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Assay Detail

CHEMBL3766852

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Binding
Inhibition of rabbit muscle glycogen phosphorylase b
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycogen phosphorylase, muscle form (CHEMBL4696)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

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 12 4.83 5.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763876 1 5.81
CHEMBL3764775 1 5.25
CHEMBL3764271 1 5.21
CHEMBL3765663 1 5.00
CHEMBL3763976 1 4.88
CHEMBL3763651 1 4.60
CHEMBL3763810 1 4.56
CHEMBL3764195 1 4.09
CHEMBL3763929 1 4.09
CHEMBL3764911 1 -
CHEMBL3764090 1 -
CHEMBL3764673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763876 IC50 = 1540.0 nM 5.81
CHEMBL3764775 IC50 = 5600.0 nM 5.25
CHEMBL3764271 IC50 = 6100.0 nM 5.21
CHEMBL3765663 IC50 = 10000.0 nM 5.00
CHEMBL3763976 IC50 = 13300.0 nM 4.88
CHEMBL3763651 IC50 = 25000.0 nM 4.60
CHEMBL3763810 IC50 = 27700.0 nM 4.56
CHEMBL3764195 IC50 = 80500.0 nM 4.09
CHEMBL3763929 IC50 = 81300.0 nM 4.09
CHEMBL3764911 IC50 = 324700.0 nM -
CHEMBL3764090 IC50 = 800000.0 nM -
CHEMBL3764673 IC50 = 280000.0 nM -