Assay Detail
Binding
CHEMBL5115458
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PLK4 incubated for 60 mins by Lanthascreen Eu kinase binding assay
43
Total Activities
43
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
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 | 43 | 7.80 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5209160 | — | — | 1 | 10.00 |
| CHEMBL5185001 | — | — | 1 | 9.70 |
| CHEMBL5171469 | — | — | 1 | 9.52 |
| CHEMBL5188129 | — | — | 1 | 9.15 |
| CHEMBL5183346 | — | — | 1 | 9.15 |
| CHEMBL5171233 | — | — | 1 | 9.15 |
| CHEMBL5200865 | — | — | 1 | 9.10 |
| CHEMBL5185324 | — | — | 1 | 9.00 |
| CHEMBL5194020 | — | — | 1 | 8.96 |
| CHEMBL5191641 | — | — | 1 | 8.74 |
| CHEMBL5176789 | — | — | 1 | 8.57 |
| CHEMBL5185225 | — | — | 1 | 8.52 |
| CHEMBL5190548 | — | — | 1 | 8.43 |
| CHEMBL5207473 | — | — | 1 | 8.42 |
| CHEMBL5201909 | — | — | 1 | 8.40 |
| CHEMBL5175294 | — | — | 1 | 8.26 |
| CHEMBL5187941 | — | — | 1 | 8.25 |
| CHEMBL5198607 | — | — | 1 | 8.19 |
| CHEMBL5200125 | — | — | 1 | 8.15 |
| CHEMBL5180759 | — | — | 1 | 8.10 |
| CHEMBL5208535 | — | — | 1 | 8.06 |
| CHEMBL5175172 | — | — | 1 | 7.98 |
| CHEMBL5199896 | — | — | 1 | 7.84 |
| CHEMBL5169342 | — | — | 1 | 7.76 |
| CHEMBL5183478 | — | — | 1 | 7.70 |
| CHEMBL5200812 | — | — | 1 | 7.68 |
| CHEMBL5179518 | — | — | 1 | 7.67 |
| CHEMBL5198928 | — | — | 1 | 7.65 |
| CHEMBL5181286 | — | — | 1 | 7.63 |
| CHEMBL5192169 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5209160 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5185001 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5171469 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5188129 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5183346 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5171233 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5200865 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5185324 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5194020 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5191641 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5176789 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5185225 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5190548 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5207473 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5201909 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5175294 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5187941 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5198607 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5200125 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5180759 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5208535 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5175172 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5199896 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL5169342 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL5183478 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL5200812 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL5179518 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL5198928 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL5181286 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL5192169 | — | IC50 | = | 47.9 | nM | 7.32 |
| CHEMBL5187903 | — | IC50 | = | 78.5 | nM | 7.11 |
| CHEMBL5190474 | — | IC50 | = | 117.9 | nM | 6.93 |
| CHEMBL5192817 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5181116 | — | IC50 | = | 241.3 | nM | 6.62 |
| CHEMBL5176750 | — | IC50 | = | 453.9 | nM | 6.34 |
| CHEMBL5186873 | — | IC50 | = | 483.9 | nM | 6.32 |
| CHEMBL5173615 | — | IC50 | = | 489.1 | nM | 6.31 |
| CHEMBL5205336 | — | IC50 | = | 533.0 | nM | 6.27 |
| CHEMBL5179755 | — | IC50 | = | 535.8 | nM | 6.27 |
| CHEMBL5185066 | — | IC50 | = | 725.6 | nM | 6.14 |
| CHEMBL5192030 | — | IC50 | = | 968.9 | nM | 6.01 |
| CHEMBL5184864 | — | IC50 | = | 1293.1 | nM | 5.89 |
| CHEMBL5198803 | — | IC50 | = | 3176.0 | nM | 5.50 |