Assay Detail
Binding
CHEMBL1959284
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Inhibition of VEGF-induced VEGFR2 autophosphorylation in human U251 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA
12
Total Activities
12
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
N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.67 | 5.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 5.61 |
| CHEMBL1956895 | — | — | 1 | 4.83 |
| CHEMBL1956890 | — | — | 1 | 4.75 |
| CHEMBL1956897 | — | — | 1 | 4.64 |
| CHEMBL1956896 | — | — | 1 | 4.64 |
| CHEMBL1956888 | — | — | 1 | 4.62 |
| CHEMBL1956898 | — | — | 1 | 4.59 |
| CHEMBL1956894 | — | — | 1 | 4.19 |
| CHEMBL1956891 | — | — | 1 | 4.18 |
| CHEMBL1956893 | — | — | 1 | - |
| CHEMBL1956892 | — | — | 1 | - |
| CHEMBL1956889 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL1956895 | — | IC50 | = | 14900.0 | nM | 4.83 |
| CHEMBL1956890 | — | IC50 | = | 17900.0 | nM | 4.75 |
| CHEMBL1956897 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL1956896 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL1956888 | — | IC50 | = | 23800.0 | nM | 4.62 |
| CHEMBL1956898 | — | IC50 | = | 25700.0 | nM | 4.59 |
| CHEMBL1956894 | — | IC50 | = | 64500.0 | nM | 4.19 |
| CHEMBL1956891 | — | IC50 | = | 65300.0 | nM | 4.18 |
| CHEMBL1956893 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1956892 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1956889 | — | IC50 | = | 113400.0 | nM | - |