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Assay Detail

CHEMBL645934

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

Binding
Inhibitory activity against acyl coenzyme A:cholesterol acyltransferase in rat microsomes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel acyl-CoA:cholesterol acyltransferase inhibitors. Synthesis and biological activity of 3-quinolylurea derivatives.
Tawada H, Harcourt M, Kawamura N, Kajino M, Ishikawa E, Sugiyama Y, Ikeda H, Meguro K.
J Med Chem (1994) 37 : 2079 -2084
PubMed 8027989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.27 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64976 1 8.24
CHEMBL62332 1 8.05
CHEMBL62063 1 8.04
CHEMBL63019 1 8.03
CHEMBL63674 1 7.92
CHEMBL62876 1 7.92
CHEMBL65108 1 7.85
CHEMBL63408 1 7.85
CHEMBL304930 1 7.82
CHEMBL62894 1 7.78
CHEMBL62464 1 7.67
CHEMBL413330 1 7.66
CHEMBL291356 1 7.62
CHEMBL65602 1 7.55
CHEMBL63593 1 7.54
CHEMBL303527 1 7.04
CHEMBL278042 1 6.92
CHEMBL65347 1 6.90
CHEMBL433299 1 6.83
CHEMBL67373 1 6.80
CHEMBL67782 1 6.67
CHEMBL62463 1 6.27
CHEMBL292544 1 6.10
CHEMBL303281 1 6.06
CHEMBL63878 1 6.03
CHEMBL302238 1 5.89
CHEMBL305124 1 -
CHEMBL65368 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64976 IC50 = 5.8 nM 8.24
CHEMBL62332 IC50 = 8.9 nM 8.05
CHEMBL62063 IC50 = 9.2 nM 8.04
CHEMBL63019 IC50 = 9.3 nM 8.03
CHEMBL63674 IC50 = 12.0 nM 7.92
CHEMBL62876 IC50 = 12.0 nM 7.92
CHEMBL65108 IC50 = 14.0 nM 7.85
CHEMBL63408 IC50 = 14.0 nM 7.85
CHEMBL304930 IC50 = 15.0 nM 7.82
CHEMBL62894 IC50 = 16.8 nM 7.78
CHEMBL62464 IC50 = 21.2 nM 7.67
CHEMBL413330 IC50 = 21.7 nM 7.66
CHEMBL291356 IC50 = 24.0 nM 7.62
CHEMBL65602 IC50 = 28.0 nM 7.55
CHEMBL63593 IC50 = 28.7 nM 7.54
CHEMBL303527 IC50 = 90.6 nM 7.04
CHEMBL278042 IC50 = 121.0 nM 6.92
CHEMBL65347 IC50 = 125.0 nM 6.90
CHEMBL433299 IC50 = 149.0 nM 6.83
CHEMBL67373 IC50 = 160.0 nM 6.80
CHEMBL67782 IC50 = 215.0 nM 6.67
CHEMBL62463 IC50 = 534.0 nM 6.27
CHEMBL292544 IC50 = 800.0 nM 6.10
CHEMBL303281 IC50 = 864.0 nM 6.06
CHEMBL63878 IC50 = 929.0 nM 6.03
CHEMBL302238 IC50 = 1296.0 nM 5.89
CHEMBL305124 IC50 > 1000.0 nM -
CHEMBL65368 IC50 > 1000.0 nM -