Assay Detail
Binding
CHEMBL2344597
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Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.47 | 4.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 4.92 |
| CHEMBL2337363 | — | — | 1 | 4.88 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 4.72 |
| CHEMBL2337369 | — | — | 1 | 4.67 |
| CHEMBL2337362 | — | — | 1 | 4.52 |
| CHEMBL2337371 | — | — | 1 | 4.51 |
| CHEMBL2337364 | — | — | 1 | 4.41 |
| CHEMBL2337372 | — | — | 1 | 4.39 |
| CHEMBL2337368 | — | — | 1 | 4.32 |
| CHEMBL2337366 | — | — | 1 | 4.15 |
| CHEMBL2337365 | — | — | 1 | 4.07 |
| CHEMBL2337370 | — | — | 1 | 4.05 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL2337367 | — | — | 1 | - |
| CHEMBL2337374 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2337363 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL535 | SUNITINIB | IC50 | = | 18900.0 | nM | 4.72 |
| CHEMBL2337369 | — | IC50 | = | 21300.0 | nM | 4.67 |
| CHEMBL2337362 | — | IC50 | = | 30300.0 | nM | 4.52 |
| CHEMBL2337371 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL2337364 | — | IC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL2337372 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL2337368 | — | IC50 | = | 47800.0 | nM | 4.32 |
| CHEMBL2337366 | — | IC50 | = | 70100.0 | nM | 4.15 |
| CHEMBL2337365 | — | IC50 | = | 86100.0 | nM | 4.07 |
| CHEMBL2337370 | — | IC50 | = | 89100.0 | nM | 4.05 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124700.0 | nM | - |
| CHEMBL2337367 | — | IC50 | = | 192000.0 | nM | - |
| CHEMBL2337374 | — | IC50 | = | 123800.0 | nM | - |