Assay Detail
Binding
CHEMBL5328473
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from rat liver homogenate S1R incubated for 120 mins by liquid scintillation counting method
22
Total Activities
22
Compounds Tested
1
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
Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.98 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5406931 | — | — | 1 | 9.12 |
| CHEMBL5424448 | — | — | 1 | 8.74 |
| CHEMBL5430002 | — | — | 1 | 8.68 |
| CHEMBL5421889 | — | — | 1 | 8.60 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.59 |
| CHEMBL5433306 | — | — | 1 | 8.52 |
| CHEMBL5437311 | — | — | 1 | 8.46 |
| CHEMBL828 | PHENOTHIAZINE | 2.0 | 1 | 8.37 |
| CHEMBL5406376 | — | — | 1 | 8.21 |
| CHEMBL5434592 | — | — | 1 | 8.19 |
| CHEMBL5434285 | — | — | 1 | 8.12 |
| CHEMBL5421208 | — | — | 1 | 8.07 |
| CHEMBL5394434 | — | — | 1 | 8.00 |
| CHEMBL5396488 | — | — | 1 | 7.96 |
| CHEMBL5395079 | — | — | 1 | 7.96 |
| CHEMBL73824 | — | — | 1 | 7.85 |
| CHEMBL5432579 | — | — | 1 | 7.60 |
| CHEMBL5437477 | — | — | 1 | 7.44 |
| CHEMBL5405188 | — | — | 1 | 7.10 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.91 |
| CHEMBL5420704 | — | — | 1 | 6.68 |
| CHEMBL5408285 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5406931 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL5424448 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL5430002 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5421889 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL5433306 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5437311 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL828 | PHENOTHIAZINE | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL5406376 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL5434592 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5434285 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL5421208 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL5394434 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5396488 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5395079 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL73824 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5432579 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL5437477 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5405188 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL5420704 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL5408285 | — | Ki | = | 435.0 | nM | 6.36 |