Assay Detail
Binding
CHEMBL5250948
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of hexa His-tagged DYRK2 (72 to 479 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as substrate phosphorylation using 4E-BP1 as substrate in presence of [gamma33-P]ATP incubated for 2 hrs by scintillation counter analysis
30
Total Activities
30
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 2 (CHEMBL4376) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Potent DYRK2 Inhibitors with High Selectivity, Great Solubility, and Excellent Safety Properties for the Treatment of Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.91 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5289179 | — | — | 1 | 9.22 |
| CHEMBL5286478 | — | — | 1 | 8.40 |
| CHEMBL5272300 | — | — | 1 | 7.82 |
| CHEMBL5278493 | — | — | 1 | 7.80 |
| CHEMBL5277818 | — | — | 1 | 7.66 |
| CHEMBL5271186 | — | — | 1 | 7.55 |
| CHEMBL5289131 | — | — | 1 | 7.54 |
| CHEMBL5277043 | — | — | 1 | 7.48 |
| CHEMBL5280825 | — | — | 1 | 7.25 |
| CHEMBL5286238 | — | — | 1 | 7.17 |
| CHEMBL5272422 | — | — | 1 | 7.16 |
| CHEMBL5273713 | — | — | 1 | 7.00 |
| CHEMBL5280350 | — | — | 1 | 6.72 |
| CHEMBL5279010 | — | — | 1 | 6.67 |
| CHEMBL5270999 | — | — | 1 | 6.57 |
| CHEMBL5278425 | — | — | 1 | 6.45 |
| CHEMBL5281152 | — | — | 1 | 6.37 |
| CHEMBL5279534 | — | — | 1 | 6.30 |
| CHEMBL5272665 | — | — | 1 | 6.27 |
| CHEMBL5274593 | — | — | 1 | 6.20 |
| CHEMBL5286408 | — | — | 1 | 6.16 |
| CHEMBL5289173 | — | — | 1 | 6.11 |
| CHEMBL5274485 | — | — | 1 | 6.11 |
| CHEMBL5287497 | — | — | 1 | 5.98 |
| CHEMBL5277535 | — | — | 1 | 5.85 |
| CHEMBL5276852 | — | — | 1 | 5.83 |
| CHEMBL5274190 | — | — | 1 | - |
| CHEMBL5286388 | — | — | 1 | - |
| CHEMBL5288208 | — | — | 1 | - |
| CHEMBL5288741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5289179 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5286478 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5272300 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5278493 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5277818 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5271186 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5289131 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5277043 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5280825 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5286238 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5272422 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5273713 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5280350 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5279010 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5270999 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL5278425 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL5281152 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5279534 | — | IC50 | = | 498.0 | nM | 6.30 |
| CHEMBL5272665 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL5274593 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL5286408 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL5289173 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL5274485 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL5287497 | — | IC50 | = | 1053.0 | nM | 5.98 |
| CHEMBL5277535 | — | IC50 | = | 1415.0 | nM | 5.85 |
| CHEMBL5276852 | — | IC50 | = | 1474.0 | nM | 5.83 |
| CHEMBL5274190 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5286388 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5288208 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5288741 | — | IC50 | > | 10000.0 | nM | - |