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Assay Detail

CHEMBL693810

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Functional
In vitro inhibition of cholesterol biosynthesis in human HepG2 cells.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HepG2
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Squalene monooxygenase (CHEMBL3592)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors.
Gotteland JP, Loubat C, Planty B, Junquéro D, Delhon A, Halazy S.
Bioorg Med Chem Lett (1998) 8 : 1337 -1342
PubMed 9871762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.49 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281025 1 7.22
CHEMBL27154 1 7.05
CHEMBL26950 1 7.05
CHEMBL26151 1 6.82
CHEMBL26964 1 6.77
CHEMBL26596 1 6.77
CHEMBL284197 1 6.70
CHEMBL282077 1 6.70
CHEMBL27941 1 6.68
CHEMBL26077 1 6.64
CHEMBL26597 1 6.60
CHEMBL281666 1 6.59
CHEMBL26723 1 6.54
CHEMBL25755 1 6.52
CHEMBL27365 1 6.48
CHEMBL26592 1 6.41
CHEMBL280972 1 6.35
CHEMBL26091 1 5.75
CHEMBL26082 1 5.19
CHEMBL27195 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281025 IC50 = 60.0 nM 7.22
CHEMBL27154 IC50 = 90.0 nM 7.05
CHEMBL26950 IC50 = 90.0 nM 7.05
CHEMBL26151 IC50 = 150.0 nM 6.82
CHEMBL26964 IC50 = 170.0 nM 6.77
CHEMBL26596 IC50 = 170.0 nM 6.77
CHEMBL284197 IC50 = 200.0 nM 6.70
CHEMBL282077 IC50 = 200.0 nM 6.70
CHEMBL27941 IC50 = 210.0 nM 6.68
CHEMBL26077 IC50 = 230.0 nM 6.64
CHEMBL26597 IC50 = 250.0 nM 6.60
CHEMBL281666 IC50 = 255.0 nM 6.59
CHEMBL26723 IC50 = 290.0 nM 6.54
CHEMBL25755 IC50 = 300.0 nM 6.52
CHEMBL27365 IC50 = 330.0 nM 6.48
CHEMBL26592 IC50 = 390.0 nM 6.41
CHEMBL280972 IC50 = 450.0 nM 6.35
CHEMBL26091 IC50 = 1800.0 nM 5.75
CHEMBL26082 IC50 = 6400.0 nM 5.19
CHEMBL27195 IC50 = 10000.0 nM 5.00