Assay Detail
Binding
CHEMBL892958
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Inhibition of human VEGFR2 in presence of 1 uM 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 | 6.71 | 7.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.56 |
| CHEMBL396472 | — | — | 1 | 7.34 |
| CHEMBL242349 | — | — | 1 | 7.30 |
| CHEMBL242555 | — | — | 1 | 7.27 |
| CHEMBL243839 | — | — | 1 | 7.12 |
| CHEMBL243837 | — | — | 1 | 7.10 |
| CHEMBL243629 | — | — | 1 | 6.99 |
| CHEMBL243410 | — | — | 1 | 6.96 |
| CHEMBL428741 | — | — | 1 | 6.95 |
| CHEMBL243628 | — | — | 1 | 6.95 |
| CHEMBL398154 | — | — | 1 | 6.87 |
| CHEMBL241919 | — | — | 1 | 6.72 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.70 |
| CHEMBL241918 | — | — | 1 | 6.43 |
| CHEMBL428039 | — | — | 1 | 6.42 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.07 |
| CHEMBL29197 | — | — | 1 | 5.83 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 5.50 |
| CHEMBL242131 | — | — | 1 | 5.36 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | IC50 | = | 27.3 | nM | 7.56 |
| CHEMBL396472 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL242349 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL242555 | — | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL243839 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL243837 | — | IC50 | = | 80.2 | nM | 7.10 |
| CHEMBL243629 | — | IC50 | = | 102.3 | nM | 6.99 |
| CHEMBL243410 | — | IC50 | = | 109.3 | nM | 6.96 |
| CHEMBL428741 | — | IC50 | = | 113.4 | nM | 6.95 |
| CHEMBL243628 | — | IC50 | = | 111.6 | nM | 6.95 |
| CHEMBL398154 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL241919 | — | IC50 | = | 188.7 | nM | 6.72 |
| CHEMBL101253 | VATALANIB | IC50 | = | 198.3 | nM | 6.70 |
| CHEMBL241918 | — | IC50 | = | 371.5 | nM | 6.43 |
| CHEMBL428039 | — | IC50 | = | 378.7 | nM | 6.42 |
| CHEMBL180022 | NERATINIB | IC50 | = | 858.2 | nM | 6.07 |
| CHEMBL29197 | — | IC50 | = | 1489.0 | nM | 5.83 |
| CHEMBL607707 | PELITINIB | IC50 | = | 3131.0 | nM | 5.50 |
| CHEMBL242131 | — | IC50 | = | 4389.0 | nM | 5.36 |
| CHEMBL939 | GEFITINIB | IC50 | > | 10000.0 | nM | - |