Assay Detail
Binding
CHEMBL1109142
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Inhibition of Plk2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting
25
Total Activities
25
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 PLK2 (CHEMBL5938) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.17 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094477 | — | — | 1 | 8.70 |
| CHEMBL559845 | — | — | 1 | 8.05 |
| CHEMBL1095457 | — | — | 1 | 7.92 |
| CHEMBL1097022 | — | — | 1 | 7.92 |
| CHEMBL1094478 | — | — | 1 | 7.85 |
| CHEMBL1094135 | — | — | 1 | 7.62 |
| CHEMBL1095771 | — | — | 1 | 7.57 |
| CHEMBL1095717 | — | — | 1 | 7.09 |
| CHEMBL1097071 | — | — | 1 | 6.96 |
| CHEMBL1094408 | NMS-1286937 | — | 1 | 6.62 |
| CHEMBL1099104 | — | — | 1 | 6.58 |
| CHEMBL1095772 | — | — | 1 | 6.29 |
| CHEMBL1097373 | — | — | 1 | 5.68 |
| CHEMBL1096095 | — | — | 1 | 5.57 |
| CHEMBL1097374 | — | — | 1 | - |
| CHEMBL1096028 | — | — | 1 | - |
| CHEMBL1095716 | — | — | 1 | - |
| CHEMBL1094484 | — | — | 1 | - |
| CHEMBL1094815 | — | — | 1 | - |
| CHEMBL1094816 | — | — | 1 | - |
| CHEMBL1094817 | — | — | 1 | - |
| CHEMBL1094488 | — | — | 1 | - |
| CHEMBL1094820 | — | — | 1 | - |
| CHEMBL1094821 | — | — | 1 | - |
| CHEMBL1094822 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094477 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL559845 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1095457 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1097022 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1094478 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1094135 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1095771 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1095717 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1097071 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL1094408 | NMS-1286937 | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL1099104 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL1095772 | — | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL1097373 | — | IC50 | = | 2104.0 | nM | 5.68 |
| CHEMBL1096095 | — | IC50 | = | 2666.0 | nM | 5.57 |
| CHEMBL1097374 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1096028 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1095716 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094484 | — | IC50 | - | — | - | |
| CHEMBL1094815 | — | IC50 | - | — | - | |
| CHEMBL1094816 | — | IC50 | - | — | - | |
| CHEMBL1094817 | — | IC50 | - | — | - | |
| CHEMBL1094488 | — | IC50 | - | — | - | |
| CHEMBL1094820 | — | IC50 | - | — | - | |
| CHEMBL1094821 | — | IC50 | - | — | - | |
| CHEMBL1094822 | — | IC50 | - | — | - |