Assay Detail
Binding
CHEMBL3742945
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in rat brain by competition binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel indole-based sigma-2 receptor ligands: synthesis, structureaffinity relationship and antiproliferative activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.86 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3742357 | — | — | 1 | 8.59 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 8.33 |
| CHEMBL3741752 | — | — | 1 | 7.96 |
| CHEMBL3740945 | — | — | 1 | 7.78 |
| CHEMBL210858 | — | — | 1 | 6.99 |
| CHEMBL3741305 | — | — | 1 | 6.61 |
| CHEMBL3739449 | — | — | 1 | 6.59 |
| CHEMBL3739531 | — | — | 1 | 6.59 |
| CHEMBL3740227 | — | — | 1 | 6.58 |
| CHEMBL3740736 | — | — | 1 | 6.41 |
| CHEMBL3740876 | — | — | 1 | 6.31 |
| CHEMBL3354882 | — | — | 1 | 6.28 |
| CHEMBL3740764 | — | — | 1 | 6.21 |
| CHEMBL3740497 | — | — | 1 | 5.96 |
| CHEMBL3741494 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3742357 | — | Ki | = | 2.58 | nM | 8.59 |
| CHEMBL61479 | SIRAMESINE | Ki | = | 4.69 | nM | 8.33 |
| CHEMBL3741752 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3740945 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL210858 | — | Ki | = | 102.3 | nM | 6.99 |
| CHEMBL3741305 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL3739449 | — | Ki | = | 255.6 | nM | 6.59 |
| CHEMBL3739531 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL3740227 | — | Ki | = | 262.5 | nM | 6.58 |
| CHEMBL3740736 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL3740876 | — | Ki | = | 493.5 | nM | 6.31 |
| CHEMBL3354882 | — | Ki | = | 530.8 | nM | 6.28 |
| CHEMBL3740764 | — | Ki | = | 614.0 | nM | 6.21 |
| CHEMBL3740497 | — | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL3741494 | — | Ki | = | 2158.0 | nM | 5.67 |