Assay Detail
Binding
CHEMBL3591177
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Inhibition of human recombinant DYRK1A expressed in Escherichia coli using RS peptide as substrate
25
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
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.94 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589662 | — | — | 1 | 8.22 |
| CHEMBL3589666 | — | — | 1 | 7.75 |
| CHEMBL3589661 | — | — | 1 | 7.70 |
| CHEMBL3589667 | — | — | 1 | 7.66 |
| CHEMBL3589665 | — | — | 1 | 7.64 |
| CHEMBL3589660 | — | — | 1 | 7.51 |
| CHEMBL3589663 | — | — | 1 | 7.50 |
| CHEMBL3589673 | — | — | 1 | 7.41 |
| CHEMBL3589674 | — | — | 1 | 7.39 |
| CHEMBL3589675 | — | — | 1 | 7.25 |
| CHEMBL3589672 | — | — | 1 | 6.92 |
| CHEMBL3589775 | — | — | 1 | 6.89 |
| CHEMBL3589774 | — | — | 1 | 6.77 |
| CHEMBL3589671 | — | — | 1 | 6.75 |
| CHEMBL3589664 | — | — | 1 | 6.50 |
| CHEMBL3589669 | — | — | 1 | 5.70 |
| CHEMBL3589668 | — | — | 1 | 5.64 |
| CHEMBL3589653 | — | — | 1 | 5.58 |
| CHEMBL3589670 | — | — | 1 | 5.00 |
| CHEMBL3589659 | — | — | 1 | - |
| CHEMBL3589658 | — | — | 1 | - |
| CHEMBL3589657 | — | — | 1 | - |
| CHEMBL3589656 | — | — | 1 | - |
| CHEMBL3589655 | — | — | 1 | - |
| CHEMBL3589654 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589662 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3589666 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3589661 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3589667 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3589665 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3589660 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3589663 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3589673 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3589674 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3589675 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3589672 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3589775 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3589774 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3589671 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3589664 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3589669 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3589668 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3589653 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3589670 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3589659 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3589658 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3589657 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3589656 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3589655 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3589654 | — | IC50 | > | 10000.0 | nM | - |