Assay Detail
Binding
CHEMBL2394340
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Inhibition of DYRK1A (unknown origin)
24
Total Activities
24
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
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.77 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2392364 | — | — | 1 | 8.40 |
| CHEMBL1877990 | — | — | 1 | 8.15 |
| CHEMBL1868723 | — | — | 1 | 8.00 |
| CHEMBL2392365 | — | — | 1 | 7.96 |
| CHEMBL1904905 | — | — | 1 | 7.75 |
| CHEMBL1885536 | — | — | 1 | 7.60 |
| CHEMBL1898197 | — | — | 1 | 7.58 |
| CHEMBL1902528 | — | — | 1 | 7.21 |
| CHEMBL1899256 | — | — | 1 | 7.10 |
| CHEMBL2392368 | — | — | 1 | 6.97 |
| CHEMBL1892019 | — | — | 1 | 6.89 |
| CHEMBL2392367 | — | — | 1 | 6.77 |
| CHEMBL2392360 | — | — | 1 | 6.69 |
| CHEMBL1899640 | — | — | 1 | 6.56 |
| CHEMBL1885748 | — | — | 1 | 6.55 |
| CHEMBL1884711 | — | — | 1 | 6.46 |
| CHEMBL2392359 | — | — | 1 | 6.25 |
| CHEMBL1872011 | — | — | 1 | 5.84 |
| CHEMBL1898211 | — | — | 1 | 5.63 |
| CHEMBL2392228 | — | — | 1 | 5.46 |
| CHEMBL1882945 | — | — | 1 | 5.34 |
| CHEMBL2392362 | — | — | 1 | 5.33 |
| CHEMBL2392361 | — | — | 1 | 5.20 |
| CHEMBL1331525 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2392364 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1877990 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1868723 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2392365 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1904905 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1885536 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1898197 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1902528 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1899256 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2392368 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL1892019 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL2392367 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL2392360 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL1899640 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL1885748 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL1884711 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL2392359 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL1872011 | — | IC50 | = | 1434.0 | nM | 5.84 |
| CHEMBL1898211 | — | IC50 | = | 2352.0 | nM | 5.63 |
| CHEMBL2392228 | — | IC50 | = | 3454.0 | nM | 5.46 |
| CHEMBL1882945 | — | IC50 | = | 4579.0 | nM | 5.34 |
| CHEMBL2392362 | — | IC50 | = | 4654.0 | nM | 5.33 |
| CHEMBL2392361 | — | IC50 | = | 6361.0 | nM | 5.20 |
| CHEMBL1331525 | — | IC50 | > | 10000.0 | nM | - |