Assay Detail
Binding
CHEMBL860941
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Inhibitory activity against VEGFR2
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.29 | 7.77 |
| Ki | 1 | 7.58 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383671 | — | — | 1 | 7.77 |
| CHEMBL205142 | — | — | 1 | 7.77 |
| CHEMBL206146 | — | — | 1 | 7.70 |
| CHEMBL206145 | — | — | 1 | 7.70 |
| CHEMBL380905 | — | — | 1 | 7.62 |
| CHEMBL380957 | — | — | 1 | 7.62 |
| CHEMBL377300 | BRIVANIB | 3.0 | 2 | 7.60 |
| CHEMBL427202 | — | — | 1 | 7.40 |
| CHEMBL205710 | — | — | 1 | 7.38 |
| CHEMBL206545 | — | — | 1 | 7.18 |
| CHEMBL383077 | — | — | 1 | 7.16 |
| CHEMBL205283 | — | — | 1 | 7.11 |
| CHEMBL207842 | — | — | 1 | 7.06 |
| CHEMBL381104 | — | — | 1 | 6.68 |
| CHEMBL377302 | — | — | 1 | 6.51 |
| CHEMBL381973 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205142 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL383671 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL206145 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL206146 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL380957 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL380905 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL377300 | BRIVANIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL377300 | BRIVANIB | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL427202 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL205710 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL206545 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL383077 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL205283 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL207842 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL381104 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL377302 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL381973 | — | IC50 | = | 470.0 | nM | 6.33 |