Assay Detail
Binding
CHEMBL5157650
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 measured by competitive radioligand receptor binding assay
9
Total Activities
9
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 8-aminomorphans with high KOR affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.65 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.27 |
| CHEMBL5203422 | — | — | 1 | 8.19 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.18 |
| CHEMBL5185196 | — | — | 1 | 8.00 |
| CHEMBL5190238 | — | — | 1 | 7.85 |
| CHEMBL5204863 | — | — | 1 | 7.77 |
| CHEMBL5173028 | — | — | 1 | 7.25 |
| CHEMBL5200121 | — | — | 1 | 6.77 |
| CHEMBL5178401 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL5203422 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL5185196 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5190238 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5204863 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5173028 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL5200121 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5178401 | — | Ki | = | 292.0 | nM | 6.54 |