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Assay Detail

CHEMBL691950

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

Binding
In vitro inhibitory activity against HMG CoA reductase
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 1. Structural modification of 5-substituted 3,5-dihydroxypentanoic acids and their lactone derivatives.
Stokker GE, Hoffman WF, Alberts AW, Cragoe EJ, Deana AA, Gilfillan JL, Huff JW, Novello FC, Prugh JD, Smith RL.
J Med Chem (1985) 28 : 347 -358
PubMed 3973903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.35 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54440 MEVASTATIN 2.0 1 8.00
CHEMBL2367922 1 6.05
CHEMBL118591 1 5.80
CHEMBL118592 1 5.72
CHEMBL2368928 2 4.97
CHEMBL120354 1 4.82
CHEMBL2367920 1 4.70
CHEMBL332558 1 4.70
CHEMBL120524 1 4.05
CHEMBL118866 1 -
CHEMBL120403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54440 MEVASTATIN IC50 = 10.0 nM 8.00
CHEMBL2367922 IC50 = 890.0 nM 6.05
CHEMBL118591 IC50 = 1600.0 nM 5.80
CHEMBL118592 IC50 = 1900.0 nM 5.72
CHEMBL2368928 IC50 = 10800.0 nM 4.97
CHEMBL120354 IC50 = 15200.0 nM 4.82
CHEMBL2367920 IC50 = 20000.0 nM 4.70
CHEMBL332558 IC50 = 19800.0 nM 4.70
CHEMBL2368928 IC50 = 22000.0 nM 4.66
CHEMBL120524 IC50 = 90000.0 nM 4.05
CHEMBL118866 IC50 = 129000.0 nM -
CHEMBL120403 IC50 = 107000.0 nM -