Assay Detail
Binding
CHEMBL3767620
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Inhibition of c-Met (unknown origin)
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.53 | 9.89 |
| Ki | 3 | 7.92 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3188267 | CAPMATINIB | 4.0 | 1 | 9.89 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 9.40 |
| CHEMBL460472 | — | — | 1 | 8.92 |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | 8.52 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 8.41 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.40 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 8.40 |
| CHEMBL2133806 | JNJ-38877605 | 1.0 | 1 | 8.40 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 8.32 |
| CHEMBL450786 | PHA-665752 | — | 1 | 8.05 |
| CHEMBL496102 | AMG-208 | 2.0 | 1 | 8.05 |
| CHEMBL1738731 | — | — | 1 | 7.85 |
| CHEMBL2103882 | TIVANTINIB | 3.0 | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3188267 | CAPMATINIB | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL1822792 | MK-2461 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL460472 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3402762 | TEPOTINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL460702 | BMS-777607 | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL601719 | CRIZOTINIB | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1236107 | SGX-523 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2133806 | JNJ-38877605 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2001019 | PF-04217903 | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL450786 | PHA-665752 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL496102 | AMG-208 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1738731 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2103882 | TIVANTINIB | Ki | = | 355.0 | nM | 6.45 |