Assay Detail
Binding
CHEMBL2163157
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FMS-mediated proliferation in CSF1-stimulated bone marrow-derived mouse macrophages assessed as inhibition of incorporation of bromodeoxyuridine into the DNA after 30 hrs by ELISA
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL5570) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.17 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158289 | — | — | 1 | 9.19 |
| CHEMBL2158287 | — | — | 1 | 8.64 |
| CHEMBL1908842 | — | — | 1 | 8.59 |
| CHEMBL2158227 | — | — | 1 | 8.51 |
| CHEMBL2158296 | — | — | 1 | 8.51 |
| CHEMBL2158298 | — | — | 1 | 8.49 |
| CHEMBL2158230 | — | — | 1 | 8.49 |
| CHEMBL2158301 | — | — | 1 | 8.40 |
| CHEMBL2158231 | — | — | 1 | 8.36 |
| CHEMBL2158288 | — | — | 1 | 8.36 |
| CHEMBL2158225 | — | — | 1 | 8.33 |
| CHEMBL2158297 | — | — | 1 | 8.33 |
| CHEMBL2158224 | — | — | 1 | 8.31 |
| CHEMBL256712 | — | — | 1 | 8.25 |
| CHEMBL2158299 | — | — | 1 | 8.19 |
| CHEMBL2158290 | — | — | 1 | 8.17 |
| CHEMBL2158221 | — | — | 1 | 8.14 |
| CHEMBL2158291 | — | — | 1 | 8.02 |
| CHEMBL2158228 | — | — | 1 | 7.96 |
| CHEMBL2158223 | — | — | 1 | 7.96 |
| CHEMBL2158302 | — | — | 1 | 7.89 |
| CHEMBL2158295 | — | — | 1 | 7.89 |
| CHEMBL2158292 | — | — | 1 | 7.75 |
| CHEMBL2158226 | — | — | 1 | 7.68 |
| CHEMBL2158300 | — | — | 1 | 7.66 |
| CHEMBL2158294 | — | — | 1 | 7.64 |
| CHEMBL2158303 | — | — | 1 | 7.60 |
| CHEMBL2158293 | — | — | 1 | 7.31 |
| CHEMBL2158229 | — | — | 1 | - |
| CHEMBL2158222 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158289 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL2158287 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1908842 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2158227 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2158296 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2158298 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2158230 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2158301 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2158231 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2158288 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2158225 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2158297 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2158224 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL256712 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2158299 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL2158290 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2158221 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2158291 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL2158228 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2158223 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2158302 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2158295 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2158292 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2158226 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2158300 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2158294 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2158303 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2158293 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2158229 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL2158222 | — | IC50 | - | — | - |