Assay Detail
Binding
CHEMBL756701
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Binding affinity towards mu receptor in rat brain using [3H]DAMGO
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.75 | 8.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.69 |
| CHEMBL338198 | — | — | 1 | 8.19 |
| CHEMBL339725 | — | — | 1 | 8.11 |
| CHEMBL126611 | — | — | 1 | 8.07 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | — | 1 | 8.03 |
| CHEMBL2370620 | — | — | 1 | 7.45 |
| CHEMBL126794 | — | — | 1 | 7.42 |
| CHEMBL339724 | — | — | 1 | 7.33 |
| CHEMBL129323 | — | — | 1 | 7.23 |
| CHEMBL338113 | — | — | 1 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 2.06 | nM | 8.69 |
| CHEMBL338198 | — | Ki | = | 6.41 | nM | 8.19 |
| CHEMBL339725 | — | Ki | = | 7.86 | nM | 8.11 |
| CHEMBL126611 | — | Ki | = | 8.57 | nM | 8.07 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | Ki | = | 9.43 | nM | 8.03 |
| CHEMBL2370620 | — | Ki | = | 35.2 | nM | 7.45 |
| CHEMBL126794 | — | Ki | = | 37.7 | nM | 7.42 |
| CHEMBL339724 | — | Ki | = | 46.9 | nM | 7.33 |
| CHEMBL129323 | — | Ki | = | 58.9 | nM | 7.23 |
| CHEMBL338113 | — | Ki | = | 96.5 | nM | 7.01 |