Assay Detail
Functional
CHEMBL758272
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration for inhibition of Opioid receptor mu 1 induced contractions in guinea pig ileum (GPI) smooth muscle assays
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.54 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL283287 | — | — | 1 | 7.23 |
| CHEMBL611687 | — | — | 1 | 7.17 |
| CHEMBL611432 | — | — | 1 | 7.01 |
| CHEMBL610262 | — | — | 1 | 6.96 |
| CHEMBL610261 | — | — | 1 | 6.79 |
| CHEMBL611688 | — | — | 1 | 6.75 |
| CHEMBL611434 | — | — | 1 | 6.68 |
| CHEMBL611437 | — | — | 1 | 6.35 |
| CHEMBL611435 | — | — | 1 | 6.28 |
| CHEMBL611431 | — | — | 1 | 6.18 |
| CHEMBL611685 | — | — | 1 | 6.14 |
| CHEMBL31421 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL283287 | — | IC50 | = | 59.4 | nM | 7.23 |
| CHEMBL611687 | — | IC50 | = | 67.7 | nM | 7.17 |
| CHEMBL611432 | — | IC50 | = | 98.7 | nM | 7.01 |
| CHEMBL610262 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL610261 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL611688 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL611434 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL611437 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL611435 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL611431 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL611685 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL31421 | — | IC50 | = | 11600.0 | nM | 4.94 |