Assay Detail
Binding
CHEMBL754734
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Binding affinity for kappa opioid receptor was evaluated by displacing [3H]- diprenorphine
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.04 | 7.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 7.69 |
| CHEMBL55033 | — | — | 1 | 6.73 |
| CHEMBL54329 | — | — | 1 | 6.62 |
| CHEMBL52307 | — | — | 1 | 6.06 |
| CHEMBL607263 | — | — | 1 | 5.95 |
| CHEMBL54581 | — | — | 1 | 5.58 |
| CHEMBL54780 | — | — | 1 | 5.35 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 5.19 |
| CHEMBL293135 | — | — | 1 | 5.19 |
| CHEMBL301066 | — | — | 1 | - |
| CHEMBL53216 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL55033 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL54329 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL52307 | — | Ki | = | 866.0 | nM | 6.06 |
| CHEMBL607263 | — | Ki | = | 1116.0 | nM | 5.95 |
| CHEMBL54581 | — | Ki | = | 2640.0 | nM | 5.58 |
| CHEMBL54780 | — | Ki | = | 4425.0 | nM | 5.35 |
| CHEMBL70 | MORPHINE | Ki | = | 6424.0 | nM | 5.19 |
| CHEMBL293135 | — | Ki | = | 6428.0 | nM | 5.19 |
| CHEMBL301066 | — | Ki | > | 25000.0 | nM | - |
| CHEMBL53216 | — | Ki | > | 25000.0 | nM | - |