Assay Detail
Binding
CHEMBL902485
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Inhibition of human Tie2 by HTRF method
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 8 | 6.98 | 7.99 |
| Log IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273564 | GW795493X | — | 1 | 7.99 |
| CHEMBL247228 | GW770249X | — | 1 | 7.87 |
| CHEMBL436806 | — | — | 1 | 7.09 |
| CHEMBL247252 | — | — | 1 | 6.74 |
| CHEMBL437369 | — | — | 1 | 6.69 |
| CHEMBL391184 | — | — | 1 | 6.65 |
| CHEMBL396107 | GW795486X | — | 1 | 6.42 |
| CHEMBL247790 | — | — | 1 | 6.39 |
| CHEMBL194911 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273564 | GW795493X | IC50 | = | 10.23 | nM | 7.99 |
| CHEMBL247228 | GW770249X | IC50 | = | 13.49 | nM | 7.87 |
| CHEMBL436806 | — | IC50 | = | 81.28 | nM | 7.09 |
| CHEMBL247252 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL437369 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL391184 | — | IC50 | = | 223.87 | nM | 6.65 |
| CHEMBL396107 | GW795486X | IC50 | = | 380.19 | nM | 6.42 |
| CHEMBL247790 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL194911 | — | Log IC50 | - | — | - |