Assay Detail
Binding
CHEMBL4622607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal Hex-tagged DYRK1A (127 to 485 residues) expressed in Escherichia coli BL21 (DE3) incubated for 1.5 hrs by TR-FRET assay
10
Total Activities
10
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
Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.37 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495696 | GW778894X | — | 1 | 8.30 |
| CHEMBL4646866 | — | — | 1 | 8.15 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | — | 1 | 7.92 |
| CHEMBL359554 | — | — | 1 | 7.42 |
| CHEMBL366259 | — | — | 1 | 7.19 |
| CHEMBL4637319 | — | — | 1 | 7.12 |
| CHEMBL4636572 | — | — | 1 | 7.01 |
| CHEMBL359794 | — | — | 1 | 6.99 |
| CHEMBL4643515 | — | — | 1 | 6.86 |
| CHEMBL360866 | — | — | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495696 | GW778894X | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4646866 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL359554 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL366259 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4637319 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4636572 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL359794 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4643515 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL360866 | — | IC50 | = | 186.0 | nM | 6.73 |