Assay Detail
Binding
CHEMBL809526
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Ability to inhibit [3H](+)-DTG binding to rat liver Sigma receptor type 2 in presence of dextrallorphan
26
Total Activities
12
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
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.40 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL141381 | — | — | 3 | 8.19 |
| CHEMBL322468 | — | — | 3 | 7.87 |
| CHEMBL110319 | — | — | 3 | 7.78 |
| CHEMBL143800 | — | — | 3 | 7.67 |
| CHEMBL146659 | — | — | 3 | 7.65 |
| CHEMBL356639 | — | — | 1 | 7.62 |
| CHEMBL38791 | — | — | 2 | 7.60 |
| CHEMBL145296 | — | — | 3 | 7.42 |
| CHEMBL109124 | — | — | 2 | 7.28 |
| CHEMBL145422 | — | — | 1 | 7.28 |
| CHEMBL145780 | — | — | 1 | 7.10 |
| CHEMBL358527 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL141381 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL141381 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL322468 | — | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL110319 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL143800 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL146659 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL356639 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL38791 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL141381 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL146659 | — | Ki | = | 34.5 | nM | 7.46 |
| CHEMBL143800 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL322468 | — | Ki | = | 35.5 | nM | 7.45 |
| CHEMBL110319 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL145296 | — | Ki | = | 38.2 | nM | 7.42 |
| CHEMBL145296 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL145296 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL145422 | — | Ki | = | 52.6 | nM | 7.28 |
| CHEMBL109124 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL322468 | — | Ki | = | 71.8 | nM | 7.14 |
| CHEMBL145780 | — | Ki | = | 80.2 | nM | 7.10 |
| CHEMBL143800 | — | Ki | = | 81.3 | nM | 7.09 |
| CHEMBL109124 | — | Ki | = | 81.7 | nM | 7.09 |
| CHEMBL146659 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL110319 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL358527 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL38791 | — | Ki | > | 80.0 | nM | - |