Assay Detail
Binding
CHEMBL753635
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Inhibition of [3H]pentazocine binding to Opioid receptor sigma 1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.69 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48582 | SAFINAMIDE MESYLATE | 4.0 | 1 | 7.71 |
| CHEMBL85371 | — | — | 1 | 7.71 |
| CHEMBL83621 | — | — | 1 | 7.46 |
| CHEMBL82327 | — | — | 1 | 6.55 |
| CHEMBL85962 | — | — | 1 | 6.55 |
| CHEMBL315738 | — | — | 1 | 6.55 |
| CHEMBL85054 | — | — | 1 | 6.26 |
| CHEMBL311029 | — | — | 1 | 6.23 |
| CHEMBL85899 | — | — | 1 | 5.18 |
| CHEMBL315093 | — | — | 1 | - |
| CHEMBL84167 | — | — | 1 | - |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48582 | SAFINAMIDE MESYLATE | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL85371 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL83621 | — | IC50 | = | 34.4 | nM | 7.46 |
| CHEMBL82327 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL85962 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL315738 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL85054 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL311029 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL85899 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL315093 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL84167 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL741 | LAMOTRIGINE | IC50 | > | 10000.0 | nM | - |