Assay Detail
ADMET
CHEMBL4689214
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Inhibition of rat DYRK1A (1 to 499 residues) assessed as residual activity by ADP-Glo assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.22 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4783398 | — | — | 1 | 6.92 |
| CHEMBL4758072 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4783398 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4758072 | — | IC50 | = | 3000.0 | nM | 5.52 |