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Assay Detail

CHEMBL641703

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

Binding
In vitro inhibition of acyl coenzyme A:cholesterol acyltransferase 1, rat liver microsomal assay
35
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Substituted (1,2-diarylethyl)amide acyl-CoA:cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity.
Clader JW, Berger JG, Burrier RE, Davis HR, Domalski M, Dugar S, Kogan TP, Salisbury B, Vaccaro W.
J Med Chem (1995) 38 : 1600 -1607
PubMed 7752185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.83 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41240 1 6.82
CHEMBL40998 1 6.52
CHEMBL289558 1 6.46
CHEMBL42748 1 6.44
CHEMBL41186 1 6.44
CHEMBL40318 1 6.34
CHEMBL41350 1 6.30
CHEMBL441971 1 6.10
CHEMBL41233 3 6.05
CHEMBL296077 1 6.00
CHEMBL418627 1 5.82
CHEMBL42979 1 5.82
CHEMBL41351 1 5.80
CHEMBL39075 1 5.75
CHEMBL42230 1 5.75
CHEMBL38881 1 5.64
CHEMBL289997 1 5.62
CHEMBL42303 1 5.55
CHEMBL277986 CL-277082 1 5.50
CHEMBL44043 1 5.46
CHEMBL289124 1 5.40
CHEMBL296920 1 5.30
CHEMBL41208 1 5.30
CHEMBL44349 1 5.30
CHEMBL22373 CL-976 1 5.22
CHEMBL441970 1 5.00
CHEMBL295584 1 -
CHEMBL43805 1 -
CHEMBL40354 1 -
CHEMBL446610 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41240 IC50 = 150.0 nM 6.82
CHEMBL40998 IC50 = 300.0 nM 6.52
CHEMBL289558 IC50 = 350.0 nM 6.46
CHEMBL42748 IC50 = 360.0 nM 6.44
CHEMBL41186 IC50 = 360.0 nM 6.44
CHEMBL40318 IC50 = 460.0 nM 6.34
CHEMBL41350 IC50 = 500.0 nM 6.30
CHEMBL441971 IC50 = 800.0 nM 6.10
CHEMBL41233 IC50 = 900.0 nM 6.05
CHEMBL296077 IC50 = 1000.0 nM 6.00
CHEMBL41233 IC50 = 1400.0 nM 5.85
CHEMBL418627 IC50 = 1500.0 nM 5.82
CHEMBL42979 IC50 = 1500.0 nM 5.82
CHEMBL41351 IC50 = 1600.0 nM 5.80
CHEMBL39075 IC50 = 1800.0 nM 5.75
CHEMBL42230 IC50 = 1800.0 nM 5.75
CHEMBL41233 IC50 = 1800.0 nM 5.75
CHEMBL38881 IC50 = 2300.0 nM 5.64
CHEMBL289997 IC50 = 2400.0 nM 5.62
CHEMBL42303 IC50 = 2800.0 nM 5.55
CHEMBL277986 CL-277082 IC50 = 3200.0 nM 5.50
CHEMBL44043 IC50 = 3500.0 nM 5.46
CHEMBL289124 IC50 = 4000.0 nM 5.40
CHEMBL296920 IC50 = 5000.0 nM 5.30
CHEMBL44349 IC50 = 5000.0 nM 5.30
CHEMBL41208 IC50 = 5000.0 nM 5.30
CHEMBL22373 CL-976 IC50 = 6000.0 nM 5.22
CHEMBL441970 IC50 = 10000.0 nM 5.00
CHEMBL43805 IC50 > 10000.0 nM -
CHEMBL295584 IC50 > 10000.0 nM -
CHEMBL446610 IC50 > 10000.0 nM -
CHEMBL42634 IC50 > 10000.0 nM -
CHEMBL44233 IC50 > 10000.0 nM -
CHEMBL42197 IC50 > 10000.0 nM -
CHEMBL40354 IC50 > 10000.0 nM -