Assay Detail
Binding
CHEMBL2066305
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.79 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.15 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.70 |
| CHEMBL2063319 | — | — | 1 | 7.32 |
| CHEMBL2063321 | — | — | 1 | 7.04 |
| CHEMBL2063323 | — | — | 1 | 7.00 |
| CHEMBL2063324 | — | — | 1 | 6.92 |
| CHEMBL2063325 | — | — | 1 | 6.77 |
| CHEMBL2063318 | — | — | 1 | 6.75 |
| CHEMBL2063436 | — | — | 1 | 6.72 |
| CHEMBL2063328 | — | — | 1 | 6.66 |
| CHEMBL2063327 | — | — | 1 | 6.62 |
| CHEMBL2063338 | — | — | 1 | 6.62 |
| CHEMBL2063320 | — | — | 1 | 6.52 |
| CHEMBL2063335 | — | — | 1 | 6.51 |
| CHEMBL2063331 | — | — | 1 | 6.43 |
| CHEMBL2063326 | — | — | 1 | 6.43 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 6.37 |
| CHEMBL2063332 | — | — | 1 | 6.32 |
| CHEMBL2063322 | — | — | 1 | 6.25 |
| CHEMBL2063333 | — | — | 1 | - |
| CHEMBL2063334 | — | — | 1 | - |
| CHEMBL2063336 | — | — | 1 | - |
| CHEMBL2063337 | — | — | 1 | - |
| CHEMBL2063330 | — | — | 1 | - |
| CHEMBL2063434 | — | — | 1 | - |
| CHEMBL2063435 | — | — | 1 | - |
| CHEMBL2063329 | — | — | 1 | - |
| CHEMBL1807466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223360 | LINIFANIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2063319 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2063321 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2063323 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2063324 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2063325 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2063318 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2063436 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2063328 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2063327 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2063338 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2063320 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2063335 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2063331 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2063326 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2063332 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2063322 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL2063333 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063334 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063336 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063337 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063330 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063434 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063435 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063329 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807466 | — | IC50 | > | 1000.0 | nM | - |