Assay Detail
Binding
CHEMBL957977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant VEGFR2
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
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.61 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201511 | MALEIMIDE | — | 1 | 8.60 |
| CHEMBL529663 | — | — | 1 | 7.51 |
| CHEMBL488811 | — | — | 1 | 5.82 |
| CHEMBL453336 | — | — | 1 | 5.80 |
| CHEMBL519590 | — | — | 1 | 5.64 |
| CHEMBL486437 | — | — | 1 | 5.51 |
| CHEMBL453593 | — | — | 1 | 5.38 |
| CHEMBL488646 | — | — | 1 | 5.36 |
| CHEMBL488645 | — | — | 1 | 5.28 |
| CHEMBL529217 | — | — | 1 | 5.28 |
| CHEMBL505253 | — | — | 1 | 5.23 |
| CHEMBL509635 | — | — | 1 | 5.10 |
| CHEMBL521201 | — | — | 1 | 4.96 |
| CHEMBL452812 | — | — | 1 | 4.89 |
| CHEMBL509435 | — | — | 1 | 4.82 |
| CHEMBL507056 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201511 | MALEIMIDE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL529663 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL488811 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL453336 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL519590 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL486437 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL453593 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL488646 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL488645 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL529217 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL505253 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL509635 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL521201 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL452812 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL509435 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL507056 | — | IC50 | = | 31000.0 | nM | 4.51 |