Assay Detail
Binding
CHEMBL4399178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST tagged VEGFR-2 expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate in presence of ATP by Kinase-Glo luminescence assay
27
Total Activities
27
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
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.47 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 8.30 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.00 |
| CHEMBL4558790 | — | — | 1 | 6.92 |
| CHEMBL4573547 | — | — | 1 | 6.77 |
| CHEMBL4574832 | — | — | 1 | 6.77 |
| CHEMBL4566054 | — | — | 1 | 6.72 |
| CHEMBL4465126 | — | — | 1 | 6.66 |
| CHEMBL4449189 | — | — | 1 | 6.58 |
| CHEMBL4590013 | — | — | 1 | 6.55 |
| CHEMBL4549103 | — | — | 1 | 6.54 |
| CHEMBL4469216 | — | — | 1 | 6.47 |
| CHEMBL4448435 | — | — | 1 | 6.39 |
| CHEMBL4474945 | — | — | 1 | 6.38 |
| CHEMBL4539297 | — | — | 1 | 6.32 |
| CHEMBL4467107 | — | — | 1 | 6.31 |
| CHEMBL4438418 | — | — | 1 | 6.24 |
| CHEMBL4474922 | — | — | 1 | 6.13 |
| CHEMBL4561629 | — | — | 1 | 6.02 |
| CHEMBL4470636 | — | — | 1 | 5.96 |
| CHEMBL4434973 | — | — | 1 | 5.84 |
| CHEMBL4570955 | — | — | 1 | 5.72 |
| CHEMBL4471650 | — | — | 1 | 5.71 |
| CHEMBL4557976 | — | — | 1 | - |
| CHEMBL4453308 | — | — | 1 | - |
| CHEMBL4450118 | — | — | 1 | - |
| CHEMBL4547466 | — | — | 1 | - |
| CHEMBL4441990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946170 | REGORAFENIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4558790 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4573547 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4574832 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4566054 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4465126 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4449189 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4590013 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4549103 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4469216 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4448435 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4474945 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4539297 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4467107 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4438418 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4474922 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4561629 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4470636 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4434973 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4570955 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4471650 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL4557976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4453308 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4450118 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4547466 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4441990 | — | IC50 | > | 10000.0 | nM | - |