Assay Detail
Binding
CHEMBL5545073
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CSF1R using pEY as substrate incubated for 40 mins in presence of [gamma33P]-ATP by scintillation counting
32
Total Activities
31
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 | 32 | 6.68 | 8.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.98 |
| CHEMBL3674570 | EDICOTINIB | 2.0 | 1 | 8.49 |
| CHEMBL3616960 | — | — | 2 | 8.00 |
| CHEMBL5575602 | — | — | 1 | 7.51 |
| CHEMBL5569009 | — | — | 1 | 7.48 |
| CHEMBL5574298 | — | — | 1 | 7.19 |
| CHEMBL5563281 | — | — | 1 | 7.11 |
| CHEMBL5565301 | — | — | 1 | 7.00 |
| CHEMBL5575718 | — | — | 1 | 6.80 |
| CHEMBL5573382 | — | — | 1 | 6.53 |
| CHEMBL5568849 | — | — | 1 | 6.40 |
| CHEMBL5592971 | — | — | 1 | 6.40 |
| CHEMBL5569937 | — | — | 1 | 6.33 |
| CHEMBL5568734 | — | — | 1 | 6.33 |
| CHEMBL5592536 | — | — | 1 | 6.25 |
| CHEMBL5571252 | — | — | 1 | 5.70 |
| CHEMBL5573143 | — | — | 1 | 5.63 |
| CHEMBL5571428 | — | — | 1 | 5.28 |
| CHEMBL5592472 | — | — | 1 | 5.22 |
| CHEMBL5563640 | — | — | 1 | 5.18 |
| CHEMBL5570222 | — | — | 1 | 5.08 |
| CHEMBL5575524 | — | — | 1 | - |
| CHEMBL5591424 | — | — | 1 | - |
| CHEMBL5571628 | — | — | 1 | - |
| CHEMBL5571676 | — | — | 1 | - |
| CHEMBL5570301 | — | — | 1 | - |
| CHEMBL5575472 | — | — | 1 | - |
| CHEMBL5568796 | — | — | 1 | - |
| CHEMBL5590723 | — | — | 1 | - |
| CHEMBL5572366 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL3674570 | EDICOTINIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3616960 | — | IC50 | = | 9.95 | nM | 8.00 |
| CHEMBL3616960 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL5575602 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5569009 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5574298 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5563281 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5565301 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5575718 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5573382 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL5592971 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL5568849 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL5569937 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL5568734 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL5592536 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL5571252 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL5573143 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL5571428 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5592472 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL5563640 | — | IC50 | = | 6590.0 | nM | 5.18 |
| CHEMBL5570222 | — | IC50 | = | 8340.0 | nM | 5.08 |
| CHEMBL5571628 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5591424 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5575524 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5571676 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5570301 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5568796 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5590723 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5572366 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5592954 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5575472 | — | IC50 | > | 10000.0 | nM | - |