Assay Detail
Binding
CHEMBL989219
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Inhibition of VEGFR2 by HTRF assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
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 |
|---|---|---|---|
| Ki | 8 | 6.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL461293 | — | — | 1 | 8.70 |
| CHEMBL460465 | — | — | 1 | 7.62 |
| CHEMBL460468 | — | — | 1 | 6.41 |
| CHEMBL518174 | — | — | 1 | 6.40 |
| CHEMBL460466 | — | — | 1 | 6.34 |
| CHEMBL459647 | — | — | 1 | 6.00 |
| CHEMBL445799 | — | — | 1 | 5.94 |
| CHEMBL460472 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL461293 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL460465 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL460468 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL518174 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL460466 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL459647 | — | Ki | = | 999.0 | nM | 6.00 |
| CHEMBL445799 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL460472 | — | Ki | = | 4100.0 | nM | 5.39 |