Assay Detail
Functional
CHEMBL2353611
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against VEGF-stimulated HUVECs after 5 days by WST-8 assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HUVEC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.03 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | 9.52 |
| CHEMBL2348991 | — | — | 1 | 9.25 |
| CHEMBL2348996 | — | — | 1 | 8.77 |
| CHEMBL2348990 | — | — | 1 | 8.52 |
| CHEMBL2348989 | — | — | 1 | 8.04 |
| CHEMBL2348994 | — | — | 1 | 7.96 |
| CHEMBL2348992 | — | — | 1 | 7.03 |
| CHEMBL2348993 | — | — | 1 | 7.01 |
| CHEMBL2206666 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180604 | TAK-593 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2348991 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL2348996 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2348990 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2348989 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL2348994 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2348992 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2348993 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL2206666 | — | IC50 | = | 650.0 | nM | 6.19 |