Assay Detail
Binding
CHEMBL960987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human PLK3 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 PLK3 (CHEMBL4897) ↗| 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 | 6.94 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222419 | GSK-237701A | — | 1 | 8.22 |
| CHEMBL514499 | GW843682X | — | 1 | 8.05 |
| CHEMBL514162 | GW852849X | — | 1 | 8.05 |
| CHEMBL493326 | GSK-317314A | — | 1 | 7.46 |
| CHEMBL522709 | GSK-317315A | — | 1 | 7.39 |
| CHEMBL521806 | GSK-237700A | — | 1 | 7.36 |
| CHEMBL1794067 | GSK-978744A | — | 1 | 7.21 |
| CHEMBL1964264 | — | — | 1 | 6.62 |
| CHEMBL1964265 | — | — | 1 | 6.60 |
| CHEMBL1615278 | — | — | 1 | 6.57 |
| CHEMBL1964263 | — | — | 1 | 6.46 |
| CHEMBL1964261 | — | — | 1 | 6.34 |
| CHEMBL1794068 | GSK-326090A | — | 1 | 6.26 |
| CHEMBL1964262 | — | — | 1 | 6.21 |
| CHEMBL1794070 | GSK-579289A | — | 1 | 6.20 |
| CHEMBL1794069 | GSK-571989A | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222419 | GSK-237701A | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL514499 | GW843682X | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL514162 | GW852849X | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL493326 | GSK-317314A | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL522709 | GSK-317315A | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL521806 | GSK-237700A | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1794067 | GSK-978744A | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1964264 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1964265 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1615278 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1964263 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1964261 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1794068 | GSK-326090A | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1964262 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1794070 | GSK-579289A | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1794069 | GSK-571989A | IC50 | = | 1100.0 | nM | 5.96 |