Assay Detail
Binding
CHEMBL4728928
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human wild type CSF1R (I564 to S939 residues) expressed in bacterial expression system by kinome scan assay
18
Total Activities
18
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 IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 8.69 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4746711 | — | — | 1 | 9.22 |
| CHEMBL4759047 | — | — | 1 | 9.22 |
| CHEMBL4748740 | — | — | 1 | 9.00 |
| CHEMBL4741283 | — | — | 1 | 8.96 |
| CHEMBL4798876 | — | — | 1 | 8.92 |
| CHEMBL4795462 | — | — | 1 | 8.89 |
| CHEMBL4756510 | — | — | 1 | 8.72 |
| CHEMBL4763875 | — | — | 1 | 8.60 |
| CHEMBL4788945 | — | — | 1 | 8.60 |
| CHEMBL4779878 | — | — | 1 | 8.59 |
| CHEMBL4798601 | — | — | 1 | 8.47 |
| CHEMBL4227505 | SOTULETINIB | 2.0 | 1 | 8.47 |
| CHEMBL4762843 | — | — | 1 | 8.39 |
| CHEMBL4788832 | — | — | 1 | 8.17 |
| CHEMBL4751287 | — | — | 1 | 8.09 |
| CHEMBL4764974 | — | — | 1 | - |
| CHEMBL4777344 | — | — | 1 | - |
| CHEMBL4798920 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4746711 | — | Kd | = | 0.6 | nM | 9.22 |
| CHEMBL4759047 | — | Kd | = | 0.6 | nM | 9.22 |
| CHEMBL4748740 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4741283 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4798876 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL4795462 | — | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL4756510 | — | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL4763875 | — | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL4788945 | — | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL4779878 | — | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL4798601 | — | Kd | = | 3.4 | nM | 8.47 |
| CHEMBL4227505 | SOTULETINIB | Kd | = | 3.4 | nM | 8.47 |
| CHEMBL4762843 | — | Kd | = | 4.1 | nM | 8.39 |
| CHEMBL4788832 | — | Kd | = | 6.7 | nM | 8.17 |
| CHEMBL4751287 | — | Kd | = | 8.1 | nM | 8.09 |
| CHEMBL4764974 | — | Kd | - | — | - | |
| CHEMBL4777344 | — | Kd | - | — | - | |
| CHEMBL4798920 | — | Kd | - | — | - |