Assay Detail
Binding
CHEMBL769328
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Inhibition of Proto-oncogene tyrosine-kinase c-Kit
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
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| 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 | 14 | 5.77 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 6.40 |
| CHEMBL75232 | — | — | 1 | 6.16 |
| CHEMBL75196 | — | — | 1 | 6.16 |
| CHEMBL431006 | — | — | 1 | 6.00 |
| CHEMBL309331 | — | — | 1 | 5.85 |
| CHEMBL74197 | — | — | 1 | 5.70 |
| CHEMBL78303 | — | — | 1 | 5.60 |
| CHEMBL77555 | — | — | 1 | 5.57 |
| CHEMBL75462 | — | — | 1 | 5.52 |
| CHEMBL75034 | — | — | 1 | 5.46 |
| CHEMBL306295 | — | — | 1 | 5.10 |
| CHEMBL74587 | — | — | 1 | - |
| CHEMBL77933 | — | — | 1 | - |
| CHEMBL74646 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276711 | SEMAXANIB | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL75232 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL75196 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL431006 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL309331 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL74197 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL78303 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL77555 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL75462 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL75034 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL306295 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL74587 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL77933 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL74646 | — | IC50 | > | 10000.0 | nM | - |