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Assay Detail

CHEMBL691797

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

Binding
In vitro inhibitory activity was measured against rat liver HMG-CoA reductase
24
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis, biological profile, and quantitative structure-activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors.
Sit SY, Parker RA, Motoc I, Han W, Balasubramanian N, Catt JD, Brown PJ, Harte WE, Thompson MD, Wright JJ.
J Med Chem (1990) 33 : 2982 -2999
PubMed 2231596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.21 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323373 2 7.72
CHEMBL503 LOVASTATIN 4.0 1 7.57
CHEMBL320666 1 7.54
CHEMBL11804 2 7.37
CHEMBL103192 1 7.36
CHEMBL103547 1 6.80
CHEMBL318754 1 6.72
CHEMBL318102 1 6.64
CHEMBL419542 1 6.48
CHEMBL328846 1 6.24
CHEMBL103661 1 5.96
CHEMBL441642 1 5.89
CHEMBL323075 1 5.85
CHEMBL100188 1 5.80
CHEMBL2304072 1 5.24
CHEMBL322399 1 5.10
CHEMBL318256 1 5.10
CHEMBL319739 1 4.85
CHEMBL102468 1 4.52
CHEMBL2303674 1 -
CHEMBL321715 1 -
CHEMBL102484 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323373 IC50 = 19.0 nM 7.72
CHEMBL503 LOVASTATIN IC50 = 27.0 nM 7.57
CHEMBL320666 IC50 = 29.0 nM 7.54
CHEMBL11804 IC50 = 43.0 nM 7.37
CHEMBL103192 IC50 = 44.0 nM 7.36
CHEMBL103547 IC50 = 160.0 nM 6.80
CHEMBL318754 IC50 = 190.0 nM 6.72
CHEMBL318102 IC50 = 230.0 nM 6.64
CHEMBL419542 IC50 = 330.0 nM 6.48
CHEMBL328846 IC50 = 580.0 nM 6.24
CHEMBL103661 IC50 = 1100.0 nM 5.96
CHEMBL441642 IC50 = 1300.0 nM 5.89
CHEMBL323075 IC50 = 1400.0 nM 5.85
CHEMBL100188 IC50 = 1600.0 nM 5.80
CHEMBL323373 IC50 = 3700.0 nM 5.43
CHEMBL2304072 IC50 = 5700.0 nM 5.24
CHEMBL322399 IC50 = 8000.0 nM 5.10
CHEMBL318256 IC50 = 7900.0 nM 5.10
CHEMBL319739 IC50 = 14000.0 nM 4.85
CHEMBL102468 IC50 = 30000.0 nM 4.52
CHEMBL2303674 IC50 = 130000.0 nM -
CHEMBL11804 IC50 > 300000.0 nM -
CHEMBL321715 IC50 > 300000.0 nM -
CHEMBL102484 IC50 = 200000.0 nM -