Assay Detail
Binding
CHEMBL808203
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Inhibition of [3H](+)-pentazocine binding to Sigma receptor type 1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.92 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53070 | — | — | 1 | 7.85 |
| CHEMBL540283 | — | — | 1 | 7.43 |
| CHEMBL542123 | — | — | 1 | 7.31 |
| CHEMBL542368 | — | — | 1 | 7.31 |
| CHEMBL301772 | — | — | 1 | 6.94 |
| CHEMBL298997 | — | — | 1 | 6.79 |
| CHEMBL545669 | — | — | 1 | 6.62 |
| CHEMBL545668 | — | — | 1 | 6.61 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 1 | 6.46 |
| CHEMBL51146 | — | — | 1 | 6.43 |
| CHEMBL298778 | — | — | 1 | 6.34 |
| CHEMBL301487 | — | — | 1 | - |
| CHEMBL299327 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53070 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL540283 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL542123 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL542368 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL301772 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL298997 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL545669 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL545668 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL52440 | DEXTROMETHORPHAN | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL51146 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL298778 | — | Ki | = | 456.0 | nM | 6.34 |
| CHEMBL301487 | — | Ki | > | 3300.0 | nM | - |
| CHEMBL299327 | — | Ki | > | 3300.0 | nM | - |