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Assay Detail

CHEMBL686306

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Binding
Inhibition against human glycogen synthase kinase-3alpha (hGSK-3).
26
Total Activities
26
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]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Witherington J, Bordas V, Garland SL, Hickey DM, Ife RJ, Liddle J, Saunders M, Smith DG, Ward RW.
Bioorg Med Chem Lett (2003) 13 : 1577 -1580
PubMed 12699759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.83 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258483 1 8.30
CHEMBL264161 1 8.15
CHEMBL407002 1 7.96
CHEMBL407373 1 7.75
CHEMBL261596 1 7.72
CHEMBL263907 1 7.70
CHEMBL407003 1 7.57
CHEMBL406701 1 7.37
CHEMBL258701 1 7.25
CHEMBL406062 1 6.77
CHEMBL260329 1 6.62
CHEMBL260135 1 6.60
CHEMBL288448 1 6.54
CHEMBL264162 1 6.45
CHEMBL261439 1 6.37
CHEMBL261264 1 6.35
CHEMBL408634 1 6.28
CHEMBL261052 1 6.07
CHEMBL259925 1 5.90
CHEMBL407374 1 5.63
CHEMBL408809 1 5.55
CHEMBL287731 1 5.45
CHEMBL428968 1 -
CHEMBL40493 1 -
CHEMBL290147 1 -
CHEMBL40835 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258483 IC50 = 5.0 nM 8.30
CHEMBL264161 IC50 = 7.0 nM 8.15
CHEMBL407002 IC50 = 11.0 nM 7.96
CHEMBL407373 IC50 = 18.0 nM 7.75
CHEMBL261596 IC50 = 19.0 nM 7.72
CHEMBL263907 IC50 = 20.0 nM 7.70
CHEMBL407003 IC50 = 27.0 nM 7.57
CHEMBL406701 IC50 = 43.0 nM 7.37
CHEMBL258701 IC50 = 56.0 nM 7.25
CHEMBL406062 IC50 = 169.0 nM 6.77
CHEMBL260329 IC50 = 241.0 nM 6.62
CHEMBL260135 IC50 = 250.0 nM 6.60
CHEMBL288448 IC50 = 291.0 nM 6.54
CHEMBL264162 IC50 = 356.0 nM 6.45
CHEMBL261439 IC50 = 430.0 nM 6.37
CHEMBL261264 IC50 = 443.0 nM 6.35
CHEMBL408634 IC50 = 530.0 nM 6.28
CHEMBL261052 IC50 = 851.0 nM 6.07
CHEMBL259925 IC50 = 1260.0 nM 5.90
CHEMBL407374 IC50 = 2345.0 nM 5.63
CHEMBL408809 IC50 = 2810.0 nM 5.55
CHEMBL287731 IC50 = 3572.0 nM 5.45
CHEMBL428968 IC50 > 5000.0 nM -
CHEMBL40493 IC50 > 5000.0 nM -
CHEMBL290147 IC50 > 5000.0 nM -
CHEMBL40835 IC50 > 5000.0 nM -