Assay Detail
Binding
CHEMBL5047337
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Displacement of [3H]DTG from sigma 2 receptor in Wistar Han rat liver membranes measured after 120 mins by scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ<sub>1</sub>) receptor ligands with potent anti-amnesic effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.82 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5082024 | — | — | 1 | 7.76 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 7.53 |
| CHEMBL542873 | — | — | 1 | 7.28 |
| CHEMBL5089619 | — | — | 1 | 7.28 |
| CHEMBL5094446 | — | — | 1 | 7.16 |
| CHEMBL5087328 | — | — | 1 | 7.11 |
| CHEMBL5084203 | — | — | 1 | 6.94 |
| CHEMBL5093782 | — | — | 1 | 6.77 |
| CHEMBL5090805 | — | — | 1 | 6.76 |
| CHEMBL5083713 | — | — | 1 | 6.73 |
| CHEMBL555790 | — | — | 1 | 6.73 |
| CHEMBL543821 | — | — | 1 | 6.62 |
| CHEMBL5090648 | — | — | 1 | 6.52 |
| CHEMBL5082189 | — | — | 1 | 6.39 |
| CHEMBL5083085 | — | — | 1 | 6.20 |
| CHEMBL5080230 | — | — | 1 | 6.14 |
| CHEMBL5078846 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5082024 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL542873 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL5089619 | — | Ki | = | 52.5 | nM | 7.28 |
| CHEMBL5094446 | — | Ki | = | 69.8 | nM | 7.16 |
| CHEMBL5087328 | — | Ki | = | 77.8 | nM | 7.11 |
| CHEMBL5084203 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL5093782 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5090805 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL5083713 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL555790 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL543821 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL5090648 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL5082189 | — | Ki | = | 411.0 | nM | 6.39 |
| CHEMBL5083085 | — | Ki | = | 636.0 | nM | 6.20 |
| CHEMBL5080230 | — | Ki | = | 723.0 | nM | 6.14 |
| CHEMBL5078846 | — | Ki | = | 809.0 | nM | 6.09 |