Assay Detail
Binding
CHEMBL4409682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) 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 PLK3 (CHEMBL4897) ↗| 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 | 6.69 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4592698 | — | — | 1 | 8.22 |
| CHEMBL4454222 | — | — | 1 | 7.72 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.68 |
| CHEMBL4458460 | — | — | 1 | 7.66 |
| CHEMBL4548940 | — | — | 1 | 7.52 |
| CHEMBL4456400 | — | — | 1 | 7.36 |
| CHEMBL4457656 | — | — | 1 | 7.35 |
| CHEMBL4570557 | — | — | 1 | 7.33 |
| CHEMBL4441121 | — | — | 1 | 7.07 |
| CHEMBL4447251 | — | — | 1 | 7.04 |
| CHEMBL4436925 | — | — | 1 | 6.95 |
| CHEMBL4459892 | — | — | 1 | 6.93 |
| CHEMBL4448563 | — | — | 1 | 6.85 |
| CHEMBL4519294 | — | — | 1 | 6.82 |
| CHEMBL4566834 | — | — | 1 | 6.80 |
| CHEMBL4461041 | — | — | 1 | 6.79 |
| CHEMBL4529398 | — | — | 1 | 6.78 |
| CHEMBL4447495 | — | — | 1 | 6.71 |
| CHEMBL4515187 | — | — | 1 | 6.69 |
| CHEMBL4573833 | — | — | 1 | 6.44 |
| CHEMBL4574072 | — | — | 1 | 6.41 |
| CHEMBL4545446 | — | — | 1 | 6.39 |
| CHEMBL4453584 | — | — | 1 | 6.36 |
| CHEMBL4465062 | — | — | 1 | 6.36 |
| CHEMBL4531932 | — | — | 1 | 6.34 |
| CHEMBL4574255 | — | — | 1 | 6.32 |
| CHEMBL4450624 | — | — | 1 | 6.26 |
| CHEMBL4449123 | — | — | 1 | 6.16 |
| CHEMBL4442768 | — | — | 1 | 6.12 |
| CHEMBL4541823 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4592698 | — | IC50 | = | 6.04 | nM | 8.22 |
| CHEMBL4454222 | — | IC50 | = | 18.91 | nM | 7.72 |
| CHEMBL513909 | BI-2536 | IC50 | = | 20.78 | nM | 7.68 |
| CHEMBL4458460 | — | IC50 | = | 22.14 | nM | 7.66 |
| CHEMBL4548940 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL4456400 | — | IC50 | = | 43.78 | nM | 7.36 |
| CHEMBL4457656 | — | IC50 | = | 45.07 | nM | 7.35 |
| CHEMBL4570557 | — | IC50 | = | 46.93 | nM | 7.33 |
| CHEMBL4441121 | — | IC50 | = | 84.8 | nM | 7.07 |
| CHEMBL4447251 | — | IC50 | = | 91.93 | nM | 7.04 |
| CHEMBL4436925 | — | IC50 | = | 112.8 | nM | 6.95 |
| CHEMBL4459892 | — | IC50 | = | 116.6 | nM | 6.93 |
| CHEMBL4448563 | — | IC50 | = | 142.5 | nM | 6.85 |
| CHEMBL4519294 | — | IC50 | = | 150.2 | nM | 6.82 |
| CHEMBL4566834 | — | IC50 | = | 157.4 | nM | 6.80 |
| CHEMBL4461041 | — | IC50 | = | 162.8 | nM | 6.79 |
| CHEMBL4529398 | — | IC50 | = | 166.1 | nM | 6.78 |
| CHEMBL4447495 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL4515187 | — | IC50 | = | 205.2 | nM | 6.69 |
| CHEMBL4573833 | — | IC50 | = | 366.3 | nM | 6.44 |
| CHEMBL4574072 | — | IC50 | = | 385.3 | nM | 6.41 |
| CHEMBL4545446 | — | IC50 | = | 406.9 | nM | 6.39 |
| CHEMBL4453584 | — | IC50 | = | 440.6 | nM | 6.36 |
| CHEMBL4465062 | — | IC50 | = | 436.2 | nM | 6.36 |
| CHEMBL4531932 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL4574255 | — | IC50 | = | 476.7 | nM | 6.32 |
| CHEMBL4450624 | — | IC50 | = | 554.5 | nM | 6.26 |
| CHEMBL4449123 | — | IC50 | = | 699.6 | nM | 6.16 |
| CHEMBL4442768 | — | IC50 | = | 749.7 | nM | 6.12 |
| CHEMBL4541823 | — | IC50 | = | 974.33 | nM | 6.01 |
| CHEMBL4454586 | — | IC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL4587599 | — | IC50 | = | 1252.0 | nM | 5.90 |
| CHEMBL4576641 | — | IC50 | = | 1351.0 | nM | 5.87 |
| CHEMBL4515755 | — | IC50 | = | 2977.0 | nM | 5.53 |
| CHEMBL4450564 | — | IC50 | = | 3011.0 | nM | 5.52 |
| CHEMBL4468970 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4473297 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4524869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL388978 | STAUROSPORINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL4469319 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4449490 | — | IC50 | > | 10000.0 | nM | - |