Assay Detail
Binding
CHEMBL4728934
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Inhibition of CSF1R phosphorylation in M-CSF induced human THP1 cells incubated for 30 mins by ELISA assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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 IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.85 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748740 | — | — | 1 | 7.77 |
| CHEMBL4779878 | — | — | 1 | 7.20 |
| CHEMBL4763875 | — | — | 1 | 6.90 |
| CHEMBL4227505 | SOTULETINIB | 2.0 | 1 | 6.81 |
| CHEMBL4798601 | — | — | 1 | 6.75 |
| CHEMBL4759047 | — | — | 1 | 6.74 |
| CHEMBL4751287 | — | — | 1 | 6.72 |
| CHEMBL4762843 | — | — | 1 | 6.67 |
| CHEMBL4746711 | — | — | 1 | 6.61 |
| CHEMBL4788832 | — | — | 1 | 6.31 |
| CHEMBL4798920 | — | — | 1 | - |
| CHEMBL4777344 | — | — | 1 | - |
| CHEMBL4756510 | — | — | 1 | - |
| CHEMBL4798876 | — | — | 1 | - |
| CHEMBL4795462 | — | — | 1 | - |
| CHEMBL4741283 | — | — | 1 | - |
| CHEMBL4788945 | — | — | 1 | - |
| CHEMBL4764974 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748740 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4779878 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4763875 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4227505 | SOTULETINIB | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4798601 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4759047 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4751287 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4762843 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4746711 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4788832 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL4798920 | — | IC50 | - | — | - | |
| CHEMBL4777344 | — | IC50 | - | — | - | |
| CHEMBL4756510 | — | IC50 | - | — | - | |
| CHEMBL4798876 | — | IC50 | - | — | - | |
| CHEMBL4795462 | — | IC50 | - | — | - | |
| CHEMBL4741283 | — | IC50 | - | — | - | |
| CHEMBL4788945 | — | IC50 | - | — | - | |
| CHEMBL4764974 | — | IC50 | - | — | - |