Assay Detail
Binding
CHEMBL2387948
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Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Effect of anchoring 4-anilidopiperidines to opioid peptides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.14 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 8.92 |
| CHEMBL2387215 | — | — | 1 | 8.42 |
| CHEMBL2387216 | — | — | 1 | 8.11 |
| CHEMBL200199 | BIPHALIN | — | 1 | 8.06 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 7.96 |
| CHEMBL2387327 | — | — | 1 | 7.92 |
| CHEMBL214022 | — | — | 1 | 7.38 |
| CHEMBL2387211 | — | — | 1 | 7.31 |
| CHEMBL2387328 | — | — | 1 | 7.17 |
| CHEMBL2387341 | — | — | 1 | 7.07 |
| CHEMBL2387339 | — | — | 1 | 7.01 |
| CHEMBL2387213 | — | — | 1 | 7.01 |
| CHEMBL2387337 | — | — | 1 | 6.96 |
| CHEMBL2387214 | — | — | 1 | 6.92 |
| CHEMBL2387329 | — | — | 1 | 6.89 |
| CHEMBL2387210 | — | — | 1 | 6.82 |
| CHEMBL2387330 | — | — | 1 | 6.32 |
| CHEMBL2387340 | — | — | 1 | 6.24 |
| CHEMBL2387338 | — | — | 1 | 6.02 |
| CHEMBL2387212 | — | — | 1 | 5.72 |
| CHEMBL2387331 | — | — | 1 | 5.68 |
| CHEMBL20226 | DELTORPHIN II | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2387215 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2387216 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL200199 | BIPHALIN | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL316446 | ENDOMORPHIN-1 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2387327 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL214022 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2387211 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2387328 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2387341 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2387339 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL2387213 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2387337 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2387214 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2387329 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2387210 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2387330 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2387340 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2387338 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2387212 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2387331 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL20226 | DELTORPHIN II | IC50 | > | 3000.0 | nM | - |