Assay Detail
Binding
CHEMBL2215714
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Inhibition of human VEGFR2 for 5 mins prior to addition of 10 uM ATP using poly-GluTyr by AlphaScreen analysis
9
Total Activities
9
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
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.15 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206666 | — | — | 1 | 8.15 |
| CHEMBL2206663 | — | — | 1 | 7.92 |
| CHEMBL2206668 | — | — | 1 | 7.75 |
| CHEMBL2203321 | — | — | 1 | 7.54 |
| CHEMBL2206662 | — | — | 1 | 7.28 |
| CHEMBL2206665 | — | — | 1 | 7.10 |
| CHEMBL2206667 | — | — | 1 | 6.19 |
| CHEMBL2206661 | — | — | 1 | 5.28 |
| CHEMBL2206664 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206666 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2206663 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2206668 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2203321 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2206662 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2206665 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2206667 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2206661 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2206664 | — | IC50 | > | 10000.0 | nM | - |