Assay Detail
Binding
CHEMBL5250277
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Displacement of [3H]N-methylspiperone from D3 receptor in HEK293 cell membrane assessed as inhibition constant
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.16 | 6.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5274285 | — | — | 1 | 6.93 |
| CHEMBL5289958 | — | — | 1 | 6.46 |
| CHEMBL5272689 | — | — | 1 | 6.42 |
| CHEMBL5288298 | — | — | 1 | 6.29 |
| CHEMBL5182602 | — | — | 1 | 6.02 |
| CHEMBL5204764 | — | — | 1 | 5.61 |
| CHEMBL5170381 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5274285 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL5289958 | — | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL5272689 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL5288298 | — | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL5182602 | — | Ki | = | 948.0 | nM | 6.02 |
| CHEMBL5204764 | — | Ki | = | 2463.0 | nM | 5.61 |
| CHEMBL5170381 | — | Ki | = | 4079.0 | nM | 5.39 |