Assay Detail
Binding
CHEMBL2327587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HGF-stimulated c-MET (unknown origin) autophosphorylation at tyrosine 1349 expressed in human GTL16 cells after 2 hrs by Western blotting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | GTL16 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.32 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323775 | MK-8033 | 1.0 | 1 | 7.54 |
| CHEMBL1802829 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323775 | MK-8033 | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1802829 | — | IC50 | = | 80.0 | nM | 7.10 |