Assay Detail
Binding
CHEMBL989220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition VEGFR2-mediated survival of HUVEC
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HUVEC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.65 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460465 | — | — | 1 | 7.28 |
| CHEMBL461293 | — | — | 1 | 7.07 |
| CHEMBL460466 | — | — | 1 | 6.84 |
| CHEMBL460468 | — | — | 1 | 6.68 |
| CHEMBL518174 | — | — | 1 | 6.63 |
| CHEMBL459647 | — | — | 1 | 6.48 |
| CHEMBL460472 | — | — | 1 | 6.16 |
| CHEMBL445799 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460465 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL461293 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL460466 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL460468 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL518174 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL459647 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL460472 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL445799 | — | IC50 | = | 921.0 | nM | 6.04 |