Assay Detail
Binding
CHEMBL2215009
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Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane after 2 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at the δ opioid receptor. Discovery of two highly potent and selective δ opioid agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.81 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206325 | — | — | 1 | 9.43 |
| CHEMBL2370152 | — | — | 1 | 9.01 |
| CHEMBL2206330 | — | — | 1 | 9.00 |
| CHEMBL191751 | — | — | 1 | 8.91 |
| CHEMBL2206326 | — | — | 1 | 8.81 |
| CHEMBL2206329 | — | — | 1 | 8.78 |
| CHEMBL2206323 | — | — | 1 | 8.73 |
| CHEMBL2206328 | — | — | 1 | 8.56 |
| CHEMBL31421 | — | — | 1 | 8.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206325 | — | Ki | = | 0.369 | nM | 9.43 |
| CHEMBL2370152 | — | Ki | = | 0.978 | nM | 9.01 |
| CHEMBL2206330 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL191751 | — | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL2206326 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL2206329 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL2206323 | — | Ki | = | 1.84 | nM | 8.73 |
| CHEMBL2206328 | — | Ki | = | 2.72 | nM | 8.56 |
| CHEMBL31421 | — | Ki | = | 8.39 | nM | 8.08 |