Assay Detail
Binding
CHEMBL808284
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was tested for binding affinity of Sigma opioid receptor type 2 in rat liver membranes using [3H]DTG ligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.48 | 6.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112783 | — | — | 1 | 6.84 |
| CHEMBL2112787 | — | — | 1 | 6.74 |
| CHEMBL2112788 | — | — | 1 | 6.71 |
| CHEMBL2112760 | — | — | 1 | 6.64 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.52 |
| CHEMBL2112784 | — | — | 1 | 6.46 |
| CHEMBL2112789 | — | — | 1 | 6.17 |
| CHEMBL2112791 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112783 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL2112787 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL2112788 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL2112760 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL2112784 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL2112789 | — | Ki | = | 675.0 | nM | 6.17 |
| CHEMBL2112791 | — | Ki | = | 1660.0 | nM | 5.78 |