Assay Detail
Binding
CHEMBL4409681
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 hr by Z'-LYTE assay
41
Total Activities
41
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 PLK2 (CHEMBL5938) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.71 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4592698 | — | — | 1 | 8.40 |
| CHEMBL4454222 | — | — | 1 | 8.33 |
| CHEMBL4548940 | — | — | 1 | 8.10 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.87 |
| CHEMBL4458460 | — | — | 1 | 7.52 |
| CHEMBL4457656 | — | — | 1 | 7.47 |
| CHEMBL4436925 | — | — | 1 | 7.44 |
| CHEMBL4441121 | — | — | 1 | 7.21 |
| CHEMBL4450564 | — | — | 1 | 7.12 |
| CHEMBL4448563 | — | — | 1 | 7.07 |
| CHEMBL4456400 | — | — | 1 | 6.97 |
| CHEMBL4570557 | — | — | 1 | 6.97 |
| CHEMBL4459892 | — | — | 1 | 6.91 |
| CHEMBL4447251 | — | — | 1 | 6.88 |
| CHEMBL4531932 | — | — | 1 | 6.82 |
| CHEMBL4447495 | — | — | 1 | 6.78 |
| CHEMBL4566834 | — | — | 1 | 6.71 |
| CHEMBL4519294 | — | — | 1 | 6.64 |
| CHEMBL4449123 | — | — | 1 | 6.58 |
| CHEMBL4461041 | — | — | 1 | 6.54 |
| CHEMBL4545446 | — | — | 1 | 6.50 |
| CHEMBL4450624 | — | — | 1 | 6.47 |
| CHEMBL4529398 | — | — | 1 | 6.41 |
| CHEMBL4573833 | — | — | 1 | 6.40 |
| CHEMBL4453584 | — | — | 1 | 6.30 |
| CHEMBL4574072 | — | — | 1 | 6.20 |
| CHEMBL4465062 | — | — | 1 | 6.19 |
| CHEMBL4574255 | — | — | 1 | 6.19 |
| CHEMBL4442768 | — | — | 1 | 6.14 |
| CHEMBL4515187 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4592698 | — | IC50 | = | 3.98 | nM | 8.40 |
| CHEMBL4454222 | — | IC50 | = | 4.72 | nM | 8.33 |
| CHEMBL4548940 | — | IC50 | = | 7.98 | nM | 8.10 |
| CHEMBL513909 | BI-2536 | IC50 | = | 13.55 | nM | 7.87 |
| CHEMBL4458460 | — | IC50 | = | 30.51 | nM | 7.52 |
| CHEMBL4457656 | — | IC50 | = | 33.83 | nM | 7.47 |
| CHEMBL4436925 | — | IC50 | = | 36.04 | nM | 7.44 |
| CHEMBL4441121 | — | IC50 | = | 61.17 | nM | 7.21 |
| CHEMBL4450564 | — | IC50 | = | 75.77 | nM | 7.12 |
| CHEMBL4448563 | — | IC50 | = | 85.11 | nM | 7.07 |
| CHEMBL4570557 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4456400 | — | IC50 | = | 107.2 | nM | 6.97 |
| CHEMBL4459892 | — | IC50 | = | 122.2 | nM | 6.91 |
| CHEMBL4447251 | — | IC50 | = | 131.7 | nM | 6.88 |
| CHEMBL4531932 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4447495 | — | IC50 | = | 167.3 | nM | 6.78 |
| CHEMBL4566834 | — | IC50 | = | 195.9 | nM | 6.71 |
| CHEMBL4519294 | — | IC50 | = | 230.9 | nM | 6.64 |
| CHEMBL4449123 | — | IC50 | = | 265.1 | nM | 6.58 |
| CHEMBL4461041 | — | IC50 | = | 290.5 | nM | 6.54 |
| CHEMBL4545446 | — | IC50 | = | 314.2 | nM | 6.50 |
| CHEMBL4450624 | — | IC50 | = | 338.7 | nM | 6.47 |
| CHEMBL4529398 | — | IC50 | = | 385.3 | nM | 6.41 |
| CHEMBL4573833 | — | IC50 | = | 397.3 | nM | 6.40 |
| CHEMBL4453584 | — | IC50 | = | 498.0 | nM | 6.30 |
| CHEMBL4574072 | — | IC50 | = | 626.2 | nM | 6.20 |
| CHEMBL4465062 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL4574255 | — | IC50 | = | 640.8 | nM | 6.19 |
| CHEMBL4442768 | — | IC50 | = | 718.3 | nM | 6.14 |
| CHEMBL4515187 | — | IC50 | = | 743.9 | nM | 6.13 |
| CHEMBL4541823 | — | IC50 | = | 868.7 | nM | 6.06 |
| CHEMBL4576641 | — | IC50 | = | 873.6 | nM | 6.06 |
| CHEMBL4587599 | — | IC50 | = | 898.4 | nM | 6.05 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 957.2 | nM | 6.02 |
| CHEMBL4454586 | — | IC50 | = | 1796.9 | nM | 5.75 |
| CHEMBL4515755 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL4468970 | — | IC50 | = | 3474.0 | nM | 5.46 |
| CHEMBL4469319 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4449490 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4473297 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4524869 | — | IC50 | > | 10000.0 | nM | - |