Assay Detail
Binding
CHEMBL2390017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.31 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386796 | — | — | 1 | 8.15 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.15 |
| CHEMBL2386789 | — | — | 1 | 7.92 |
| CHEMBL2386792 | — | — | 1 | 7.92 |
| CHEMBL2386794 | — | — | 1 | 7.92 |
| CHEMBL2386806 | — | — | 1 | 7.92 |
| CHEMBL2386803 | — | — | 1 | 7.75 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.70 |
| CHEMBL2386793 | — | — | 1 | 7.66 |
| CHEMBL2386812 | — | — | 1 | 7.58 |
| CHEMBL2386795 | — | — | 1 | 7.57 |
| CHEMBL2386802 | — | — | 1 | 7.55 |
| CHEMBL2386788 | — | — | 1 | 7.51 |
| CHEMBL2386818 | — | — | 1 | 7.46 |
| CHEMBL2386810 | — | — | 1 | 7.42 |
| CHEMBL2386790 | — | — | 1 | 7.42 |
| CHEMBL2386801 | — | — | 1 | 7.30 |
| CHEMBL2386808 | — | — | 1 | 7.30 |
| CHEMBL2386797 | — | — | 1 | 7.27 |
| CHEMBL2386800 | — | — | 1 | 7.15 |
| CHEMBL2386816 | — | — | 1 | 7.14 |
| CHEMBL2386798 | — | — | 1 | 7.09 |
| CHEMBL2386809 | — | — | 1 | 7.07 |
| CHEMBL2386813 | — | — | 1 | 7.00 |
| CHEMBL2386805 | — | — | 1 | 7.00 |
| CHEMBL2063324 | — | — | 1 | 6.92 |
| CHEMBL2386807 | — | — | 1 | 6.92 |
| CHEMBL1807392 | — | — | 1 | 6.89 |
| CHEMBL2386799 | — | — | 1 | 6.89 |
| CHEMBL2386817 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386796 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2386789 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2386792 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2386794 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2386806 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2386803 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2386793 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2386812 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2386795 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2386802 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2386788 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2386818 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2386790 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2386810 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2386808 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2386801 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2386797 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2386800 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2386816 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2386798 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2386809 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2386813 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2386805 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2386807 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2063324 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1807392 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2386799 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2386817 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2386814 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2105709 | QUIZARTINIB DIHYDROCHLORIDE | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2386804 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2386815 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386791 | — | IC50 | > | 1000.0 | nM | - |