Assay Detail
Binding
CHEMBL4676327
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by solid scintillation counting method
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Cell 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
Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.50 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4754707 | — | — | 2 | 8.32 |
| CHEMBL4741170 | — | — | 2 | 7.89 |
| CHEMBL4754599 | — | — | 2 | 6.40 |
| CHEMBL1196613 | — | — | 1 | 6.37 |
| CHEMBL1193345 | — | — | 1 | 6.37 |
| CHEMBL4756207 | — | — | 1 | 6.18 |
| CHEMBL1190691 | — | — | 1 | 5.82 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4754707 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4741170 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4754707 | — | Ki | = | 366.0 | nM | 6.44 |
| CHEMBL4754599 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL1196613 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL1193345 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL4754599 | — | Ki | = | 527.0 | nM | 6.28 |
| CHEMBL4756207 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL1190691 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3989843 | TRANYLCYPROMINE | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4741170 | — | Ki | = | 1900.0 | nM | 5.72 |