Assay Detail
Binding
CHEMBL5516698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length VRK2 (unknown origin) assessed as inhibition constant using human histone H3 peptide as substrate preincubated for 30 mins followed by substrate and ATP addition incubated for 60 mins by Cheng-Prusoff equation based TR-FRET assay
2
Total Activities
2
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
Serine/threonine-protein kinase VRK2 (CHEMBL1649059) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.65 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3604889 | — | — | 1 | 7.75 |
| CHEMBL573107 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3604889 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL573107 | — | Ki | = | 28.0 | nM | 7.55 |