Assay Detail
Binding
CHEMBL4268564
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
11
Total Activities
11
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 | 11 | 8.22 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103868 | CABOZANTINIB S-MALATE | 4.0 | 1 | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.48 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.44 |
| CHEMBL4292884 | — | — | 1 | 8.39 |
| CHEMBL4282387 | — | — | 1 | 8.30 |
| CHEMBL4285792 | — | — | 1 | 8.21 |
| CHEMBL4277848 | — | — | 1 | 8.18 |
| CHEMBL4292983 | — | — | 1 | 8.14 |
| CHEMBL4276790 | — | — | 1 | 7.92 |
| CHEMBL4285034 | — | — | 1 | 7.91 |
| CHEMBL4287439 | — | — | 1 | 7.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103868 | CABOZANTINIB S-MALATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4292884 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4282387 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4285792 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4277848 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4292983 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4276790 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4285034 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL4287439 | — | IC50 | = | 12.2 | nM | 7.91 |