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Assay Detail

CHEMBL5243661

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

Binding
Inhibition of small intimal microsomal fraction of cholesterol-fed rabbit ACAT using [1-14C]oleoyl CoA incubated for 5 mins
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Small intestine
Subcellular Microsome
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Targeting Sterol <i>O</i>-Acyltransferase/Acyl-CoA:Cholesterol Acyltransferase (ACAT): A Perspective on Small-Molecule Inhibitors and Their Therapeutic Potential.
Bhattacharjee P, Rutland N, Iyer MR.
J Med Chem (2022) 65 : 16062 -16098
PubMed 36473091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.20 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102026 1 8.22
CHEMBL5275835 1 7.96
CHEMBL278856 1 7.89
CHEMBL296055 1 7.77
CHEMBL23602 1 7.70
CHEMBL405810 1 7.58
CHEMBL46423 NEVANIMIBE 2.0 1 7.43
CHEMBL295248 1 7.35
CHEMBL417531 1 7.34
CHEMBL542103 NEVANIMIBE HYDROCHLORIDE 2.0 1 7.28
CHEMBL42673 1 7.25
CHEMBL69844 1 7.24
CHEMBL5282347 1 7.24
CHEMBL5282801 1 7.20
CHEMBL22373 CL-976 1 6.85
CHEMBL5285031 1 6.80
CHEMBL113475 1 6.44
CHEMBL5266932 1 6.43
CHEMBL89873 1 6.04
CHEMBL5275997 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102026 IC50 = 6.0 nM 8.22
CHEMBL5275835 IC50 = 11.0 nM 7.96
CHEMBL278856 IC50 = 13.0 nM 7.89
CHEMBL296055 IC50 = 17.0 nM 7.77
CHEMBL23602 IC50 = 20.0 nM 7.70
CHEMBL405810 IC50 = 26.0 nM 7.58
CHEMBL46423 NEVANIMIBE IC50 = 37.0 nM 7.43
CHEMBL295248 IC50 = 45.0 nM 7.35
CHEMBL417531 IC50 = 46.0 nM 7.34
CHEMBL542103 NEVANIMIBE HYDROCHLORIDE IC50 = 52.0 nM 7.28
CHEMBL42673 IC50 = 56.0 nM 7.25
CHEMBL69844 IC50 = 58.0 nM 7.24
CHEMBL5282347 IC50 = 57.0 nM 7.24
CHEMBL5282801 IC50 = 63.0 nM 7.20
CHEMBL22373 CL-976 IC50 = 140.0 nM 6.85
CHEMBL5285031 IC50 = 160.0 nM 6.80
CHEMBL113475 IC50 = 360.0 nM 6.44
CHEMBL5266932 IC50 = 370.0 nM 6.43
CHEMBL89873 IC50 = 910.0 nM 6.04
CHEMBL5275997 IC50 = 1000.0 nM 6.00