Assay Detail
Binding
CHEMBL2388921
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Inhibition of recombinant DYRK1A (unknown origin) after 120 mins in presence of [33P]-ATP
28
Total Activities
28
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
Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.16 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386744 | — | — | 1 | 9.80 |
| CHEMBL2386747 | — | — | 1 | 9.66 |
| CHEMBL2386745 | — | — | 1 | 9.44 |
| CHEMBL2386748 | — | — | 1 | 9.03 |
| CHEMBL2386764 | — | — | 1 | 9.01 |
| CHEMBL2386746 | — | — | 1 | 9.00 |
| CHEMBL2386762 | — | — | 1 | 8.95 |
| CHEMBL2386753 | — | — | 1 | 8.78 |
| CHEMBL2386763 | — | — | 1 | 8.74 |
| CHEMBL2386770 | — | — | 1 | 8.44 |
| CHEMBL2386766 | — | — | 1 | 8.41 |
| CHEMBL2386749 | — | — | 1 | 8.31 |
| CHEMBL2386760 | — | — | 1 | 8.29 |
| CHEMBL2386765 | — | — | 1 | 8.22 |
| CHEMBL2386754 | — | — | 1 | 8.22 |
| CHEMBL2386752 | — | — | 1 | 8.06 |
| CHEMBL2386743 | — | — | 1 | 8.02 |
| CHEMBL2386761 | — | — | 1 | 7.88 |
| CHEMBL2386751 | — | — | 1 | 7.87 |
| CHEMBL2386769 | — | — | 1 | 7.74 |
| CHEMBL2386759 | — | — | 1 | 7.58 |
| CHEMBL2386755 | — | — | 1 | 7.47 |
| CHEMBL2386768 | — | — | 1 | 7.45 |
| CHEMBL2386767 | — | — | 1 | 7.41 |
| CHEMBL2386750 | — | — | 1 | 7.37 |
| CHEMBL2386757 | — | — | 1 | 6.71 |
| CHEMBL2386756 | — | — | 1 | 6.37 |
| CHEMBL2386758 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386744 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL2386747 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL2386745 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL2386748 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL2386764 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL2386746 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL2386762 | — | IC50 | = | 1.13 | nM | 8.95 |
| CHEMBL2386753 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL2386763 | — | IC50 | = | 1.81 | nM | 8.74 |
| CHEMBL2386770 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2386766 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL2386749 | — | IC50 | = | 4.91 | nM | 8.31 |
| CHEMBL2386760 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2386765 | — | IC50 | = | 6.06 | nM | 8.22 |
| CHEMBL2386754 | — | IC50 | = | 6.02 | nM | 8.22 |
| CHEMBL2386752 | — | IC50 | = | 8.63 | nM | 8.06 |
| CHEMBL2386743 | — | IC50 | = | 9.53 | nM | 8.02 |
| CHEMBL2386761 | — | IC50 | = | 13.08 | nM | 7.88 |
| CHEMBL2386751 | — | IC50 | = | 13.64 | nM | 7.87 |
| CHEMBL2386769 | — | IC50 | = | 18.26 | nM | 7.74 |
| CHEMBL2386759 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL2386755 | — | IC50 | = | 33.93 | nM | 7.47 |
| CHEMBL2386768 | — | IC50 | = | 35.64 | nM | 7.45 |
| CHEMBL2386767 | — | IC50 | = | 39.03 | nM | 7.41 |
| CHEMBL2386750 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL2386757 | — | IC50 | = | 194.4 | nM | 6.71 |
| CHEMBL2386756 | — | IC50 | = | 431.2 | nM | 6.37 |
| CHEMBL2386758 | — | IC50 | = | 436.1 | nM | 6.36 |