Assay Detail
Binding
CHEMBL4151857
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Inhibition of DYRK1A (unknown origin) using DYRKtide as substrate by ATP regenerative NADH consuming assay
18
Total Activities
9
Compounds Tested
2
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
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.04 | 6.67 |
| Ki | 9 | 6.36 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4164814 | — | — | 2 | 6.98 |
| CHEMBL2152265 | — | — | 2 | 6.80 |
| CHEMBL1765714 | — | — | 2 | 6.60 |
| CHEMBL4171089 | — | — | 2 | 6.42 |
| CHEMBL4168671 | — | — | 2 | 6.24 |
| CHEMBL4171209 | — | — | 2 | 5.78 |
| CHEMBL3986079 | — | — | 2 | 5.70 |
| CHEMBL4172746 | — | — | 2 | - |
| CHEMBL4167484 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4164814 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL2152265 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL4164814 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL1765714 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL2152265 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL4171089 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL1765714 | — | IC50 | = | 532.0 | nM | 6.27 |
| CHEMBL4168671 | — | Ki | = | 575.0 | nM | 6.24 |
| CHEMBL4171089 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4168671 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4171209 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL3986079 | — | Ki | = | 2015.0 | nM | 5.70 |
| CHEMBL4171209 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3986079 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4172746 | — | Ki | - | — | - | |
| CHEMBL4172746 | — | IC50 | - | — | - | |
| CHEMBL4167484 | — | Ki | > | 2800.0 | nM | - |
| CHEMBL4167484 | — | IC50 | > | 6000.0 | nM | - |