Assay Detail
Binding
CHEMBL5553572
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Inhibition of N-terminal GST-tagged human recombinant c-MET (956 to 1390 residues) expressed in Baculovirus infected Sf9 cell expression system by ELISA analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of new 1,3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, <i>in vivo</i> and <i>in silico</i> studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.89 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 8.41 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.82 |
| CHEMBL5594061 | — | — | 1 | 7.75 |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | 7.72 |
| CHEMBL5593609 | — | — | 1 | 7.62 |
| CHEMBL3764045 | TAS-115 | 1.0 | 1 | 7.50 |
| CHEMBL5574745 | — | — | 1 | 7.19 |
| CHEMBL5571331 | — | — | 1 | 6.82 |
| CHEMBL5568824 | — | — | 1 | 6.77 |
| CHEMBL5595346 | — | — | 1 | 6.60 |
| CHEMBL5565651 | — | — | 1 | 6.42 |
| CHEMBL5583996 | — | — | 1 | 6.39 |
| CHEMBL5575208 | — | — | 1 | 6.35 |
| CHEMBL5574737 | — | — | 1 | 6.28 |
| CHEMBL5572702 | — | — | 1 | 6.21 |
| CHEMBL5565430 | — | — | 1 | 6.14 |
| CHEMBL5579755 | — | — | 1 | 6.09 |
| CHEMBL5574727 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460702 | BMS-777607 | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5594061 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3545307 | MERESTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5593609 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3764045 | TAS-115 | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5574745 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5571331 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5568824 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5595346 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5565651 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5583996 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5575208 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5574737 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5572702 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5565430 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5579755 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5574727 | — | IC50 | = | 1040.0 | nM | 5.98 |