Assay Detail
Binding
CHEMBL5165908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant rat DYRK1A (1 to 499 residues ) expressed in bacterial expression system using KKISGRLSPIMTEQ as substrate measured after 30 mins in presence of ATP by ADP-Glo assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.73 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178368 | — | — | 1 | 7.89 |
| CHEMBL5188318 | — | — | 1 | 7.33 |
| CHEMBL5186093 | — | — | 1 | 7.06 |
| CHEMBL5186471 | — | — | 1 | 6.88 |
| CHEMBL5194011 | — | — | 1 | 6.83 |
| CHEMBL5196946 | — | — | 1 | 6.29 |
| CHEMBL5177344 | — | — | 1 | 6.23 |
| CHEMBL5183366 | — | — | 1 | 6.04 |
| CHEMBL5181620 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178368 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5188318 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5186093 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5186471 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5194011 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL5196946 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL5177344 | — | IC50 | = | 594.0 | nM | 6.23 |
| CHEMBL5183366 | — | IC50 | = | 916.3 | nM | 6.04 |
| CHEMBL5181620 | — | IC50 | = | 917.0 | nM | 6.04 |