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Assay Detail

CHEMBL691947

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

Binding
Inhibition of rat liver microsomal HMG-CoA reductase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of cholesterol biosynthesis. 2. 3,5-Dihydroxy-7-(N-pyrrolyl)-6-heptenoates, a novel series of HMG-CoA reductase inhibitors.
Procopiou PA, Draper CD, Hutson JL, Inglis GG, Ross BC, Watson NS.
J Med Chem (1993) 36 : 3658 -3662
PubMed 8246234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.28 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445123 1 9.52
CHEMBL119609 1 9.30
CHEMBL121451 1 8.70
CHEMBL120922 1 8.70
CHEMBL333642 1 8.70
CHEMBL331680 1 8.70
CHEMBL503 LOVASTATIN 4.0 1 8.52
CHEMBL333904 1 8.30
CHEMBL690 PRAVASTATIN SODIUM 4.0 1 8.30
CHEMBL332735 1 7.60
CHEMBL332205 1 7.16
CHEMBL420893 1 7.15
CHEMBL121541 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445123 IC50 = 0.3 nM 9.52
CHEMBL119609 IC50 = 0.5 nM 9.30
CHEMBL121451 IC50 = 2.0 nM 8.70
CHEMBL120922 IC50 = 2.0 nM 8.70
CHEMBL333642 IC50 = 2.0 nM 8.70
CHEMBL331680 IC50 = 2.0 nM 8.70
CHEMBL503 LOVASTATIN IC50 = 3.0 nM 8.52
CHEMBL333904 IC50 = 5.0 nM 8.30
CHEMBL690 PRAVASTATIN SODIUM IC50 = 5.0 nM 8.30
CHEMBL332735 IC50 = 25.0 nM 7.60
CHEMBL332205 IC50 = 69.0 nM 7.16
CHEMBL420893 IC50 = 71.0 nM 7.15
CHEMBL121541 IC50 = 105.0 nM 6.98