Assay Detail
Binding
CHEMBL929417
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Inhibition of human VEGFR2
17
Total Activities
17
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 |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.31 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410686 | — | — | 1 | 7.89 |
| CHEMBL409673 | — | — | 1 | 7.77 |
| CHEMBL256116 | — | — | 1 | 7.72 |
| CHEMBL409442 | — | — | 1 | 7.60 |
| CHEMBL261592 | — | — | 1 | 7.60 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 7.60 |
| CHEMBL255902 | — | — | 1 | 7.57 |
| CHEMBL412081 | — | — | 1 | 7.52 |
| CHEMBL258694 | — | — | 1 | 7.51 |
| CHEMBL259951 | — | — | 1 | 7.44 |
| CHEMBL264943 | — | — | 1 | 7.02 |
| CHEMBL258695 | — | — | 1 | 6.95 |
| CHEMBL412082 | — | — | 1 | 6.92 |
| CHEMBL260199 | — | — | 1 | 6.91 |
| CHEMBL265431 | — | — | 1 | 6.82 |
| CHEMBL265191 | — | — | 1 | 6.78 |
| CHEMBL259996 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410686 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL409673 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL256116 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL409442 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL261592 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL377300 | BRIVANIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL255902 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL412081 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL258694 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL259951 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL264943 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL258695 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL412082 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL260199 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL265431 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL265191 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL259996 | — | IC50 | = | 223.0 | nM | 6.65 |