Assay Detail
Binding
CHEMBL2395767
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis
33
Total Activities
33
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
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 | 33 | 7.58 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178153 | — | — | 1 | 9.40 |
| CHEMBL2391071 | — | — | 1 | 9.02 |
| CHEMBL2391070 | — | — | 1 | 8.80 |
| CHEMBL2391065 | — | — | 1 | 8.74 |
| CHEMBL2391061 | — | — | 1 | 8.57 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.55 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.34 |
| CHEMBL2391072 | — | — | 1 | 8.33 |
| CHEMBL162522 | — | — | 1 | 8.24 |
| CHEMBL2391068 | — | — | 1 | 8.00 |
| CHEMBL1327876 | — | — | 1 | 7.95 |
| CHEMBL1479800 | — | — | 1 | 7.87 |
| CHEMBL2391066 | — | — | 1 | 7.82 |
| CHEMBL273041 | — | — | 1 | 7.70 |
| CHEMBL2391073 | — | — | 1 | 7.61 |
| CHEMBL272551 | — | — | 1 | 7.55 |
| CHEMBL2391060 | — | — | 1 | 7.52 |
| CHEMBL2391062 | — | — | 1 | 7.45 |
| CHEMBL2391057 | — | — | 1 | 7.42 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.42 |
| CHEMBL2391069 | — | — | 1 | 7.40 |
| CHEMBL2391064 | — | — | 1 | 7.29 |
| CHEMBL2391076 | — | — | 1 | 7.22 |
| CHEMBL2391059 | — | — | 1 | 7.17 |
| CHEMBL2391063 | — | — | 1 | 7.16 |
| CHEMBL2391077 | — | — | 1 | 7.11 |
| CHEMBL2391078 | — | — | 1 | 6.86 |
| CHEMBL2391067 | — | — | 1 | 6.72 |
| CHEMBL1422857 | — | — | 1 | 6.70 |
| CHEMBL2391074 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178153 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2391071 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL2391070 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2391065 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2391061 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL2391072 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL162522 | — | Ki | = | 5.81 | nM | 8.24 |
| CHEMBL2391068 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL1327876 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL1479800 | — | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL2391066 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL273041 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2391073 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL272551 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL2391060 | — | Ki | = | 29.9 | nM | 7.52 |
| CHEMBL2391062 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL2391057 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL2391069 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2391064 | — | Ki | = | 51.8 | nM | 7.29 |
| CHEMBL2391076 | — | Ki | = | 59.9 | nM | 7.22 |
| CHEMBL2391059 | — | Ki | = | 68.1 | nM | 7.17 |
| CHEMBL2391063 | — | Ki | = | 68.7 | nM | 7.16 |
| CHEMBL2391077 | — | Ki | = | 78.4 | nM | 7.11 |
| CHEMBL2391078 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL2391067 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL1422857 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL2391074 | — | Ki | = | 551.0 | nM | 6.26 |
| CHEMBL2391079 | — | Ki | = | 843.0 | nM | 6.07 |
| CHEMBL2391075 | — | Ki | = | 969.0 | nM | 6.01 |
| CHEMBL2391080 | — | Ki | = | 1075.0 | nM | 5.97 |