Assay Detail
Binding
CHEMBL5042808
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Inhibition of DYRK2 (unknown origin) using Ulight-MBP as substrate and ATP as co-substrate incubated for 40 mins and measured after 1 hr by TR-FRET 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 2 (CHEMBL4376) ↗| 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 | 20 | 7.77 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084504 | — | — | 1 | 9.00 |
| CHEMBL4460561 | — | — | 1 | 8.52 |
| CHEMBL5077927 | — | — | 1 | 8.40 |
| CHEMBL5089294 | — | — | 1 | 8.30 |
| CHEMBL5094409 | — | — | 1 | 8.22 |
| CHEMBL5073976 | — | — | 1 | 8.22 |
| CHEMBL5070553 | — | — | 1 | 8.22 |
| CHEMBL5072926 | — | — | 1 | 8.05 |
| CHEMBL5088511 | — | — | 1 | 8.05 |
| CHEMBL5080497 | — | — | 1 | 8.00 |
| CHEMBL5073869 | — | — | 1 | 7.68 |
| CHEMBL5071425 | — | — | 1 | 7.66 |
| CHEMBL5093661 | — | — | 1 | 7.48 |
| CHEMBL5077422 | — | — | 1 | 7.47 |
| CHEMBL4575900 | — | — | 1 | 7.34 |
| CHEMBL5089171 | — | — | 1 | 7.28 |
| CHEMBL5092833 | — | — | 1 | 6.94 |
| CHEMBL5079873 | — | — | 1 | 6.93 |
| CHEMBL5073581 | — | — | 1 | 6.87 |
| CHEMBL5084166 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084504 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4460561 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5077927 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5089294 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5094409 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5073976 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5070553 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5072926 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5088511 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5080497 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5073869 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5071425 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5093661 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5077422 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4575900 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5089171 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5092833 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5079873 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5073581 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL5084166 | — | IC50 | = | 195.0 | nM | 6.71 |