Assay Detail
Binding
CHEMBL5381874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PLK4 (unknown origin) incubated for 1 hr by FRET assay
50
Total Activities
50
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
Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.74 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185001 | — | — | 1 | 9.70 |
| CHEMBL5428085 | — | — | 1 | 9.52 |
| CHEMBL5404983 | — | — | 1 | 9.52 |
| CHEMBL5439790 | — | — | 1 | 9.40 |
| CHEMBL5402864 | — | — | 1 | 9.05 |
| CHEMBL5420150 | — | — | 1 | 9.00 |
| CHEMBL5432542 | — | — | 1 | 8.92 |
| CHEMBL5424463 | — | — | 1 | 8.68 |
| CHEMBL5404721 | — | — | 1 | 8.59 |
| CHEMBL5185225 | — | — | 1 | 8.52 |
| CHEMBL5426828 | — | — | 1 | 8.43 |
| CHEMBL5397250 | — | — | 1 | 8.27 |
| CHEMBL5435158 | — | — | 1 | 8.17 |
| CHEMBL5397303 | — | — | 1 | 8.07 |
| CHEMBL5430106 | — | — | 1 | 8.05 |
| CHEMBL5438019 | — | — | 1 | 8.03 |
| CHEMBL5401850 | — | — | 1 | 8.01 |
| CHEMBL5429187 | — | — | 1 | 7.98 |
| CHEMBL5411040 | — | — | 1 | 7.94 |
| CHEMBL5418250 | — | — | 1 | 7.80 |
| CHEMBL5432162 | — | — | 1 | 7.74 |
| CHEMBL5409434 | — | — | 1 | 7.71 |
| CHEMBL5396900 | — | — | 1 | 7.70 |
| CHEMBL5433434 | — | — | 1 | 7.67 |
| CHEMBL5425999 | — | — | 1 | 7.67 |
| CHEMBL5424704 | — | — | 1 | 7.63 |
| CHEMBL5425790 | — | — | 1 | 7.62 |
| CHEMBL5401624 | — | — | 1 | 7.62 |
| CHEMBL5415864 | — | — | 1 | 7.62 |
| CHEMBL5413063 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185001 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5428085 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5404983 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5439790 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5402864 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5420150 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5432542 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5424463 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5404721 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5185225 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5426828 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5397250 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5435158 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5397303 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5430106 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5438019 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5401850 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5429187 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5411040 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5418250 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5432162 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL5409434 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL5396900 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL5433434 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL5425999 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL5424704 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL5401624 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL5415864 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL5425790 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL5413063 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL5434198 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL5438955 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL5405656 | — | IC50 | = | 32.1 | nM | 7.49 |
| CHEMBL5412525 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL5430972 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL5411852 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL5420791 | — | IC50 | = | 51.4 | nM | 7.29 |
| CHEMBL5439446 | — | IC50 | = | 61.2 | nM | 7.21 |
| CHEMBL5429009 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL5396416 | — | IC50 | = | 85.4 | nM | 7.07 |
| CHEMBL5407310 | — | IC50 | = | 90.7 | nM | 7.04 |
| CHEMBL5435416 | — | IC50 | = | 121.9 | nM | 6.91 |
| CHEMBL5408496 | — | IC50 | = | 186.1 | nM | 6.73 |
| CHEMBL5420852 | — | IC50 | = | 214.4 | nM | 6.67 |
| CHEMBL5429940 | — | IC50 | = | 243.5 | nM | 6.61 |
| CHEMBL5423111 | — | IC50 | = | 352.7 | nM | 6.45 |
| CHEMBL5399599 | — | IC50 | = | 410.6 | nM | 6.39 |
| CHEMBL5400736 | — | IC50 | = | 420.6 | nM | 6.38 |
| CHEMBL5399648 | — | IC50 | = | 511.2 | nM | 6.29 |
| CHEMBL5418921 | — | IC50 | = | 1510.1 | nM | 5.82 |