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Assay Detail

CHEMBL646706

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

Binding
In vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase in rat hepatic microsomes was measured by using AIV assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: heterocyclic bioisosteres for the urea group in DuP 128
Wilde RG, Klaczkiewicz JD, Billheimer JT, Wexler RR, Gillies PJ
Bioorg Med Chem Lett (1995) 5 : 177 -180
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 8.00
CHEMBL50132 1 7.52
CHEMBL33780 1 7.52
CHEMBL298742 1 7.40
CHEMBL300506 1 7.40
CHEMBL53397 1 7.10
CHEMBL54217 1 7.10
CHEMBL50131 1 7.05
CHEMBL53942 1 7.05
CHEMBL54032 1 6.85
CHEMBL49993 1 6.66
CHEMBL301542 1 6.64
CHEMBL53728 1 6.52
CHEMBL51087 1 6.40
CHEMBL53613 1 6.20
CHEMBL51000 1 6.16
CHEMBL52911 1 6.16
CHEMBL50528 1 6.12
CHEMBL51827 1 5.85
CHEMBL50359 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 10.0 nM 8.00
CHEMBL50132 IC50 = 30.0 nM 7.52
CHEMBL33780 IC50 = 30.0 nM 7.52
CHEMBL298742 IC50 = 40.0 nM 7.40
CHEMBL300506 IC50 = 40.0 nM 7.40
CHEMBL53397 IC50 = 80.0 nM 7.10
CHEMBL54217 IC50 = 80.0 nM 7.10
CHEMBL50131 IC50 = 90.0 nM 7.05
CHEMBL53942 IC50 = 90.0 nM 7.05
CHEMBL54032 IC50 = 140.0 nM 6.85
CHEMBL49993 IC50 = 220.0 nM 6.66
CHEMBL301542 IC50 = 230.0 nM 6.64
CHEMBL53728 IC50 = 300.0 nM 6.52
CHEMBL51087 IC50 = 400.0 nM 6.40
CHEMBL53613 IC50 = 630.0 nM 6.20
CHEMBL51000 IC50 = 700.0 nM 6.16
CHEMBL52911 IC50 = 690.0 nM 6.16
CHEMBL50528 IC50 = 750.0 nM 6.12
CHEMBL51827 IC50 = 1400.0 nM 5.85
CHEMBL50359 IC50 = 50000.0 nM 4.30