Assay Detail
Binding
CHEMBL4143483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition human recombinant full length GST-tagged Plk2 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 PLK2 (CHEMBL5938) ↗| 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 | 7.22 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166771 | — | — | 1 | 8.47 |
| CHEMBL4171770 | — | — | 1 | 8.31 |
| CHEMBL4175722 | — | — | 1 | 8.15 |
| CHEMBL4176983 | — | — | 1 | 8.11 |
| CHEMBL4169129 | — | — | 1 | 8.09 |
| CHEMBL4163892 | — | — | 1 | 8.07 |
| CHEMBL4168155 | — | — | 1 | 7.99 |
| CHEMBL4164012 | — | — | 1 | 7.95 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.87 |
| CHEMBL4160611 | — | — | 1 | 7.78 |
| CHEMBL4174667 | — | — | 1 | 7.76 |
| CHEMBL4177399 | — | — | 1 | 7.75 |
| CHEMBL4171224 | — | — | 1 | 7.73 |
| CHEMBL4170176 | — | — | 1 | 7.70 |
| CHEMBL4162262 | — | — | 1 | 7.66 |
| CHEMBL4173620 | — | — | 1 | 7.62 |
| CHEMBL4161572 | — | — | 1 | 7.54 |
| CHEMBL4165706 | — | — | 1 | 7.26 |
| CHEMBL4172511 | — | — | 1 | 7.14 |
| CHEMBL4164082 | — | — | 1 | 7.04 |
| CHEMBL4161861 | — | — | 1 | 6.92 |
| CHEMBL4171281 | — | — | 1 | 6.91 |
| CHEMBL4174735 | — | — | 1 | 6.80 |
| CHEMBL4160679 | — | — | 1 | 6.80 |
| CHEMBL4168834 | — | — | 1 | 6.72 |
| CHEMBL4176689 | — | — | 1 | 6.72 |
| CHEMBL4175615 | — | — | 1 | 6.72 |
| CHEMBL4161027 | — | — | 1 | 6.68 |
| CHEMBL4164433 | — | — | 1 | 6.66 |
| CHEMBL4168951 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166771 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4171770 | — | IC50 | = | 4.88 | nM | 8.31 |
| CHEMBL4175722 | — | IC50 | = | 7.06 | nM | 8.15 |
| CHEMBL4176983 | — | IC50 | = | 7.86 | nM | 8.11 |
| CHEMBL4169129 | — | IC50 | = | 8.16 | nM | 8.09 |
| CHEMBL4163892 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4168155 | — | IC50 | = | 10.17 | nM | 7.99 |
| CHEMBL4164012 | — | IC50 | = | 11.35 | nM | 7.95 |
| CHEMBL513909 | BI-2536 | IC50 | = | 13.55 | nM | 7.87 |
| CHEMBL4160611 | — | IC50 | = | 16.52 | nM | 7.78 |
| CHEMBL4174667 | — | IC50 | = | 17.41 | nM | 7.76 |
| CHEMBL4177399 | — | IC50 | = | 17.77 | nM | 7.75 |
| CHEMBL4171224 | — | IC50 | = | 18.62 | nM | 7.73 |
| CHEMBL4170176 | — | IC50 | = | 19.85 | nM | 7.70 |
| CHEMBL4162262 | — | IC50 | = | 21.77 | nM | 7.66 |
| CHEMBL4173620 | — | IC50 | = | 23.87 | nM | 7.62 |
| CHEMBL4161572 | — | IC50 | = | 28.51 | nM | 7.54 |
| CHEMBL4165706 | — | IC50 | = | 54.4 | nM | 7.26 |
| CHEMBL4172511 | — | IC50 | = | 71.55 | nM | 7.14 |
| CHEMBL4164082 | — | IC50 | = | 90.93 | nM | 7.04 |
| CHEMBL4161861 | — | IC50 | = | 120.6 | nM | 6.92 |
| CHEMBL4171281 | — | IC50 | = | 124.5 | nM | 6.91 |
| CHEMBL4174735 | — | IC50 | = | 158.8 | nM | 6.80 |
| CHEMBL4160679 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4168834 | — | IC50 | = | 189.6 | nM | 6.72 |
| CHEMBL4176689 | — | IC50 | = | 190.7 | nM | 6.72 |
| CHEMBL4175615 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4161027 | — | IC50 | = | 206.7 | nM | 6.68 |
| CHEMBL4164433 | — | IC50 | = | 217.7 | nM | 6.66 |
| CHEMBL4168951 | — | IC50 | = | 242.5 | nM | 6.62 |
| CHEMBL4165409 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL4164991 | — | IC50 | = | 354.7 | nM | 6.45 |
| CHEMBL4172312 | — | IC50 | = | 384.3 | nM | 6.42 |
| CHEMBL4173322 | — | IC50 | = | 478.3 | nM | 6.32 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 957.2 | nM | 6.02 |
| CHEMBL4172185 | — | IC50 | = | 969.2 | nM | 6.01 |
| CHEMBL4167865 | — | IC50 | = | 1500.0 | nM | 5.82 |