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Assay Detail

CHEMBL641889

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

Binding
Inhibition of Acyl coenzyme A:cholesterol acyltransferase (ACAT) in J774 Macrophage cell culture
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Macrophage
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL4464)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing two heterocyclic head groups
Wilde RG, Billheimer JT
Bioorg Med Chem Lett (1995) 5 : 173 -176
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.02 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300883 1 8.00
CHEMBL300913 1 7.22
CHEMBL48164 1 7.22
CHEMBL49265 1 7.05
CHEMBL51643 1 7.00
CHEMBL50171 1 6.72
CHEMBL51282 1 6.43
CHEMBL431940 1 6.35
CHEMBL48383 1 6.16
CHEMBL297241 1 6.10
CHEMBL298651 1 6.03
CHEMBL48500 1 5.61
CHEMBL49855 1 5.52
CHEMBL299178 1 5.52
CHEMBL301495 1 5.46
CHEMBL445610 1 5.41
CHEMBL50471 1 5.41
CHEMBL48271 1 5.41
CHEMBL50381 1 5.26
CHEMBL301924 1 5.26
CHEMBL406757 1 5.18
CHEMBL48840 1 5.14
CHEMBL275305 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300883 IC50 = 10.0 nM 8.00
CHEMBL300913 IC50 = 60.0 nM 7.22
CHEMBL48164 IC50 = 60.0 nM 7.22
CHEMBL49265 IC50 = 90.0 nM 7.05
CHEMBL51643 IC50 = 100.0 nM 7.00
CHEMBL50171 IC50 = 190.0 nM 6.72
CHEMBL51282 IC50 = 370.0 nM 6.43
CHEMBL431940 IC50 = 450.0 nM 6.35
CHEMBL48383 IC50 = 690.0 nM 6.16
CHEMBL297241 IC50 = 790.0 nM 6.10
CHEMBL298651 IC50 = 940.0 nM 6.03
CHEMBL48500 IC50 = 2440.0 nM 5.61
CHEMBL49855 IC50 = 2990.0 nM 5.52
CHEMBL299178 IC50 = 3050.0 nM 5.52
CHEMBL301495 IC50 = 3430.0 nM 5.46
CHEMBL445610 IC50 = 3870.0 nM 5.41
CHEMBL50471 IC50 = 3920.0 nM 5.41
CHEMBL48271 IC50 = 3930.0 nM 5.41
CHEMBL50381 IC50 = 5500.0 nM 5.26
CHEMBL301924 IC50 = 5500.0 nM 5.26
CHEMBL406757 IC50 = 6550.0 nM 5.18
CHEMBL48840 IC50 = 7270.0 nM 5.14
CHEMBL275305 IC50 = 7960.0 nM 5.10