Assay Detail
Functional
CHEMBL891364
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Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Intestine |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.71 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412923 | — | — | 1 | 9.57 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 8.39 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.16 |
| CHEMBL396506 | — | — | 1 | - |
| CHEMBL232303 | — | — | 1 | - |
| CHEMBL412924 | — | — | 1 | - |
| CHEMBL397177 | — | — | 1 | - |
| CHEMBL412922 | — | — | 1 | - |
| CHEMBL397176 | — | — | 1 | - |
| CHEMBL266988 | — | — | 1 | - |
| CHEMBL412921 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412923 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL316446 | ENDOMORPHIN-1 | IC50 | = | 4.03 | nM | 8.39 |
| CHEMBL333357 | ENDOMORPHIN 2 | IC50 | = | 6.88 | nM | 8.16 |
| CHEMBL396506 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL232303 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL412924 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL397177 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL412922 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL397176 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL266988 | — | IC50 | - | — | - | |
| CHEMBL412921 | — | IC50 | - | — | - |