Assay Detail
Binding
CHEMBL2163155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FMS mediated phosphorylation using SYEGNSYTFIDPTQ as substrate after 80 mins by fluorescence polarization
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 39 | 8.68 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL438533 | — | — | 1 | 9.52 |
| CHEMBL2158300 | — | — | 1 | 9.21 |
| CHEMBL1908842 | — | — | 1 | 9.16 |
| CHEMBL2158302 | — | — | 1 | 9.15 |
| CHEMBL398509 | — | — | 1 | 9.10 |
| CHEMBL254702 | — | — | 1 | 9.10 |
| CHEMBL2158288 | — | — | 1 | 9.08 |
| CHEMBL252436 | — | — | 1 | 9.00 |
| CHEMBL2158289 | — | — | 1 | 9.00 |
| CHEMBL2158221 | — | — | 1 | 8.96 |
| CHEMBL2158293 | — | — | 1 | 8.96 |
| CHEMBL2158230 | — | — | 1 | 8.96 |
| CHEMBL2158225 | — | — | 1 | 8.96 |
| CHEMBL2158287 | — | — | 1 | 8.92 |
| CHEMBL2158229 | — | — | 1 | 8.89 |
| CHEMBL2158292 | — | — | 1 | 8.89 |
| CHEMBL2158297 | — | — | 1 | 8.89 |
| CHEMBL2158301 | — | — | 1 | 8.89 |
| CHEMBL2158291 | — | — | 1 | 8.85 |
| CHEMBL2158228 | — | — | 1 | 8.85 |
| CHEMBL2158227 | — | — | 1 | 8.82 |
| CHEMBL2158294 | — | — | 1 | 8.80 |
| CHEMBL2158226 | — | — | 1 | 8.80 |
| CHEMBL2158296 | — | — | 1 | 8.77 |
| CHEMBL2158298 | — | — | 1 | 8.77 |
| CHEMBL2158223 | — | — | 1 | 8.74 |
| CHEMBL399763 | — | — | 1 | 8.70 |
| CHEMBL256712 | — | — | 1 | 8.62 |
| CHEMBL2158224 | — | — | 1 | 8.62 |
| CHEMBL2158295 | — | — | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL438533 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2158300 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL1908842 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL2158302 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL398509 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL254702 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2158288 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL252436 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2158289 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2158293 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2158225 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2158230 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2158221 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2158287 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2158301 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2158229 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2158297 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2158292 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2158228 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2158291 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2158227 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2158294 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2158226 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2158296 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2158298 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2158223 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL399763 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL256712 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2158224 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2158295 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2158290 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2158231 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2158303 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2158299 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL265432 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2158222 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL400754 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL428056 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL253864 | — | IC50 | = | 400.0 | nM | 6.40 |