Assay Detail
Binding
CHEMBL848648
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Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.64 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.48 |
| CHEMBL129159 | — | — | 1 | 8.74 |
| CHEMBL129237 | — | — | 1 | 8.66 |
| CHEMBL339033 | — | — | 1 | 7.49 |
| CHEMBL129768 | — | — | 1 | 7.19 |
| CHEMBL339963 | — | — | 1 | 6.74 |
| CHEMBL340211 | AZAPERONE | 2.0 | 1 | 6.47 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL129159 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL129237 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL339033 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL129768 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL339963 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL340211 | AZAPERONE | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL60859 | BMY-14802 | Ki | = | 490.0 | nM | 6.31 |