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Assay Detail

CHEMBL3873256

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

Binding
Competitive inhibition of rabbit muscle glycogen phosphorylase-a assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen measured after 1 min by Dixon plot method
8
Total Activities
8
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

Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase.
Kantsadi AL, Bokor É, Kun S, Stravodimos GA, Chatzileontiadou DSM, Leonidas DD, Juhász-Tóth É, Szakács A, Batta G, Docsa T, Gergely P, Somsák L.
Eur J Med Chem (2016) 123 : 737 -745
PubMed 27522507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.92 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770455 1 7.19
CHEMBL3770514 1 6.65
CHEMBL3936229 1 -
CHEMBL3954904 1 -
CHEMBL3921272 1 -
CHEMBL3946226 1 -
CHEMBL3968658 1 -
CHEMBL3937338 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770455 Ki = 65.0 nM 7.19
CHEMBL3770514 Ki = 226.0 nM 6.65
CHEMBL3936229 Ki - -
CHEMBL3954904 Ki - -
CHEMBL3921272 Ki - -
CHEMBL3946226 Ki - -
CHEMBL3968658 Ki - -
CHEMBL3937338 Ki - -