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Assay Detail

CHEMBL4733696

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

Binding
Inhibition of GSK3beta (unknown origin)
8
Total Activities
8
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

PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.
Jiang X,Zhou J,Wang Y,Liu X,Xu K,Xu J,Feng F,Sun H
Eur J Med Chem (2021) 210 : 112949 -112949
PubMed 33097303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.69 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50894 ALSTERPAULLONE 1 8.40
CHEMBL3545157 TIDEGLUSIB 2.0 1 8.30
CHEMBL2177161 1 8.30
CHEMBL412142 LADUVIGLUSIB 1.0 1 8.15
CHEMBL296586 KENPAULLONE 1 7.64
CHEMBL405759 1 7.52
CHEMBL102714 SB-216763 1 7.47
CHEMBL284861 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50894 ALSTERPAULLONE IC50 = 4.0 nM 8.40
CHEMBL3545157 TIDEGLUSIB IC50 = 5.0 nM 8.30
CHEMBL2177161 IC50 = 5.0 nM 8.30
CHEMBL412142 LADUVIGLUSIB IC50 = 7.0 nM 8.15
CHEMBL296586 KENPAULLONE IC50 = 23.0 nM 7.64
CHEMBL405759 IC50 = 30.0 nM 7.52
CHEMBL102714 SB-216763 IC50 = 34.0 nM 7.47
CHEMBL284861 IC50 = 2000.0 nM 5.70