Assay Detail
Binding
CHEMBL848651
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Binding affinity was evaluated against sigma-2 binding site in rat liver using [3H]DTG -(+)-Dextrallorphan as radioligand
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.27 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20377 | — | — | 1 | 8.09 |
| CHEMBL152057 | — | — | 1 | 8.04 |
| CHEMBL154397 | — | — | 1 | 7.61 |
| CHEMBL142596 | — | — | 1 | 7.55 |
| CHEMBL346153 | — | — | 1 | 7.49 |
| CHEMBL356909 | — | — | 1 | 7.47 |
| CHEMBL152426 | — | — | 1 | 7.37 |
| CHEMBL349793 | — | — | 1 | 7.32 |
| CHEMBL358109 | — | — | 1 | 7.30 |
| CHEMBL151136 | — | — | 1 | 7.22 |
| CHEMBL152478 | — | — | 1 | 6.99 |
| CHEMBL153758 | — | — | 1 | 6.91 |
| CHEMBL152618 | — | — | 1 | 6.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20377 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL152057 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL154397 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL142596 | — | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL346153 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL356909 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL152426 | — | Ki | = | 43.1 | nM | 7.37 |
| CHEMBL349793 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL358109 | — | Ki | = | 50.5 | nM | 7.30 |
| CHEMBL151136 | — | Ki | = | 59.8 | nM | 7.22 |
| CHEMBL152478 | — | Ki | = | 103.6 | nM | 6.99 |
| CHEMBL153758 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL152618 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 1540.0 | nM | 5.81 |