Assay Detail
Binding
CHEMBL873269
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Binding affinity was evaluated using [3H]pentazocine binding to sigma-1 receptor from guinea pig brain
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.96 | 6.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138438 | — | — | 1 | 6.15 |
| CHEMBL2112760 | — | — | 1 | 6.05 |
| CHEMBL336706 | — | — | 1 | 6.02 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 5.83 |
| CHEMBL336707 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138438 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL2112760 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL336706 | — | IC50 | = | 949.0 | nM | 6.02 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL336707 | — | IC50 | = | 1830.0 | nM | 5.74 |