Assay Detail
Binding
CHEMBL1786937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CDK5/p25 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 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.51 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296586 | KENPAULLONE | — | 1 | 6.00 |
| CHEMBL1782168 | — | — | 1 | 5.52 |
| CHEMBL430574 | PAULLONE | — | 1 | 5.38 |
| CHEMBL1782170 | — | — | 1 | 5.14 |
| CHEMBL1782169 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296586 | KENPAULLONE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1782168 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL430574 | PAULLONE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1782170 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1782169 | — | IC50 | > | 10000.0 | nM | - |