Assay Detail
Binding
CHEMBL5256649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST tagged recombinant human VEGFR2 (aa805 to 1356 residues) expressed in baculovirus expression system using Poly- (Glu4:Tyr)-biotin as substrate incubated for 80 mins in presence of ATP by kinase glo method
8
Total Activities
8
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 of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.59 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5278505 | — | — | 1 | 5.92 |
| CHEMBL5287545 | — | — | 1 | 5.83 |
| CHEMBL3701255 | — | — | 1 | 5.75 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 5.63 |
| CHEMBL3701241 | — | — | 1 | 5.52 |
| CHEMBL5269016 | — | — | 1 | 5.47 |
| CHEMBL3701243 | — | — | 1 | 5.43 |
| CHEMBL5268467 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5278505 | — | IC50 | = | 1206.0 | nM | 5.92 |
| CHEMBL5287545 | — | IC50 | = | 1486.0 | nM | 5.83 |
| CHEMBL3701255 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 2358.0 | nM | 5.63 |
| CHEMBL3701241 | — | IC50 | = | 3029.0 | nM | 5.52 |
| CHEMBL5269016 | — | IC50 | = | 3377.0 | nM | 5.47 |
| CHEMBL3701243 | — | IC50 | = | 3686.0 | nM | 5.43 |
| CHEMBL5268467 | — | IC50 | = | 7010.0 | nM | 5.15 |