Assay Detail
Binding
CHEMBL4012620
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay
60
Total Activities
60
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
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 5.31 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.60 |
| CHEMBL4074518 | — | — | 1 | 5.92 |
| CHEMBL4100645 | — | — | 1 | 5.91 |
| CHEMBL4103605 | — | — | 1 | 5.91 |
| CHEMBL4071997 | — | — | 1 | 5.75 |
| CHEMBL4091975 | — | — | 1 | 5.73 |
| CHEMBL4091741 | — | — | 1 | 5.73 |
| CHEMBL4065800 | — | — | 1 | 5.72 |
| CHEMBL4072731 | — | — | 1 | 5.64 |
| CHEMBL4085010 | — | — | 1 | 5.62 |
| CHEMBL4103890 | — | — | 1 | 5.51 |
| CHEMBL4079338 | — | — | 1 | 5.50 |
| CHEMBL4059958 | — | — | 1 | 5.47 |
| CHEMBL4078084 | — | — | 1 | 5.46 |
| CHEMBL4066302 | — | — | 1 | 5.43 |
| CHEMBL4087656 | — | — | 1 | 5.41 |
| CHEMBL4101428 | — | — | 1 | 5.41 |
| CHEMBL4092765 | — | — | 1 | 5.39 |
| CHEMBL4096271 | — | — | 1 | 5.39 |
| CHEMBL4062187 | — | — | 1 | 5.38 |
| CHEMBL4074713 | — | — | 1 | 5.37 |
| CHEMBL4060326 | — | — | 1 | 5.36 |
| CHEMBL4093721 | — | — | 1 | 5.34 |
| CHEMBL4083050 | — | — | 1 | 5.31 |
| CHEMBL4103897 | — | — | 1 | 5.30 |
| CHEMBL4092638 | — | — | 1 | 5.27 |
| CHEMBL4088552 | — | — | 1 | 5.25 |
| CHEMBL4104034 | — | — | 1 | 5.21 |
| CHEMBL4085974 | — | — | 1 | 5.21 |
| CHEMBL4087221 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223360 | LINIFANIB | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4074518 | — | IC50 | = | 1208.0 | nM | 5.92 |
| CHEMBL4103605 | — | IC50 | = | 1225.0 | nM | 5.91 |
| CHEMBL4100645 | — | IC50 | = | 1224.0 | nM | 5.91 |
| CHEMBL4071997 | — | IC50 | = | 1791.0 | nM | 5.75 |
| CHEMBL4091975 | — | IC50 | = | 1845.0 | nM | 5.73 |
| CHEMBL4091741 | — | IC50 | = | 1856.0 | nM | 5.73 |
| CHEMBL4065800 | — | IC50 | = | 1921.0 | nM | 5.72 |
| CHEMBL4072731 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL4085010 | — | IC50 | = | 2391.0 | nM | 5.62 |
| CHEMBL4103890 | — | IC50 | = | 3109.0 | nM | 5.51 |
| CHEMBL4079338 | — | IC50 | = | 3145.0 | nM | 5.50 |
| CHEMBL4059958 | — | IC50 | = | 3360.0 | nM | 5.47 |
| CHEMBL4078084 | — | IC50 | = | 3503.0 | nM | 5.46 |
| CHEMBL4066302 | — | IC50 | = | 3695.0 | nM | 5.43 |
| CHEMBL4087656 | — | IC50 | = | 3940.0 | nM | 5.41 |
| CHEMBL4101428 | — | IC50 | = | 3857.0 | nM | 5.41 |
| CHEMBL4092765 | — | IC50 | = | 4079.0 | nM | 5.39 |
| CHEMBL4096271 | — | IC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL4062187 | — | IC50 | = | 4164.0 | nM | 5.38 |
| CHEMBL4074713 | — | IC50 | = | 4293.0 | nM | 5.37 |
| CHEMBL4060326 | — | IC50 | = | 4322.0 | nM | 5.36 |
| CHEMBL4093721 | — | IC50 | = | 4523.0 | nM | 5.34 |
| CHEMBL4083050 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL4103897 | — | IC50 | = | 5002.0 | nM | 5.30 |
| CHEMBL4092638 | — | IC50 | = | 5352.0 | nM | 5.27 |
| CHEMBL4088552 | — | IC50 | = | 5613.0 | nM | 5.25 |
| CHEMBL4104034 | — | IC50 | = | 6235.0 | nM | 5.21 |
| CHEMBL4085974 | — | IC50 | = | 6229.0 | nM | 5.21 |
| CHEMBL4087221 | — | IC50 | = | 6235.0 | nM | 5.21 |
| CHEMBL4069008 | — | IC50 | = | 6228.0 | nM | 5.21 |
| CHEMBL4099624 | — | IC50 | = | 6816.0 | nM | 5.17 |
| CHEMBL4064941 | — | IC50 | = | 6920.0 | nM | 5.16 |
| CHEMBL4101778 | — | IC50 | = | 8008.0 | nM | 5.10 |
| CHEMBL4101438 | — | IC50 | = | 8634.0 | nM | 5.06 |
| CHEMBL4084878 | — | IC50 | = | 9046.0 | nM | 5.04 |
| CHEMBL4100492 | — | IC50 | = | 9760.0 | nM | 5.01 |
| CHEMBL4074755 | — | IC50 | = | 10462.0 | nM | 4.98 |
| CHEMBL4074745 | — | IC50 | = | 10917.0 | nM | 4.96 |
| CHEMBL4066145 | — | IC50 | = | 11382.0 | nM | 4.94 |
| CHEMBL4102831 | — | IC50 | = | 15935.0 | nM | 4.80 |
| CHEMBL4083910 | — | IC50 | = | 26163.0 | nM | 4.58 |
| CHEMBL941 | IMATINIB | IC50 | = | 27186.0 | nM | 4.57 |
| CHEMBL4100372 | — | IC50 | = | 36890.0 | nM | 4.43 |
| CHEMBL4073536 | — | IC50 | = | 41966.0 | nM | 4.38 |
| CHEMBL4063976 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4076032 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4071160 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4085962 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4096138 | — | IC50 | > | 50000.0 | nM | - |