Assay Detail
Binding
CHEMBL2410100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PLK4
6
Total Activities
6
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
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.90 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302449 | GO-6976 | — | 1 | 8.47 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 8.38 |
| CHEMBL1980391 | RG-1530 | 1.0 | 1 | 7.96 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.96 |
| CHEMBL2407901 | — | — | 1 | 7.60 |
| CHEMBL2407902 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302449 | GO-6976 | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1289926 | AXITINIB | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1980391 | RG-1530 | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL572878 | TOZASERTIB | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2407901 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2407902 | — | Ki | = | 100.0 | nM | 7.00 |