Assay Detail
Binding
CHEMBL5034569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DYRK1A (unknown origin) by TR FRET assay
14
Total Activities
14
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
Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.01 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5078833 | — | — | 1 | 8.52 |
| CHEMBL5093650 | — | — | 1 | 8.40 |
| CHEMBL5088687 | — | — | 1 | 8.30 |
| CHEMBL5092157 | — | — | 1 | 8.22 |
| CHEMBL5082044 | — | — | 1 | 8.15 |
| CHEMBL5083159 | — | — | 1 | 8.15 |
| CHEMBL5091510 | — | — | 1 | 8.05 |
| CHEMBL5073598 | — | — | 1 | 8.00 |
| CHEMBL5090159 | — | — | 1 | 7.82 |
| CHEMBL5090676 | — | — | 1 | 7.82 |
| CHEMBL5081888 | — | — | 1 | 7.77 |
| CHEMBL5081341 | — | — | 1 | 7.75 |
| CHEMBL5092828 | — | — | 1 | 7.60 |
| CHEMBL5092245 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5078833 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5093650 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5088687 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5092157 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5082044 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5083159 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5091510 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5073598 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5090159 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5090676 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5081888 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5081341 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5092828 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5092245 | — | IC50 | = | 30.0 | nM | 7.52 |