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Assay Detail

CHEMBL2176154

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

Binding
Inhibition of ACAT activity in human MC65 cells using NBD-cholesterol staining after 48 hrs by fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MC65
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL2782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of Acyl-CoA: cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules.
Pokhrel L, Maezawa I, Nguyen TD, Chang KO, Jin LW, Hua DH.
J Med Chem (2012) 55 : 8969 -8973
PubMed 23025824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.14 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22373 CL-976 1 6.70
CHEMBL2170736 1 6.52
CHEMBL2170728 1 6.10
CHEMBL520938 1 5.92
CHEMBL2170821 1 5.85
CHEMBL2170832 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22373 CL-976 IC50 = 200.0 nM 6.70
CHEMBL2170736 IC50 = 300.0 nM 6.52
CHEMBL2170728 IC50 = 800.0 nM 6.10
CHEMBL520938 IC50 = 1200.0 nM 5.92
CHEMBL2170821 IC50 = 1400.0 nM 5.85
CHEMBL2170832 IC50 = 1800.0 nM 5.75