Assay Detail
Binding
CHEMBL748774
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The opioid receptor affinity(Ki) was evaluated by competition with [3H]DAMGO (mu) on guinea pig brain membranes
7
Total Activities
7
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 | Intermediate |
Publication
7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.02 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.42 |
| CHEMBL132420 | — | — | 1 | 7.62 |
| CHEMBL132897 | — | — | 1 | 6.87 |
| CHEMBL422258 | — | — | 1 | 6.69 |
| CHEMBL335936 | — | — | 1 | 6.66 |
| CHEMBL334715 | — | — | 1 | 6.48 |
| CHEMBL334970 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL132420 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL132897 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL422258 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL335936 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL334715 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL334970 | — | Ki | = | 368.0 | nM | 6.43 |