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Assay Detail

CHEMBL4233200

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

Binding
Inhibition of ACAT1 in human monocytes-derived macrophages reduction in cholesteryl oleate formation preincubated for 2 hrs followed by [14C]-oleic acid/sodium oleate addition measured after 2 hrs in absence of albumin by TLC assay
1
Total Activities
1
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

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

Publication

Design, synthesis and pharmacology of aortic-selective acyl-CoA: Cholesterol O-acyltransferase (ACAT/SOAT) inhibitors.
Shibuya K, Kawamine K, Miura T, Ozaki C, Edano T, Mizuno K, Yoshinaka Y, Tsunenari Y.
Bioorg Med Chem (2018) 26 : 4001 -4013
PubMed 29945757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101309 AVASIMIBE 2.0 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101309 AVASIMIBE IC50 = 25.0 nM 7.60