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Assay Detail

CHEMBL3766854

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

Binding
Inhibition of glycogen phosphorylase in Wistar rat hepatocytes assessed as decrease in glucagon stimulated glucose release after 3 hrs by glucose oxidase method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Hepatocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycogen phosphorylase, liver form (CHEMBL3239)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Glucose-derived spiro-isoxazolines are anti-hyperglycemic agents against type 2 diabetes through glycogen phosphorylase inhibition.
Goyard D, Kónya B, Chajistamatiou AS, Chrysina ED, Leroy J, Balzarin S, Tournier M, Tousch D, Petit P, Duret C, Maurel P, Somsák L, Docsa T, Gergely P, Praly JP, Azay-Milhau J, Vidal S.
Eur J Med Chem (2016) 108 : 444 -454
PubMed 26708111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.61 4.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765349 1 4.87
CHEMBL3763876 1 4.52
CHEMBL594021 1 4.44
CHEMBL3763929 1 -
CHEMBL3763976 1 -
CHEMBL3764195 1 -
CHEMBL3764911 1 -
CHEMBL3764775 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765349 IC50 = 13580.0 nM 4.87
CHEMBL3763876 IC50 = 30070.0 nM 4.52
CHEMBL594021 IC50 = 36000.0 nM 4.44
CHEMBL3763929 IC50 > 100000.0 nM -
CHEMBL3763976 IC50 > 100000.0 nM -
CHEMBL3764195 IC50 > 100000.0 nM -
CHEMBL3764911 IC50 > 100000.0 nM -
CHEMBL3764775 IC50 > 100000.0 nM -