Assay Detail
Binding
CHEMBL902486
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Inhibition of human VEGFR2 by HTRF method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.10 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273564 | GW795493X | — | 1 | 8.15 |
| CHEMBL247228 | GW770249X | — | 1 | 8.11 |
| CHEMBL194911 | — | — | 1 | 7.81 |
| CHEMBL436806 | — | — | 1 | 7.62 |
| CHEMBL396107 | GW795486X | — | 1 | 6.86 |
| CHEMBL437369 | — | — | 1 | 6.73 |
| CHEMBL391184 | — | — | 1 | 6.48 |
| CHEMBL247252 | — | — | 1 | 6.35 |
| CHEMBL247790 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273564 | GW795493X | IC50 | = | 7.079 | nM | 8.15 |
| CHEMBL247228 | GW770249X | IC50 | = | 7.762 | nM | 8.11 |
| CHEMBL194911 | — | IC50 | = | 15.49 | nM | 7.81 |
| CHEMBL436806 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL396107 | GW795486X | IC50 | = | 138.04 | nM | 6.86 |
| CHEMBL437369 | — | IC50 | = | 186.21 | nM | 6.73 |
| CHEMBL391184 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL247252 | — | IC50 | = | 446.68 | nM | 6.35 |
| CHEMBL247790 | — | IC50 | = | 1737.8 | nM | 5.76 |