Assay Detail
Binding
CHEMBL5115582
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PLK4 (unknown origin)
3
Total Activities
3
Compounds Tested
2
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, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.30 | 8.15 |
| Ki | 1 | 8.12 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1980391 | RG-1530 | 1.0 | 1 | 8.15 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.12 |
| CHEMBL5175418 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1980391 | RG-1530 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL572878 | TOZASERTIB | Ki | = | 7.66 | nM | 8.12 |
| CHEMBL5175418 | — | IC50 | = | 351.5 | nM | 6.45 |