Assay Detail
Binding
CHEMBL3825019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged rat recombinant DYRK1A expressed in Escherichia coli using myelin basic protein as substrate incubated for 30 mins in presence of [gamma-33 ATP] by liquid scintillation counting analysis
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
Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.84 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3823483 | — | — | 1 | 7.55 |
| CHEMBL3823505 | — | — | 1 | 6.75 |
| CHEMBL3823532 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3823483 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3823505 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3823532 | — | IC50 | = | 620.0 | nM | 6.21 |