Assay Detail
Binding
CHEMBL4344348
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DYRK1A (unknown origin) by FRET-based Lantha-screen Eu kinase binding assay
21
Total Activities
21
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
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.10 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4550946 | — | — | 1 | 7.89 |
| CHEMBL4575812 | — | — | 1 | 7.86 |
| CHEMBL4442374 | — | — | 1 | 7.72 |
| CHEMBL4474836 | — | — | 1 | 7.60 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.57 |
| CHEMBL4456985 | — | — | 1 | 7.57 |
| CHEMBL4440790 | — | — | 1 | 7.41 |
| CHEMBL4514653 | — | — | 1 | 7.25 |
| CHEMBL4521356 | — | — | 1 | 7.19 |
| CHEMBL4579529 | — | — | 1 | 7.13 |
| CHEMBL4563765 | — | — | 1 | 7.08 |
| CHEMBL4437998 | — | — | 1 | 7.01 |
| CHEMBL4552025 | — | — | 1 | 7.01 |
| CHEMBL4513287 | — | — | 1 | 6.95 |
| CHEMBL4564623 | — | — | 1 | 6.86 |
| CHEMBL2012558 | — | — | 1 | 6.82 |
| CHEMBL4483653 | — | — | 1 | 6.78 |
| CHEMBL4476003 | — | — | 1 | 6.78 |
| CHEMBL4438785 | — | — | 1 | 6.67 |
| CHEMBL4539999 | — | — | 1 | 6.02 |
| CHEMBL4528315 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4550946 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4575812 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4442374 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4474836 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL269538 | HARMINE | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4456985 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4440790 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4514653 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4521356 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4579529 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4563765 | — | IC50 | = | 83.5 | nM | 7.08 |
| CHEMBL4437998 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4552025 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4513287 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4564623 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL2012558 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4483653 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4476003 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4438785 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4539999 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4528315 | — | IC50 | = | 1020.0 | nM | 5.99 |