Assay Detail
Binding
CHEMBL5254664
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Inhibition of DYRK1A (unknown origin)
26
Total Activities
25
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
DYRK1A kinase inhibition with emphasis on neurodegeneration: A comprehensive evolution story-cum-perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.82 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386747 | — | — | 2 | 9.66 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.27 |
| CHEMBL4283751 | — | — | 1 | 8.10 |
| CHEMBL3421968 | — | — | 1 | 7.77 |
| CHEMBL370100 | REBECCAMYCIN | — | 1 | 7.72 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.48 |
| CHEMBL1802358 | — | — | 1 | 7.40 |
| CHEMBL5288413 | — | — | 1 | 7.30 |
| CHEMBL270636 | — | — | 1 | 7.22 |
| CHEMBL513265 | — | — | 1 | 7.10 |
| CHEMBL4288096 | — | — | 1 | 6.96 |
| CHEMBL5272802 | — | — | 1 | 6.96 |
| CHEMBL5275785 | — | — | 1 | 6.74 |
| CHEMBL5275342 | — | — | 1 | 6.64 |
| CHEMBL1232500 | — | — | 1 | 6.62 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | 3.0 | 1 | 6.48 |
| CHEMBL5267794 | — | — | 1 | 5.62 |
| CHEMBL5290599 | — | — | 1 | 5.60 |
| CHEMBL5281344 | — | — | 1 | 5.55 |
| CHEMBL5288877 | — | — | 1 | 5.40 |
| CHEMBL36654 | ROEMERINE | — | 1 | 4.82 |
| CHEMBL5277847 | — | — | 1 | 4.72 |
| CHEMBL2386744 | — | — | 1 | - |
| CHEMBL5285333 | — | — | 1 | - |
| CHEMBL5290314 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386747 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4283751 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3421968 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL370100 | REBECCAMYCIN | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL269538 | HARMINE | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1802358 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5288413 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL270636 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL513265 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5272802 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4288096 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5275785 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL5275342 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1232500 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2386747 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5267794 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5290599 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5281344 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL5288877 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL36654 | ROEMERINE | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5277847 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5290314 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5285333 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2386744 | — | IC50 | = | 160.0 | nM | - |