Assay Detail
Binding
CHEMBL3056602
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Displacement of [3H](+)pentazocine from sigma-1 receptor in Cavia porcellus (guinea pig) brain membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Novel 2(3H)-Benzothiazolones as Highly Potent and Selective Sigma-1 Receptor Ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.61 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272899 | — | — | 1 | 9.25 |
| CHEMBL274699 | — | — | 1 | 9.22 |
| CHEMBL2260851 | — | — | 1 | 8.92 |
| CHEMBL2260849 | — | — | 1 | 8.90 |
| CHEMBL141209 | — | — | 1 | 8.89 |
| CHEMBL2260846 | — | — | 1 | 8.85 |
| CHEMBL14875 | — | — | 1 | 8.64 |
| CHEMBL2260852 | — | — | 1 | 8.54 |
| CHEMBL2260850 | — | — | 1 | 8.43 |
| CHEMBL274010 | — | — | 1 | 8.07 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.04 |
| CHEMBL2260847 | — | — | 1 | 7.55 |
| CHEMBL2260848 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272899 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL274699 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2260851 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2260849 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL141209 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL2260846 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL14875 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2260852 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2260850 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL274010 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL2260847 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2260848 | — | Ki | > | 1000.0 | nM | - |