Assay Detail
Binding
CHEMBL1831503
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 after 30 mins by radioligand binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Arylamides hybrids of two high-affinity σ2 receptor ligands as tools for the development of PET radiotracers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.94 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53325 | — | — | 1 | 9.42 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL1830692 | — | — | 1 | 7.61 |
| CHEMBL1830687 | — | — | 1 | 7.59 |
| CHEMBL1830691 | — | — | 1 | 7.46 |
| CHEMBL1830685 | — | — | 1 | 7.34 |
| CHEMBL1830690 | — | — | 1 | 6.84 |
| CHEMBL1830683 | — | — | 1 | 6.82 |
| CHEMBL1830689 | — | — | 1 | 6.57 |
| CHEMBL1830684 | — | — | 1 | 6.27 |
| CHEMBL1828651 | — | — | 1 | 6.15 |
| CHEMBL1830682 | — | — | 1 | 5.67 |
| CHEMBL1830688 | — | — | 1 | 5.59 |
| CHEMBL1830686 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53325 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.09 | nM | 8.51 |
| CHEMBL1830692 | — | Ki | = | 24.7 | nM | 7.61 |
| CHEMBL1830687 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL1830691 | — | Ki | = | 35.1 | nM | 7.46 |
| CHEMBL1830685 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL1830690 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL1830683 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL1830689 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL1830684 | — | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL1828651 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL1830682 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL1830688 | — | Ki | = | 2570.0 | nM | 5.59 |
| CHEMBL1830686 | — | Ki | = | 4400.0 | nM | 5.36 |