Assay Detail
Binding
CHEMBL904994
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Displacement of [3H]U-69593 from kappa opioid receptor in Hartley guinea pig cerebellum P2 synaptosome membrane
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| 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 | 6.52 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228409 | — | — | 1 | 7.03 |
| CHEMBL228503 | — | — | 1 | 6.76 |
| CHEMBL389948 | — | — | 1 | 6.75 |
| CHEMBL228516 | — | — | 1 | 6.69 |
| CHEMBL374818 | — | — | 1 | 6.56 |
| CHEMBL331325 | — | — | 1 | 6.31 |
| CHEMBL389949 | — | — | 1 | 6.08 |
| CHEMBL388800 | — | — | 1 | 6.00 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | - |
| CHEMBL434559 | — | — | 1 | - |
| CHEMBL375274 | — | — | 1 | - |
| CHEMBL389023 | — | — | 1 | - |
| CHEMBL228512 | — | — | 1 | - |
| CHEMBL266122 | — | — | 1 | - |
| CHEMBL413892 | — | — | 1 | - |
| CHEMBL413676 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228409 | — | Ki | = | 94.2 | nM | 7.03 |
| CHEMBL228503 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL389948 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL228516 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL374818 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL331325 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL389949 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL388800 | — | Ki | = | 998.0 | nM | 6.00 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | > | 4000.0 | nM | - |
| CHEMBL434559 | — | Ki | - | — | - | |
| CHEMBL375274 | — | Ki | - | — | - | |
| CHEMBL389023 | — | Ki | - | — | - | |
| CHEMBL228512 | — | Ki | - | — | - | |
| CHEMBL266122 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL413892 | — | Ki | - | — | - | |
| CHEMBL413676 | — | Ki | - | — | - |