Assay Detail
Functional
CHEMBL686357
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for the inhibition concentration in the guinea pig ileal longitudinal muscle preparation (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
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different mu receptor subtypes in different tissues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.69 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.54 |
| CHEMBL278086 | ETHYLKETAZOCINE | — | 1 | 8.01 |
| CHEMBL283898 | 6beta-[(Chloromercuri)acetamido]-17-(cyclopropyl-methyl)-4,5alpha-epoxy-3,14-duhydroxymorphinan Methanesulphonate | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | IC50 | = | 2.92 | nM | 8.54 |
| CHEMBL278086 | ETHYLKETAZOCINE | IC50 | = | 9.73 | nM | 8.01 |
| CHEMBL283898 | 6beta-[(Chloromercuri)acetamido]-17-(cyclopropyl-methyl)-4,5alpha-epoxy-3,14-duhydroxymorphinan Methanesulphonate | IC50 | = | 300.0 | nM | 6.52 |