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Assay Detail

CHEMBL692247

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

Functional
Inhibition of the incorporation of sodium [14C]acetate into cholesterol in HEP G2 cells.
22
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids.
Jendralla H, Granzer E, von Kerekjarto B, Krause R, Schacht U, Baader E, Bartmann W, Beck G, Bergmann A, Kesseler K.
J Med Chem (1991) 34 : 2962 -2983
PubMed 1656041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.58 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102168 1 9.30
CHEMBL318707 1 8.74
CHEMBL177545 1 8.39
CHEMBL321768 1 8.25
CHEMBL100165 1 7.52
CHEMBL503 LOVASTATIN 4.0 1 7.30
CHEMBL329307 1 7.26
CHEMBL99838 1 7.00
CHEMBL101497 1 6.60
CHEMBL323344 2 5.77
CHEMBL321713 1 5.60
CHEMBL317142 1 5.46
CHEMBL101824 1 5.19
CHEMBL101600 2 5.00
CHEMBL102199 1 4.70
CHEMBL103139 1 -
CHEMBL101831 1 -
CHEMBL321076 1 -
CHEMBL102112 1 -
CHEMBL317777 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102168 IC50 = 0.5 nM 9.30
CHEMBL318707 IC50 = 1.8 nM 8.74
CHEMBL177545 IC50 = 4.1 nM 8.39
CHEMBL321768 IC50 = 5.6 nM 8.25
CHEMBL100165 IC50 = 30.0 nM 7.52
CHEMBL503 LOVASTATIN IC50 = 50.0 nM 7.30
CHEMBL329307 IC50 = 55.0 nM 7.26
CHEMBL99838 IC50 = 100.0 nM 7.00
CHEMBL101497 IC50 = 250.0 nM 6.60
CHEMBL323344 IC50 = 1700.0 nM 5.77
CHEMBL321713 IC50 = 2500.0 nM 5.60
CHEMBL317142 IC50 = 3500.0 nM 5.46
CHEMBL101824 IC50 = 6500.0 nM 5.19
CHEMBL101600 IC50 = 10000.0 nM 5.00
CHEMBL323344 IC50 = 12000.0 nM 4.92
CHEMBL101600 IC50 = 15000.0 nM 4.82
CHEMBL102199 IC50 = 20000.0 nM 4.70
CHEMBL103139 IC50 > 5000.0 nM -
CHEMBL101831 IC50 > 1700.0 nM -
CHEMBL321076 IC50 > 1000.0 nM -
CHEMBL102112 IC50 > 5000.0 nM -
CHEMBL317777 IC50 > 500.0 nM -