Assay Detail
Functional
CHEMBL904997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Tissue | Vas deferens |
| 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 | 14 | 7.81 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374818 | — | — | 1 | 9.29 |
| CHEMBL331325 | — | — | 1 | 9.23 |
| CHEMBL266122 | — | — | 1 | 8.86 |
| CHEMBL228516 | — | — | 1 | 8.26 |
| CHEMBL413676 | — | — | 1 | 7.80 |
| CHEMBL375274 | — | — | 1 | 6.56 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 6.46 |
| CHEMBL228512 | — | — | 1 | 6.01 |
| CHEMBL228503 | — | — | 1 | - |
| CHEMBL389023 | — | — | 1 | - |
| CHEMBL388800 | — | — | 1 | - |
| CHEMBL389949 | — | — | 1 | - |
| CHEMBL413892 | — | — | 1 | - |
| CHEMBL389948 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374818 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL331325 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL266122 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL228516 | — | IC50 | = | 5.56 | nM | 8.26 |
| CHEMBL413676 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL375274 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL333357 | ENDOMORPHIN 2 | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL228512 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL228503 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL389023 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL388800 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL389949 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL413892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL389948 | — | IC50 | > | 10000.0 | nM | - |