Assay Detail
Binding
CHEMBL4396022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged VEGFR2 cytoplasmic domain (790 to 1356 residues) expressed in baculovirus expression system using Ulight-JAK-1(Tyr1023) peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by spectrometric method
13
Total Activities
13
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 Dioxino[2,3-f]quinazoline derivative VEGFR-2 inhibitors exerting significant antipro-liferative activity in HUVECs and mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.34 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 9.15 |
| CHEMBL4455006 | — | — | 1 | 9.00 |
| CHEMBL4466426 | — | — | 1 | 8.82 |
| CHEMBL4449250 | — | — | 1 | 8.82 |
| CHEMBL4528373 | — | — | 1 | 8.77 |
| CHEMBL4514617 | — | — | 1 | 8.62 |
| CHEMBL4581503 | — | — | 1 | 8.62 |
| CHEMBL4516513 | — | — | 1 | 8.47 |
| CHEMBL4531859 | — | — | 1 | 8.40 |
| CHEMBL4435366 | — | — | 1 | 8.38 |
| CHEMBL4472616 | — | — | 1 | 7.95 |
| CHEMBL4470543 | — | — | 1 | 7.51 |
| CHEMBL4461971 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289601 | LENVATINIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4455006 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4466426 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4449250 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4528373 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4514617 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4581503 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4516513 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4531859 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4435366 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4472616 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4470543 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4461971 | — | IC50 | = | 1081.0 | nM | 5.97 |