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Assay Detail

CHEMBL1936449

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

Binding
Inhibition of ACAT1- mediated cholesteryl ester synthesis in macrophages
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Conformationally restricted analog and biotin-labeled probe based on beauveriolide III.
Doi T, Muraoka T, Ohshiro T, Matsuda D, Yoshida M, Takahashi T, Omura S, Tomoda H.
Bioorg Med Chem Lett (2012) 22 : 696 -699
PubMed 22079027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.72 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449307 1 7.70
CHEMBL505016 1 7.40
CHEMBL1933478 1 6.96
CHEMBL1933480 1 6.55
CHEMBL1933479 1 6.51
CHEMBL409855 BEAUVERIOLIDE III 1 6.39
CHEMBL516093 BEAUVERIOLIDE I 1 6.11
CHEMBL1933481 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449307 IC50 = 20.0 nM 7.70
CHEMBL505016 IC50 = 40.0 nM 7.40
CHEMBL1933478 IC50 = 110.0 nM 6.96
CHEMBL1933480 IC50 = 280.0 nM 6.55
CHEMBL1933479 IC50 = 310.0 nM 6.51
CHEMBL409855 BEAUVERIOLIDE III IC50 = 410.0 nM 6.39
CHEMBL516093 BEAUVERIOLIDE I IC50 = 780.0 nM 6.11
CHEMBL1933481 IC50 = 800.0 nM 6.10