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Assay Detail

CHEMBL641890

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 by using J774 assay.
37
Total Activities
37
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 heterocyclic groups bioisosteric for an imidazole
Wilde RG, Billheimer JT, Germain SJ, Gillies PJ, Higley C, Kezar HS, Maduskuie TP, Shimshick ES, Wexler RR
Bioorg Med Chem Lett (1995) 5 : 167 -172
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.23 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 6.00
CHEMBL45913 1 5.82
CHEMBL48034 1 5.80
CHEMBL46017 1 5.69
CHEMBL49001 1 5.67
CHEMBL46174 1 5.59
CHEMBL45964 1 5.56
CHEMBL431934 1 5.55
CHEMBL291197 1 5.52
CHEMBL416998 1 5.51
CHEMBL300518 1 5.48
CHEMBL432696 1 5.46
CHEMBL298199 1 5.42
CHEMBL295286 1 5.38
CHEMBL45740 1 5.36
CHEMBL44610 1 5.36
CHEMBL46387 1 5.35
CHEMBL45184 1 5.34
CHEMBL49957 1 5.33
CHEMBL50554 1 5.32
CHEMBL416816 1 5.27
CHEMBL49398 1 5.26
CHEMBL43712 1 5.26
CHEMBL49367 1 5.22
CHEMBL45915 1 5.18
CHEMBL47863 1 5.16
CHEMBL45484 1 5.15
CHEMBL417187 1 5.08
CHEMBL49215 1 5.03
CHEMBL295251 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 1000.0 nM 6.00
CHEMBL45913 IC50 = 1530.0 nM 5.82
CHEMBL48034 IC50 = 1600.0 nM 5.80
CHEMBL46017 IC50 = 2060.0 nM 5.69
CHEMBL49001 IC50 = 2140.0 nM 5.67
CHEMBL46174 IC50 = 2580.0 nM 5.59
CHEMBL45964 IC50 = 2730.0 nM 5.56
CHEMBL431934 IC50 = 2790.0 nM 5.55
CHEMBL291197 IC50 = 3020.0 nM 5.52
CHEMBL416998 IC50 = 3100.0 nM 5.51
CHEMBL300518 IC50 = 3310.0 nM 5.48
CHEMBL432696 IC50 = 3500.0 nM 5.46
CHEMBL298199 IC50 = 3800.0 nM 5.42
CHEMBL295286 IC50 = 4180.0 nM 5.38
CHEMBL44610 IC50 = 4350.0 nM 5.36
CHEMBL45740 IC50 = 4370.0 nM 5.36
CHEMBL46387 IC50 = 4510.0 nM 5.35
CHEMBL45184 IC50 = 4540.0 nM 5.34
CHEMBL49957 IC50 = 4720.0 nM 5.33
CHEMBL50554 IC50 = 4800.0 nM 5.32
CHEMBL416816 IC50 = 5320.0 nM 5.27
CHEMBL49398 IC50 = 5470.0 nM 5.26
CHEMBL43712 IC50 = 5500.0 nM 5.26
CHEMBL49367 IC50 = 6020.0 nM 5.22
CHEMBL45915 IC50 = 6530.0 nM 5.18
CHEMBL47863 IC50 = 6960.0 nM 5.16
CHEMBL45484 IC50 = 7100.0 nM 5.15
CHEMBL417187 IC50 = 8330.0 nM 5.08
CHEMBL49215 IC50 = 9300.0 nM 5.03
CHEMBL295251 IC50 = 10600.0 nM 4.97
CHEMBL297676 IC50 = 11000.0 nM 4.96
CHEMBL46318 IC50 = 19100.0 nM 4.72
CHEMBL297991 IC50 = 25000.0 nM 4.60
CHEMBL48106 IC50 = 27300.0 nM 4.56
CHEMBL295608 IC50 = 54500.0 nM 4.26
CHEMBL295079 IC50 = 60000.0 nM 4.22
CHEMBL289648 IC50 = 72500.0 nM 4.14