Assay Detail
Binding
CHEMBL5252744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-fused VEGFR3 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 3 (CHEMBL1955) ↗| 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 | 6.91 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL153843 | — | — | 1 | 7.75 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.62 |
| CHEMBL5288744 | — | — | 1 | 7.30 |
| CHEMBL75232 | — | — | 1 | 7.19 |
| CHEMBL5276611 | — | — | 1 | 6.75 |
| CHEMBL5280119 | — | — | 1 | 6.63 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.61 |
| CHEMBL4104297 | — | — | 1 | 6.38 |
| CHEMBL4080062 | BFH-772 | 2.0 | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL153843 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL535 | SUNITINIB | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5288744 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL75232 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5276611 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL5280119 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL4104297 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4080062 | BFH-772 | IC50 | = | 1100.0 | nM | 5.96 |