Assay Detail
Functional
CHEMBL910169
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Inhibition of Ang1-stimulated TIE2 phosphorylation in EA.hy 926 endothelial cell line
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Endothelial cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.20 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL386637 | — | — | 1 | 8.10 |
| CHEMBL374985 | — | — | 1 | 7.66 |
| CHEMBL220532 | — | — | 1 | 7.58 |
| CHEMBL374079 | — | — | 1 | 7.48 |
| CHEMBL219103 | — | — | 1 | 7.41 |
| CHEMBL376475 | — | — | 1 | 7.08 |
| CHEMBL218110 | — | — | 1 | 7.01 |
| CHEMBL220482 | — | — | 1 | 6.60 |
| CHEMBL375617 | — | — | 1 | 5.92 |
| CHEMBL427998 | — | — | 1 | - |
| CHEMBL220750 | — | — | 1 | - |
| CHEMBL221544 | — | — | 1 | - |
| CHEMBL221193 | — | — | 1 | - |
| CHEMBL373621 | — | — | 1 | - |
| CHEMBL218631 | — | — | 1 | - |
| CHEMBL375819 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL386637 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL374985 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL220532 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL374079 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL219103 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL376475 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL218110 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL220482 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL375617 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL427998 | — | IC50 | - | — | - | |
| CHEMBL220750 | — | IC50 | - | — | - | |
| CHEMBL221544 | — | IC50 | - | — | - | |
| CHEMBL221193 | — | IC50 | - | — | - | |
| CHEMBL373621 | — | IC50 | - | — | - | |
| CHEMBL218631 | — | IC50 | - | — | - | |
| CHEMBL375819 | — | IC50 | - | — | - |