Assay Detail
Binding
CHEMBL5545071
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Inhibition of CSF-1R (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.53 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227505 | SOTULETINIB | 2.0 | 1 | 9.00 |
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 7.77 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227505 | SOTULETINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3813873 | PEXIDARTINIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1908391 | MASITINIB | IC50 | = | 1480.0 | nM | 5.83 |