Assay Detail
Binding
CHEMBL5342457
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to non-autoinhibited CSF1R (564 to 939) (unknown origin) expressed in Escherichia coli BL21 strain assessed as dissociation constant incubated for 1 hr under shaking condition by qPCR method
10
Total Activities
10
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
Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 10 | 6.93 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 8.24 |
| CHEMBL5440766 | — | — | 1 | 7.28 |
| CHEMBL5418087 | — | — | 1 | 6.89 |
| CHEMBL5439126 | — | — | 1 | 6.77 |
| CHEMBL5406924 | — | — | 1 | 6.50 |
| CHEMBL5436321 | — | — | 1 | 6.47 |
| CHEMBL5436096 | — | — | 1 | 6.39 |
| CHEMBL5405639 | — | — | 1 | - |
| CHEMBL5417945 | — | — | 1 | - |
| CHEMBL5397490 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3813873 | PEXIDARTINIB | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL5440766 | — | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL5418087 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL5439126 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL5406924 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL5436321 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL5436096 | — | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL5405639 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL5417945 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL5397490 | — | Kd | > | 1000.0 | nM | - |