Assay Detail
Binding
CHEMBL907182
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Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain homogenate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.28 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.22 |
| CHEMBL267027 | — | — | 1 | 9.19 |
| CHEMBL443311 | — | — | 1 | 8.72 |
| CHEMBL217395 | — | — | 1 | 8.19 |
| CHEMBL216251 | — | — | 1 | 7.27 |
| CHEMBL384497 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL267027 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL443311 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL217395 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL216251 | — | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL384497 | — | Ki | = | 78.6 | nM | 7.11 |