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Assay Detail

CHEMBL1104444

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

Binding
Inhibition of squalene synthase in rat liver microsomes assessed as conversion of [1-3H]FPP to [3H]squalene level after 60 mins by liquid scintillation counting
5
Total Activities
5
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 Autocuration

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs).
Lolli ML, Rolando B, Tosco P, Chaurasia S, Di Stilo A, Lazzarato L, Gorassini E, Ferracini R, Oliaro-Bosso S, Fruttero R, Gasco A.
Bioorg Med Chem (2010) 18 : 2428 -2438
PubMed 20299227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.22 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL997 IBANDRONIC ACID 4.0 1 6.19
CHEMBL1091856 1 5.43
CHEMBL1091027 1 5.10
CHEMBL1090779 1 4.75
CHEMBL1093434 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL997 IBANDRONIC ACID IC50 = 640.0 nM 6.19
CHEMBL1091856 IC50 = 3710.0 nM 5.43
CHEMBL1091027 IC50 = 7950.0 nM 5.10
CHEMBL1090779 IC50 = 17680.0 nM 4.75
CHEMBL1093434 IC50 = 22950.0 nM 4.64