Assay Detail
Binding
CHEMBL951933
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Inhibition of KDR by HTRF assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.04 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385937 | — | — | 1 | 8.70 |
| CHEMBL408070 | — | — | 1 | 8.30 |
| CHEMBL429582 | — | — | 1 | 8.22 |
| CHEMBL271154 | — | — | 1 | 7.89 |
| CHEMBL407063 | — | — | 1 | 7.77 |
| CHEMBL272888 | — | — | 1 | 7.62 |
| CHEMBL405401 | — | — | 1 | 7.50 |
| CHEMBL405666 | — | — | 1 | 7.39 |
| CHEMBL271140 | — | — | 1 | 7.27 |
| CHEMBL272850 | — | — | 1 | 6.92 |
| CHEMBL411632 | — | — | 1 | 6.90 |
| CHEMBL409914 | — | — | 1 | 6.77 |
| CHEMBL272902 | — | — | 1 | 6.69 |
| CHEMBL271141 | — | — | 1 | 6.57 |
| CHEMBL271375 | — | — | 1 | 6.23 |
| CHEMBL271760 | — | — | 1 | 6.02 |
| CHEMBL409734 | — | — | 1 | 5.95 |
| CHEMBL438016 | — | — | 1 | 5.59 |
| CHEMBL411050 | — | — | 1 | 5.42 |
| CHEMBL259247 | — | — | 1 | - |
| CHEMBL259465 | — | — | 1 | - |
| CHEMBL272673 | — | — | 1 | - |
| CHEMBL271372 | — | — | 1 | - |
| CHEMBL271201 | — | — | 1 | - |
| CHEMBL270765 | — | — | 1 | - |
| CHEMBL541726 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385937 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL408070 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL429582 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL271154 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL407063 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL272888 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL405401 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL405666 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL271140 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL272850 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL411632 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL409914 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL272902 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL271141 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL271375 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL271760 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL409734 | — | IC50 | = | 1123.0 | nM | 5.95 |
| CHEMBL438016 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL411050 | — | IC50 | = | 3784.0 | nM | 5.42 |
| CHEMBL259247 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL259465 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL272673 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL271372 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL271201 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL270765 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL541726 | — | IC50 | > | 25000.0 | nM | - |