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Assay Detail

CHEMBL692518

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

Functional
The compound was tested in vitro for inhibition of rat hepatic HMG-CoA reductase.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety.
Robl JA, Duncan LA, Pluscec J, Karanewsky DS, Gordon EM, Ciosek CP, Rich LC, Dehmel VC, Slusarchyk DA, Harrity TW.
J Med Chem (1991) 34 : 2804 -2815
PubMed 1895299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.06 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97121 1 8.92
CHEMBL94800 1 8.89
CHEMBL329478 1 8.85
CHEMBL96953 1 8.60
CHEMBL418776 1 8.40
CHEMBL94584 1 8.29
CHEMBL94994 1 7.90
CHEMBL92891 1 7.71
CHEMBL690 PRAVASTATIN SODIUM 4.0 1 7.62
CHEMBL94575 1 7.54
CHEMBL314756 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97121 IC50 = 1.2 nM 8.92
CHEMBL94800 IC50 = 1.3 nM 8.89
CHEMBL329478 IC50 = 1.4 nM 8.85
CHEMBL96953 IC50 = 2.5 nM 8.60
CHEMBL418776 IC50 = 4.0 nM 8.40
CHEMBL94584 IC50 = 5.1 nM 8.29
CHEMBL94994 IC50 = 12.7 nM 7.90
CHEMBL92891 IC50 = 19.4 nM 7.71
CHEMBL690 PRAVASTATIN SODIUM IC50 = 24.0 nM 7.62
CHEMBL94575 IC50 = 29.0 nM 7.54
CHEMBL314756 IC50 = 1300.0 nM 5.89