Assay Detail
Binding
CHEMBL828016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of bound [3H]diprenorphine from membranes expressing cloned human kappa opioid receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.80 | 10.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL86324 | — | — | 1 | 10.24 |
| CHEMBL183248 | — | — | 1 | 9.51 |
| CHEMBL365486 | — | — | 1 | 9.44 |
| CHEMBL181279 | — | — | 1 | 9.36 |
| CHEMBL362248 | — | — | 1 | 9.32 |
| CHEMBL180803 | — | — | 1 | 9.28 |
| CHEMBL365198 | — | — | 1 | 9.20 |
| CHEMBL23472 | ICI-204448 | — | 1 | 8.57 |
| CHEMBL360678 | — | — | 1 | 8.54 |
| CHEMBL185554 | — | — | 1 | 8.43 |
| CHEMBL181922 | — | — | 1 | 8.02 |
| CHEMBL362458 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL86324 | — | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL183248 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL365486 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL181279 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL362248 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL180803 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL365198 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL23472 | ICI-204448 | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL360678 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL185554 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL181922 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL362458 | — | Ki | = | 2300.0 | nM | 5.64 |