Assay Detail
Binding
CHEMBL4715301
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Inhibition of c-Met (unknown origin) using poly Glu-Tyr as substrate preincubated for 10 mins followed by ATP addition by phosphoenolpyruvate/pyruvate kinase/lactate dehydrogenase coupled radiometric assay
21
Total Activities
21
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 of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.33 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784332 | — | — | 1 | 8.15 |
| CHEMBL4753090 | — | — | 1 | 8.10 |
| CHEMBL4790331 | — | — | 1 | 8.00 |
| CHEMBL4783289 | — | — | 1 | 7.82 |
| CHEMBL4787386 | — | — | 1 | 7.70 |
| CHEMBL4791034 | — | — | 1 | 7.70 |
| CHEMBL4778083 | — | — | 1 | 7.68 |
| CHEMBL4750387 | — | — | 1 | 7.62 |
| CHEMBL4793526 | — | — | 1 | 7.52 |
| CHEMBL4786582 | — | — | 1 | 7.40 |
| CHEMBL4760101 | — | — | 1 | 7.40 |
| CHEMBL4743756 | — | — | 1 | 7.30 |
| CHEMBL4762193 | — | — | 1 | 7.30 |
| CHEMBL2170957 | — | — | 1 | 7.22 |
| CHEMBL4740644 | — | — | 1 | 7.10 |
| CHEMBL4748465 | — | — | 1 | 7.10 |
| CHEMBL4740776 | — | — | 1 | 6.70 |
| CHEMBL2431818 | — | — | 1 | 6.70 |
| CHEMBL4763399 | — | — | 1 | 6.62 |
| CHEMBL4764695 | — | — | 1 | 6.40 |
| CHEMBL1822377 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784332 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4753090 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4790331 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4783289 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4787386 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4791034 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4778083 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4750387 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4793526 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4786582 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4760101 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4743756 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4762193 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2170957 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4740644 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4748465 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4740776 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2431818 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4763399 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4764695 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1822377 | — | Ki | = | 400.0 | nM | 6.40 |