Assay Detail
Binding
CHEMBL924759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST tagged VEGFR2 expressed in Sf9 cells
28
Total Activities
28
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 of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.15 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254964 | — | — | 1 | 8.05 |
| CHEMBL254760 | — | — | 1 | 8.00 |
| CHEMBL258240 | — | — | 1 | 8.00 |
| CHEMBL258453 | — | — | 1 | 7.96 |
| CHEMBL402550 | — | — | 1 | 7.77 |
| CHEMBL404639 | — | — | 1 | 7.77 |
| CHEMBL402036 | — | — | 1 | 7.72 |
| CHEMBL402792 | — | — | 1 | 7.60 |
| CHEMBL404495 | — | — | 1 | 7.60 |
| CHEMBL258396 | — | — | 1 | 7.55 |
| CHEMBL258185 | — | — | 1 | 7.51 |
| CHEMBL404881 | — | — | 1 | 7.50 |
| CHEMBL402004 | — | — | 1 | 7.50 |
| CHEMBL256972 | — | — | 1 | 7.05 |
| CHEMBL256767 | — | — | 1 | 7.03 |
| CHEMBL402042 | — | — | 1 | 6.95 |
| CHEMBL257546 | — | — | 1 | 6.90 |
| CHEMBL256974 | — | — | 1 | 6.89 |
| CHEMBL438877 | — | — | 1 | 6.88 |
| CHEMBL257987 | — | — | 1 | 6.84 |
| CHEMBL256786 | — | — | 1 | 6.76 |
| CHEMBL401838 | — | — | 1 | 6.54 |
| CHEMBL256920 | — | — | 1 | 6.46 |
| CHEMBL254761 | — | — | 1 | 6.46 |
| CHEMBL402504 | — | — | 1 | 6.41 |
| CHEMBL256715 | — | — | 1 | 6.25 |
| CHEMBL403747 | — | — | 1 | 6.23 |
| CHEMBL257802 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254964 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL254760 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL258240 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL258453 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL402550 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL404639 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL402036 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL402792 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL404495 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL258396 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL258185 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL404881 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL402004 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL256972 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL256767 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL402042 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL257546 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL256974 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL438877 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL257987 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL256786 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL401838 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL256920 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL254761 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL402504 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL256715 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL403747 | — | IC50 | = | 593.0 | nM | 6.23 |
| CHEMBL257802 | — | IC50 | = | 1134.0 | nM | 5.95 |