Assay Detail
Binding
CHEMBL4430364
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Inhibition of PLK4 (unknown origin)
21
Total Activities
20
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 PLK4 (CHEMBL3788) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.16 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4553351 | — | — | 1 | 9.35 |
| CHEMBL4516793 | — | — | 2 | 9.16 |
| CHEMBL4448596 | — | — | 1 | 9.03 |
| CHEMBL4470693 | — | — | 1 | 8.92 |
| CHEMBL4440053 | — | — | 1 | 8.92 |
| CHEMBL4437913 | — | — | 1 | 8.82 |
| CHEMBL4440812 | — | — | 1 | 8.80 |
| CHEMBL4461353 | — | — | 1 | 8.77 |
| CHEMBL4457197 | — | — | 1 | 8.68 |
| CHEMBL4434704 | — | — | 1 | 8.62 |
| CHEMBL4590185 | — | — | 1 | 8.34 |
| CHEMBL4475381 | — | — | 1 | 8.23 |
| CHEMBL4437872 | — | — | 1 | 7.89 |
| CHEMBL4579738 | — | — | 1 | 7.54 |
| CHEMBL4467348 | — | — | 1 | 7.52 |
| CHEMBL4546145 | — | — | 1 | 7.27 |
| CHEMBL4449539 | — | — | 1 | 7.19 |
| CHEMBL4562664 | — | — | 1 | 6.66 |
| CHEMBL4466113 | — | — | 1 | 6.31 |
| CHEMBL4457259 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4553351 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL4516793 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4448596 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4516793 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4470693 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4440053 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4437913 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4440812 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4461353 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4457197 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4434704 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4590185 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4475381 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4437872 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4579738 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4467348 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4546145 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4449539 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4562664 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4466113 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4457259 | — | IC50 | = | 540.0 | nM | 6.27 |