Assay Detail
Binding
CHEMBL3404456
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Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.20 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | 7.92 |
| CHEMBL3402760 | — | — | 1 | 7.82 |
| CHEMBL3402756 | — | — | 1 | 7.82 |
| CHEMBL3402758 | — | — | 1 | 7.55 |
| CHEMBL3402761 | — | — | 1 | 7.47 |
| CHEMBL3402742 | — | — | 1 | 7.11 |
| CHEMBL3402757 | — | — | 1 | 6.85 |
| CHEMBL3402743 | — | — | 1 | 6.82 |
| CHEMBL3402759 | — | — | 1 | 6.70 |
| CHEMBL3402741 | — | — | 1 | 5.96 |
| CHEMBL3402754 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3402762 | TEPOTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3402760 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3402756 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3402758 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3402761 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3402742 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3402757 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3402743 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3402759 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3402741 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3402754 | — | IC50 | > | 1.0 | nM | - |