Assay Detail
Binding
CHEMBL960986
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PLK1 kinase domain expressed in baculovirus-infected Trichoplusia ni cells by scintillation proximity assay
16
Total Activities
16
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 |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.54 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222419 | GSK-237701A | — | 1 | 9.10 |
| CHEMBL493326 | GSK-317314A | — | 1 | 9.00 |
| CHEMBL1794067 | GSK-978744A | — | 1 | 9.00 |
| CHEMBL514499 | GW843682X | — | 1 | 8.70 |
| CHEMBL514162 | GW852849X | — | 1 | 8.70 |
| CHEMBL1615278 | — | — | 1 | 8.70 |
| CHEMBL1794070 | GSK-579289A | — | 1 | 8.70 |
| CHEMBL522709 | GSK-317315A | — | 1 | 8.52 |
| CHEMBL1964262 | — | — | 1 | 8.52 |
| CHEMBL1964263 | — | — | 1 | 8.52 |
| CHEMBL1964264 | — | — | 1 | 8.52 |
| CHEMBL1964261 | — | — | 1 | 8.40 |
| CHEMBL1964265 | — | — | 1 | 8.40 |
| CHEMBL1794069 | GSK-571989A | — | 1 | 8.22 |
| CHEMBL1794068 | GSK-326090A | — | 1 | 8.15 |
| CHEMBL521806 | GSK-237700A | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222419 | GSK-237701A | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL493326 | GSK-317314A | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1794067 | GSK-978744A | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL514499 | GW843682X | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL514162 | GW852849X | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1615278 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1794070 | GSK-579289A | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL522709 | GSK-317315A | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1964262 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1964263 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1964264 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1964261 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1964265 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1794069 | GSK-571989A | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1794068 | GSK-326090A | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL521806 | GSK-237700A | IC50 | = | 30.0 | nM | 7.52 |