Assay Detail
Binding
CHEMBL5716613
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Inhibition of wild type human c-Met expressed in mouse 3T3 cells assessed as reduction in cellular c-Met phosphorylation incubated for 1 hr followed by 20 mins stimulation with HGF by ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.08 | 8.77 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5722969 | — | — | 1 | 8.77 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.90 |
| CHEMBL2431819 | — | — | 1 | 7.87 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5722969 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL2431819 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL2001019 | PF-04217903 | IC50 | = | 16.9 | nM | 7.77 |