Assay Detail
Binding
CHEMBL3364610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged PLK4 (1 to 391 residues) expressed in Escherichia coli incubated for 30 mins by ELISA method
30
Total Activities
30
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: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.42 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353351 | — | — | 1 | 9.15 |
| CHEMBL3353352 | — | — | 1 | 9.10 |
| CHEMBL3353348 | — | — | 1 | 8.96 |
| CHEMBL3353350 | — | — | 1 | 8.92 |
| CHEMBL3353361 | — | — | 1 | 8.89 |
| CHEMBL3353346 | — | — | 1 | 8.85 |
| CHEMBL3353347 | — | — | 1 | 8.85 |
| CHEMBL3353342 | — | — | 1 | 8.80 |
| CHEMBL3353360 | — | — | 1 | 8.74 |
| CHEMBL3353345 | — | — | 1 | 8.70 |
| CHEMBL3353353 | — | — | 1 | 8.70 |
| CHEMBL3353341 | — | — | 1 | 8.66 |
| CHEMBL3353355 | — | — | 1 | 8.66 |
| CHEMBL3353354 | — | — | 1 | 8.64 |
| CHEMBL3353359 | — | — | 1 | 8.62 |
| CHEMBL2407749 | — | — | 1 | 8.62 |
| CHEMBL3353349 | — | — | 1 | 8.59 |
| CHEMBL3353358 | — | — | 1 | 8.47 |
| CHEMBL3353340 | — | — | 1 | 8.44 |
| CHEMBL2407897 | — | — | 1 | 8.40 |
| CHEMBL3353343 | — | — | 1 | 8.34 |
| CHEMBL3353356 | — | — | 1 | 8.31 |
| CHEMBL3353344 | — | — | 1 | 8.20 |
| CHEMBL3353362 | — | — | 1 | 8.17 |
| CHEMBL3353357 | — | — | 1 | 8.14 |
| CHEMBL2407900 | — | — | 1 | 8.14 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.37 |
| CHEMBL3353337 | — | — | 1 | 6.64 |
| CHEMBL3353338 | — | — | 1 | 6.00 |
| CHEMBL3353339 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353351 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3353352 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3353348 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3353350 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3353361 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3353346 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3353347 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3353342 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3353360 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3353345 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3353353 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3353341 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3353355 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3353354 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3353359 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2407749 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3353349 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3353358 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3353340 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2407897 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3353343 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3353356 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3353344 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3353362 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3353357 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2407900 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1289926 | AXITINIB | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3353337 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3353338 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3353339 | — | IC50 | > | 50000.0 | nM | - |