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Assay Detail

CHEMBL885668

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Binding
Inhibition of human ACAT1 expressed in Hi5 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BTI-TN-5B1-4
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.
An S, Park YD, Paik YK, Jeong TS, Lee WS.
Bioorg Med Chem Lett (2007) 17 : 1112 -1116
PubMed 17157006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.37 4.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395857 1 4.86
CHEMBL8951 1 4.65
CHEMBL276448 1 4.51
CHEMBL8805 1 4.27
CHEMBL9470 SHIKONIN 1 4.15
CHEMBL8806 1 4.11
CHEMBL9499 1 4.02
CHEMBL403516 ACETYLSHIKONIN 1 -
CHEMBL397309 BETA-HYDROXYISOVALERYLSHIKONIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395857 IC50 = 13800.0 nM 4.86
CHEMBL8951 IC50 = 22400.0 nM 4.65
CHEMBL276448 IC50 = 30700.0 nM 4.51
CHEMBL8805 IC50 = 53700.0 nM 4.27
CHEMBL9470 SHIKONIN IC50 = 70400.0 nM 4.15
CHEMBL8806 IC50 = 77600.0 nM 4.11
CHEMBL9499 IC50 = 94800.0 nM 4.02
CHEMBL403516 ACETYLSHIKONIN IC50 = 128900.0 nM -
CHEMBL397309 BETA-HYDROXYISOVALERYLSHIKONIN IC50 = 186900.0 nM -