Assay Detail
Binding
CHEMBL5157899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by competitive radioligand receptor binding assay
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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Synthesis of tropane-based σ<sub>1</sub> receptor antagonists with antiallodynic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.11 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175714 | — | — | 1 | 9.35 |
| CHEMBL5187130 | — | — | 1 | 9.10 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL5186790 | — | — | 1 | 8.18 |
| CHEMBL5185178 | — | — | 1 | 7.75 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175714 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL5187130 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5186790 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL5185178 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL28564 | ELIPRODIL | Ki | = | 94.0 | nM | 7.03 |