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Assay Detail

CHEMBL4433652

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

Binding
Inhibition of human recombinant GSK3beta using GSM as substrate incubated for 30 mins by luminescence based assay
6
Total Activities
6
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 the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.
De Simone A, La Pietra V, Betari N, Petragnani N, Conte M, Daniele S, Pietrobono D, Martini C, Petralla S, Casadei R, Davani L, Frabetti F, Russomanno P, Novellino E, Montanari S, Tumiatti V, Ballerini P, Sarno F, Nebbioso A, Altucci L, Monti B, Andrisano V, Milelli A.
ACS Med Chem Lett (2019) 10 : 469 -474
PubMed 30996781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.44 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322970 1 7.30
CHEMBL4449010 1 5.57
CHEMBL4575045 1 5.39
CHEMBL4590543 1 5.01
CHEMBL4443876 1 4.70
CHEMBL277294 PHTHALIMIDE 1 4.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322970 IC50 = 50.0 nM 7.30
CHEMBL4449010 IC50 = 2690.0 nM 5.57
CHEMBL4575045 IC50 = 4110.0 nM 5.39
CHEMBL4590543 IC50 = 9850.0 nM 5.01
CHEMBL4443876 IC50 = 19960.0 nM 4.70
CHEMBL277294 PHTHALIMIDE IC50 = 20220.0 nM 4.69