Assay Detail
Binding
CHEMBL804719
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Binding affinity for sigma-1 receptor by displacing [3H]-(+) pentazocine
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 7.64 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL357431 | — | — | 1 | 8.47 |
| CHEMBL144552 | — | — | 1 | 8.38 |
| CHEMBL146239 | — | — | 1 | 8.28 |
| CHEMBL146238 | — | — | 1 | 8.23 |
| CHEMBL145921 | — | — | 1 | 7.86 |
| CHEMBL343237 | — | — | 1 | 7.68 |
| CHEMBL145867 | — | — | 1 | 7.08 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 7.05 |
| CHEMBL148108 | — | — | 1 | 6.84 |
| CHEMBL143950 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL357431 | — | Ki | = | 3.35 | nM | 8.47 |
| CHEMBL144552 | — | Ki | = | 4.15 | nM | 8.38 |
| CHEMBL146239 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL146238 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL145921 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL343237 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL145867 | — | Ki | = | 82.9 | nM | 7.08 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 88.5 | nM | 7.05 |
| CHEMBL148108 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL143950 | — | Ki | = | 326.0 | nM | 6.49 |