Assay Detail
Binding
CHEMBL3369647
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Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA
31
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H441 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.76 | 8.52 |
| Inhibition | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3334569 | — | — | 1 | 8.52 |
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | 8.52 |
| CHEMBL2170816 | — | — | 1 | 8.22 |
| CHEMBL3334557 | — | — | 2 | 8.22 |
| CHEMBL3334540 | — | — | 1 | 8.15 |
| CHEMBL3334551 | — | — | 2 | 8.15 |
| CHEMBL3334552 | — | — | 2 | 8.10 |
| CHEMBL3334556 | — | — | 2 | 8.00 |
| CHEMBL3334561 | — | — | 2 | 8.00 |
| CHEMBL3334542 | — | — | 2 | 7.96 |
| CHEMBL3334565 | — | — | 1 | 7.92 |
| CHEMBL3334564 | — | — | 1 | 7.92 |
| CHEMBL3334541 | — | — | 1 | 7.72 |
| CHEMBL3334546 | — | — | 1 | 7.70 |
| CHEMBL3334549 | — | — | 1 | 7.58 |
| CHEMBL3334563 | — | — | 1 | 7.58 |
| CHEMBL3334570 | — | — | 1 | 7.57 |
| CHEMBL3334562 | — | — | 1 | 7.51 |
| CHEMBL3334568 | — | — | 1 | 7.50 |
| CHEMBL3334550 | — | — | 1 | 7.48 |
| CHEMBL3334560 | — | — | 1 | 7.21 |
| CHEMBL3334545 | — | — | 1 | 7.20 |
| CHEMBL2431841 | — | — | 1 | 7.16 |
| CHEMBL3334544 | — | — | 1 | 7.11 |
| CHEMBL3334553 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3334567 | SAVOLITINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3334569 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2170816 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334557 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334540 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334551 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334552 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3334561 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3334556 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3334542 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3334565 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3334564 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3334541 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3334546 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3334563 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3334549 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3334570 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3334562 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3334568 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3334550 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3334560 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3334545 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2431841 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3334544 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3334553 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3334561 | — | Inhibition | = | 15.9 | % | - |
| CHEMBL3334556 | — | Inhibition | = | 34.7 | % | - |
| CHEMBL3334557 | — | Inhibition | = | 61.0 | % | - |
| CHEMBL3334542 | — | Inhibition | = | 36.9 | % | - |
| CHEMBL3334551 | — | Inhibition | = | 50.1 | % | - |
| CHEMBL3334552 | — | Inhibition | = | 18.8 | % | - |