Assay Detail
Binding
CHEMBL3788752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HGF-mediated MET autophosphorylation in human PC3 cells preincubated for 1 hr followed by stimulation with human HGF measured after 10 mins by electrochemiluminescence immunoassay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.23 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2029678 | — | — | 1 | 8.70 |
| CHEMBL566685 | — | — | 1 | 8.52 |
| CHEMBL3414926 | — | — | 1 | 8.30 |
| CHEMBL3786314 | — | — | 1 | 8.30 |
| CHEMBL3785909 | AMG-337 | 2.0 | 1 | 8.30 |
| CHEMBL3787004 | — | — | 1 | 8.22 |
| CHEMBL3785199 | — | — | 1 | 8.15 |
| CHEMBL3785094 | — | — | 1 | 8.15 |
| CHEMBL494979 | — | — | 1 | 8.10 |
| CHEMBL3787109 | — | — | 1 | 8.10 |
| CHEMBL3786005 | — | — | 1 | 8.10 |
| CHEMBL3786495 | — | — | 1 | 8.05 |
| CHEMBL3785374 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2029678 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL566685 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3414926 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3786314 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3785909 | AMG-337 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3787004 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3785199 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3785094 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL494979 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3787109 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3786005 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3786495 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3785374 | — | IC50 | = | 11.0 | nM | 7.96 |