Assay Detail
Binding
CHEMBL957978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant VEGFR3
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 3 (CHEMBL1955) ↗| 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 | 5.64 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201511 | MALEIMIDE | — | 1 | 8.30 |
| CHEMBL529663 | — | — | 1 | 7.43 |
| CHEMBL453336 | — | — | 1 | 5.77 |
| CHEMBL453593 | — | — | 1 | 5.60 |
| CHEMBL488811 | — | — | 1 | 5.60 |
| CHEMBL509635 | — | — | 1 | 5.50 |
| CHEMBL519590 | — | — | 1 | 5.50 |
| CHEMBL505253 | — | — | 1 | 5.47 |
| CHEMBL529217 | — | — | 1 | 5.44 |
| CHEMBL488646 | — | — | 1 | 5.32 |
| CHEMBL488645 | — | — | 1 | 5.28 |
| CHEMBL486437 | — | — | 1 | 5.25 |
| CHEMBL452812 | — | — | 1 | 5.06 |
| CHEMBL521201 | — | — | 1 | 5.03 |
| CHEMBL509435 | — | — | 1 | 4.96 |
| CHEMBL507056 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201511 | MALEIMIDE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL529663 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL453336 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL453593 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL488811 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL509635 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL519590 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL505253 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL529217 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL488646 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL488645 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL486437 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL452812 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL521201 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL509435 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL507056 | — | IC50 | = | 18000.0 | nM | 4.75 |