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Assay Detail

CHEMBL692723

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

Functional
Concentration required to inhibit HMG-CoA reductase by 50% was determined in Hep G2 cell line
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase.
Bone EA, Davidson AH, Lewis CN, Todd RS.
J Med Chem (1992) 35 : 3388 -3393
PubMed 1527791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.88 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487720 1 7.92
CHEMBL175236 1 7.54
CHEMBL503 LOVASTATIN 4.0 1 7.43
CHEMBL115307 1 5.85
CHEMBL323880 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487720 IC50 = 12.0 nM 7.92
CHEMBL175236 IC50 = 29.0 nM 7.54
CHEMBL503 LOVASTATIN IC50 = 37.0 nM 7.43
CHEMBL115307 IC50 = 1400.0 nM 5.85
CHEMBL323880 IC50 = 2220.0 nM 5.65