Assay Detail
Binding
CHEMBL5256393
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Covalent inhibition of CDK4 (unknown origin) using histone H1 as substrate incubated for 10 mins in presence of [gamma-32P]ATP by radioactivity based kinase assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.64 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5277376 | — | — | 1 | 7.75 |
| CHEMBL4860767 | — | — | 1 | 7.64 |
| CHEMBL5277470 | — | — | 1 | 7.60 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5277376 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4860767 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5277470 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 26.0 | nM | 7.58 |