Assay Detail
Binding
CHEMBL818936
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Vascular endothelial growth factor receptor 2
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
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 | 14 | 7.85 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333021 | L-21649 | 1.0 | 1 | 8.52 |
| CHEMBL324335 | — | — | 1 | 8.40 |
| CHEMBL118400 | — | — | 1 | 8.15 |
| CHEMBL331465 | — | — | 1 | 8.05 |
| CHEMBL445062 | — | — | 1 | 8.00 |
| CHEMBL324153 | — | — | 1 | 7.96 |
| CHEMBL116324 | — | — | 1 | 7.89 |
| CHEMBL118386 | — | — | 1 | 7.85 |
| CHEMBL115480 | — | — | 1 | 7.85 |
| CHEMBL92461 | — | — | 1 | 7.72 |
| CHEMBL333640 | — | — | 1 | 7.72 |
| CHEMBL117166 | — | — | 1 | 7.70 |
| CHEMBL329350 | — | — | 1 | 7.43 |
| CHEMBL92279 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333021 | L-21649 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL324335 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL118400 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL331465 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL445062 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL324153 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL116324 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL118386 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL115480 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL92461 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL333640 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL117166 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL329350 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL92279 | — | IC50 | = | 224.0 | nM | 6.65 |