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Assay Detail

CHEMBL5252011

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

Binding
Inhibition of GSK3-beta (unknown origin)
3
Total Activities
3
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

Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-<i>b</i>]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors.
Hartz RA, Ahuja VT, Sivaprakasam P, Xiao H, Krause CM, Clarke WJ, Kish K, Lewis H, Szapiel N, Ravirala R, Mutalik S, Nakmode D, Shah D, Burton CR, Macor JE, Dubowchik GM.
J Med Chem (2023) 66 : 4231 -4252
PubMed 36950863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.82 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5291119 1 8.70
CHEMBL102714 SB-216763 1 7.47
CHEMBL3601951 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5291119 IC50 = 2.0 nM 8.70
CHEMBL102714 SB-216763 IC50 = 34.0 nM 7.47
CHEMBL3601951 IC50 = 53.0 nM 7.28