Assay Detail
Binding
CHEMBL5342456
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to autoinhibited CSF1R (538 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 | 7.71 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439126 | — | — | 1 | 8.64 |
| CHEMBL5436096 | — | — | 1 | 8.21 |
| CHEMBL5436321 | — | — | 1 | 8.17 |
| CHEMBL5418087 | — | — | 1 | 8.14 |
| CHEMBL5397490 | — | — | 1 | 8.10 |
| CHEMBL5406924 | — | — | 1 | 7.58 |
| CHEMBL5440766 | — | — | 1 | 7.42 |
| CHEMBL5405639 | — | — | 1 | 7.28 |
| CHEMBL5417945 | — | — | 1 | 7.14 |
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439126 | — | Kd | = | 2.3 | nM | 8.64 |
| CHEMBL5436096 | — | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL5436321 | — | Kd | = | 6.8 | nM | 8.17 |
| CHEMBL5418087 | — | Kd | = | 7.2 | nM | 8.14 |
| CHEMBL5397490 | — | Kd | = | 7.9 | nM | 8.10 |
| CHEMBL5406924 | — | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL5440766 | — | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL5405639 | — | Kd | = | 52.0 | nM | 7.28 |
| CHEMBL5417945 | — | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL3813873 | PEXIDARTINIB | Kd | = | 360.0 | nM | 6.44 |