Assay Detail
Binding
CHEMBL4155090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant rat DYRK1A kinase domain (1 to 499 residues) expressed in bacterial expression system using KKISGRLSPIMTEQ as substrate after 30 mins by ADP-Glo reagent based luminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.37 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4163110 | — | — | 1 | 7.01 |
| CHEMBL4177432 | — | — | 1 | 6.57 |
| CHEMBL4166554 | — | — | 1 | 6.13 |
| CHEMBL4174068 | — | — | 1 | 5.78 |
| CHEMBL4170635 | — | — | 1 | - |
| CHEMBL1642 | IMATINIB MESYLATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4163110 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4177432 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4166554 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4174068 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL4170635 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1642 | IMATINIB MESYLATE | IC50 | - | — | - |