Assay Detail
Binding
CHEMBL3369646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of c-Met (unknown origin) using Poly E4Y substrate and ATP incubated for 45 mins by fluorescence polarization assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 33 | 7.64 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3334540 | — | — | 1 | 8.40 |
| CHEMBL2170816 | — | — | 1 | 8.30 |
| CHEMBL3334551 | — | — | 1 | 8.30 |
| CHEMBL3334556 | — | — | 1 | 8.30 |
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | 8.30 |
| CHEMBL3334564 | — | — | 1 | 8.22 |
| CHEMBL3334550 | — | — | 1 | 8.22 |
| CHEMBL3334549 | — | — | 1 | 8.22 |
| CHEMBL3334542 | — | — | 1 | 8.22 |
| CHEMBL3334541 | — | — | 1 | 8.22 |
| CHEMBL3334565 | — | — | 1 | 8.15 |
| CHEMBL3334562 | — | — | 1 | 8.15 |
| CHEMBL3334569 | — | — | 1 | 8.15 |
| CHEMBL3334557 | — | — | 1 | 8.05 |
| CHEMBL3334552 | — | — | 1 | 8.05 |
| CHEMBL3334560 | — | — | 1 | 7.96 |
| CHEMBL3334561 | — | — | 1 | 7.89 |
| CHEMBL3334563 | — | — | 1 | 7.77 |
| CHEMBL3334546 | — | — | 1 | 7.72 |
| CHEMBL3334545 | — | — | 1 | 7.62 |
| CHEMBL3334544 | — | — | 1 | 7.58 |
| CHEMBL3334570 | — | — | 1 | 7.52 |
| CHEMBL3334568 | — | — | 1 | 7.50 |
| CHEMBL3334553 | — | — | 1 | 7.02 |
| CHEMBL3334543 | — | — | 1 | 6.89 |
| CHEMBL3334547 | — | — | 1 | 6.85 |
| CHEMBL3334559 | — | — | 1 | 6.71 |
| CHEMBL2431841 | — | — | 1 | 6.68 |
| CHEMBL3334555 | — | — | 1 | 6.64 |
| CHEMBL3334548 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3334540 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2170816 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3334567 | SAVOLITINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3334556 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3334551 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3334564 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334550 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334549 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334542 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334541 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3334565 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334562 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334569 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3334557 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3334552 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3334560 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3334561 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3334563 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3334546 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3334545 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3334544 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3334570 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3334568 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3334553 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3334543 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3334547 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL3334559 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL2431841 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3334555 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3334548 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL3334558 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL3334566 | — | IC50 | = | 787.0 | nM | 6.10 |
| CHEMBL3334554 | — | IC50 | > | 1000.0 | nM | - |