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Assay Detail

CHEMBL1954902

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

Binding
Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6009)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P.
ACS Med Chem Lett (2011) 2 : 407 -412
PubMed 24900321 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.68 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1835919 PF-04620110 1.0 1 8.10
CHEMBL473967 1 7.80
CHEMBL1952025 1 7.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1835919 PF-04620110 IC50 = 8.0 nM 8.10
CHEMBL473967 IC50 = 16.0 nM 7.80
CHEMBL1952025 IC50 = 71.0 nM 7.15