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Assay Detail

CHEMBL646054

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

Binding
Concentration required for the in vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase (ACAT) in liver microsomes isolated from cholesterol-fed rats
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 12. Syntheses and biological activity of structurally novel tetrazole amides
O'Brien PM, Sliskovic DR, Anderson MK, Bousley RF, Krause BR, Stanfield RL
Bioorg Med Chem Lett (1995) 5 : 289 -294
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.43 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99056 1 7.10
CHEMBL317244 1 7.10
CHEMBL22373 CL-976 1 6.96
CHEMBL101629 1 6.92
CHEMBL100936 1 6.85
CHEMBL318373 1 6.75
CHEMBL98716 1 6.72
CHEMBL101601 1 6.62
CHEMBL101883 1 6.60
CHEMBL100697 1 6.51
CHEMBL101278 1 6.46
CHEMBL98742 1 6.46
CHEMBL316471 1 6.42
CHEMBL99029 1 6.42
CHEMBL97926 1 6.36
CHEMBL100993 1 6.34
CHEMBL101937 1 6.31
CHEMBL100533 1 6.29
CHEMBL98598 1 6.27
CHEMBL101865 1 6.22
CHEMBL101977 1 6.19
CHEMBL321102 1 6.09
CHEMBL98365 1 6.07
CHEMBL98612 1 5.77
CHEMBL45333 1 5.03
CHEMBL317503 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99056 IC50 = 80.0 nM 7.10
CHEMBL317244 IC50 = 80.0 nM 7.10
CHEMBL22373 CL-976 IC50 = 110.0 nM 6.96
CHEMBL101629 IC50 = 120.0 nM 6.92
CHEMBL100936 IC50 = 140.0 nM 6.85
CHEMBL318373 IC50 = 180.0 nM 6.75
CHEMBL98716 IC50 = 190.0 nM 6.72
CHEMBL101601 IC50 = 240.0 nM 6.62
CHEMBL101883 IC50 = 250.0 nM 6.60
CHEMBL100697 IC50 = 310.0 nM 6.51
CHEMBL101278 IC50 = 350.0 nM 6.46
CHEMBL98742 IC50 = 350.0 nM 6.46
CHEMBL316471 IC50 = 380.0 nM 6.42
CHEMBL99029 IC50 = 380.0 nM 6.42
CHEMBL97926 IC50 = 440.0 nM 6.36
CHEMBL100993 IC50 = 460.0 nM 6.34
CHEMBL101937 IC50 = 490.0 nM 6.31
CHEMBL100533 IC50 = 510.0 nM 6.29
CHEMBL98598 IC50 = 540.0 nM 6.27
CHEMBL101865 IC50 = 600.0 nM 6.22
CHEMBL101977 IC50 = 650.0 nM 6.19
CHEMBL321102 IC50 = 810.0 nM 6.09
CHEMBL98365 IC50 = 850.0 nM 6.07
CHEMBL98612 IC50 = 1700.0 nM 5.77
CHEMBL45333 IC50 = 9400.0 nM 5.03
CHEMBL317503 IC50 > 10000.0 nM -