Assay Detail
Binding
CHEMBL986331
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Displacement of [3H]DTH from sigma 2 receptor in rat liver homogenate in presence of (+)-pentazocine
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.59 | 9.47 |
| IC50 | 1 | 9.92 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 9.92 |
| CHEMBL77220 | — | — | 1 | 9.47 |
| CHEMBL523473 | — | — | 1 | 8.23 |
| CHEMBL490214 | — | — | 1 | 7.59 |
| CHEMBL491833 | — | — | 1 | 7.33 |
| CHEMBL491834 | — | — | 1 | 7.24 |
| CHEMBL484258 | — | — | 1 | 6.91 |
| CHEMBL473989 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL61479 | SIRAMESINE | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL77220 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL523473 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL490214 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL491833 | — | Ki | = | 46.9 | nM | 7.33 |
| CHEMBL491834 | — | Ki | = | 57.7 | nM | 7.24 |
| CHEMBL484258 | — | Ki | = | 123.5 | nM | 6.91 |
| CHEMBL473989 | — | Ki | = | 444.3 | nM | 6.35 |