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Assay Detail

CHEMBL3136000

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

Binding
Inhibition of human DGAT1
17
Total Activities
17
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

Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1
Plowright AT, Barton P, Bennett S, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RDM, Ertan A, Gutierrez PM, Kemmitt PD, Leach AG, Svensson PH, Turnbull AV, Waring MJ
Medchemcomm (2013) 4 : 151 -158
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.18 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2036730 1 8.70
CHEMBL3133014 1 8.52
CHEMBL3133009 1 8.52
CHEMBL3133006 1 8.52
CHEMBL3133007 1 8.40
CHEMBL3133084 1 8.40
CHEMBL3133010 1 8.30
CHEMBL3133013 1 8.30
CHEMBL3133017 1 8.30
CHEMBL3133008 1 8.22
CHEMBL3133005 1 8.15
CHEMBL3133011 1 8.15
CHEMBL3133016 1 8.10
CHEMBL3133012 1 8.10
CHEMBL3133015 1 7.82
CHEMBL3132863 1 7.75
CHEMBL3133083 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2036730 IC50 = 2.0 nM 8.70
CHEMBL3133014 IC50 = 3.0 nM 8.52
CHEMBL3133009 IC50 = 3.0 nM 8.52
CHEMBL3133006 IC50 = 3.0 nM 8.52
CHEMBL3133007 IC50 = 4.0 nM 8.40
CHEMBL3133084 IC50 = 4.0 nM 8.40
CHEMBL3133010 IC50 = 5.0 nM 8.30
CHEMBL3133013 IC50 = 5.0 nM 8.30
CHEMBL3133017 IC50 = 5.0 nM 8.30
CHEMBL3133008 IC50 = 6.0 nM 8.22
CHEMBL3133005 IC50 = 7.0 nM 8.15
CHEMBL3133011 IC50 = 7.0 nM 8.15
CHEMBL3133016 IC50 = 8.0 nM 8.10
CHEMBL3133012 IC50 = 8.0 nM 8.10
CHEMBL3133015 IC50 = 15.0 nM 7.82
CHEMBL3132863 IC50 = 18.0 nM 7.75
CHEMBL3133083 IC50 = 140.0 nM 6.85