Assay Detail
Binding
CHEMBL749475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against NK1 receptor by displacement of [3H]SP from bovine retina membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Retina |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.43 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL103851 | — | — | 1 | 8.52 |
| CHEMBL103510 | — | — | 1 | 8.15 |
| CHEMBL105560 | — | — | 1 | 8.05 |
| CHEMBL419352 | — | — | 1 | 7.96 |
| CHEMBL290364 | — | — | 1 | 7.92 |
| CHEMBL102569 | — | — | 1 | 7.89 |
| CHEMBL319700 | — | — | 1 | 7.85 |
| CHEMBL105201 | — | — | 1 | 7.85 |
| CHEMBL103221 | — | — | 1 | 7.68 |
| CHEMBL321710 | — | — | 1 | 7.57 |
| CHEMBL323317 | — | — | 1 | 7.54 |
| CHEMBL102887 | — | — | 1 | 7.28 |
| CHEMBL101288 | — | — | 1 | 7.00 |
| CHEMBL105631 | — | — | 1 | 6.72 |
| CHEMBL101420 | — | — | 1 | 6.51 |
| CHEMBL105800 | — | — | 1 | 6.22 |
| CHEMBL102525 | — | — | 1 | 5.57 |
| CHEMBL103607 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL103851 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL103510 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL105560 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL419352 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL290364 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL102569 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL319700 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL105201 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL103221 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL321710 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL323317 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL102887 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL101288 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL105631 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL101420 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL105800 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL102525 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL103607 | — | IC50 | > | 10000.0 | nM | - |