Assay Detail
Binding
CHEMBL892960
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Inhibition of human VEGFR2 in presence of 1 mM ATP
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 | Intermediate |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.22 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242555 | — | — | 1 | 6.85 |
| CHEMBL243837 | — | — | 1 | 6.75 |
| CHEMBL396472 | — | — | 1 | 6.73 |
| CHEMBL242349 | — | — | 1 | 6.60 |
| CHEMBL243839 | — | — | 1 | 6.53 |
| CHEMBL243410 | — | — | 1 | 6.52 |
| CHEMBL428741 | — | — | 1 | 6.46 |
| CHEMBL243628 | — | — | 1 | 6.26 |
| CHEMBL241919 | — | — | 1 | 6.21 |
| CHEMBL243629 | — | — | 1 | 6.11 |
| CHEMBL398154 | — | — | 1 | 6.00 |
| CHEMBL241918 | — | — | 1 | 5.89 |
| CHEMBL428039 | — | — | 1 | 5.86 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.32 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 5.17 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | - |
| CHEMBL242131 | — | — | 1 | - |
| CHEMBL29197 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242555 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL243837 | — | IC50 | = | 178.8 | nM | 6.75 |
| CHEMBL396472 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL242349 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL243839 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL243410 | — | IC50 | = | 303.3 | nM | 6.52 |
| CHEMBL428741 | — | IC50 | = | 347.6 | nM | 6.46 |
| CHEMBL243628 | — | IC50 | = | 550.2 | nM | 6.26 |
| CHEMBL241919 | — | IC50 | = | 612.7 | nM | 6.21 |
| CHEMBL243629 | — | IC50 | = | 783.1 | nM | 6.11 |
| CHEMBL398154 | — | IC50 | = | 1009.0 | nM | 6.00 |
| CHEMBL241918 | — | IC50 | = | 1285.0 | nM | 5.89 |
| CHEMBL428039 | — | IC50 | = | 1397.0 | nM | 5.86 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 4834.0 | nM | 5.32 |
| CHEMBL101253 | VATALANIB | IC50 | = | 6754.0 | nM | 5.17 |
| CHEMBL607707 | PELITINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL242131 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL29197 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | IC50 | > | 10000.0 | nM | - |