Assay Detail
Binding
CHEMBL5034563
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Binding affinity to DYRK1A (unknown origin) assessed as inhibition constant by ADP hunter plus assay
21
Total Activities
21
Compounds Tested
2
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 |
|---|---|---|---|
| Ki | 20 | 6.36 | 8.00 |
| IC50 | 1 | 7.47 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081341 | — | — | 1 | 8.00 |
| CHEMBL5083242 | — | — | 1 | 7.70 |
| CHEMBL5092245 | — | — | 1 | 7.70 |
| CHEMBL5091344 | — | — | 1 | 7.50 |
| CHEMBL5072383 | — | — | 1 | 7.47 |
| CHEMBL5091537 | — | — | 1 | 7.23 |
| CHEMBL2023701 | — | — | 1 | 7.00 |
| CHEMBL5090400 | — | — | 1 | 6.92 |
| CHEMBL5076663 | — | — | 1 | 6.92 |
| CHEMBL5086979 | — | — | 1 | 6.72 |
| CHEMBL5085619 | — | — | 1 | 6.05 |
| CHEMBL5077073 | — | — | 1 | 5.82 |
| CHEMBL5089793 | — | — | 1 | 5.82 |
| CHEMBL41044 | — | — | 1 | 5.82 |
| CHEMBL2432026 | — | — | 1 | 5.64 |
| CHEMBL5088612 | — | — | 1 | 5.62 |
| CHEMBL89697 | — | — | 1 | 5.36 |
| CHEMBL3751985 | — | — | 1 | 5.21 |
| CHEMBL5081135 | — | — | 1 | 5.19 |
| CHEMBL5075490 | — | — | 1 | 4.60 |
| CHEMBL5071361 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081341 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5083242 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5092245 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5091344 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5072383 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5091537 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2023701 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5090400 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL5076663 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL5086979 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL5085619 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL5077073 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5089793 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL41044 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2432026 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL5088612 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL89697 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL3751985 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL5081135 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL5075490 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL5071361 | — | Ki | > | 200000.0 | nM | - |