Assay Detail
Binding
CHEMBL3411683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive binding to PLK4 (unknown origin) by double reciprocal plot analysis in presence of ATP
3
Total Activities
3
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 Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 9.58 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408945 | — | — | 1 | 10.00 |
| CHEMBL3408947 | OCIFISERTIB | 2.0 | 1 | 9.59 |
| CHEMBL3408946 | — | — | 1 | 9.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408945 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3408947 | OCIFISERTIB | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL3408946 | — | Ki | = | 0.73 | nM | 9.14 |