Assay Detail
Binding
CHEMBL2175142
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Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain homogenates
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.54 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783450 | — | — | 1 | 8.22 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.22 |
| CHEMBL2170313 | — | — | 1 | 7.96 |
| CHEMBL2170314 | — | — | 1 | 7.77 |
| CHEMBL1783458 | — | — | 1 | 7.70 |
| CHEMBL2170178 | — | — | 1 | 7.55 |
| CHEMBL2170312 | — | — | 1 | 7.30 |
| CHEMBL2170180 | — | — | 1 | 7.14 |
| CHEMBL2170302 | — | — | 1 | 6.89 |
| CHEMBL2170179 | — | — | 1 | 6.87 |
| CHEMBL2170301 | — | — | 1 | 6.60 |
| CHEMBL2170303 | — | — | 1 | - |
| CHEMBL2170311 | — | — | 1 | - |
| CHEMBL2170310 | — | — | 1 | - |
| CHEMBL2170309 | — | — | 1 | - |
| CHEMBL2170308 | — | — | 1 | - |
| CHEMBL1783455 | — | — | 1 | - |
| CHEMBL2170307 | — | — | 1 | - |
| CHEMBL2170306 | — | — | 1 | - |
| CHEMBL2170305 | — | — | 1 | - |
| CHEMBL1783426 | — | — | 1 | - |
| CHEMBL2170304 | — | — | 1 | - |
| CHEMBL2170315 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783450 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170313 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2170314 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1783458 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2170178 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2170312 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2170180 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL2170302 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL2170179 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2170301 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL2170303 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170311 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170310 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170309 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170308 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1783455 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170307 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170306 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170305 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1783426 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170304 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2170315 | — | Ki | > | 10000.0 | nM | - |