Assay Detail
Binding
CHEMBL4266643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length GST-tagged DYRK1A expressed in baculovirus expression system assessed as decrease in tau phosphorylation at S396 preincubated for 10 mins followed by tau addition by Western blot analysis
3
Total Activities
3
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
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.54 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14285 | — | — | 1 | 7.05 |
| CHEMBL109269 | — | — | 1 | 6.40 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14285 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL109269 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL269538 | HARMINE | IC50 | = | 700.0 | nM | 6.16 |