Assay Detail
Binding
CHEMBL965019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer
7
Total Activities
7
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
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.35 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.66 |
| CHEMBL513224 | — | — | 1 | 8.13 |
| CHEMBL477036 | — | — | 1 | 7.42 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.79 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.58 |
| CHEMBL518434 | — | — | 1 | 6.50 |
| CHEMBL477037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL513224 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL477036 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL60859 | BMY-14802 | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL518434 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL477037 | — | Ki | > | 10000.0 | nM | - |