Assay Detail
Binding
CHEMBL839712
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Inhibition of [3H]U-69593 binding to opioid receptor kappa from guinea pig brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.84 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607407 | — | — | 1 | 9.04 |
| CHEMBL607351 | — | — | 1 | 8.93 |
| CHEMBL607482 | — | — | 1 | 8.61 |
| CHEMBL607405 | — | — | 1 | 7.99 |
| CHEMBL326684 | — | — | 1 | 7.60 |
| CHEMBL607483 | — | — | 1 | 7.48 |
| CHEMBL607404 | — | — | 1 | 7.47 |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 7.21 |
| CHEMBL607406 | — | — | 1 | 7.08 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607407 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL607351 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL607482 | — | Ki | = | 2.46 | nM | 8.61 |
| CHEMBL607405 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL326684 | — | Ki | = | 25.2 | nM | 7.60 |
| CHEMBL607483 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL607404 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL963 | OXYMORPHONE | Ki | = | 61.6 | nM | 7.21 |
| CHEMBL607406 | — | Ki | = | 83.2 | nM | 7.08 |
| CHEMBL70 | MORPHINE | Ki | = | 113.0 | nM | 6.95 |