Assay Detail
Binding
CHEMBL1775445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins
11
Total Activities
11
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
Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.63 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.66 |
| CHEMBL1774575 | — | — | 1 | 8.40 |
| CHEMBL1774577 | — | — | 1 | 8.30 |
| CHEMBL1649601 | — | — | 1 | 8.27 |
| CHEMBL1774576 | — | — | 1 | 8.25 |
| CHEMBL1774578 | — | — | 1 | 8.15 |
| CHEMBL3084360 | — | — | 1 | 7.36 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.16 |
| CHEMBL1774582 | — | — | 1 | 6.70 |
| CHEMBL1774581 | — | — | 1 | 6.40 |
| CHEMBL3084361 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1774575 | — | Ki | = | 3.95 | nM | 8.40 |
| CHEMBL1774577 | — | Ki | = | 5.02 | nM | 8.30 |
| CHEMBL1649601 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL1774576 | — | Ki | = | 5.61 | nM | 8.25 |
| CHEMBL1774578 | — | Ki | = | 7.01 | nM | 8.15 |
| CHEMBL3084360 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 69.4 | nM | 7.16 |
| CHEMBL1774582 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL1774581 | — | Ki | = | 397.0 | nM | 6.40 |
| CHEMBL3084361 | — | Ki | = | 520.0 | nM | 6.28 |