Assay Detail
Binding
CHEMBL910166
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Inhibition of TIE2 by HTRF assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 23 | 7.66 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385937 | — | — | 1 | 9.00 |
| CHEMBL375840 | — | — | 1 | 8.70 |
| CHEMBL427998 | — | — | 1 | 8.52 |
| CHEMBL220874 | — | — | 1 | 8.52 |
| CHEMBL386637 | — | — | 1 | 8.30 |
| CHEMBL373621 | — | — | 1 | 8.10 |
| CHEMBL219584 | — | — | 1 | 8.00 |
| CHEMBL375819 | — | — | 1 | 7.96 |
| CHEMBL374079 | — | — | 1 | 7.89 |
| CHEMBL376475 | — | — | 1 | 7.89 |
| CHEMBL220532 | — | — | 1 | 7.85 |
| CHEMBL374985 | — | — | 1 | 7.77 |
| CHEMBL375617 | — | — | 1 | 7.68 |
| CHEMBL219103 | — | — | 1 | 7.52 |
| CHEMBL218110 | — | — | 1 | 7.36 |
| CHEMBL218631 | — | — | 1 | 7.33 |
| CHEMBL220482 | — | — | 1 | 7.20 |
| CHEMBL221019 | — | — | 1 | 7.07 |
| CHEMBL220750 | — | — | 1 | 6.85 |
| CHEMBL221544 | — | — | 1 | 6.66 |
| CHEMBL221193 | — | — | 1 | 6.21 |
| CHEMBL450024 | — | — | 1 | 6.21 |
| CHEMBL218632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385937 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL375840 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL427998 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL220874 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL386637 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL373621 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL219584 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL375819 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL374079 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL376475 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL220532 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL374985 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL375617 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL219103 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL218110 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL218631 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL220482 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL221019 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL220750 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL221544 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL221193 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL450024 | — | IC50 | = | 623.0 | nM | 6.21 |
| CHEMBL218632 | — | IC50 | < | 1.0 | nM | - |