Assay Detail
Binding
CHEMBL908503
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Inhibition of Tie2 by HTRF assay
35
Total Activities
35
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
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.34 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221484 | — | — | 1 | 9.00 |
| CHEMBL218632 | — | — | 1 | 9.00 |
| CHEMBL385956 | — | — | 1 | 8.40 |
| CHEMBL220550 | — | — | 1 | 8.40 |
| CHEMBL218646 | — | — | 1 | 8.40 |
| CHEMBL266311 | — | — | 1 | 8.22 |
| CHEMBL219158 | — | — | 1 | 8.00 |
| CHEMBL426211 | — | — | 1 | 8.00 |
| CHEMBL375793 | — | — | 1 | 7.89 |
| CHEMBL220640 | — | — | 1 | 7.66 |
| CHEMBL374997 | — | — | 1 | 7.52 |
| CHEMBL373882 | — | — | 1 | 7.52 |
| CHEMBL218576 | — | — | 1 | 7.41 |
| CHEMBL219583 | — | — | 1 | 7.40 |
| CHEMBL219996 | — | — | 1 | 7.37 |
| CHEMBL221087 | — | — | 1 | 7.28 |
| CHEMBL278965 | — | — | 1 | 7.23 |
| CHEMBL218040 | — | — | 1 | 7.21 |
| CHEMBL374259 | — | — | 1 | 7.21 |
| CHEMBL218057 | — | — | 1 | 7.17 |
| CHEMBL220540 | — | — | 1 | 7.07 |
| CHEMBL221119 | — | — | 1 | 7.00 |
| CHEMBL220549 | — | — | 1 | 6.99 |
| CHEMBL219218 | — | — | 1 | 6.97 |
| CHEMBL218425 | — | — | 1 | 6.82 |
| CHEMBL373682 | — | — | 1 | 6.74 |
| CHEMBL276395 | — | — | 1 | 6.44 |
| CHEMBL218431 | — | — | 1 | 6.41 |
| CHEMBL220052 | — | — | 1 | 6.40 |
| CHEMBL222067 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221484 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL218632 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL385956 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL220550 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL218646 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL266311 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL219158 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL426211 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL375793 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL220640 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL374997 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL373882 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL218576 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL219583 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL219996 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL221087 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL278965 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL218040 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL374259 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL218057 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL220540 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL221119 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL220549 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL219218 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL218425 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL373682 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL276395 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL218431 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL220052 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL222067 | — | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL221121 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL375447 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL375577 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL385178 | — | IC50 | >= | 25000.0 | nM | - |
| CHEMBL375792 | — | IC50 | > | 25000.0 | nM | - |