Assay Detail
Binding
CHEMBL4673836
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Inhibition of DYRK1A (unknown origin) by [33P]-ATP filter binding kinase assay
20
Total Activities
20
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
Probing the ATP-Binding Pocket of Protein Kinase DYRK1A with Benzothiazole Fragment Molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.28 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1532203 | — | — | 1 | 6.40 |
| CHEMBL1213041 | — | — | 1 | 6.16 |
| CHEMBL4747967 | — | — | 1 | 6.10 |
| CHEMBL4780479 | — | — | 1 | 5.96 |
| CHEMBL4794978 | — | — | 1 | 5.96 |
| CHEMBL4759909 | — | — | 1 | 5.89 |
| CHEMBL1538954 | — | — | 1 | 5.64 |
| CHEMBL4556783 | — | — | 1 | 5.54 |
| CHEMBL4746739 | — | — | 1 | 5.50 |
| CHEMBL4754469 | — | — | 1 | 5.41 |
| CHEMBL4784222 | — | — | 1 | 5.14 |
| CHEMBL4759082 | — | — | 1 | 4.98 |
| CHEMBL1486796 | — | — | 1 | 4.91 |
| CHEMBL4741377 | — | — | 1 | 4.80 |
| CHEMBL2029515 | — | — | 1 | 4.63 |
| CHEMBL4750244 | — | — | 1 | 4.58 |
| CHEMBL4743605 | — | — | 1 | 4.55 |
| CHEMBL4763711 | — | — | 1 | 4.53 |
| CHEMBL4798633 | — | — | 1 | 4.46 |
| CHEMBL2206133 | — | — | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1532203 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1213041 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4747967 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4780479 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4794978 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4759909 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1538954 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4556783 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4746739 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4754469 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4784222 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4759082 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL1486796 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL4741377 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL2029515 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4750244 | — | IC50 | = | 26500.0 | nM | 4.58 |
| CHEMBL4743605 | — | IC50 | = | 28100.0 | nM | 4.55 |
| CHEMBL4763711 | — | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL4798633 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2206133 | — | IC50 | = | 36000.0 | nM | 4.44 |