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Assay Detail

CHEMBL3136463

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

Binding
Inhibition of recombinant human DGAT1 expressed in sf9 cell membrane assessed as inhibition of radioactive trioleoylglycerol formation after 30 mins by liquid scintillation counting
16
Total Activities
16
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

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 the discovery of AZD2353
Waring MJ, Birch AM, Birtles S, Buckett LK, Butlin RJ, Campbell L, Gutierrez PM, Kemmitt PD, Leach AG, MacFaul PA, O'Donnell C, Turnbull AV
Medchemcomm (2013) 4 : 159 -164
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.89 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3133098 1 8.20
CHEMBL3133093 1 8.10
CHEMBL3133091 1 8.10
CHEMBL3133092 1 7.90
CHEMBL3133087 1 7.70
CHEMBL3133088 1 7.60
CHEMBL3133094 1 7.00
CHEMBL3133095 1 6.90
CHEMBL3133096 1 6.90
CHEMBL3133089 1 6.70
CHEMBL3133086 1 6.50
CHEMBL3133100 1 6.20
CHEMBL3133090 1 6.10
CHEMBL3133097 1 5.90
CHEMBL3133085 1 5.20
CHEMBL3133099 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3133098 IC50 = 6.31 nM 8.20
CHEMBL3133093 IC50 = 7.943 nM 8.10
CHEMBL3133091 IC50 = 7.943 nM 8.10
CHEMBL3133092 IC50 = 12.59 nM 7.90
CHEMBL3133087 IC50 = 19.95 nM 7.70
CHEMBL3133088 IC50 = 25.12 nM 7.60
CHEMBL3133094 IC50 = 100.0 nM 7.00
CHEMBL3133095 IC50 = 125.89 nM 6.90
CHEMBL3133096 IC50 = 125.89 nM 6.90
CHEMBL3133089 IC50 = 199.53 nM 6.70
CHEMBL3133086 IC50 = 316.23 nM 6.50
CHEMBL3133100 IC50 = 630.96 nM 6.20
CHEMBL3133090 IC50 = 794.33 nM 6.10
CHEMBL3133097 IC50 = 1258.93 nM 5.90
CHEMBL3133085 IC50 = 6309.57 nM 5.20
CHEMBL3133099 IC50 = 6309.57 nM 5.20