Assay Detail
Binding
CHEMBL3404062
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.66 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3403514 | — | — | 1 | 8.24 |
| CHEMBL3403513 | — | — | 1 | 8.17 |
| CHEMBL3403510 | — | — | 1 | 7.73 |
| CHEMBL3297898 | — | — | 1 | 7.72 |
| CHEMBL3403512 | — | — | 1 | 7.70 |
| CHEMBL3403515 | — | — | 1 | 7.68 |
| CHEMBL3403509 | — | — | 1 | 7.49 |
| CHEMBL3403517 | — | — | 1 | 7.48 |
| CHEMBL3403518 | — | — | 1 | 7.42 |
| CHEMBL3403519 | — | — | 1 | 6.92 |
| CHEMBL3403511 | — | — | 1 | - |
| CHEMBL3403516 | — | — | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3403514 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3403513 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3403510 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL3297898 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL3403512 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL3403515 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL3403509 | — | IC50 | = | 32.3 | nM | 7.49 |
| CHEMBL3403517 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL3403518 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL3403519 | — | IC50 | = | 121.3 | nM | 6.92 |
| CHEMBL3403511 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL3403516 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124.7 | nM | - |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12.9 | nM | - |
| CHEMBL535 | SUNITINIB | IC50 | = | 18.9 | nM | - |