Assay Detail
Binding
CHEMBL1912879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant GST-fused DYRK1A expressed in Escherichia coli using myelin protein and [33P-gamma]-ATP after 30 mins by scintillation counting
14
Total Activities
14
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 new 3-(6-hydroxyindol-2-yl)-5-(Phenyl) pyridine or pyrazine V-Shaped molecules as kinase inhibitors and cytotoxic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.07 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910195 | — | — | 1 | 7.22 |
| CHEMBL1910201 | — | — | 1 | 6.64 |
| CHEMBL1910377 | — | — | 1 | 6.52 |
| CHEMBL1910192 | — | — | 1 | 6.47 |
| CHEMBL1910197 | — | — | 1 | 6.46 |
| CHEMBL1910198 | — | — | 1 | 6.27 |
| CHEMBL1910193 | — | — | 1 | 6.00 |
| CHEMBL1910196 | — | — | 1 | 5.80 |
| CHEMBL1910191 | — | — | 1 | 5.64 |
| CHEMBL1910200 | — | — | 1 | 5.57 |
| CHEMBL1910194 | — | — | 1 | 5.51 |
| CHEMBL1910190 | — | — | 1 | 5.48 |
| CHEMBL1910199 | — | — | 1 | 5.30 |
| CHEMBL479170 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910195 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1910201 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1910377 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1910192 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1910197 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1910198 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1910193 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1910196 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1910191 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1910200 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1910194 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1910190 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1910199 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL479170 | — | IC50 | - | — | - |