Assay Detail
Binding
CHEMBL2353609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 (unknown origin) using biotinylated poly(Glu:Tyr) as substrate after 60 mins by AlphaScreen assay in presence of 1000 uM of ATP
4
Total Activities
4
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
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.01 | 10.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | 10.03 |
| CHEMBL2348996 | — | — | 1 | 9.72 |
| CHEMBL2348989 | — | — | 1 | 8.96 |
| CHEMBL2206666 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180604 | TAK-593 | IC50 | = | 0.093 | nM | 10.03 |
| CHEMBL2348996 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL2348989 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2206666 | — | IC50 | = | 49.0 | nM | 7.31 |