Assay Detail
Binding
CHEMBL759292
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Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593
8
Total Activities
8
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
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.80 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.55 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.33 |
| CHEMBL10986 | — | — | 1 | 8.16 |
| CHEMBL151243 | — | — | 1 | 8.05 |
| CHEMBL148843 | — | — | 1 | 7.26 |
| CHEMBL359088 | — | — | 1 | 7.08 |
| CHEMBL149611 | — | — | 1 | 7.05 |
| CHEMBL150052 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL19019 | NALTREXONE | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL10986 | — | Ki | = | 6.91 | nM | 8.16 |
| CHEMBL151243 | — | Ki | = | 8.84 | nM | 8.05 |
| CHEMBL148843 | — | Ki | = | 54.6 | nM | 7.26 |
| CHEMBL359088 | — | Ki | = | 83.1 | nM | 7.08 |
| CHEMBL149611 | — | Ki | = | 89.3 | nM | 7.05 |
| CHEMBL150052 | — | Ki | = | 122.0 | nM | 6.91 |