Assay Detail
Binding
CHEMBL677134
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Flt-kinase
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.43 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL78303 | — | — | 1 | 7.40 |
| CHEMBL74587 | — | — | 1 | 7.22 |
| CHEMBL74850 | — | — | 1 | 7.22 |
| CHEMBL75196 | — | — | 1 | 7.16 |
| CHEMBL74391 | — | — | 1 | 7.16 |
| CHEMBL75232 | — | — | 1 | 7.11 |
| CHEMBL306295 | — | — | 1 | 7.10 |
| CHEMBL74197 | — | — | 1 | 6.82 |
| CHEMBL74550 | — | — | 1 | 6.64 |
| CHEMBL309331 | — | — | 1 | 6.64 |
| CHEMBL75077 | — | — | 1 | 6.62 |
| CHEMBL431006 | — | — | 1 | 6.62 |
| CHEMBL306707 | — | — | 1 | 6.58 |
| CHEMBL75034 | — | — | 1 | 6.58 |
| CHEMBL75462 | — | — | 1 | 6.48 |
| CHEMBL74646 | — | — | 1 | 6.46 |
| CHEMBL78160 | — | — | 1 | 6.38 |
| CHEMBL433321 | — | — | 1 | 6.33 |
| CHEMBL77555 | — | — | 1 | 6.22 |
| CHEMBL77933 | — | — | 1 | 6.22 |
| CHEMBL312526 | — | — | 1 | 6.21 |
| CHEMBL74143 | — | — | 1 | 6.19 |
| CHEMBL419458 | — | — | 1 | 6.12 |
| CHEMBL306284 | — | — | 1 | 5.77 |
| CHEMBL307476 | — | — | 1 | 5.64 |
| CHEMBL74034 | — | — | 1 | 5.58 |
| CHEMBL306512 | — | — | 1 | 5.52 |
| CHEMBL75076 | — | — | 1 | 5.44 |
| CHEMBL74848 | — | — | 1 | 5.01 |
| CHEMBL75130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL78303 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL74587 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL74850 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL75196 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL74391 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL75232 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL306295 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL74197 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL74550 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL309331 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL75077 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL431006 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL306707 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL75034 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL75462 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL74646 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL78160 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL433321 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL77555 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL77933 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL312526 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL74143 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL419458 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL306284 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL307476 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL74034 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL306512 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL75076 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL74848 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL75130 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL312789 | — | IC50 | > | 10000.0 | nM | - |