Assay Detail
Binding
CHEMBL4143485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition human recombinant GST-tagged Plk3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay
37
Total Activities
37
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
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.05 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.68 |
| CHEMBL4166771 | — | — | 1 | 7.41 |
| CHEMBL4168155 | — | — | 1 | 7.09 |
| CHEMBL4176983 | — | — | 1 | 6.84 |
| CHEMBL4169129 | — | — | 1 | 6.78 |
| CHEMBL4177399 | — | — | 1 | 6.69 |
| CHEMBL4170176 | — | — | 1 | 6.61 |
| CHEMBL4162262 | — | — | 1 | 6.47 |
| CHEMBL4173322 | — | — | 1 | 6.32 |
| CHEMBL4173620 | — | — | 1 | 6.13 |
| CHEMBL4161572 | — | — | 1 | 5.91 |
| CHEMBL4172511 | — | — | 1 | 5.90 |
| CHEMBL4176689 | — | — | 1 | 5.87 |
| CHEMBL4168834 | — | — | 1 | 5.81 |
| CHEMBL4161861 | — | — | 1 | 5.75 |
| CHEMBL4175615 | — | — | 1 | 5.74 |
| CHEMBL4165409 | — | — | 1 | 5.72 |
| CHEMBL4165706 | — | — | 1 | 5.62 |
| CHEMBL4164012 | — | — | 1 | 5.57 |
| CHEMBL4171224 | — | — | 1 | 5.55 |
| CHEMBL4171770 | — | — | 1 | 5.35 |
| CHEMBL4164082 | — | — | 1 | 5.26 |
| CHEMBL4163892 | — | — | 1 | 5.15 |
| CHEMBL4174667 | — | — | 1 | 5.00 |
| CHEMBL4160611 | — | — | 1 | 5.00 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | - |
| CHEMBL4164991 | — | — | 1 | - |
| CHEMBL4174735 | — | — | 1 | - |
| CHEMBL4160679 | — | — | 1 | - |
| CHEMBL4171281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | IC50 | = | 20.78 | nM | 7.68 |
| CHEMBL4166771 | — | IC50 | = | 38.52 | nM | 7.41 |
| CHEMBL4168155 | — | IC50 | = | 80.72 | nM | 7.09 |
| CHEMBL4176983 | — | IC50 | = | 145.6 | nM | 6.84 |
| CHEMBL4169129 | — | IC50 | = | 165.3 | nM | 6.78 |
| CHEMBL4177399 | — | IC50 | = | 203.9 | nM | 6.69 |
| CHEMBL4170176 | — | IC50 | = | 245.6 | nM | 6.61 |
| CHEMBL4162262 | — | IC50 | = | 342.2 | nM | 6.47 |
| CHEMBL4173322 | — | IC50 | = | 482.8 | nM | 6.32 |
| CHEMBL4173620 | — | IC50 | = | 742.8 | nM | 6.13 |
| CHEMBL4161572 | — | IC50 | = | 1225.0 | nM | 5.91 |
| CHEMBL4172511 | — | IC50 | = | 1263.0 | nM | 5.90 |
| CHEMBL4176689 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL4168834 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4161861 | — | IC50 | = | 1774.0 | nM | 5.75 |
| CHEMBL4175615 | — | IC50 | = | 1818.0 | nM | 5.74 |
| CHEMBL4165409 | — | IC50 | = | 1902.0 | nM | 5.72 |
| CHEMBL4165706 | — | IC50 | = | 2403.0 | nM | 5.62 |
| CHEMBL4164012 | — | IC50 | = | 2689.0 | nM | 5.57 |
| CHEMBL4171224 | — | IC50 | = | 2789.0 | nM | 5.55 |
| CHEMBL4171770 | — | IC50 | = | 4442.0 | nM | 5.35 |
| CHEMBL4164082 | — | IC50 | = | 5491.0 | nM | 5.26 |
| CHEMBL4163892 | — | IC50 | = | 7146.0 | nM | 5.15 |
| CHEMBL4174667 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4160611 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4172185 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4175722 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4167865 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4172312 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4164433 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4168951 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4161027 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4171281 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4160679 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4174735 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4164991 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL388978 | STAUROSPORINE | IC50 | > | 10000.0 | nM | - |