Assay Detail
Binding
CHEMBL3299341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay
18
Total Activities
18
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 and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.47 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3297900 | — | — | 1 | 8.07 |
| CHEMBL3297899 | — | — | 1 | 7.97 |
| CHEMBL3297999 | — | — | 1 | 7.81 |
| CHEMBL3297898 | — | — | 1 | 7.72 |
| CHEMBL3298000 | — | — | 1 | 7.70 |
| CHEMBL3297891 | — | — | 1 | 7.49 |
| CHEMBL3297998 | — | — | 1 | 7.46 |
| CHEMBL3297897 | — | — | 1 | 7.37 |
| CHEMBL3297816 | — | — | 1 | 7.30 |
| CHEMBL3297894 | — | — | 1 | 7.24 |
| CHEMBL3297893 | — | — | 1 | 7.18 |
| CHEMBL3297895 | — | — | 1 | 7.15 |
| CHEMBL3297892 | — | — | 1 | 7.12 |
| CHEMBL3297896 | — | — | 1 | 6.99 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL53463 | DOXORUBICIN | 4.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3297900 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3297899 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL3297999 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL3297898 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL3298000 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL3297891 | — | IC50 | = | 32.2 | nM | 7.49 |
| CHEMBL3297998 | — | IC50 | = | 34.4 | nM | 7.46 |
| CHEMBL3297897 | — | IC50 | = | 43.1 | nM | 7.37 |
| CHEMBL3297816 | — | IC50 | = | 50.3 | nM | 7.30 |
| CHEMBL3297894 | — | IC50 | = | 58.2 | nM | 7.24 |
| CHEMBL3297893 | — | IC50 | = | 66.2 | nM | 7.18 |
| CHEMBL3297895 | — | IC50 | = | 70.2 | nM | 7.15 |
| CHEMBL3297892 | — | IC50 | = | 76.3 | nM | 7.12 |
| CHEMBL3297896 | — | IC50 | = | 102.1 | nM | 6.99 |
| CHEMBL535 | SUNITINIB | IC50 | = | 18.9 | nM | - |
| CHEMBL53463 | DOXORUBICIN | IC50 | - | — | - | |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124.7 | nM | - |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12.9 | nM | - |