Assay Detail
Binding
CHEMBL3778243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged DYRK1A catalytic domain expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP
20
Total Activities
20
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
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.42 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774448 | — | — | 1 | 7.70 |
| CHEMBL568150 | — | — | 1 | 7.52 |
| CHEMBL3775393 | — | — | 1 | 7.40 |
| CHEMBL3774830 | — | — | 1 | 7.00 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 6.89 |
| CHEMBL3774704 | — | — | 1 | 6.89 |
| CHEMBL3775111 | — | — | 1 | 6.77 |
| CHEMBL3775949 | — | — | 1 | 6.60 |
| CHEMBL3193172 | — | — | 1 | 6.22 |
| CHEMBL3775754 | — | — | 1 | 6.16 |
| CHEMBL3774696 | — | — | 1 | 6.06 |
| CHEMBL3775193 | — | — | 1 | 6.03 |
| CHEMBL3775821 | — | — | 1 | 6.02 |
| CHEMBL3775538 | — | — | 1 | 5.97 |
| CHEMBL3774736 | — | — | 1 | 5.96 |
| CHEMBL3775969 | — | — | 1 | 5.92 |
| CHEMBL3774667 | — | — | 1 | 5.89 |
| CHEMBL1612487 | — | — | 1 | 5.74 |
| CHEMBL38043 | — | — | 1 | 5.19 |
| CHEMBL571292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774448 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL568150 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3775393 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3774830 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL269538 | HARMINE | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3774704 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3775111 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3775949 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3193172 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3775754 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3774696 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3775193 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3775821 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3775538 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3774736 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3775969 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3774667 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1612487 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL38043 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL571292 | — | IC50 | > | 10000.0 | nM | - |