Assay Detail
Binding
CHEMBL3380225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (+)-[3H]-pentazocine from sigma1 recetor in guinea-pig brain membranes without cerebellum by radioligand binding assay
19
Total Activities
19
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
Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity from σ2 receptor affinity in mixed P-gp/σ2 receptor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.93 | 8.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3355371 | — | — | 1 | 8.61 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.35 |
| CHEMBL3355365 | — | — | 1 | 7.76 |
| CHEMBL3352847 | — | — | 1 | 7.72 |
| CHEMBL3355378 | — | — | 1 | 7.29 |
| CHEMBL3355376 | — | — | 1 | 7.23 |
| CHEMBL3355366 | — | — | 1 | 7.17 |
| CHEMBL3355375 | — | — | 1 | 6.91 |
| CHEMBL3355377 | — | — | 1 | 6.90 |
| CHEMBL3355369 | — | — | 1 | 6.89 |
| CHEMBL3355362 | — | — | 1 | 6.82 |
| CHEMBL3355374 | — | — | 1 | 6.76 |
| CHEMBL3355373 | — | — | 1 | 6.67 |
| CHEMBL3355367 | — | — | 1 | 6.47 |
| CHEMBL3355363 | — | — | 1 | 6.37 |
| CHEMBL3355368 | — | — | 1 | 6.26 |
| CHEMBL3355364 | — | — | 1 | 6.03 |
| CHEMBL3354882 | — | — | 1 | 5.86 |
| CHEMBL3355370 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3355371 | — | Ki | = | 2.44 | nM | 8.61 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.52 | nM | 8.35 |
| CHEMBL3355365 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL3352847 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL3355378 | — | Ki | = | 50.8 | nM | 7.29 |
| CHEMBL3355376 | — | Ki | = | 59.2 | nM | 7.23 |
| CHEMBL3355366 | — | Ki | = | 67.4 | nM | 7.17 |
| CHEMBL3355375 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL3355377 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL3355369 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL3355362 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL3355374 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL3355373 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL3355367 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL3355363 | — | Ki | = | 431.0 | nM | 6.37 |
| CHEMBL3355368 | — | Ki | = | 544.0 | nM | 6.26 |
| CHEMBL3355364 | — | Ki | = | 939.0 | nM | 6.03 |
| CHEMBL3354882 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL3355370 | — | Ki | = | 2703.0 | nM | 5.57 |