Assay Detail
Binding
CHEMBL807414
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Tested for its binding affinity towards sigma-1 site in rat brain using E3H1-(+)-SKF 10047 as radioligand in rat brain
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.32 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75217 | — | — | 1 | 7.66 |
| CHEMBL72219 | — | — | 1 | 7.62 |
| CHEMBL73501 | — | — | 1 | 7.57 |
| CHEMBL72506 | — | — | 1 | 7.57 |
| CHEMBL73017 | — | — | 1 | 7.50 |
| CHEMBL307668 | — | — | 1 | 7.50 |
| CHEMBL451542 | — | — | 1 | 7.47 |
| CHEMBL74736 | — | — | 1 | 7.47 |
| CHEMBL307628 | — | — | 1 | 7.41 |
| CHEMBL309172 | — | — | 1 | 7.40 |
| CHEMBL73234 | CARBETAPENTANE | 4.0 | 1 | 7.39 |
| CHEMBL73762 | — | — | 1 | 7.35 |
| CHEMBL74305 | — | — | 1 | 7.23 |
| CHEMBL440686 | — | — | 1 | 6.67 |
| CHEMBL308707 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75217 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL72219 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL73501 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL72506 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL73017 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL307668 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL451542 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL74736 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL307628 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL309172 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL73234 | CARBETAPENTANE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL73762 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL74305 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL440686 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL308707 | — | Ki | = | 884.0 | nM | 6.05 |