Assay Detail
Binding
CHEMBL986333
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] (+)-pentazocine from sigma 1 receptor in rat liver homogenate
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.23 | 7.68 |
| IC50 | 1 | 7.77 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.77 |
| CHEMBL473989 | — | — | 1 | 7.68 |
| CHEMBL523473 | — | — | 1 | 7.68 |
| CHEMBL491834 | — | — | 1 | 7.37 |
| CHEMBL484258 | — | — | 1 | 7.00 |
| CHEMBL491833 | — | — | 1 | 6.93 |
| CHEMBL490214 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL473989 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL523473 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL491834 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL484258 | — | Ki | = | 98.9 | nM | 7.00 |
| CHEMBL491833 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL490214 | — | Ki | = | 201.0 | nM | 6.70 |