Assay Detail
Binding
CHEMBL3405394
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Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in Sprague-Dawley rat liver membranes after 120 mins by beta counting in presence of (+)-pentazocine
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of tetrahydroindazole derivatives as sigma-2 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.13 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.71 |
| CHEMBL3401447 | — | — | 1 | 7.33 |
| CHEMBL3401452 | — | — | 1 | 7.13 |
| CHEMBL3401450 | — | — | 1 | 7.05 |
| CHEMBL3401451 | — | — | 1 | 6.85 |
| CHEMBL3401449 | — | — | 1 | 6.09 |
| CHEMBL3401446 | — | — | 1 | 4.95 |
| CHEMBL3401448 | — | — | 1 | 4.74 |
| CHEMBL3401454 | — | — | 1 | 4.74 |
| CHEMBL3401453 | — | — | 1 | 4.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL3401447 | — | Ki | = | 46.6 | nM | 7.33 |
| CHEMBL3401452 | — | Ki | = | 74.5 | nM | 7.13 |
| CHEMBL3401450 | — | Ki | = | 89.8 | nM | 7.05 |
| CHEMBL3401451 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL3401449 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL3401446 | — | Ki | = | 11350.0 | nM | 4.95 |
| CHEMBL3401448 | — | Ki | = | 18250.0 | nM | 4.74 |
| CHEMBL3401454 | — | Ki | = | 18400.0 | nM | 4.74 |
| CHEMBL3401453 | — | Ki | = | 21500.0 | nM | 4.67 |