Assay Detail
Binding
CHEMBL4368500
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1993 cells incubated for 4 hrs by HTRF assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1993 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.35 | 8.70 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | 8.70 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 6.67 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.67 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3334567 | SAVOLITINIB | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL460702 | BMS-777607 | IC50 | = | 213.8 | nM | 6.67 |
| CHEMBL1230609 | FORETINIB | IC50 | = | 213.8 | nM | 6.67 |
| CHEMBL601719 | CRIZOTINIB | Inhibition | - | % | - |