Assay Detail
Binding
CHEMBL5047336
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Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain 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 | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
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 | 8.17 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555790 | — | — | 1 | 9.47 |
| CHEMBL543821 | — | — | 1 | 9.07 |
| CHEMBL5093782 | — | — | 1 | 9.05 |
| CHEMBL5083713 | — | — | 1 | 8.94 |
| CHEMBL542873 | — | — | 1 | 8.93 |
| CHEMBL5080230 | — | — | 1 | 8.83 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.41 |
| CHEMBL5082024 | — | — | 1 | 8.35 |
| CHEMBL5094446 | — | — | 1 | 7.78 |
| CHEMBL5087328 | — | — | 1 | 7.69 |
| CHEMBL5089619 | — | — | 1 | 7.63 |
| CHEMBL5090648 | — | — | 1 | 7.45 |
| CHEMBL5090805 | — | — | 1 | 7.36 |
| CHEMBL5084203 | — | — | 1 | 7.23 |
| CHEMBL5083085 | — | — | 1 | 6.42 |
| CHEMBL5082189 | — | — | 1 | - |
| CHEMBL5078846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555790 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL543821 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL5093782 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL5083713 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL542873 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL5080230 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 3.93 | nM | 8.41 |
| CHEMBL5082024 | — | Ki | = | 4.43 | nM | 8.35 |
| CHEMBL5094446 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL5087328 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL5089619 | — | Ki | = | 23.5 | nM | 7.63 |
| CHEMBL5090648 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL5090805 | — | Ki | = | 43.4 | nM | 7.36 |
| CHEMBL5084203 | — | Ki | = | 59.4 | nM | 7.23 |
| CHEMBL5083085 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL5082189 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5078846 | — | Ki | > | 5000.0 | nM | - |