IC50 = 103.0 nM 6.99
CHEMBL2334079 IC50 = 116.0 nM 6.94
CHEMBL2334071 IC50 = 120.0 nM 6.92
CHEMBL2334070 IC50 = 119.0 nM 6.92
CHEMBL2334068 IC50 = 125.0 nM 6.90
CHEMBL2334090 IC50 = 145.0 nM 6.84
CHEMBL2334084 IC50 = 149.0 nM 6.83
CHEMBL2334069 IC50 = 152.0 nM 6.82
CHEMBL2334087 IC50 = 190.0 nM 6.72
CHEMBL2334077 IC50 = 194.0 nM 6.71
CHEMBL2334072 IC50 = 240.0 nM 6.62
CHEMBL2334101 IC50 = 280.0 nM 6.55
CHEMBL2334099 IC50 = 311.0 nM 6.51
CHEMBL2334076 IC50 = 344.0 nM 6.46
CHEMBL2334083 IC50 = 392.0 nM 6.41
CHEMBL2334080 IC50 = 460.0 nM 6.34
CHEMBL2334074 IC50 = 482.0 nM 6.32
CHEMBL2334086 IC50 = 513.0 nM 6.29
CHEMBL2334073 IC50 = 774.0 nM 6.11