Assay Detail
Binding
CHEMBL1786933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CDK9/cyclin T expressed in insect cells assessed as incorporation of [gamma-33P]-ATP in to pRB fragment (773 to 928) 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 |
Publication
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.34 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296586 | KENPAULLONE | — | 1 | 7.19 |
| CHEMBL1782168 | — | — | 1 | 6.66 |
| CHEMBL1782170 | — | — | 1 | 6.62 |
| CHEMBL430574 | PAULLONE | — | 1 | 6.09 |
| CHEMBL1782169 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296586 | KENPAULLONE | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1782168 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1782170 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL430574 | PAULLONE | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1782169 | — | IC50 | = | 7400.0 | nM | 5.13 |