Assay Detail
Functional
CHEMBL837258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGF-stimulated human umbilical vein endothelial cell proliferation
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Endothelial cell |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor (CHEMBL2095227) ↗| Type | PROTEIN FAMILY |
| 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 | 21 | 7.89 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193306 | — | — | 1 | 8.96 |
| CHEMBL371373 | — | — | 1 | 8.74 |
| CHEMBL192101 | — | — | 1 | 8.68 |
| CHEMBL195398 | — | — | 1 | 8.68 |
| CHEMBL190980 | — | — | 1 | 8.44 |
| CHEMBL191913 | — | — | 1 | 8.40 |
| CHEMBL195847 | — | — | 1 | 8.17 |
| CHEMBL370515 | — | — | 1 | 8.17 |
| CHEMBL365318 | — | — | 1 | 8.12 |
| CHEMBL194498 | — | — | 1 | 7.77 |
| CHEMBL373365 | — | — | 1 | 7.75 |
| CHEMBL191594 | — | — | 1 | 7.72 |
| CHEMBL194872 | — | — | 1 | 7.60 |
| CHEMBL195903 | — | — | 1 | 7.57 |
| CHEMBL366019 | — | — | 1 | 7.51 |
| CHEMBL370023 | — | — | 1 | 7.46 |
| CHEMBL370266 | — | — | 1 | 7.34 |
| CHEMBL193136 | — | — | 1 | 7.30 |
| CHEMBL192318 | — | — | 1 | 7.21 |
| CHEMBL195771 | — | — | 1 | 7.04 |
| CHEMBL195218 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193306 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL371373 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL192101 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL195398 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL190980 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL191913 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL195847 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL370515 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL365318 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL194498 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL373365 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL191594 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL194872 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL195903 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL366019 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL370023 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL370266 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL193136 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL192318 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL195771 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL195218 | — | IC50 | = | 100.0 | nM | 7.00 |