Assay Detail
Binding
CHEMBL989217
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Inhibition of c-Met phosphorylation by HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
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 | 7 | 8.79 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460465 | — | — | 1 | 9.00 |
| CHEMBL518174 | — | — | 1 | 9.00 |
| CHEMBL460466 | — | — | 1 | 9.00 |
| CHEMBL460468 | — | — | 1 | 8.96 |
| CHEMBL461293 | — | — | 1 | 8.89 |
| CHEMBL445799 | — | — | 1 | 8.57 |
| CHEMBL459647 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460465 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL518174 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL460466 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL460468 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL461293 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL445799 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL459647 | — | Ki | = | 8.0 | nM | 8.10 |