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Assay Detail

CHEMBL646537

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

Binding
In vitro inhibition of intestinal Acyl coenzyme A:cholesterol acyltransferase in cholesterol-fed rabbits.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acyl-CoA:cholesterol acyltransferase (CHEMBL6141)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Substituted N,N-diphenyl ureas as potent inhibitors of acyl-CoA:Cholesterol acyltransferase (ACAT)
Trivedi B, Stoeber T, Stanfield R, Essenburg A, Hamelehle K, Krause B
Bioorg Med Chem Lett (1993) 3 : 259 -262
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.35 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88148 1 8.05
CHEMBL90110 1 8.05
CHEMBL87050 1 7.96
CHEMBL89694 1 7.96
CHEMBL313793 1 7.89
CHEMBL87183 1 7.82
CHEMBL86421 1 7.72
CHEMBL89642 1 7.58
CHEMBL89544 1 7.54
CHEMBL86802 1 7.50
CHEMBL86722 1 7.42
CHEMBL89843 1 7.18
CHEMBL264863 1 7.00
CHEMBL277986 CL-277082 1 6.92
CHEMBL89574 1 6.78
CHEMBL86681 1 6.60
CHEMBL177678 1 6.30
CHEMBL89873 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88148 IC50 = 9.0 nM 8.05
CHEMBL90110 IC50 = 9.0 nM 8.05
CHEMBL87050 IC50 = 11.0 nM 7.96
CHEMBL89694 IC50 = 11.0 nM 7.96
CHEMBL313793 IC50 = 13.0 nM 7.89
CHEMBL87183 IC50 = 15.0 nM 7.82
CHEMBL86421 IC50 = 19.0 nM 7.72
CHEMBL89642 IC50 = 26.0 nM 7.58
CHEMBL89544 IC50 = 29.0 nM 7.54
CHEMBL86802 IC50 = 32.0 nM 7.50
CHEMBL86722 IC50 = 38.0 nM 7.42
CHEMBL89843 IC50 = 66.0 nM 7.18
CHEMBL264863 IC50 = 100.0 nM 7.00
CHEMBL277986 CL-277082 IC50 = 120.0 nM 6.92
CHEMBL89574 IC50 = 168.0 nM 6.78
CHEMBL86681 IC50 = 250.0 nM 6.60
CHEMBL177678 IC50 = 500.0 nM 6.30
CHEMBL89873 IC50 = 910.0 nM 6.04