Assay Detail
Functional
CHEMBL904996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
16
Total Activities
16
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
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.75 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228409 | — | — | 1 | 9.92 |
| CHEMBL389948 | — | — | 1 | 9.80 |
| CHEMBL374818 | — | — | 1 | 9.77 |
| CHEMBL228516 | — | — | 1 | 9.70 |
| CHEMBL228503 | — | — | 1 | 9.68 |
| CHEMBL331325 | — | — | 1 | 9.59 |
| CHEMBL266122 | — | — | 1 | 9.42 |
| CHEMBL413676 | — | — | 1 | 8.88 |
| CHEMBL389023 | — | — | 1 | 8.72 |
| CHEMBL388800 | — | — | 1 | 8.71 |
| CHEMBL375274 | — | — | 1 | 8.63 |
| CHEMBL434559 | — | — | 1 | 8.56 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.16 |
| CHEMBL389949 | — | — | 1 | 7.84 |
| CHEMBL413892 | — | — | 1 | 6.41 |
| CHEMBL228512 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228409 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL389948 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL374818 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL228516 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL228503 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL331325 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL266122 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL413676 | — | IC50 | = | 1.33 | nM | 8.88 |
| CHEMBL389023 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL388800 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL375274 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL434559 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL333357 | ENDOMORPHIN 2 | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL389949 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL413892 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL228512 | — | IC50 | = | 541.0 | nM | 6.27 |