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Assay Detail

CHEMBL692516

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

Binding
Inhibition of HMG-CoA reductase in rat liver microsomes
17
Total Activities
17
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 Expert

Target

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

Publication

Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin.
Heathcock CH, Hadley CR, Rosen T, Theisen PD, Hecker SJ.
J Med Chem (1987) 30 : 1858 -1873
PubMed 3656359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.20 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293944 1 9.00
CHEMBL3350219 1 8.80
CHEMBL54440 MEVASTATIN 2.0 1 7.89
CHEMBL54045 1 7.50
CHEMBL299644 1 6.50
CHEMBL55028 1 6.20
CHEMBL55303 1 6.20
CHEMBL3350220 1 5.70
CHEMBL2115471 1 5.70
CHEMBL2115055 1 5.40
CHEMBL416308 1 5.30
CHEMBL53758 1 5.15
CHEMBL2115472 1 5.00
CHEMBL291954 1 4.60
CHEMBL2115058 1 4.10
CHEMBL2115056 1 -
CHEMBL56180 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293944 IC50 = 1.0 nM 9.00
CHEMBL3350219 IC50 = 1.6 nM 8.80
CHEMBL54440 MEVASTATIN IC50 = 13.0 nM 7.89
CHEMBL54045 IC50 = 32.0 nM 7.50
CHEMBL299644 IC50 = 320.0 nM 6.50
CHEMBL55028 IC50 = 630.0 nM 6.20
CHEMBL55303 IC50 = 630.0 nM 6.20
CHEMBL3350220 IC50 = 2000.0 nM 5.70
CHEMBL2115471 IC50 = 2000.0 nM 5.70
CHEMBL2115055 IC50 = 4000.0 nM 5.40
CHEMBL416308 IC50 = 5000.0 nM 5.30
CHEMBL53758 IC50 = 7100.0 nM 5.15
CHEMBL2115472 IC50 = 10000.0 nM 5.00
CHEMBL291954 IC50 = 25000.0 nM 4.60
CHEMBL2115058 IC50 = 79000.0 nM 4.10
CHEMBL2115056 IC50 > 25000.0 nM -
CHEMBL56180 IC50 = 110000.0 nM -