Assay Detail
Binding
CHEMBL1640701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PLK1 by flash plate based radioactive enzyme assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.23 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1630117 | — | — | 1 | 5.70 |
| CHEMBL1630108 | — | — | 1 | 5.57 |
| CHEMBL1630118 | — | — | 1 | 5.54 |
| CHEMBL1630111 | — | — | 1 | 5.41 |
| CHEMBL1630114 | — | — | 1 | 5.26 |
| CHEMBL1630112 | — | — | 1 | 5.25 |
| CHEMBL1630115 | — | — | 1 | 5.21 |
| CHEMBL1630109 | — | — | 1 | 5.17 |
| CHEMBL1630113 | — | — | 1 | 5.07 |
| CHEMBL1630110 | — | — | 1 | 5.04 |
| CHEMBL1630107 | — | — | 1 | 4.92 |
| CHEMBL1630116 | — | — | 1 | 4.57 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1630117 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1630108 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1630118 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1630111 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1630114 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL1630112 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1630115 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1630109 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL1630113 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL1630110 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1630107 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1630116 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL554 | LAPATINIB | IC50 | > | 100000.0 | nM | - |