Assay Detail
Binding
CHEMBL5115459
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PAK4 (unknown origin) incubated for 60 mins by time-resolved HTRF assay
26
Total Activities
26
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 PAK 4 (CHEMBL4482) ↗| 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 | 26 | 6.06 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5209160 | — | — | 1 | 7.02 |
| CHEMBL5188129 | — | — | 1 | 6.64 |
| CHEMBL5186873 | — | — | 1 | 6.56 |
| CHEMBL5185324 | — | — | 1 | 6.41 |
| CHEMBL5200865 | — | — | 1 | 6.40 |
| CHEMBL5199896 | — | — | 1 | 6.34 |
| CHEMBL5171469 | — | — | 1 | 6.29 |
| CHEMBL5175294 | — | — | 1 | 6.21 |
| CHEMBL5176789 | — | — | 1 | 6.18 |
| CHEMBL5171233 | — | — | 1 | 6.17 |
| CHEMBL5176750 | — | — | 1 | 5.98 |
| CHEMBL5208535 | — | — | 1 | 5.96 |
| CHEMBL5187941 | — | — | 1 | 5.88 |
| CHEMBL5205336 | — | — | 1 | 5.82 |
| CHEMBL5185001 | — | — | 1 | 5.76 |
| CHEMBL5179518 | — | — | 1 | 5.71 |
| CHEMBL5181286 | — | — | 1 | 5.36 |
| CHEMBL5192817 | — | — | 1 | 5.23 |
| CHEMBL5173615 | — | — | 1 | 5.23 |
| CHEMBL5194020 | — | — | 1 | - |
| CHEMBL5169342 | — | — | 1 | - |
| CHEMBL5180759 | — | — | 1 | - |
| CHEMBL5198607 | — | — | 1 | - |
| CHEMBL5175172 | — | — | 1 | - |
| CHEMBL5187903 | — | — | 1 | - |
| CHEMBL5198928 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5209160 | — | IC50 | = | 96.1 | nM | 7.02 |
| CHEMBL5188129 | — | IC50 | = | 231.1 | nM | 6.64 |
| CHEMBL5186873 | — | IC50 | = | 273.4 | nM | 6.56 |
| CHEMBL5185324 | — | IC50 | = | 389.2 | nM | 6.41 |
| CHEMBL5200865 | — | IC50 | = | 395.1 | nM | 6.40 |
| CHEMBL5199896 | — | IC50 | = | 458.2 | nM | 6.34 |
| CHEMBL5171469 | — | IC50 | = | 515.2 | nM | 6.29 |
| CHEMBL5175294 | — | IC50 | = | 610.6 | nM | 6.21 |
| CHEMBL5176789 | — | IC50 | = | 654.8 | nM | 6.18 |
| CHEMBL5171233 | — | IC50 | = | 668.3 | nM | 6.17 |
| CHEMBL5176750 | — | IC50 | = | 1051.8 | nM | 5.98 |
| CHEMBL5208535 | — | IC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL5187941 | — | IC50 | = | 1324.8 | nM | 5.88 |
| CHEMBL5205336 | — | IC50 | = | 1501.2 | nM | 5.82 |
| CHEMBL5185001 | — | IC50 | = | 1750.1 | nM | 5.76 |
| CHEMBL5179518 | — | IC50 | = | 1961.1 | nM | 5.71 |
| CHEMBL5181286 | — | IC50 | = | 4336.2 | nM | 5.36 |
| CHEMBL5192817 | — | IC50 | = | 5898.6 | nM | 5.23 |
| CHEMBL5173615 | — | IC50 | = | 5937.1 | nM | 5.23 |
| CHEMBL5194020 | — | IC50 | - | — | - | |
| CHEMBL5169342 | — | IC50 | - | — | - | |
| CHEMBL5180759 | — | IC50 | - | — | - | |
| CHEMBL5198607 | — | IC50 | - | — | - | |
| CHEMBL5175172 | — | IC50 | - | — | - | |
| CHEMBL5187903 | — | IC50 | - | — | - | |
| CHEMBL5198928 | — | IC50 | - | — | - |