Assay Detail
Binding
CHEMBL757977
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Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes
13
Total Activities
13
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
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.88 | 9.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL606603 | — | — | 1 | 9.63 |
| CHEMBL607479 | — | — | 1 | 9.39 |
| CHEMBL109390 | — | — | 1 | 9.30 |
| CHEMBL278789 | DERMORPHIN | — | 1 | 8.91 |
| CHEMBL607403 | — | — | 1 | 8.26 |
| CHEMBL607480 | — | — | 1 | 8.16 |
| CHEMBL607401 | — | — | 1 | 7.66 |
| CHEMBL607402 | — | — | 1 | 7.33 |
| CHEMBL606601 | — | — | 1 | 7.32 |
| CHEMBL442577 | — | — | 1 | 7.27 |
| CHEMBL607481 | — | — | 1 | 7.09 |
| CHEMBL26861 | — | — | 1 | 6.57 |
| CHEMBL606602 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL606603 | — | Ki | = | 0.233 | nM | 9.63 |
| CHEMBL607479 | — | Ki | = | 0.411 | nM | 9.39 |
| CHEMBL109390 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL278789 | DERMORPHIN | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL607403 | — | Ki | = | 5.49 | nM | 8.26 |
| CHEMBL607480 | — | Ki | = | 6.92 | nM | 8.16 |
| CHEMBL607401 | — | Ki | = | 21.68 | nM | 7.66 |
| CHEMBL607402 | — | Ki | = | 47.1 | nM | 7.33 |
| CHEMBL606601 | — | Ki | = | 47.5 | nM | 7.32 |
| CHEMBL442577 | — | Ki | = | 53.9 | nM | 7.27 |
| CHEMBL607481 | — | Ki | = | 80.3 | nM | 7.09 |
| CHEMBL26861 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL606602 | — | Ki | = | 2565.0 | nM | 5.59 |