Assay Detail
Binding
CHEMBL954298
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Inhibition of Dyrk1 autophosphorylation
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.26 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511636 | — | — | 1 | 6.22 |
| CHEMBL498718 | — | — | 1 | 6.22 |
| CHEMBL485533 | — | — | 1 | 5.92 |
| CHEMBL511962 | — | — | 1 | 5.60 |
| CHEMBL380093 | — | — | 1 | 5.60 |
| CHEMBL472491 | — | — | 1 | 5.60 |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | 5.30 |
| CHEMBL470631 | — | — | 1 | 5.30 |
| CHEMBL512149 | — | — | 1 | 4.82 |
| CHEMBL469346 | — | — | 1 | 4.70 |
| CHEMBL512658 | — | — | 1 | 4.70 |
| CHEMBL469776 | — | — | 1 | 4.70 |
| CHEMBL469770 | — | — | 1 | 4.52 |
| CHEMBL470851 | — | — | 1 | 4.40 |
| CHEMBL470632 | — | — | 1 | - |
| CHEMBL472499 | — | — | 1 | - |
| CHEMBL498719 | — | — | 1 | - |
| CHEMBL513188 | — | — | 1 | - |
| CHEMBL496666 | — | — | 1 | - |
| CHEMBL523580 | — | — | 1 | - |
| CHEMBL496675 | — | — | 1 | - |
| CHEMBL484166 | — | — | 1 | - |
| CHEMBL484334 | — | — | 1 | - |
| CHEMBL485532 | — | — | 1 | - |
| CHEMBL511841 | — | — | 1 | - |
| CHEMBL519700 | — | — | 1 | - |
| CHEMBL470817 | — | — | 1 | - |
| CHEMBL469777 | — | — | 1 | - |
| CHEMBL469775 | — | — | 1 | - |
| CHEMBL496665 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511636 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL498718 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL485533 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL511962 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL380093 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL472491 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL14762 | SELICICLIB | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL470631 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL512149 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL469776 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL512658 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL469346 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL469770 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL470851 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL469347 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL469348 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL469570 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL470411 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL509892 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL513717 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL470632 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL472499 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL498719 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL513188 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL496666 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL523580 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL496675 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL484166 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL484334 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL485532 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL511841 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL519700 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL470817 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL469777 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL469775 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL496665 | — | IC50 | > | 50000.0 | nM | - |