Assay Detail
Binding
CHEMBL5350656
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Displacement of [3H]DTG from sigma 2 receptor in Sprague-Dawley rat liver assessed as inhibition constant by liquid scintillation counter analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Dual Piperidine-Based Histamine H<sub>3</sub> and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.42 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5436799 | — | — | 1 | 8.40 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 8.19 |
| CHEMBL5427817 | — | — | 1 | 8.00 |
| CHEMBL5433976 | — | — | 1 | 8.00 |
| CHEMBL5440901 | — | — | 1 | 7.80 |
| CHEMBL5432307 | — | — | 1 | 7.77 |
| CHEMBL4597895 | — | — | 1 | 7.72 |
| CHEMBL4776141 | — | — | 1 | 7.65 |
| CHEMBL5421122 | — | — | 1 | 7.60 |
| CHEMBL4159046 | — | — | 1 | 7.57 |
| CHEMBL5404813 | — | — | 1 | 7.54 |
| CHEMBL5413280 | — | — | 1 | 7.48 |
| CHEMBL4598396 | — | — | 1 | 7.34 |
| CHEMBL5411175 | — | — | 1 | 7.33 |
| CHEMBL5419356 | — | — | 1 | 7.33 |
| CHEMBL5398497 | — | — | 1 | 7.19 |
| CHEMBL1823340 | — | — | 1 | 7.17 |
| CHEMBL4743583 | — | — | 1 | 7.12 |
| CHEMBL4783744 | — | — | 1 | 7.00 |
| CHEMBL5431002 | — | — | 1 | 6.99 |
| CHEMBL5413694 | — | — | 1 | 6.94 |
| CHEMBL2170062 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5436799 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL462605 | PITOLISANT | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5427817 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL5433976 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5440901 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5432307 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4597895 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4776141 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL5421122 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4159046 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5404813 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL5413280 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4598396 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL5411175 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5419356 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5398497 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL1823340 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4743583 | — | Ki | = | 75.2 | nM | 7.12 |
| CHEMBL4783744 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL5431002 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL5413694 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL2170062 | — | Ki | = | 9300.0 | nM | 5.03 |