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Assay Detail

CHEMBL660744

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

Binding
Concentration required for the inhibition of cholesterol O-acyl transferase (ACAT) from rat liver
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL285)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

RP 70676: A potent systematically available inhibitor of acyl-CoA:cholesterol O-acyl transferase (ACAT)
Ashton M, Bridge A, Bush R, Dron D, Harris N, Jones G, Lythgoe D, Riddell D, Smith C
Bioorg Med Chem Lett (1992) 2 : 375 -380
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.60 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 8.00
CHEMBL127304 1 7.96
CHEMBL340487 1 7.85
CHEMBL264816 1 7.62
CHEMBL33780 1 7.60
CHEMBL127928 1 7.42
CHEMBL333544 1 7.36
CHEMBL330794 1 7.32
CHEMBL333228 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 10.0 nM 8.00
CHEMBL127304 IC50 = 11.0 nM 7.96
CHEMBL340487 IC50 = 14.0 nM 7.85
CHEMBL264816 IC50 = 24.0 nM 7.62
CHEMBL33780 IC50 = 25.0 nM 7.60
CHEMBL127928 IC50 = 38.0 nM 7.42
CHEMBL333544 IC50 = 44.0 nM 7.36
CHEMBL330794 IC50 = 48.0 nM 7.32
CHEMBL333228 IC50 = 50.0 nM 7.30