Assay Detail
Binding
CHEMBL5165904
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Haspin (470 to 798 residues) expressed in bacterial expression system using ARTKQTARKSTGGKAPRKQLA as substrate measured after 30 mins in presence of ATP by ADP-Glo assay
18
Total Activities
18
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 haspin (CHEMBL1075163) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.04 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5186093 | — | — | 1 | 8.52 |
| CHEMBL5178368 | — | — | 1 | 8.52 |
| CHEMBL5188318 | — | — | 1 | 7.92 |
| CHEMBL5181620 | — | — | 1 | 7.30 |
| CHEMBL5177344 | — | — | 1 | 7.25 |
| CHEMBL5194011 | — | — | 1 | 7.19 |
| CHEMBL5186471 | — | — | 1 | 7.16 |
| CHEMBL5196946 | — | — | 1 | 7.04 |
| CHEMBL5208358 | — | — | 1 | 6.94 |
| CHEMBL5183366 | — | — | 1 | 6.92 |
| CHEMBL5202187 | — | — | 1 | 6.91 |
| CHEMBL5208474 | — | — | 1 | 6.80 |
| CHEMBL5198375 | — | — | 1 | 6.77 |
| CHEMBL5190257 | — | — | 1 | 6.70 |
| CHEMBL5179862 | — | — | 1 | 6.37 |
| CHEMBL5181571 | — | — | 1 | 6.32 |
| CHEMBL5181177 | — | — | 1 | 6.05 |
| CHEMBL5198391 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5186093 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5178368 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5188318 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5181620 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5177344 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5194011 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5186471 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5196946 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5208358 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5183366 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5202187 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5208474 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5198375 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5190257 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL5179862 | — | IC50 | = | 432.0 | nM | 6.37 |
| CHEMBL5181571 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL5181177 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL5198391 | — | IC50 | = | 1041.0 | nM | 5.98 |