Assay Detail
Binding
CHEMBL812787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for inhibitory activity towards tyrosine kinase Vascular endothelial growth factor receptor 2
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.88 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431996 | — | — | 1 | 8.40 |
| CHEMBL89010 | — | — | 1 | 7.70 |
| CHEMBL89363 | — | — | 1 | 7.70 |
| CHEMBL88483 | — | — | 1 | 7.52 |
| CHEMBL314995 | — | — | 1 | 7.52 |
| CHEMBL91815 | — | — | 1 | 7.52 |
| CHEMBL88771 | — | — | 1 | 7.30 |
| CHEMBL313821 | — | — | 1 | 7.22 |
| CHEMBL88606 | — | — | 1 | 7.16 |
| CHEMBL432941 | — | — | 1 | 7.16 |
| CHEMBL315753 | — | — | 1 | 7.05 |
| CHEMBL420609 | — | — | 1 | 6.42 |
| CHEMBL328029 | — | — | 1 | 6.32 |
| CHEMBL86531 | — | — | 1 | 6.22 |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 6.16 |
| CHEMBL91250 | — | — | 1 | 4.92 |
| CHEMBL88462 | — | — | 1 | 4.70 |
| CHEMBL313746 | — | — | 1 | - |
| CHEMBL419682 | — | — | 1 | - |
| CHEMBL313500 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431996 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL89010 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL89363 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL88483 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL314995 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL91815 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL88771 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL313821 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL88606 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL432941 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL315753 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL420609 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL328029 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL86531 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL91250 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL88462 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL313746 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL419682 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL313500 | — | IC50 | > | 20000.0 | nM | - |