Assay Detail
Binding
CHEMBL808278
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Binding affinity for sigma-2 receptor by displacing [3H]DTG in presence of dextrallorphan
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.55 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL145867 | — | — | 1 | 8.31 |
| CHEMBL146239 | — | — | 1 | 8.18 |
| CHEMBL357431 | — | — | 1 | 7.92 |
| CHEMBL145921 | — | — | 1 | 7.85 |
| CHEMBL148108 | — | — | 1 | 7.60 |
| CHEMBL343237 | — | — | 1 | 7.48 |
| CHEMBL146238 | — | — | 1 | 7.24 |
| CHEMBL144552 | — | — | 1 | 7.07 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 6.95 |
| CHEMBL143950 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL145867 | — | Ki | = | 4.91 | nM | 8.31 |
| CHEMBL146239 | — | Ki | = | 6.61 | nM | 8.18 |
| CHEMBL357431 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL145921 | — | Ki | = | 14.2 | nM | 7.85 |
| CHEMBL148108 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL343237 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL146238 | — | Ki | = | 57.3 | nM | 7.24 |
| CHEMBL144552 | — | Ki | = | 84.4 | nM | 7.07 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL143950 | — | Ki | = | 119.0 | nM | 6.92 |