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Assay Detail

CHEMBL687159

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

Binding
In vitro inhibitory activity against isolated enzyme HMG-CoA reductase
5
Total Activities
5
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 (CHEMBL2764)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis of tetrazol-1-yl analogs of HMG-COA reductase inhibitor BMS180431 (formerly BMY21950)
Sit S, Parker RA, Wright J
Bioorg Med Chem Lett (1992) 2 : 1085 -1088
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.02 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503 LOVASTATIN 4.0 1 7.57
CHEMBL11804 1 7.37
CHEMBL11891 1 6.92
CHEMBL276717 1 6.20
CHEMBL268767 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503 LOVASTATIN IC50 = 27.0 nM 7.57
CHEMBL11804 IC50 = 43.0 nM 7.37
CHEMBL11891 IC50 = 120.0 nM 6.92
CHEMBL276717 IC50 = 630.0 nM 6.20
CHEMBL268767 IC50 > 100000.0 nM -