Assay Detail
Binding
CHEMBL5252745
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-fused VEGFR1 kinase domain transphosphorylation expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate measured after 10 mins in presence of gamma-[33P]-ATP by scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.70 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.82 |
| CHEMBL75232 | — | — | 1 | 7.11 |
| CHEMBL5288744 | — | — | 1 | 7.09 |
| CHEMBL153843 | — | — | 1 | 6.89 |
| CHEMBL5276611 | — | — | 1 | 6.65 |
| CHEMBL5280119 | — | — | 1 | 6.48 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.40 |
| CHEMBL4104297 | — | — | 1 | 6.09 |
| CHEMBL4080062 | BFH-772 | 2.0 | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL75232 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5288744 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL153843 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5276611 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL5280119 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL4104297 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4080062 | BFH-772 | IC50 | = | 1700.0 | nM | 5.77 |