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Assay Detail

CHEMBL3222770

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

Binding
Inhibition of human recombinant DGAT1 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A after 30 mins by scintillation counting
34
Total Activities
34
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

Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors
Goldberg FW, Birch AM, Leach AG, Groombridge SD, Snelson WL, Gutierrez PM, Hammond CD, Birtles S, Buckett LK
Medchemcomm (2013) 4 : 165 -174
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.50 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3222247 1 8.30
CHEMBL3133098 1 8.20
CHEMBL3222262 1 8.11
CHEMBL3222257 1 8.00
CHEMBL3222250 1 8.00
CHEMBL3222245 1 7.80
CHEMBL3222259 1 7.80
CHEMBL3222256 1 7.80
CHEMBL3222253 1 7.80
CHEMBL3222258 1 7.70
CHEMBL3222232 1 7.70
CHEMBL3222249 1 7.70
CHEMBL3222230 1 7.60
CHEMBL3222248 1 7.60
CHEMBL3222231 1 7.50
CHEMBL3222239 1 7.50
CHEMBL3222238 1 7.50
CHEMBL3222261 1 7.50
CHEMBL3222235 1 7.40
CHEMBL3222242 1 7.40
CHEMBL3222255 1 7.40
CHEMBL3222233 1 7.40
CHEMBL3222237 1 7.30
CHEMBL3222244 1 7.30
CHEMBL3222234 1 7.30
CHEMBL3222243 1 7.30
CHEMBL3222246 1 7.30
CHEMBL3222236 1 7.30
CHEMBL3222241 1 7.20
CHEMBL3222251 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3222247 IC50 = 5.012 nM 8.30
CHEMBL3133098 IC50 = 6.31 nM 8.20
CHEMBL3222262 IC50 = 7.7 nM 8.11
CHEMBL3222257 IC50 = 10.0 nM 8.00
CHEMBL3222250 IC50 = 10.0 nM 8.00
CHEMBL3222245 IC50 = 15.85 nM 7.80
CHEMBL3222259 IC50 = 15.85 nM 7.80
CHEMBL3222256 IC50 = 15.85 nM 7.80
CHEMBL3222253 IC50 = 15.85 nM 7.80
CHEMBL3222258 IC50 = 19.95 nM 7.70
CHEMBL3222232 IC50 = 19.95 nM 7.70
CHEMBL3222249 IC50 = 19.95 nM 7.70
CHEMBL3222230 IC50 = 25.12 nM 7.60
CHEMBL3222248 IC50 = 25.12 nM 7.60
CHEMBL3222239 IC50 = 31.62 nM 7.50
CHEMBL3222238 IC50 = 31.62 nM 7.50
CHEMBL3222261 IC50 = 31.62 nM 7.50
CHEMBL3222231 IC50 = 31.62 nM 7.50
CHEMBL3222235 IC50 = 39.81 nM 7.40
CHEMBL3222242 IC50 = 39.81 nM 7.40
CHEMBL3222255 IC50 = 39.81 nM 7.40
CHEMBL3222233 IC50 = 39.81 nM 7.40
CHEMBL3222243 IC50 = 50.12 nM 7.30
CHEMBL3222236 IC50 = 50.12 nM 7.30
CHEMBL3222246 IC50 = 50.12 nM 7.30
CHEMBL3222234 IC50 = 50.12 nM 7.30
CHEMBL3222244 IC50 = 50.12 nM 7.30
CHEMBL3222237 IC50 = 50.12 nM 7.30
CHEMBL3222241 IC50 = 63.1 nM 7.20
CHEMBL3222251 IC50 = 79.43 nM 7.10
CHEMBL3222240 IC50 = 79.43 nM 7.10
CHEMBL3222260 IC50 = 79.43 nM 7.10
CHEMBL3222254 IC50 = 251.19 nM 6.60
CHEMBL3222252 IC50 = 316.23 nM 6.50