Assay Detail
Binding
CHEMBL910167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDR
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 |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.18 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219584 | — | — | 1 | 9.00 |
| CHEMBL220874 | — | — | 1 | 9.00 |
| CHEMBL427998 | — | — | 1 | 8.70 |
| CHEMBL385937 | — | — | 1 | 8.70 |
| CHEMBL218632 | — | — | 1 | 8.52 |
| CHEMBL221019 | — | — | 1 | 8.40 |
| CHEMBL218631 | — | — | 1 | 8.22 |
| CHEMBL373621 | — | — | 1 | 7.96 |
| CHEMBL450024 | — | — | 1 | 6.77 |
| CHEMBL221193 | — | — | 1 | 6.77 |
| CHEMBL375617 | — | — | 1 | 6.41 |
| CHEMBL374985 | — | — | 1 | 6.32 |
| CHEMBL374079 | — | — | 1 | 6.10 |
| CHEMBL218110 | — | — | 1 | 6.09 |
| CHEMBL221544 | — | — | 1 | 6.05 |
| CHEMBL220532 | — | — | 1 | 6.00 |
| CHEMBL386637 | — | — | 1 | 5.99 |
| CHEMBL376475 | — | — | 1 | 5.96 |
| CHEMBL220750 | — | — | 1 | 5.52 |
| CHEMBL220482 | — | — | 1 | - |
| CHEMBL219103 | — | — | 1 | - |
| CHEMBL375819 | — | — | 1 | - |
| CHEMBL375840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219584 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL220874 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL427998 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL385937 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL218632 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL221019 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL218631 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL373621 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL450024 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL221193 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL375617 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL374985 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL374079 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL218110 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL221544 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL220532 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL386637 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL376475 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL220750 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL220482 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL219103 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL375819 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL375840 | — | IC50 | < | 1.0 | nM | - |