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Assay Detail

CHEMBL686307

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Binding
Inhibition of human glycogen synthase kinase-3alpha (hGSK-3)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glycogen synthase kinase-3 alpha (CHEMBL2850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Witherington J, Bordas V, Haigh D, Hickey DM, Ife RJ, Rawlings AD, Slingsby BP, Smith DG, Ward RW.
Bioorg Med Chem Lett (2003) 13 : 1581 -1584
PubMed 12699760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.60 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288143 1 8.40
CHEMBL41783 1 8.30
CHEMBL259271 1 8.30
CHEMBL261518 1 8.30
CHEMBL264161 1 8.15
CHEMBL261549 1 8.15
CHEMBL409738 1 8.15
CHEMBL406125 1 8.05
CHEMBL261441 1 7.96
CHEMBL259744 1 7.66
CHEMBL258701 1 7.25
CHEMBL261366 1 7.00
CHEMBL260135 1 6.60
CHEMBL261127 1 6.16
CHEMBL261661 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288143 IC50 = 4.0 nM 8.40
CHEMBL41783 IC50 = 5.0 nM 8.30
CHEMBL259271 IC50 = 5.0 nM 8.30
CHEMBL261518 IC50 = 5.0 nM 8.30
CHEMBL264161 IC50 = 7.0 nM 8.15
CHEMBL261549 IC50 = 7.0 nM 8.15
CHEMBL409738 IC50 = 7.0 nM 8.15
CHEMBL406125 IC50 = 9.0 nM 8.05
CHEMBL261441 IC50 = 11.0 nM 7.96
CHEMBL259744 IC50 = 22.0 nM 7.66
CHEMBL258701 IC50 = 56.0 nM 7.25
CHEMBL261366 IC50 = 99.0 nM 7.00
CHEMBL260135 IC50 = 250.0 nM 6.60
CHEMBL261127 IC50 = 691.0 nM 6.16
CHEMBL261661 IC50 = 2697.0 nM 5.57