Assay Detail
Binding
CHEMBL1008807
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Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.17 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521582 | — | — | 1 | 8.62 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.25 |
| CHEMBL495519 | — | — | 1 | 7.55 |
| CHEMBL495520 | — | — | 1 | 7.48 |
| CHEMBL314424 | — | — | 1 | 7.35 |
| CHEMBL489601 | — | — | 1 | 7.34 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.29 |
| CHEMBL498600 | — | — | 1 | 7.25 |
| CHEMBL495726 | — | — | 1 | 7.12 |
| CHEMBL497586 | — | — | 1 | 7.12 |
| CHEMBL490424 | — | — | 1 | 7.09 |
| CHEMBL560 | — | — | 1 | 7.08 |
| CHEMBL507255 | — | — | 1 | 7.06 |
| CHEMBL496753 | — | — | 1 | 7.06 |
| CHEMBL502790 | — | — | 1 | 7.05 |
| CHEMBL505059 | — | — | 1 | 6.87 |
| CHEMBL443649 | — | — | 1 | 6.63 |
| CHEMBL444690 | — | — | 1 | 6.61 |
| CHEMBL487088 | — | — | 1 | 6.54 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521582 | — | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL495519 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL495520 | — | Ki | = | 33.4 | nM | 7.48 |
| CHEMBL314424 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL489601 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL281594 | VANOXERINE | Ki | = | 50.8 | nM | 7.29 |
| CHEMBL498600 | — | Ki | = | 56.6 | nM | 7.25 |
| CHEMBL495726 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL497586 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL490424 | — | Ki | = | 81.8 | nM | 7.09 |
| CHEMBL560 | — | Ki | = | 83.4 | nM | 7.08 |
| CHEMBL507255 | — | Ki | = | 87.4 | nM | 7.06 |
| CHEMBL496753 | — | Ki | = | 87.3 | nM | 7.06 |
| CHEMBL502790 | — | Ki | = | 88.3 | nM | 7.05 |
| CHEMBL505059 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL443649 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL444690 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL487088 | — | Ki | = | 292.0 | nM | 6.54 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 893.0 | nM | 6.05 |