Assay Detail
Binding
CHEMBL4003695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged full-length recombinant human NEK2 expressed in baculovirus infected sf21 cells using biotin labelled-STK-3 substrate measured after 60 mins by HTRF assay
26
Total Activities
26
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 Nek2 (CHEMBL3835) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.06 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062453 | — | — | 1 | 9.00 |
| CHEMBL4063211 | — | — | 1 | 8.52 |
| CHEMBL4091089 | — | — | 1 | 8.15 |
| CHEMBL4087758 | — | — | 1 | 7.06 |
| CHEMBL4105643 | — | — | 1 | 6.41 |
| CHEMBL4101298 | — | — | 1 | 6.32 |
| CHEMBL4062949 | — | — | 1 | 6.23 |
| CHEMBL4065063 | — | — | 1 | 6.09 |
| CHEMBL4102393 | — | — | 1 | 6.08 |
| CHEMBL4083300 | — | — | 1 | 6.03 |
| CHEMBL4076354 | — | — | 1 | 5.98 |
| CHEMBL4082341 | — | — | 1 | 5.92 |
| CHEMBL4098835 | — | — | 1 | 5.89 |
| CHEMBL4084616 | — | — | 1 | 5.80 |
| CHEMBL4064022 | — | — | 1 | 5.66 |
| CHEMBL4076233 | — | — | 1 | 5.62 |
| CHEMBL4060438 | — | — | 1 | 5.49 |
| CHEMBL4086508 | — | — | 1 | 5.00 |
| CHEMBL4083100 | — | — | 1 | 5.00 |
| CHEMBL4071842 | — | — | 1 | 5.00 |
| CHEMBL4073648 | — | — | 1 | 4.95 |
| CHEMBL4102006 | — | — | 1 | 4.71 |
| CHEMBL4091785 | — | — | 1 | 4.37 |
| CHEMBL4061228 | — | — | 1 | - |
| CHEMBL4094275 | — | — | 1 | - |
| CHEMBL4091915 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062453 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4063211 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4091089 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4087758 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4105643 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL4101298 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4062949 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL4065063 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL4102393 | — | IC50 | = | 838.0 | nM | 6.08 |
| CHEMBL4083300 | — | IC50 | = | 927.0 | nM | 6.03 |
| CHEMBL4076354 | — | IC50 | = | 1037.0 | nM | 5.98 |
| CHEMBL4082341 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4098835 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4084616 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4064022 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4076233 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4060438 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL4086508 | — | IC50 | = | 10030.0 | nM | 5.00 |
| CHEMBL4083100 | — | IC50 | = | 10030.0 | nM | 5.00 |
| CHEMBL4071842 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4073648 | — | IC50 | = | 11190.0 | nM | 4.95 |
| CHEMBL4102006 | — | IC50 | = | 19280.0 | nM | 4.71 |
| CHEMBL4091785 | — | IC50 | = | 42600.0 | nM | 4.37 |
| CHEMBL4061228 | — | IC50 | = | 197000.0 | nM | - |
| CHEMBL4094275 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4091915 | — | IC50 | > | 200000.0 | nM | - |