Assay Detail
Functional
CHEMBL884695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cellular inhibition of VEGF induced human KDR phosphorylation in 3T3 murine fibroblasts
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.80 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196363 | — | — | 1 | 9.00 |
| CHEMBL371510 | — | — | 1 | 8.70 |
| CHEMBL382979 | — | — | 1 | 8.05 |
| CHEMBL197592 | — | — | 1 | 8.00 |
| CHEMBL370325 | — | — | 1 | 8.00 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.66 |
| CHEMBL197828 | — | — | 1 | 7.64 |
| CHEMBL382517 | — | — | 1 | 7.55 |
| CHEMBL381207 | — | — | 1 | 7.18 |
| CHEMBL199031 | — | — | 1 | 6.23 |
| CHEMBL371329 | — | — | 1 | - |
| CHEMBL372744 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196363 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL371510 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL382979 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL197592 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL370325 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL535 | SUNITINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL197828 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL382517 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL381207 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL199031 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL371329 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL372744 | — | IC50 | < | 10.0 | nM | - |