Assay Detail
Binding
CHEMBL908504
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Inhibition of KDR 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 |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.79 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221484 | — | — | 1 | 8.70 |
| CHEMBL218632 | — | — | 1 | 8.52 |
| CHEMBL385956 | — | — | 1 | 8.40 |
| CHEMBL385178 | — | — | 1 | 7.42 |
| CHEMBL220540 | — | — | 1 | 7.42 |
| CHEMBL218646 | — | — | 1 | 7.34 |
| CHEMBL219996 | — | — | 1 | 7.24 |
| CHEMBL218425 | — | — | 1 | 7.23 |
| CHEMBL220550 | — | — | 1 | 7.16 |
| CHEMBL426211 | — | — | 1 | 7.01 |
| CHEMBL220549 | — | — | 1 | 7.00 |
| CHEMBL222067 | — | — | 1 | 6.75 |
| CHEMBL219158 | — | — | 1 | 6.51 |
| CHEMBL221121 | — | — | 1 | 6.36 |
| CHEMBL218576 | — | — | 1 | 6.34 |
| CHEMBL374997 | — | — | 1 | 6.17 |
| CHEMBL375447 | — | — | 1 | 6.15 |
| CHEMBL276395 | — | — | 1 | 5.89 |
| CHEMBL374259 | — | — | 1 | 5.70 |
| CHEMBL218431 | — | — | 1 | 5.58 |
| CHEMBL278965 | — | — | 1 | 5.40 |
| CHEMBL373882 | — | — | 1 | 5.11 |
| CHEMBL373682 | — | — | 1 | - |
| CHEMBL218057 | — | — | 1 | - |
| CHEMBL218040 | — | — | 1 | - |
| CHEMBL220052 | — | — | 1 | - |
| CHEMBL220640 | — | — | 1 | - |
| CHEMBL375577 | — | — | 1 | - |
| CHEMBL375792 | — | — | 1 | - |
| CHEMBL221119 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221484 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL218632 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL385956 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL385178 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL220540 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL218646 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL219996 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL218425 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL220550 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL426211 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL220549 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL222067 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL219158 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL221121 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL218576 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL374997 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL375447 | — | IC50 | = | 705.0 | nM | 6.15 |
| CHEMBL276395 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL374259 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL218431 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL278965 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL373882 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL266311 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL221087 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL375793 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL219218 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL219583 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL221119 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL375792 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL375577 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL220640 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL220052 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL218040 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL218057 | — | IC50 | >= | 5000.0 | nM | - |
| CHEMBL373682 | — | IC50 | > | 25000.0 | nM | - |