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Assay Detail

CHEMBL691945

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

Binding
In vitro inhibition of HMG-CoA reductase in solubilized rat liver.
45
Total Activities
42
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 and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids.
Jendralla H, Granzer E, von Kerekjarto B, Krause R, Schacht U, Baader E, Bartmann W, Beck G, Bergmann A, Kesseler K.
J Med Chem (1991) 34 : 2962 -2983
PubMed 1656041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.02 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100165 1 8.57
CHEMBL177545 1 8.40
CHEMBL102168 1 8.22
CHEMBL503 LOVASTATIN 4.0 1 8.10
CHEMBL321076 1 8.00
CHEMBL329307 1 7.77
CHEMBL321768 1 7.70
CHEMBL101633 1 7.57
CHEMBL101831 1 7.52
CHEMBL316712 1 7.30
CHEMBL101497 1 7.30
CHEMBL100721 2 7.30
CHEMBL323344 2 7.22
CHEMBL420646 1 7.16
CHEMBL100357 1 7.16
CHEMBL101662 1 7.12
CHEMBL319983 1 7.10
CHEMBL321713 1 7.07
CHEMBL100694 1 7.05
CHEMBL101512 1 7.02
CHEMBL443275 1 7.02
CHEMBL99834 1 7.00
CHEMBL316938 1 7.00
CHEMBL101774 1 6.85
CHEMBL317576 1 6.82
CHEMBL100560 1 6.80
CHEMBL101806 1 6.72
CHEMBL101718 1 6.72
CHEMBL316899 1 6.60
CHEMBL330662 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100165 IC50 = 2.7 nM 8.57
CHEMBL177545 IC50 = 4.0 nM 8.40
CHEMBL102168 IC50 = 6.0 nM 8.22
CHEMBL503 LOVASTATIN IC50 = 8.0 nM 8.10
CHEMBL321076 IC50 = 10.0 nM 8.00
CHEMBL329307 IC50 = 17.0 nM 7.77
CHEMBL321768 IC50 = 20.0 nM 7.70
CHEMBL101633 IC50 = 27.0 nM 7.57
CHEMBL101831 IC50 = 30.0 nM 7.52
CHEMBL316712 IC50 = 50.0 nM 7.30
CHEMBL101497 IC50 = 50.0 nM 7.30
CHEMBL100721 IC50 = 50.0 nM 7.30
CHEMBL323344 IC50 = 60.0 nM 7.22
CHEMBL420646 IC50 = 70.0 nM 7.16
CHEMBL100357 IC50 = 70.0 nM 7.16
CHEMBL101662 IC50 = 75.0 nM 7.12
CHEMBL319983 IC50 = 80.0 nM 7.10
CHEMBL321713 IC50 = 85.0 nM 7.07
CHEMBL100694 IC50 = 90.0 nM 7.05
CHEMBL101512 IC50 = 95.0 nM 7.02
CHEMBL443275 IC50 = 95.0 nM 7.02
CHEMBL316938 IC50 = 100.0 nM 7.00
CHEMBL99834 IC50 = 100.0 nM 7.00
CHEMBL101774 IC50 = 140.0 nM 6.85
CHEMBL317576 IC50 = 150.0 nM 6.82
CHEMBL100560 IC50 = 160.0 nM 6.80
CHEMBL101806 IC50 = 190.0 nM 6.72
CHEMBL101718 IC50 = 190.0 nM 6.72
CHEMBL316899 IC50 = 250.0 nM 6.60
CHEMBL330662 IC50 = 260.0 nM 6.58
CHEMBL103712 IC50 = 270.0 nM 6.57
CHEMBL101600 IC50 = 320.0 nM 6.50
CHEMBL317142 IC50 = 380.0 nM 6.42
CHEMBL99838 IC50 = 400.0 nM 6.40
CHEMBL317777 IC50 = 400.0 nM 6.40
CHEMBL101600 IC50 = 470.0 nM 6.33
CHEMBL323344 IC50 = 500.0 nM 6.30
CHEMBL102199 IC50 = 900.0 nM 6.05
CHEMBL100721 IC50 = 950.0 nM 6.02
CHEMBL103139 IC50 = 1000.0 nM 6.00
CHEMBL101097 IC50 = 1000.0 nM 6.00
CHEMBL101824 IC50 > 1000.0 nM -
CHEMBL100884 IC50 > 1000.0 nM -
CHEMBL102112 IC50 > 1000.0 nM -
CHEMBL317726 IC50 > 1000.0 nM -