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Assay Detail

CHEMBL809128

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Functional
In vitro inhibitory activity against pig liver microsomal squalene epoxidase
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Sus scrofa
Tissue Liver
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Squalene monooxygenase (CHEMBL3592)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(Aryloxy)methylsilane derivatives as new cholesterol biosynthesis inhibitors: synthesis and hypocholesterolemic activity of a new class of squalene epoxidase inhibitors.
Gotteland JP, Brunel I, Gendre F, Désiré J, Delhon A, Junquéro D, Oms P, Halazy S.
J Med Chem (1995) 38 : 3207 -3216
PubMed 7650673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.45 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27885 1 7.70
CHEMBL15929 1 7.70
CHEMBL107546 1 7.52
CHEMBL108692 1 7.52
CHEMBL324433 1 7.22
CHEMBL107568 1 7.16
CHEMBL107608 1 7.16
CHEMBL326008 1 7.16
CHEMBL322059 1 7.05
CHEMBL323953 1 7.00
CHEMBL110608 1 6.92
CHEMBL108144 1 6.89
CHEMBL111126 1 6.82
CHEMBL326241 1 6.82
CHEMBL326204 1 6.68
CHEMBL321207 1 6.40
CHEMBL111114 1 6.06
CHEMBL109348 1 6.00
CHEMBL111684 1 6.00
CHEMBL107838 1 5.52
CHEMBL108867 1 5.30
CHEMBL111609 1 5.30
CHEMBL107810 1 5.10
CHEMBL107885 1 5.10
CHEMBL108047 1 5.00
CHEMBL323395 1 4.70
CHEMBL109936 1 -
CHEMBL1144 PRAVASTATIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27885 IC50 = 20.0 nM 7.70
CHEMBL15929 IC50 = 20.0 nM 7.70
CHEMBL107546 IC50 = 30.0 nM 7.52
CHEMBL108692 IC50 = 30.0 nM 7.52
CHEMBL324433 IC50 = 60.0 nM 7.22
CHEMBL107568 IC50 = 70.0 nM 7.16
CHEMBL107608 IC50 = 70.0 nM 7.16
CHEMBL326008 IC50 = 70.0 nM 7.16
CHEMBL322059 IC50 = 90.0 nM 7.05
CHEMBL323953 IC50 = 100.0 nM 7.00
CHEMBL110608 IC50 = 120.0 nM 6.92
CHEMBL108144 IC50 = 130.0 nM 6.89
CHEMBL111126 IC50 = 150.0 nM 6.82
CHEMBL326241 IC50 = 150.0 nM 6.82
CHEMBL326204 IC50 = 210.0 nM 6.68
CHEMBL321207 IC50 = 400.0 nM 6.40
CHEMBL111114 IC50 = 870.0 nM 6.06
CHEMBL109348 IC50 = 1000.0 nM 6.00
CHEMBL111684 IC50 = 1000.0 nM 6.00
CHEMBL107838 IC50 = 3000.0 nM 5.52
CHEMBL108867 IC50 = 5000.0 nM 5.30
CHEMBL111609 IC50 = 5000.0 nM 5.30
CHEMBL107810 IC50 = 8000.0 nM 5.10
CHEMBL107885 IC50 = 8000.0 nM 5.10
CHEMBL108047 IC50 = 10000.0 nM 5.00
CHEMBL323395 IC50 = 20000.0 nM 4.70
CHEMBL109936 IC50 > 10000.0 nM -
CHEMBL1144 PRAVASTATIN IC50 > 10000.0 nM -