Assay Detail
Binding
CHEMBL5042809
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type full length DYRK1A (unknown origin) in human U2OS cells assessed as reduction in pSER520 autophosphorylation incubated for 5 hrs by western blot analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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
Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.88 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5093661 | — | — | 1 | 7.58 |
| CHEMBL5070553 | — | — | 1 | 7.55 |
| CHEMBL5089171 | — | — | 1 | 7.50 |
| CHEMBL5077927 | — | — | 1 | 7.47 |
| CHEMBL5088511 | — | — | 1 | 7.46 |
| CHEMBL5084166 | — | — | 1 | 7.36 |
| CHEMBL5080497 | — | — | 1 | 7.33 |
| CHEMBL5071425 | — | — | 1 | 7.14 |
| CHEMBL5084504 | — | — | 1 | 7.10 |
| CHEMBL4460561 | — | — | 1 | 7.05 |
| CHEMBL5077422 | — | — | 1 | 7.05 |
| CHEMBL5082456 | — | — | 1 | 7.00 |
| CHEMBL4575900 | — | — | 1 | 6.96 |
| CHEMBL5072926 | — | — | 1 | 6.96 |
| CHEMBL5091644 | — | — | 1 | 6.89 |
| CHEMBL5092833 | — | — | 1 | 6.88 |
| CHEMBL5092736 | — | — | 1 | 6.82 |
| CHEMBL5073976 | — | — | 1 | 6.65 |
| CHEMBL5094409 | — | — | 1 | 6.64 |
| CHEMBL5088553 | — | — | 1 | 6.60 |
| CHEMBL5089294 | — | — | 1 | 6.55 |
| CHEMBL5092362 | — | — | 1 | 6.30 |
| CHEMBL5073869 | — | — | 1 | 5.78 |
| CHEMBL5094822 | — | — | 1 | 5.75 |
| CHEMBL5073581 | — | — | 1 | 5.52 |
| CHEMBL5079873 | — | — | 1 | - |
| CHEMBL5090552 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5093661 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5070553 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5089171 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5077927 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5088511 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5084166 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5080497 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5071425 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5084504 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4460561 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5077422 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5082456 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4575900 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5072926 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5091644 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5092833 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5092736 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL5073976 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL5094409 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL5088553 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5089294 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5092362 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5073869 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL5094822 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5073581 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5079873 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL5090552 | — | IC50 | - | — | - |