Assay Detail
Binding
CHEMBL3111580
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf9 cells by radiometric assay
11
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB: 1Y6A complex--medicinal chemistry consequences of a TKs analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.39 | 7.90 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1200485 | SORAFENIB TOSYLATE | 4.0 | 1 | 7.90 |
| CHEMBL3109274 | — | — | 2 | 7.82 |
| CHEMBL194176 | — | — | 1 | 7.77 |
| CHEMBL3109278 | — | — | 1 | 7.51 |
| CHEMBL3109275 | — | — | 2 | 7.29 |
| CHEMBL3109276 | — | — | 2 | 6.77 |
| CHEMBL3109277 | — | — | 2 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1200485 | SORAFENIB TOSYLATE | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL3109274 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL194176 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3109278 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL3109275 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL3109276 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3109277 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3109277 | — | Inhibition | - | % | - | |
| CHEMBL3109276 | — | Inhibition | - | % | - | |
| CHEMBL3109275 | — | Inhibition | - | % | - | |
| CHEMBL3109274 | — | Inhibition | - | % | - |