Assay Detail
Binding
CHEMBL5716591
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Inhibition of His6-tagged human c-Met M1131T mutant expressed in Sf9 cells pre-incubated with enzyme for 30 mins prior to addition of ATP using (Glu4Tyr) or Met2 peptide substrate by coupled enzymatic assay
7
Total Activities
7
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Ki | 7 | 7.71 | 8.40 |
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 |
|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.40 |
| CHEMBL5723016 | — | — | 1 | 8.10 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 7.89 |
| CHEMBL5722969 | — | — | 1 | 7.77 |
| CHEMBL5722973 | — | — | 1 | 7.41 |
| CHEMBL2431819 | — | — | 1 | 7.23 |
| CHEMBL5723028 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL5723016 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2001019 | PF-04217903 | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5722969 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5722973 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL2431819 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5723028 | — | Ki | = | 64.0 | nM | 7.19 |