Assay Detail
Binding
CHEMBL4714414
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 in human U251 cells preincubated for 60 mins followed by VEGF stimulation and measured after 10 mins by ELISA
9
Total Activities
9
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
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.56 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL492399 | VERUBULIN | 2.0 | 1 | 8.08 |
| CHEMBL2420866 | — | — | 1 | 8.03 |
| CHEMBL516047 | — | — | 1 | 7.83 |
| CHEMBL4746488 | — | — | 1 | 7.78 |
| CHEMBL2420867 | — | — | 1 | 7.26 |
| CHEMBL444724 | — | — | 1 | 7.01 |
| CHEMBL3604205 | — | — | 1 | 6.95 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL492399 | VERUBULIN | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2420866 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL516047 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL4746488 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL2420867 | — | IC50 | = | 55.2 | nM | 7.26 |
| CHEMBL444724 | — | IC50 | = | 97.5 | nM | 7.01 |
| CHEMBL3604205 | — | IC50 | = | 111.1 | nM | 6.95 |
| CHEMBL535 | SUNITINIB | IC50 | = | 18.9 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124.7 | nM | - |