Assay Detail
Binding
CHEMBL4268599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 (unknown origin)
5
Total Activities
5
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 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.73 | 10.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 10.46 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.07 |
| CHEMBL3989926 | SITRAVATINIB | 3.0 | 1 | 8.30 |
| CHEMBL3545365 | ALTIRATINIB | 2.0 | 1 | 8.04 |
| CHEMBL4286385 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 0.035 | nM | 10.46 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL3989926 | SITRAVATINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3545365 | ALTIRATINIB | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4286385 | — | IC50 | = | 16.0 | nM | 7.80 |