Assay Detail
Binding
CHEMBL4773366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (789 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo luminescent assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.34 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3633296 | — | — | 1 | 8.16 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.08 |
| CHEMBL4789418 | — | — | 1 | 7.09 |
| CHEMBL4794619 | — | — | 1 | 6.68 |
| CHEMBL4780189 | — | — | 1 | 6.68 |
| CHEMBL4791334 | — | — | 1 | - |
| CHEMBL4792511 | — | — | 1 | - |
| CHEMBL4792399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3633296 | — | IC50 | = | 6.86 | nM | 8.16 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 8.404 | nM | 8.08 |
| CHEMBL4789418 | — | IC50 | = | 80.42 | nM | 7.09 |
| CHEMBL4794619 | — | IC50 | = | 208.66 | nM | 6.68 |
| CHEMBL4780189 | — | IC50 | = | 208.15 | nM | 6.68 |
| CHEMBL4791334 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4792511 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4792399 | — | IC50 | > | 1000.0 | nM | - |