Assay Detail
Functional
CHEMBL913690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum
5
Total Activities
5
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
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.90 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.11 |
| CHEMBL375068 | — | — | 1 | 7.80 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 7.76 |
| CHEMBL267211 | — | — | 1 | 5.46 |
| CHEMBL219108 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | IC50 | = | 7.71 | nM | 8.11 |
| CHEMBL375068 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL316446 | ENDOMORPHIN-1 | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL267211 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL219108 | — | IC50 | = | 4180.0 | nM | 5.38 |