Assay Detail
Binding
CHEMBL4143267
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Inhibition of human GST-tagged c-MET using KKKSPGEYVNIEFG as substrate preincubated for 20 mins followed by [gamma-33P]ATP addition and measured after 2 hrs by filter-binding assay
10
Total Activities
10
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, optimization and biological evaluation for novel c-Met kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.43 | 8.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.98 |
| CHEMBL4170972 | — | — | 1 | 7.86 |
| CHEMBL4165119 | — | — | 1 | 7.10 |
| CHEMBL4167593 | — | — | 1 | 6.81 |
| CHEMBL4165354 | — | — | 1 | 6.72 |
| CHEMBL4172124 | — | — | 1 | 5.94 |
| CHEMBL4173269 | — | — | 1 | 5.48 |
| CHEMBL4161526 | — | — | 1 | 5.26 |
| CHEMBL4168774 | — | — | 1 | 5.19 |
| CHEMBL4161920 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 1.053 | nM | 8.98 |
| CHEMBL4170972 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4165119 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL4167593 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4165354 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4172124 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4173269 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL4161526 | — | IC50 | = | 5490.0 | nM | 5.26 |
| CHEMBL4168774 | — | IC50 | = | 6510.0 | nM | 5.19 |
| CHEMBL4161920 | — | IC50 | = | 11190.0 | nM | 4.95 |