Assay Detail
Functional
CHEMBL681790
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Irreversible antagonistic potency in guinea pig ileal longitudinal muscle (GPI)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Muscle tissue |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Importance of C-6 chirality in conferring irreversible opioid antagonism to naltrexone-derived affinity labels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.61 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278086 | ETHYLKETAZOCINE | — | 1 | 9.01 |
| CHEMBL415284 | NALORPHINE | 2.0 | 1 | 7.29 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278086 | ETHYLKETAZOCINE | IC50 | = | 0.973 | nM | 9.01 |
| CHEMBL415284 | NALORPHINE | IC50 | = | 51.3 | nM | 7.29 |
| CHEMBL70 | MORPHINE | IC50 | = | 292.0 | nM | 6.54 |