Assay Detail
Binding
CHEMBL904992
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Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosome membrane
16
Total Activities
16
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
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.93 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228503 | — | — | 1 | 8.74 |
| CHEMBL228409 | — | — | 1 | 8.64 |
| CHEMBL374818 | — | — | 1 | 8.52 |
| CHEMBL228516 | — | — | 1 | 8.34 |
| CHEMBL389948 | — | — | 1 | 8.34 |
| CHEMBL389949 | — | — | 1 | 7.94 |
| CHEMBL388800 | — | — | 1 | 7.09 |
| CHEMBL331325 | — | — | 1 | 7.00 |
| CHEMBL375274 | — | — | 1 | 6.31 |
| CHEMBL434559 | — | — | 1 | 6.26 |
| CHEMBL389023 | — | — | 1 | 5.87 |
| CHEMBL266122 | — | — | 1 | 5.84 |
| CHEMBL413676 | — | — | 1 | 5.76 |
| CHEMBL228512 | — | — | 1 | 5.52 |
| CHEMBL413892 | — | — | 1 | 5.46 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228503 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL228409 | — | Ki | = | 2.27 | nM | 8.64 |
| CHEMBL374818 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL228516 | — | Ki | = | 4.61 | nM | 8.34 |
| CHEMBL389948 | — | Ki | = | 4.61 | nM | 8.34 |
| CHEMBL389949 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL388800 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL331325 | — | Ki | = | 99.2 | nM | 7.00 |
| CHEMBL375274 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL434559 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL389023 | — | Ki | = | 1358.0 | nM | 5.87 |
| CHEMBL266122 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL413676 | — | Ki | = | 1741.0 | nM | 5.76 |
| CHEMBL228512 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL413892 | — | Ki | = | 3451.0 | nM | 5.46 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 6085.0 | nM | 5.22 |