Assay Detail
Binding
CHEMBL960946
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Inhibition of GST-fused recombinant VGFR2 catalytic domain expressed in baculovirus-infected Sf9 cells after 10 mins by DELFIA assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.59 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517469 | — | — | 1 | 8.52 |
| CHEMBL508395 | — | — | 1 | 8.52 |
| CHEMBL464211 | — | — | 1 | 8.15 |
| CHEMBL462232 | — | — | 1 | 8.10 |
| CHEMBL449757 | — | — | 1 | 8.10 |
| CHEMBL503016 | — | — | 1 | 8.10 |
| CHEMBL465131 | — | — | 1 | 8.05 |
| CHEMBL465130 | — | — | 1 | 8.00 |
| CHEMBL448276 | — | — | 1 | 7.96 |
| CHEMBL518676 | — | — | 1 | 7.92 |
| CHEMBL453613 | — | — | 1 | 7.92 |
| CHEMBL447616 | — | — | 1 | 7.92 |
| CHEMBL462835 | — | — | 1 | 7.85 |
| CHEMBL445871 | — | — | 1 | 7.85 |
| CHEMBL464510 | — | — | 1 | 7.82 |
| CHEMBL459478 | — | — | 1 | 7.80 |
| CHEMBL503524 | — | — | 1 | 7.70 |
| CHEMBL502621 | — | — | 1 | 7.64 |
| CHEMBL455655 | — | — | 1 | 7.58 |
| CHEMBL254760 | — | — | 1 | 7.58 |
| CHEMBL510676 | — | — | 1 | 7.51 |
| CHEMBL490965 | — | — | 1 | 7.43 |
| CHEMBL518209 | — | — | 1 | 7.41 |
| CHEMBL462667 | — | — | 1 | 7.24 |
| CHEMBL508776 | — | — | 1 | 6.77 |
| CHEMBL462231 | — | — | 1 | 6.64 |
| CHEMBL462023 | — | — | 1 | 6.10 |
| CHEMBL448993 | — | — | 1 | 6.06 |
| CHEMBL464409 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517469 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL508395 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL464211 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL462232 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL449757 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL503016 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL465131 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL465130 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL448276 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL518676 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL453613 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL447616 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL462835 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL445871 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL464510 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL459478 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL503524 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL502621 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL455655 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL254760 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL510676 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL490965 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL518209 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL462667 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL508776 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL462231 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL462023 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL448993 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL464409 | — | IC50 | = | 1800.0 | nM | 5.75 |