Assay Detail
Binding
CHEMBL3776531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tetracycline-inducible EGFP-DYRK1A (unknown origin) expressed in HEK293 cells coexpressing full length human EGFP-tau protein assessed as reduction in tau-Thr212 phosphorylation incubated overnight by immunofluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 6 | 6.02 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774704 | — | — | 1 | 6.70 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 6.40 |
| CHEMBL3774448 | — | — | 1 | 5.85 |
| CHEMBL568150 | — | — | 1 | 5.80 |
| CHEMBL3775111 | — | — | 1 | 5.68 |
| CHEMBL3775393 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774704 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL269538 | HARMINE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3774448 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL568150 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3775111 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3775393 | — | IC50 | = | 2100.0 | nM | 5.68 |