Assay Detail
Binding
CHEMBL5034566
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Inhibition of DYRK1A (unknown origin) assessed as accumulation of ADP by ADP hunter plus assay
27
Total Activities
27
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 | 27 | 7.21 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5091510 | — | — | 1 | 8.22 |
| CHEMBL5093650 | — | — | 1 | 8.15 |
| CHEMBL5088687 | — | — | 1 | 8.10 |
| CHEMBL5073598 | — | — | 1 | 8.10 |
| CHEMBL5078833 | — | — | 1 | 8.00 |
| CHEMBL5090159 | — | — | 1 | 7.96 |
| CHEMBL5085656 | — | — | 1 | 7.96 |
| CHEMBL5090676 | — | — | 1 | 7.92 |
| CHEMBL5081888 | — | — | 1 | 7.92 |
| CHEMBL5092157 | — | — | 1 | 7.82 |
| CHEMBL5081341 | — | — | 1 | 7.70 |
| CHEMBL5082044 | — | — | 1 | 7.60 |
| CHEMBL5083159 | — | — | 1 | 7.57 |
| CHEMBL5092245 | — | — | 1 | 7.40 |
| CHEMBL5092828 | — | — | 1 | 7.37 |
| CHEMBL5083242 | — | — | 1 | 7.30 |
| CHEMBL5076145 | — | — | 1 | 7.29 |
| CHEMBL5091344 | — | — | 1 | 7.19 |
| CHEMBL5072383 | — | — | 1 | 7.17 |
| CHEMBL5091537 | — | — | 1 | 6.92 |
| CHEMBL5090400 | — | — | 1 | 6.62 |
| CHEMBL5076663 | — | — | 1 | 6.60 |
| CHEMBL5086979 | — | — | 1 | 6.42 |
| CHEMBL5085619 | — | — | 1 | 5.75 |
| CHEMBL5077073 | — | — | 1 | 5.52 |
| CHEMBL5088612 | — | — | 1 | 5.32 |
| CHEMBL5081135 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5091510 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5093650 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5088687 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5073598 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5078833 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5090159 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5085656 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5090676 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5081888 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5092157 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5081341 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5082044 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5083159 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5092245 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5092828 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5083242 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5076145 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5091344 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5072383 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5091537 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5090400 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5076663 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5086979 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5085619 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5077073 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5088612 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5081135 | — | IC50 | = | 12800.0 | nM | 4.89 |