Assay Detail
Binding
CHEMBL2395766
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 150 mins by liquid scintillation counting analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.73 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178153 | — | — | 1 | 8.48 |
| CHEMBL2391070 | — | — | 1 | 7.59 |
| CHEMBL2391068 | — | — | 1 | 7.41 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.36 |
| CHEMBL1327876 | — | — | 1 | 7.32 |
| CHEMBL2391072 | — | — | 1 | 7.31 |
| CHEMBL2391073 | — | — | 1 | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.23 |
| CHEMBL272551 | — | — | 1 | 7.06 |
| CHEMBL2391061 | — | — | 1 | 7.05 |
| CHEMBL2391062 | — | — | 1 | 7.05 |
| CHEMBL2391071 | — | — | 1 | 7.04 |
| CHEMBL2391065 | — | — | 1 | 6.93 |
| CHEMBL2391059 | — | — | 1 | 6.87 |
| CHEMBL2391060 | — | — | 1 | 6.83 |
| CHEMBL2391066 | — | — | 1 | 6.82 |
| CHEMBL2391064 | — | — | 1 | 6.76 |
| CHEMBL2391057 | — | — | 1 | 6.75 |
| CHEMBL2391063 | — | — | 1 | 6.74 |
| CHEMBL2391076 | — | — | 1 | 6.73 |
| CHEMBL2391077 | — | — | 1 | 6.72 |
| CHEMBL2391069 | — | — | 1 | 6.70 |
| CHEMBL2391079 | — | — | 1 | 6.61 |
| CHEMBL1479800 | — | — | 1 | 6.54 |
| CHEMBL2391080 | — | — | 1 | 6.31 |
| CHEMBL2391074 | — | — | 1 | 6.11 |
| CHEMBL162522 | — | — | 1 | 5.89 |
| CHEMBL2391075 | — | — | 1 | 5.81 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 5.73 |
| CHEMBL2391078 | — | — | 1 | 5.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178153 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2391070 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL2391068 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL1327876 | — | Ki | = | 48.4 | nM | 7.32 |
| CHEMBL2391072 | — | Ki | = | 48.9 | nM | 7.31 |
| CHEMBL2391073 | — | Ki | = | 56.7 | nM | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 58.4 | nM | 7.23 |
| CHEMBL272551 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL2391061 | — | Ki | = | 88.8 | nM | 7.05 |
| CHEMBL2391062 | — | Ki | = | 89.4 | nM | 7.05 |
| CHEMBL2391071 | — | Ki | = | 91.8 | nM | 7.04 |
| CHEMBL2391065 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL2391059 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL2391060 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL2391066 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL2391064 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL2391057 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL2391063 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL2391076 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL2391077 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL2391069 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL2391079 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL1479800 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL2391080 | — | Ki | = | 485.0 | nM | 6.31 |
| CHEMBL2391074 | — | Ki | = | 778.0 | nM | 6.11 |
| CHEMBL162522 | — | Ki | = | 1274.0 | nM | 5.89 |
| CHEMBL2391075 | — | Ki | = | 1547.0 | nM | 5.81 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 1871.0 | nM | 5.73 |
| CHEMBL2391078 | — | Ki | = | 1965.0 | nM | 5.71 |
| CHEMBL2391067 | — | Ki | = | 2128.0 | nM | 5.67 |
| CHEMBL1422857 | — | Ki | = | 8136.0 | nM | 5.09 |