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Assay Detail

CHEMBL814034

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Binding
Compound was tested for inhibition of squalene synthase from rat liver microsomes using [3H]farnesyl pyrophosphate (FPP) as substrate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Liver
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.
Shen W, Garvey DS, Cohen J, Stein H, Rosenberg SH.
Bioorg Med Chem Lett (1998) 8 : 891 -896
PubMed 9871507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.39 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40991 ZARAGOZIC ACID A 1 7.92
CHEMBL445618 1 7.43
CHEMBL355009 1 6.77
CHEMBL170032 1 6.62
CHEMBL355158 1 6.24
CHEMBL354568 1 5.54
CHEMBL352367 1 5.52
CHEMBL355385 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40991 ZARAGOZIC ACID A IC50 = 12.0 nM 7.92
CHEMBL445618 IC50 = 37.0 nM 7.43
CHEMBL355009 IC50 = 170.0 nM 6.77
CHEMBL170032 IC50 = 240.0 nM 6.62
CHEMBL355158 IC50 = 580.0 nM 6.24
CHEMBL354568 IC50 = 2900.0 nM 5.54
CHEMBL352367 IC50 = 3000.0 nM 5.52
CHEMBL355385 IC50 = 9100.0 nM 5.04