Assay Detail
Binding
CHEMBL4132764
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal biotinylated DYKDDDDK tagged human VEGFR2 (790 to 1356 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr by mobility shift assay
16
Total Activities
16
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
Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.80 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.07 |
| CHEMBL4165429 | — | — | 1 | 7.16 |
| CHEMBL4166696 | — | — | 1 | 7.09 |
| CHEMBL4161991 | — | — | 1 | 6.98 |
| CHEMBL4173756 | — | — | 1 | 6.97 |
| CHEMBL4165827 | — | — | 1 | 6.86 |
| CHEMBL4177112 | — | — | 1 | 6.59 |
| CHEMBL4169257 | — | — | 1 | 6.42 |
| CHEMBL4173078 | — | — | 1 | 6.37 |
| CHEMBL4162400 | — | — | 1 | 6.19 |
| CHEMBL4172205 | — | — | 1 | 6.09 |
| CHEMBL4163106 | — | — | 1 | - |
| CHEMBL4176039 | — | — | 1 | - |
| CHEMBL4164318 | — | — | 1 | - |
| CHEMBL4165850 | — | — | 1 | - |
| CHEMBL4161351 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4165429 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL4166696 | — | IC50 | = | 81.3 | nM | 7.09 |
| CHEMBL4161991 | — | IC50 | = | 104.6 | nM | 6.98 |
| CHEMBL4173756 | — | IC50 | = | 106.1 | nM | 6.97 |
| CHEMBL4165827 | — | IC50 | = | 138.3 | nM | 6.86 |
| CHEMBL4177112 | — | IC50 | = | 257.2 | nM | 6.59 |
| CHEMBL4169257 | — | IC50 | = | 384.7 | nM | 6.42 |
| CHEMBL4173078 | — | IC50 | = | 431.2 | nM | 6.37 |
| CHEMBL4162400 | — | IC50 | = | 646.5 | nM | 6.19 |
| CHEMBL4172205 | — | IC50 | = | 808.5 | nM | 6.09 |
| CHEMBL4163106 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4176039 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4164318 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4165850 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4161351 | — | IC50 | - | — | - |