Assay Detail
Binding
CHEMBL1781410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.74 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.05 |
| CHEMBL521582 | — | — | 1 | 8.99 |
| CHEMBL1779060 | — | — | 1 | 8.12 |
| CHEMBL1779059 | — | — | 1 | 7.70 |
| CHEMBL1779058 | — | — | 1 | 7.57 |
| CHEMBL64260 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL521582 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL1779060 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL1779059 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1779058 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL64260 | — | Ki | = | 10412.0 | nM | 4.98 |