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Assay Detail

CHEMBL808968

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

Binding
In vitro inhibitory concentration against squalene synthase from male rat liver microsomes
9
Total Activities
9
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

Structurally simplified squalestatins: monocyclic 1,3-dioxane analogues.
Sharratt PJ, Hutson JL, Inglis GG, Lester MG, Procopiou PA, Watson NS
Bioorg Med Chem Lett (1994) 4 : 661 -666
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.36 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418767 1 8.22
CHEMBL160176 1 7.96
CHEMBL280978 ZARAGOZIC ACIDS A 1 7.92
CHEMBL89566 1 7.82
CHEMBL157542 1 7.41
CHEMBL368664 1 7.24
CHEMBL158930 1 6.70
CHEMBL158525 1 6.57
CHEMBL89073 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418767 IC50 = 6.0 nM 8.22
CHEMBL160176 IC50 = 11.0 nM 7.96
CHEMBL280978 ZARAGOZIC ACIDS A IC50 = 12.0 nM 7.92
CHEMBL89566 IC50 = 15.0 nM 7.82
CHEMBL157542 IC50 = 39.0 nM 7.41
CHEMBL368664 IC50 = 57.0 nM 7.24
CHEMBL158930 IC50 = 200.0 nM 6.70
CHEMBL158525 IC50 = 270.0 nM 6.57
CHEMBL89073 IC50 = 380.0 nM 6.42