Assay Detail
Binding
CHEMBL2050144
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Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA
16
Total Activities
16
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
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.49 | 4.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2047245 | — | — | 1 | 4.96 |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 4.89 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 4.72 |
| CHEMBL2047249 | — | — | 1 | 4.52 |
| CHEMBL2047251 | — | — | 1 | 4.37 |
| CHEMBL2047246 | — | — | 1 | 4.25 |
| CHEMBL2047252 | — | — | 1 | 4.14 |
| CHEMBL2047241 | — | — | 1 | 4.05 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL2047253 | — | — | 1 | - |
| CHEMBL2047250 | — | — | 1 | - |
| CHEMBL2047248 | — | — | 1 | - |
| CHEMBL2047247 | — | — | 1 | - |
| CHEMBL2047242 | — | — | 1 | - |
| CHEMBL2047244 | — | — | 1 | - |
| CHEMBL2047243 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2047245 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL535 | SUNITINIB | IC50 | = | 18900.0 | nM | 4.72 |
| CHEMBL2047249 | — | IC50 | = | 30100.0 | nM | 4.52 |
| CHEMBL2047251 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL2047246 | — | IC50 | = | 55700.0 | nM | 4.25 |
| CHEMBL2047252 | — | IC50 | = | 72900.0 | nM | 4.14 |
| CHEMBL2047241 | — | IC50 | = | 89300.0 | nM | 4.05 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124700.0 | nM | - |
| CHEMBL2047253 | — | IC50 | = | 197100.0 | nM | - |
| CHEMBL2047250 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047248 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047247 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047242 | — | IC50 | = | 133900.0 | nM | - |
| CHEMBL2047244 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047243 | — | IC50 | = | 171200.0 | nM | - |