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Assay Detail

CHEMBL1786934

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

Binding
Inhibition of human recombinant CDK2/cyclin A assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

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 5.64 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296586 KENPAULLONE 1 6.11
CHEMBL1782168 1 5.68
CHEMBL430574 PAULLONE 1 5.57
CHEMBL1782170 1 5.21
CHEMBL1782169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296586 KENPAULLONE IC50 = 780.0 nM 6.11
CHEMBL1782168 IC50 = 2100.0 nM 5.68
CHEMBL430574 PAULLONE IC50 = 2700.0 nM 5.57
CHEMBL1782170 IC50 = 6200.0 nM 5.21
CHEMBL1782169 IC50 > 10000.0 nM -