Assay Detail
Binding
CHEMBL805743
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Binding affinity towards sigma 2 receptor was determined in rat liver membrane using [3H]DTG as radioligand in presence of dextrallorphan
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.00 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20377 | — | — | 1 | 8.09 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.92 |
| CHEMBL109026 | — | — | 1 | 7.92 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.89 |
| CHEMBL324620 | — | — | 1 | 7.84 |
| CHEMBL323476 | — | — | 1 | 7.83 |
| CHEMBL107870 | — | — | 1 | 7.28 |
| CHEMBL110099 | — | — | 1 | 7.27 |
| CHEMBL107485 | — | — | 1 | 6.96 |
| CHEMBL108972 | — | — | 1 | 6.94 |
| CHEMBL321702 | — | — | 1 | 6.87 |
| CHEMBL107717 | — | — | 1 | 6.82 |
| CHEMBL107922 | — | — | 1 | 6.79 |
| CHEMBL111331 | — | — | 1 | 6.74 |
| CHEMBL107720 | — | — | 1 | 6.27 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 5.81 |
| CHEMBL325320 | — | — | 1 | 5.63 |
| CHEMBL543632 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20377 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL109026 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL324620 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL323476 | — | Ki | = | 14.9 | nM | 7.83 |
| CHEMBL107870 | — | Ki | = | 52.6 | nM | 7.28 |
| CHEMBL110099 | — | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL107485 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL108972 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL321702 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL107717 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL107922 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL111331 | — | Ki | = | 183.3 | nM | 6.74 |
| CHEMBL107720 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 1540.0 | nM | 5.81 |
| CHEMBL325320 | — | Ki | = | 2364.0 | nM | 5.63 |
| CHEMBL543632 | — | Ki | = | 7705.0 | nM | 5.11 |