Assay Detail
Functional
CHEMBL673902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGF-stimulated mitogenesis in endothelial cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | Endothelial cell |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor (CHEMBL2095227) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.25 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333021 | L-21649 | 1.0 | 1 | 7.75 |
| CHEMBL118400 | — | — | 1 | 7.70 |
| CHEMBL324335 | — | — | 1 | 7.66 |
| CHEMBL445062 | — | — | 1 | 7.64 |
| CHEMBL117166 | — | — | 1 | 7.54 |
| CHEMBL324153 | — | — | 1 | 7.51 |
| CHEMBL331465 | — | — | 1 | 7.50 |
| CHEMBL115480 | — | — | 1 | 7.16 |
| CHEMBL116324 | — | — | 1 | 7.10 |
| CHEMBL329350 | — | — | 1 | 6.82 |
| CHEMBL92461 | — | — | 1 | 6.41 |
| CHEMBL92279 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333021 | L-21649 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL118400 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL324335 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL445062 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL117166 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL324153 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL331465 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL115480 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL116324 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL329350 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL92461 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL92279 | — | IC50 | = | 622.0 | nM | 6.21 |