Assay Detail
Binding
CHEMBL1810161
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Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.84 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.52 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.30 |
| CHEMBL1807469 | — | — | 1 | 7.16 |
| CHEMBL1807392 | — | — | 1 | 6.89 |
| CHEMBL1807786 | — | — | 1 | 6.85 |
| CHEMBL1807471 | — | — | 1 | 6.80 |
| CHEMBL1807478 | — | — | 1 | 6.70 |
| CHEMBL1807467 | — | — | 1 | 6.60 |
| CHEMBL1807483 | — | — | 1 | 6.54 |
| CHEMBL1807475 | — | — | 1 | 6.39 |
| CHEMBL1807477 | — | — | 1 | 6.35 |
| CHEMBL1807480 | — | — | 1 | 6.25 |
| CHEMBL1807473 | — | — | 1 | 5.57 |
| CHEMBL1807476 | — | — | 1 | - |
| CHEMBL1807479 | — | — | 1 | - |
| CHEMBL1807484 | — | — | 1 | - |
| CHEMBL1807485 | — | — | 1 | - |
| CHEMBL1807785 | — | — | 1 | - |
| CHEMBL1807474 | — | — | 1 | - |
| CHEMBL1807788 | — | — | 1 | - |
| CHEMBL1807472 | — | — | 1 | - |
| CHEMBL1807470 | — | — | 1 | - |
| CHEMBL1807468 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1336 | SORAFENIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1807469 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1807392 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1807786 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1807471 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1807478 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1807467 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1807483 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1807475 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1807477 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1807480 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1807473 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL1807476 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807479 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807484 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1807485 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1807785 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1807474 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807788 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1807472 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807470 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807468 | — | IC50 | > | 1000.0 | nM | - |