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Assay Detail

CHEMBL4020032

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

Binding
Competitive inhibition of rabbit muscle glycogen phosphorylase b using glucose-1-phosphate as substrate in presence of constant concentrations of glycogen and AMP
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 4.82 5.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081944 1 5.26
CHEMBL558445 1 5.05
CHEMBL600003 1 4.80
CHEMBL4090219 1 4.57
CHEMBL560324 1 4.42
CHEMBL601227 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081944 Ki = 5500.0 nM 5.26
CHEMBL558445 Ki = 9000.0 nM 5.05
CHEMBL600003 Ki = 16000.0 nM 4.80
CHEMBL4090219 Ki = 27100.0 nM 4.57
CHEMBL560324 Ki = 38000.0 nM 4.42
CHEMBL601227 Ki = 151000.0 nM -