Assay Detail
Binding
CHEMBL754625
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Binding affinity to opioid receptor kappa 1 of guinea pig brain, using [3H]U-69593 as radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.29 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51204 | — | — | 1 | 9.49 |
| CHEMBL10986 | — | — | 1 | 8.42 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51204 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL10986 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 109.0 | nM | 6.96 |