Assay Detail
Binding
CHEMBL2182295
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting
3
Total Activities
3
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
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.90 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1802358 | — | — | 1 | 7.40 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.25 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1802358 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL269538 | HARMINE | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 920.0 | nM | 6.04 |