Assay Detail
Binding
CHEMBL754730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U-69593 at opioid receptor kappa 1
13
Total Activities
13
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
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.94 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1237164 | NALTRINDOLE HYDROCHLORIDE | — | 1 | 7.52 |
| CHEMBL611695 | — | — | 1 | 6.42 |
| CHEMBL608241 | — | — | 1 | 6.19 |
| CHEMBL611703 | — | — | 1 | 6.17 |
| CHEMBL611700 | — | — | 1 | 6.05 |
| CHEMBL611702 | — | — | 1 | 6.02 |
| CHEMBL611701 | — | — | 1 | 5.70 |
| CHEMBL611704 | — | — | 1 | 5.52 |
| CHEMBL611699 | — | — | 1 | 5.51 |
| CHEMBL611696 | — | — | 1 | 5.50 |
| CHEMBL611697 | — | — | 1 | 5.42 |
| CHEMBL611698 | — | — | 1 | 5.21 |
| CHEMBL611705 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1237164 | NALTRINDOLE HYDROCHLORIDE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL611695 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL608241 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL611703 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL611700 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL611702 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL611701 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL611704 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL611699 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL611696 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL611697 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL611698 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL611705 | — | Ki | > | 7000.0 | nM | - |