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Assay Detail

CHEMBL5098682

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

Binding
Inhibition of full length human GSK3beta in the presence of ATP at Km concentration
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycogen synthase kinase-3 beta (CHEMBL262)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Barlaam B, De Savi C, Dishington A, Drew L, Ferguson AD, Ferguson D, Gu C, Hande S, Hassall L, Hawkins J, Hird AW, Holmes J, Lamb ML, Lister AS, McGuire TM, Moore JE, O'Connell N, Patel A, Pike KG, Sarkar U, Shao W, Stead D, Varnes JG, Vasbinder MM, Wang L, Wu L, Xue L, Yang B, Yao T.
J Med Chem (2021) 64 : 15189 -15213
PubMed 34647738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.93 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170524 1 6.51
CHEMBL3663760 1 5.85
CHEMBL5207871 1 5.82
CHEMBL5197170 1 5.80
CHEMBL5198038 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170524 IC50 = 310.0 nM 6.51
CHEMBL3663760 IC50 = 1400.0 nM 5.85
CHEMBL5207871 IC50 = 1500.0 nM 5.82
CHEMBL5197170 IC50 = 1600.0 nM 5.80
CHEMBL5198038 IC50 = 2100.0 nM 5.68