Assay Detail
Binding
CHEMBL757511
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Ability to inhibit electrically induced contractions of guinea pig ileum having mu opioid receptors tested in vitro
8
Total Activities
8
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 | Intermediate |
Publication
Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.06 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23362 | — | — | 1 | 10.47 |
| CHEMBL23836 | — | — | 1 | 8.78 |
| CHEMBL24059 | — | — | 1 | 8.56 |
| CHEMBL22321 | — | — | 1 | 8.28 |
| CHEMBL280178 | — | — | 1 | 8.01 |
| CHEMBL23133 | — | — | 1 | 7.70 |
| CHEMBL23295 | — | — | 1 | 6.50 |
| CHEMBL23325 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23362 | — | IC50 | = | 0.034 | nM | 10.47 |
| CHEMBL23836 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL24059 | — | IC50 | = | 2.76 | nM | 8.56 |
| CHEMBL22321 | — | IC50 | = | 5.31 | nM | 8.28 |
| CHEMBL280178 | — | IC50 | = | 9.88 | nM | 8.01 |
| CHEMBL23133 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL23295 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL23325 | — | IC50 | = | 633.0 | nM | 6.20 |