Assay Detail
Binding
CHEMBL802064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.46 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109026 | — | — | 1 | 8.83 |
| CHEMBL20377 | — | — | 1 | 8.68 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.43 |
| CHEMBL107870 | — | — | 1 | 8.10 |
| CHEMBL324620 | — | — | 1 | 7.86 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.56 |
| CHEMBL543632 | — | — | 1 | 7.54 |
| CHEMBL111331 | — | — | 1 | 7.52 |
| CHEMBL321702 | — | — | 1 | 7.39 |
| CHEMBL107485 | — | — | 1 | 7.27 |
| CHEMBL323476 | — | — | 1 | 7.11 |
| CHEMBL110099 | — | — | 1 | 6.96 |
| CHEMBL107717 | — | — | 1 | 6.89 |
| CHEMBL107922 | — | — | 1 | 6.64 |
| CHEMBL107720 | — | — | 1 | 6.61 |
| CHEMBL325320 | — | — | 1 | 6.41 |
| CHEMBL108972 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109026 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL20377 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL107870 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL324620 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 27.7 | nM | 7.56 |
| CHEMBL543632 | — | Ki | = | 28.7 | nM | 7.54 |
| CHEMBL111331 | — | Ki | = | 29.9 | nM | 7.52 |
| CHEMBL321702 | — | Ki | = | 40.7 | nM | 7.39 |
| CHEMBL107485 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL323476 | — | Ki | = | 77.5 | nM | 7.11 |
| CHEMBL110099 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL107717 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL107922 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL107720 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL325320 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL108972 | — | Ki | = | 1122.0 | nM | 5.95 |