Assay Detail
Functional
CHEMBL891365
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Antagonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of DAMGO-induced effect on myenteric plexus longitudinal muscle contractions
6
Total Activities
6
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 |
|---|---|---|---|
| Kd | 6 | 7.64 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412922 | — | — | 1 | 8.59 |
| CHEMBL412924 | — | — | 1 | 8.18 |
| CHEMBL397177 | — | — | 1 | 7.60 |
| CHEMBL232303 | — | — | 1 | 7.23 |
| CHEMBL396506 | — | — | 1 | 7.17 |
| CHEMBL397176 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412922 | — | Kd | = | 2.57 | nM | 8.59 |
| CHEMBL412924 | — | Kd | = | 6.607 | nM | 8.18 |
| CHEMBL397177 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL232303 | — | Kd | = | 58.88 | nM | 7.23 |
| CHEMBL396506 | — | Kd | = | 67.61 | nM | 7.17 |
| CHEMBL397176 | — | Kd | = | 85.11 | nM | 7.07 |