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Assay Detail

CHEMBL615420

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

Binding
Ability of compound to inhibit the activity of 3-hydroxy-3-methylglutarylcoenzyme A(HMGR) reductase in rat liver microsomes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of a monocyclic, fully functional analogue of compactin.
Heathcock CH, Davis BR, Hadley CR.
J Med Chem (1989) 32 : 197 -202
PubMed 2909732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.42 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293944 1 9.00
CHEMBL60053 1 8.89
CHEMBL59166 1 8.80
CHEMBL58289 1 7.89
CHEMBL61702 1 7.50
CHEMBL434604 1 -
CHEMBL59411 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293944 IC50 = 1.0 nM 9.00
CHEMBL60053 IC50 = 1.3 nM 8.89
CHEMBL59166 IC50 = 1.6 nM 8.80
CHEMBL58289 IC50 = 13.0 nM 7.89
CHEMBL61702 IC50 = 32.0 nM 7.50
CHEMBL434604 IC50 = 320000.0 nM -
CHEMBL59411 IC50 = 600000.0 nM -