Assay Detail
Binding
CHEMBL4623159
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST fused human VEGFR2 cytoplasmic domain (790 to 1356 (end) residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay
18
Total Activities
18
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
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.93 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.33 |
| CHEMBL4644718 | — | — | 1 | 8.19 |
| CHEMBL4639712 | — | — | 1 | 7.85 |
| CHEMBL4079087 | — | — | 1 | 7.23 |
| CHEMBL4643300 | — | — | 1 | 7.19 |
| CHEMBL4069394 | — | — | 1 | 7.08 |
| CHEMBL4634687 | — | — | 1 | 7.00 |
| CHEMBL4640617 | — | — | 1 | 6.83 |
| CHEMBL4649259 | — | — | 1 | 6.64 |
| CHEMBL4641639 | — | — | 1 | 6.61 |
| CHEMBL4640302 | — | — | 1 | 6.54 |
| CHEMBL4647154 | — | — | 1 | 6.33 |
| CHEMBL4642920 | — | — | 1 | 6.31 |
| CHEMBL4648781 | — | — | 1 | 6.31 |
| CHEMBL4639539 | — | — | 1 | 6.23 |
| CHEMBL4638817 | — | — | 1 | 6.16 |
| CHEMBL4647153 | — | — | 1 | - |
| CHEMBL4641415 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4644718 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4639712 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4079087 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL4643300 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4069394 | — | IC50 | = | 82.3 | nM | 7.08 |
| CHEMBL4634687 | — | IC50 | = | 100.8 | nM | 7.00 |
| CHEMBL4640617 | — | IC50 | = | 147.6 | nM | 6.83 |
| CHEMBL4649259 | — | IC50 | = | 227.7 | nM | 6.64 |
| CHEMBL4641639 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4640302 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL4647154 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL4642920 | — | IC50 | = | 492.0 | nM | 6.31 |
| CHEMBL4648781 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL4639539 | — | IC50 | = | 584.0 | nM | 6.23 |
| CHEMBL4638817 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4647153 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4641415 | — | IC50 | > | 1000.0 | nM | - |