Assay Detail
Binding
CHEMBL5148183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DYRK1B incubated for 130 mins in presence of ATP by ADP-Glo kinase assay
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 1B (CHEMBL5543) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel benzothiophene derivatives as potent and narrow spectrum inhibitors of DYRK1A and DYRK1B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.28 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3421968 | — | — | 1 | 7.95 |
| CHEMBL5203374 | — | — | 1 | 7.18 |
| CHEMBL5199700 | — | — | 1 | 6.73 |
| CHEMBL5186861 | — | — | 1 | 6.62 |
| CHEMBL5177156 | — | — | 1 | 6.56 |
| CHEMBL5180428 | — | — | 1 | 6.43 |
| CHEMBL5189902 | — | — | 1 | 6.35 |
| CHEMBL5176835 | — | — | 1 | 6.24 |
| CHEMBL5074567 | — | — | 1 | 6.19 |
| CHEMBL5191496 | — | — | 1 | 6.18 |
| CHEMBL5203368 | — | — | 1 | 6.17 |
| CHEMBL5173386 | — | — | 1 | 6.14 |
| CHEMBL5173510 | — | — | 1 | 6.09 |
| CHEMBL5202356 | — | — | 1 | 6.01 |
| CHEMBL5170875 | — | — | 1 | 5.96 |
| CHEMBL5172326 | — | — | 1 | 5.95 |
| CHEMBL5173413 | — | — | 1 | 5.93 |
| CHEMBL5190686 | — | — | 1 | 5.84 |
| CHEMBL5174426 | — | — | 1 | 5.64 |
| CHEMBL5208317 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3421968 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL5203374 | — | Ki | = | 65.3 | nM | 7.18 |
| CHEMBL5199700 | — | Ki | = | 186.6 | nM | 6.73 |
| CHEMBL5186861 | — | Ki | = | 237.9 | nM | 6.62 |
| CHEMBL5177156 | — | Ki | = | 277.9 | nM | 6.56 |
| CHEMBL5180428 | — | Ki | = | 369.8 | nM | 6.43 |
| CHEMBL5189902 | — | Ki | = | 447.5 | nM | 6.35 |
| CHEMBL5176835 | — | Ki | = | 576.9 | nM | 6.24 |
| CHEMBL5074567 | — | Ki | = | 642.3 | nM | 6.19 |
| CHEMBL5191496 | — | Ki | = | 659.7 | nM | 6.18 |
| CHEMBL5203368 | — | Ki | = | 669.7 | nM | 6.17 |
| CHEMBL5173386 | — | Ki | = | 729.9 | nM | 6.14 |
| CHEMBL5173510 | — | Ki | = | 813.6 | nM | 6.09 |
| CHEMBL5202356 | — | Ki | = | 980.2 | nM | 6.01 |
| CHEMBL5170875 | — | Ki | = | 1104.5 | nM | 5.96 |
| CHEMBL5172326 | — | Ki | = | 1126.8 | nM | 5.95 |
| CHEMBL5173413 | — | Ki | = | 1183.0 | nM | 5.93 |
| CHEMBL5190686 | — | Ki | = | 1453.3 | nM | 5.84 |
| CHEMBL5174426 | — | Ki | = | 2312.5 | nM | 5.64 |
| CHEMBL5208317 | — | Ki | = | 4398.7 | nM | 5.36 |