Assay Detail
Binding
CHEMBL810659
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Inhibition of [3H](+)-pentazocine binding to Sigma opioid receptor of guiena pig brain membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.31 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60133 | — | — | 1 | 7.82 |
| CHEMBL53038 | — | — | 1 | 7.75 |
| CHEMBL64751 | — | — | 1 | 7.66 |
| CHEMBL62638 | — | — | 1 | 7.55 |
| CHEMBL60140 | — | — | 1 | 6.72 |
| CHEMBL305366 | — | — | 1 | 6.56 |
| CHEMBL61789 | — | — | 1 | 6.12 |
| CHEMBL59713 | — | — | 1 | 6.09 |
| CHEMBL60139 | — | — | 1 | 5.94 |
| CHEMBL64176 | — | — | 1 | 5.53 |
| CHEMBL60048 | — | — | 1 | 5.51 |
| CHEMBL64261 | — | — | 1 | 5.26 |
| CHEMBL64260 | — | — | 1 | 4.98 |
| CHEMBL291439 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60133 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL53038 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL64751 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL62638 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL60140 | — | Ki | = | 189.1 | nM | 6.72 |
| CHEMBL305366 | — | Ki | = | 276.5 | nM | 6.56 |
| CHEMBL61789 | — | Ki | = | 751.0 | nM | 6.12 |
| CHEMBL59713 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL60139 | — | Ki | = | 1159.0 | nM | 5.94 |
| CHEMBL64176 | — | Ki | = | 2932.0 | nM | 5.53 |
| CHEMBL60048 | — | Ki | = | 3078.0 | nM | 5.51 |
| CHEMBL64261 | — | Ki | = | 5484.0 | nM | 5.26 |
| CHEMBL64260 | — | Ki | = | 10412.0 | nM | 4.98 |
| CHEMBL291439 | — | Ki | = | 12900.0 | nM | 4.89 |