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Assay Detail

CHEMBL695550

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

Functional
In vitro ability to inhibit cholesterol biosynthesis in HepG2 cells in culture from [14C]mevalonate.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HepG2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 21 6.12 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15929 1 7.22
CHEMBL107546 1 7.10
CHEMBL108692 1 6.92
CHEMBL323953 1 6.85
CHEMBL107568 1 6.54
CHEMBL326241 1 6.30
CHEMBL322059 1 6.11
CHEMBL108867 1 6.00
CHEMBL107608 1 5.88
CHEMBL326008 1 5.83
CHEMBL111126 1 5.30
CHEMBL110608 1 5.30
CHEMBL324433 1 5.30
CHEMBL107885 1 5.00
CHEMBL321207 1 -
CHEMBL108144 1 -
CHEMBL111114 1 -
CHEMBL109348 1 -
CHEMBL109936 1 -
CHEMBL107838 1 -
CHEMBL326204 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15929 IC50 = 60.0 nM 7.22
CHEMBL107546 IC50 = 80.0 nM 7.10
CHEMBL108692 IC50 = 120.0 nM 6.92
CHEMBL323953 IC50 = 140.0 nM 6.85
CHEMBL107568 IC50 = 290.0 nM 6.54
CHEMBL326241 IC50 = 500.0 nM 6.30
CHEMBL322059 IC50 = 780.0 nM 6.11
CHEMBL108867 IC50 = 1000.0 nM 6.00
CHEMBL107608 IC50 = 1320.0 nM 5.88
CHEMBL326008 IC50 = 1480.0 nM 5.83
CHEMBL111126 IC50 = 5000.0 nM 5.30
CHEMBL110608 IC50 = 5000.0 nM 5.30
CHEMBL324433 IC50 = 5000.0 nM 5.30
CHEMBL107885 IC50 = 10000.0 nM 5.00
CHEMBL321207 IC50 > 10000.0 nM -
CHEMBL108144 IC50 > 10000.0 nM -
CHEMBL111114 IC50 > 10000.0 nM -
CHEMBL109348 IC50 > 10000.0 nM -
CHEMBL109936 IC50 > 10000.0 nM -
CHEMBL107838 IC50 > 10000.0 nM -
CHEMBL326204 IC50 > 10000.0 nM -