Assay Detail
Binding
CHEMBL3614959
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69,593 from KOR in mouse whole brain membranes without cerebellum
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.93 | 9.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3613172 | — | — | 1 | 9.95 |
| CHEMBL3613173 | — | — | 1 | 9.87 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | 4.0 | 1 | 9.75 |
| CHEMBL3613171 | — | — | 1 | 9.69 |
| CHEMBL3613163 | — | — | 1 | 9.64 |
| CHEMBL3613165 | — | — | 1 | 9.62 |
| CHEMBL3613164 | — | — | 1 | 9.33 |
| CHEMBL3613174 | — | — | 1 | 9.27 |
| CHEMBL3613167 | — | — | 1 | 9.09 |
| CHEMBL3613169 | — | — | 1 | 8.76 |
| CHEMBL3613168 | — | — | 1 | 8.73 |
| CHEMBL3613166 | — | — | 1 | 8.35 |
| CHEMBL3613175 | — | — | 1 | 8.08 |
| CHEMBL3613281 | — | — | 1 | 7.96 |
| CHEMBL3613280 | — | — | 1 | 7.92 |
| CHEMBL3613170 | — | — | 1 | 7.88 |
| CHEMBL3613282 | — | — | 1 | 7.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3613172 | — | Ki | = | 0.113 | nM | 9.95 |
| CHEMBL3613173 | — | Ki | = | 0.136 | nM | 9.87 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | Ki | = | 0.178 | nM | 9.75 |
| CHEMBL3613171 | — | Ki | = | 0.204 | nM | 9.69 |
| CHEMBL3613163 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3613165 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL3613164 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL3613174 | — | Ki | = | 0.543 | nM | 9.27 |
| CHEMBL3613167 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL3613169 | — | Ki | = | 1.73 | nM | 8.76 |
| CHEMBL3613168 | — | Ki | = | 1.86 | nM | 8.73 |
| CHEMBL3613166 | — | Ki | = | 4.46 | nM | 8.35 |
| CHEMBL3613175 | — | Ki | = | 8.36 | nM | 8.08 |
| CHEMBL3613281 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3613280 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL3613170 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL3613282 | — | Ki | = | 13.8 | nM | 7.86 |