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Assay Detail

CHEMBL779589

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

Functional
Compound was tested for its Cholesterol Synthesis Inhibition ability in rats.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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 11 7.41 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122112 1 7.89
CHEMBL122937 1 7.75
CHEMBL503 LOVASTATIN 4.0 1 7.60
CHEMBL54440 MEVASTATIN 2.0 1 7.52
CHEMBL333258 1 7.50
CHEMBL333933 1 7.38
CHEMBL122947 1 7.33
CHEMBL123082 1 7.30
CHEMBL334113 1 6.40
CHEMBL121716 1 -
CHEMBL122965 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122112 IC50 = 13.0 nM 7.89
CHEMBL122937 IC50 = 18.0 nM 7.75
CHEMBL503 LOVASTATIN IC50 = 25.0 nM 7.60
CHEMBL54440 MEVASTATIN IC50 = 30.0 nM 7.52
CHEMBL333258 IC50 = 32.0 nM 7.50
CHEMBL333933 IC50 = 42.0 nM 7.38
CHEMBL122947 IC50 = 47.0 nM 7.33
CHEMBL123082 IC50 = 50.0 nM 7.30
CHEMBL334113 IC50 = 400.0 nM 6.40
CHEMBL121716 IC50 > 1000.0 nM -
CHEMBL122965 IC50 > 1000.0 nM -