Assay Detail
Binding
CHEMBL5737741
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Human c-Fms Protein Kinase Assay (gamma-33P-ATP Format): c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx. 500 cpm/pmol, concentration as required). The reaction was initiated by the addition of the MgATP mix. After incubation for 40 minutes at room temperature, the reaction was stopped by the addition of 3% phosphoric acid solution. 10 μL of the reaction was then spotted onto a P30 filtermat and washed three times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to drying and scintillation counting.
9
Total Activities
3
Compounds Tested
3
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
Substituted pyridine derivatives useful as C-FMS kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.90 | 8.00 |
| kon | 3 | - | - |
| k_off | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6027874 | — | — | 3 | 8.00 |
| CHEMBL5986778 | — | — | 3 | 7.96 |
| CHEMBL3674570 | EDICOTINIB | 2.0 | 3 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6027874 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5986778 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3674570 | EDICOTINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5986778 | — | kon | = | - | — | - |
| CHEMBL5986778 | — | k_off | = | - | s-1 | - |
| CHEMBL6027874 | — | kon | = | - | — | - |
| CHEMBL6027874 | — | k_off | = | - | s-1 | - |
| CHEMBL3674570 | EDICOTINIB | kon | = | - | — | - |
| CHEMBL3674570 | EDICOTINIB | k_off | = | - | s-1 | - |