Assay Detail
Binding
CHEMBL3595190
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay
17
Total Activities
17
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
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.26 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593291 | — | — | 1 | 8.15 |
| CHEMBL3593288 | — | — | 1 | 8.00 |
| CHEMBL3593287 | — | — | 1 | 7.82 |
| CHEMBL3593292 | — | — | 1 | 7.82 |
| CHEMBL3593290 | — | — | 1 | 7.60 |
| CHEMBL3593286 | — | — | 1 | 7.51 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.38 |
| CHEMBL3593285 | — | — | 1 | 7.37 |
| CHEMBL3593284 | — | — | 1 | 7.28 |
| CHEMBL3593289 | — | — | 1 | 7.26 |
| CHEMBL3593294 | — | — | 1 | 6.92 |
| CHEMBL3593283 | — | — | 1 | 6.80 |
| CHEMBL3593293 | — | — | 1 | 6.77 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.60 |
| CHEMBL3593296 | — | — | 1 | 6.43 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 6.37 |
| CHEMBL3593295 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593291 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3593288 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3593287 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3593292 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3593290 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3593286 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3593285 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3593284 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3593289 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3593294 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3593283 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3593293 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL608533 | MIDOSTAURIN | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3593296 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3593295 | — | IC50 | > | 1000.0 | nM | - |