Assay Detail
Binding
CHEMBL829589
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human vascular endothelial growth factor receptor 2 kinase activity
35
Total Activities
35
Compounds Tested
1
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
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.26 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193306 | — | — | 1 | 8.10 |
| CHEMBL195847 | — | — | 1 | 7.96 |
| CHEMBL190980 | — | — | 1 | 7.96 |
| CHEMBL195700 | — | — | 1 | 7.89 |
| CHEMBL195398 | — | — | 1 | 7.80 |
| CHEMBL371373 | — | — | 1 | 7.77 |
| CHEMBL191913 | — | — | 1 | 7.77 |
| CHEMBL365318 | — | — | 1 | 7.75 |
| CHEMBL373365 | — | — | 1 | 7.66 |
| CHEMBL192101 | — | — | 1 | 7.64 |
| CHEMBL194872 | — | — | 1 | 7.54 |
| CHEMBL363639 | — | — | 1 | 7.47 |
| CHEMBL191594 | — | — | 1 | 7.44 |
| CHEMBL195853 | — | — | 1 | 7.40 |
| CHEMBL370515 | — | — | 1 | 7.31 |
| CHEMBL195903 | — | — | 1 | 7.28 |
| CHEMBL370266 | — | — | 1 | 7.24 |
| CHEMBL194498 | — | — | 1 | 7.24 |
| CHEMBL195218 | — | — | 1 | 7.21 |
| CHEMBL366019 | — | — | 1 | 7.18 |
| CHEMBL372662 | — | — | 1 | 7.18 |
| CHEMBL193136 | — | — | 1 | 7.15 |
| CHEMBL370023 | — | — | 1 | 7.12 |
| CHEMBL195771 | — | — | 1 | 7.11 |
| CHEMBL192318 | — | — | 1 | 7.10 |
| CHEMBL365109 | — | — | 1 | 7.10 |
| CHEMBL194929 | — | — | 1 | 6.96 |
| CHEMBL365336 | — | — | 1 | 6.92 |
| CHEMBL365178 | — | — | 1 | 6.89 |
| CHEMBL436117 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193306 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL195847 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL190980 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL195700 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL195398 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL371373 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL191913 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL365318 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL373365 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL192101 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL194872 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL363639 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL191594 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL195853 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL370515 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL195903 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL194498 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL370266 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL195218 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL366019 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL372662 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL193136 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL370023 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL195771 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL192318 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL365109 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL194929 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL365336 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL365178 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL436117 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL195254 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL193256 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL364962 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL195845 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL192100 | — | IC50 | = | 1200.0 | nM | 5.92 |