Assay Detail
Binding
CHEMBL3108566
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Competitive inhibition of rat recombinant 6xHis-tagged DYRK1A catalytic domain (1 to 502) expressed in Escherichia coli BL21 (DE3) using ATP as substrate by Michaelis-Menten plot analysis
7
Total Activities
7
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
Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.19 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3102950 | — | — | 1 | 8.64 |
| CHEMBL3102951 | — | — | 1 | 8.26 |
| CHEMBL3102953 | — | — | 1 | 8.12 |
| CHEMBL3102955 | — | — | 1 | 8.00 |
| CHEMBL3102954 | — | — | 1 | 7.92 |
| CHEMBL3102956 | — | — | 1 | - |
| CHEMBL3102952 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3102950 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3102951 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3102953 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL3102955 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL3102954 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL3102956 | — | Ki | - | — | - | |
| CHEMBL3102952 | — | Ki | < | 2.0 | nM | - |