Assay Detail
Functional
CHEMBL758066
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In vitro biological activity by electrically induced smooth muscle contractions in guinea pig ileum (Opioid receptor mu 1); inhibitory concentration was evaluated
6
Total Activities
6
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 | Intermediate |
Publication
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.70 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL355178 | — | — | 1 | 8.92 |
| CHEMBL278789 | DERMORPHIN | — | 1 | 8.43 |
| CHEMBL168110 | — | — | 1 | 7.35 |
| CHEMBL317956 | DELTORPHIN C | — | 1 | 5.26 |
| CHEMBL169860 | — | — | 1 | 5.17 |
| CHEMBL169439 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL355178 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL278789 | DERMORPHIN | IC50 | = | 3.74 | nM | 8.43 |
| CHEMBL168110 | — | IC50 | = | 44.4 | nM | 7.35 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 5437.0 | nM | 5.26 |
| CHEMBL169860 | — | IC50 | = | 6705.0 | nM | 5.17 |
| CHEMBL169439 | — | IC50 | = | 8214.0 | nM | 5.08 |