Assay Detail
Binding
CHEMBL5323100
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Inhibition of CSF1-induced CSF1R signalling in mouse BMDM cells assessed as reduction in ERK1/2 phosphorylation preincubated for 30 mins followed by CSF1 addition and measured after 10 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | BMDM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL5570) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
A highly selective purine-based inhibitor of CSF1R potently inhibits osteoclast differentiation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.99 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5407395 | — | — | 1 | 7.40 |
| CHEMBL5404686 | — | — | 1 | 7.08 |
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 7.00 |
| CHEMBL5431736 | — | — | 1 | 7.00 |
| CHEMBL5415149 | — | — | 1 | 6.97 |
| CHEMBL5413223 | — | — | 1 | 6.48 |
| CHEMBL5406229 | — | — | 1 | - |
| CHEMBL5401076 | — | — | 1 | - |
| CHEMBL5417420 | — | — | 1 | - |
| CHEMBL5416633 | — | — | 1 | - |
| CHEMBL5424810 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5407395 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5404686 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3813873 | PEXIDARTINIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5431736 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5415149 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5413223 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5406229 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL5401076 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL5417420 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL5416633 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL5424810 | — | IC50 | > | 300.0 | nM | - |