Assay Detail
Binding
CHEMBL1959285
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Inhibition of VEGF-induced VEGFR1 autophosphorylation in human A498 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 | A498 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| 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 | 4.29 | 4.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL150315 | — | — | 1 | 4.75 |
| CHEMBL1956896 | — | — | 1 | 4.29 |
| CHEMBL1956891 | — | — | 1 | 4.10 |
| CHEMBL1956888 | — | — | 1 | 4.00 |
| CHEMBL1956897 | — | — | 1 | - |
| CHEMBL1956892 | — | — | 1 | - |
| CHEMBL1956898 | — | — | 1 | - |
| CHEMBL1956895 | — | — | 1 | - |
| CHEMBL1956893 | — | — | 1 | - |
| CHEMBL1956889 | — | — | 1 | - |
| CHEMBL1956890 | — | — | 1 | - |
| CHEMBL1956894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL150315 | — | IC50 | = | 17700.0 | nM | 4.75 |
| CHEMBL1956896 | — | IC50 | = | 50800.0 | nM | 4.29 |
| CHEMBL1956891 | — | IC50 | = | 79900.0 | nM | 4.10 |
| CHEMBL1956888 | — | IC50 | = | 99300.0 | nM | 4.00 |
| CHEMBL1956897 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1956892 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1956898 | — | IC50 | = | 156500.0 | nM | - |
| CHEMBL1956895 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL1956893 | — | IC50 | = | 138100.0 | nM | - |
| CHEMBL1956889 | — | IC50 | = | 129300.0 | nM | - |
| CHEMBL1956890 | — | IC50 | = | 126300.0 | nM | - |
| CHEMBL1956894 | — | IC50 | = | 118600.0 | nM | - |