Assay Detail
Binding
CHEMBL2183134
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Displacement of [3H]U69593 from KOR in guinea pig brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.92 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179259 | — | — | 1 | 9.30 |
| CHEMBL2179264 | — | — | 1 | 9.30 |
| CHEMBL2179258 | — | — | 1 | 9.10 |
| CHEMBL473136 | — | — | 1 | 9.05 |
| CHEMBL2179262 | — | — | 1 | 8.89 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 8.82 |
| CHEMBL2179260 | — | — | 1 | 8.72 |
| CHEMBL2179263 | — | — | 1 | 8.59 |
| CHEMBL2179261 | — | — | 1 | 8.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179259 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2179264 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2179258 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL473136 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2179262 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2179260 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2179263 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2179261 | — | Ki | = | 2.8 | nM | 8.55 |