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Assay Detail

CHEMBL4020036

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

Binding
Competitive inhibition of rabbit muscle glycogen phosphorylase-b in presence of varying levels of glucose-1-phosphate and constant concentration of glycogen and AMP preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
6
Total Activities
6
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

Nanomolar Inhibitors of Glycogen Phosphorylase Based on β-d-Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study.
Bokor É, Kyriakis E, Solovou TGA, Koppány C, Kantsadi AL, Szabó KE, Szakács A, Stravodimos GA, Docsa T, Skamnaki VT, Zographos SE, Gergely P, Leonidas DD, Somsák L.
J Med Chem (2017) 60 : 9251 -9262
PubMed 28925695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.52 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101331 1 6.72
CHEMBL4095486 1 5.57
CHEMBL4068103 1 5.32
CHEMBL4087784 1 4.45
CHEMBL4105675 1 -
CHEMBL4098082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101331 Ki = 191.0 nM 6.72
CHEMBL4095486 Ki = 2670.0 nM 5.57
CHEMBL4068103 Ki = 4800.0 nM 5.32
CHEMBL4087784 Ki = 35200.0 nM 4.45
CHEMBL4105675 Ki = 354300.0 nM -
CHEMBL4098082 Ki = 107100.0 nM -