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Assay Detail

CHEMBL1786941

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

Binding
Inhibition of porcine brain GSK3 assessed as incorporation of [gamma-33P]-ATP into YRRAAVPPSPSLSRHSSPHQSpEDEEE after 30 mins by scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Power DP, Lozach O, Meijer L, Grayson DH, Connon SJ.
Bioorg Med Chem Lett (2010) 20 : 4940 -4944
PubMed 20621478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.16 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296586 KENPAULLONE 1 7.11
CHEMBL1782168 1 6.09
CHEMBL430574 PAULLONE 1 5.96
CHEMBL1782170 1 5.47
CHEMBL1782169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296586 KENPAULLONE IC50 = 78.0 nM 7.11
CHEMBL1782168 IC50 = 810.0 nM 6.09
CHEMBL430574 PAULLONE IC50 = 1100.0 nM 5.96
CHEMBL1782170 IC50 = 3400.0 nM 5.47
CHEMBL1782169 IC50 > 10000.0 nM -