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Assay Detail

CHEMBL692524

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

Binding
Compound was evaluated for the inhibition of HMG-CoA reductase (COR) in rats.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2 H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors.
Sliskovic DR, Picard JA, Roark WH, Roth BD, Ferguson E, Krause BR, Newton RS, Sekerke C, Shaw MK.
J Med Chem (1991) 34 : 367 -373
PubMed 1992138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.10 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54440 MEVASTATIN 2.0 1 7.60
CHEMBL333258 1 7.60
CHEMBL503 LOVASTATIN 4.0 1 7.55
CHEMBL333933 1 7.50
CHEMBL122112 1 7.28
CHEMBL122937 1 7.10
CHEMBL123082 1 6.70
CHEMBL122947 1 6.46
CHEMBL334113 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54440 MEVASTATIN IC50 = 25.0 nM 7.60
CHEMBL333258 IC50 = 25.0 nM 7.60
CHEMBL503 LOVASTATIN IC50 = 28.0 nM 7.55
CHEMBL333933 IC50 = 32.0 nM 7.50
CHEMBL122112 IC50 = 53.0 nM 7.28
CHEMBL122937 IC50 = 79.0 nM 7.10
CHEMBL123082 IC50 = 200.0 nM 6.70
CHEMBL122947 IC50 = 350.0 nM 6.46
CHEMBL334113 IC50 = 720.0 nM 6.14