Assay Detail
Binding
CHEMBL1676916
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Displacement of [3H]DTG from sigma 2 receptor in Wistar Hannover rat liver membrane in presence of (+)-pentazocine
18
Total Activities
18
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
Analogues of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.18 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL73854 | — | — | 1 | 9.31 |
| CHEMBL53325 | — | — | 1 | 9.17 |
| CHEMBL419822 | — | — | 1 | 8.93 |
| CHEMBL1672043 | — | — | 1 | 8.62 |
| CHEMBL1672039 | — | — | 1 | 8.33 |
| CHEMBL1672032 | — | — | 1 | 8.23 |
| CHEMBL1672035 | — | — | 1 | 8.07 |
| CHEMBL1672033 | — | — | 1 | 8.07 |
| CHEMBL1672037 | — | — | 1 | 8.04 |
| CHEMBL1672040 | — | — | 1 | 8.01 |
| CHEMBL1672031 | — | — | 1 | 8.00 |
| CHEMBL1672038 | — | — | 1 | 7.96 |
| CHEMBL1672030 | — | — | 1 | 7.88 |
| CHEMBL1672034 | — | — | 1 | 7.84 |
| CHEMBL1672036 | — | — | 1 | 7.82 |
| CHEMBL1672042 | — | — | 1 | 7.73 |
| CHEMBL1672041 | — | — | 1 | 7.63 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL73854 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL53325 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL419822 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL1672043 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1672039 | — | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL1672032 | — | Ki | = | 5.92 | nM | 8.23 |
| CHEMBL1672035 | — | Ki | = | 8.52 | nM | 8.07 |
| CHEMBL1672033 | — | Ki | = | 8.49 | nM | 8.07 |
| CHEMBL1672037 | — | Ki | = | 9.03 | nM | 8.04 |
| CHEMBL1672040 | — | Ki | = | 9.72 | nM | 8.01 |
| CHEMBL1672031 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL1672038 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL1672030 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL1672034 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL1672036 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL1672042 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL1672041 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 25.7 | nM | 7.59 |