Assay Detail
Binding
CHEMBL3372350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor by scintillation counting analysis
17
Total Activities
17
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
From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.52 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.35 |
| CHEMBL583580 | — | — | 1 | 6.84 |
| CHEMBL259582 | — | — | 1 | 6.82 |
| CHEMBL3354875 | — | — | 1 | 6.58 |
| CHEMBL3354882 | — | — | 1 | 5.86 |
| CHEMBL3354886 | — | — | 1 | 5.66 |
| CHEMBL3354877 | — | — | 1 | 5.53 |
| CHEMBL3352842 | — | — | 1 | - |
| CHEMBL3354888 | — | — | 1 | - |
| CHEMBL3354887 | — | — | 1 | - |
| CHEMBL3354878 | — | — | 1 | - |
| CHEMBL3354885 | — | — | 1 | - |
| CHEMBL3354884 | — | — | 1 | - |
| CHEMBL3354883 | — | — | 1 | - |
| CHEMBL3354879 | — | — | 1 | - |
| CHEMBL3354881 | — | — | 1 | - |
| CHEMBL3354880 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.52 | nM | 8.35 |
| CHEMBL583580 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL259582 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL3354875 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3354882 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL3354886 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL3354877 | — | Ki | = | 2934.0 | nM | 5.53 |
| CHEMBL3352842 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354888 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354887 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354878 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354885 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354884 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354883 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354879 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354881 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3354880 | — | Ki | > | 5000.0 | nM | - |