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Assay Detail

CHEMBL999228

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

Binding
Inhibition of rat liver squalene synthase by liqiud scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Zaragozic acids D and D2: potent inhibitors of squalene synthase and of Ras farnesyl-protein transferase.
Dufresne C, Wilson KE, Singh SB, Zink DL, Bergstrom JD, Rew D, Polishook JD, Meinz M, Huang L, Silverman KC.
J Nat Prod (1993) 56 : 1923 -1929
PubMed 8289063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.06 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504845 ZARAGOZIC ACID B 1 9.70
CHEMBL505374 ZARAGOZIC ACID C 1 9.40
CHEMBL280978 ZARAGOZIC ACIDS A 1 9.30
CHEMBL502210 ZARAGOZIC ACID D2 1 8.70
CHEMBL502872 ZARAGOZIC ACID D 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504845 ZARAGOZIC ACID B IC50 = 0.2 nM 9.70
CHEMBL505374 ZARAGOZIC ACID C IC50 = 0.4 nM 9.40
CHEMBL280978 ZARAGOZIC ACIDS A IC50 = 0.5 nM 9.30
CHEMBL502210 ZARAGOZIC ACID D2 IC50 = 2.0 nM 8.70
CHEMBL502872 ZARAGOZIC ACID D IC50 = 6.0 nM 8.22