Assay Detail
Binding
CHEMBL873301
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Binding affinity against opioid receptor mu by displacement of radioligand [3H]DAGO in rat brain membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.48 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2371282 | — | — | 1 | 8.92 |
| CHEMBL60444 | — | — | 1 | 8.77 |
| CHEMBL436434 | — | — | 1 | 8.24 |
| CHEMBL2371283 | — | — | 1 | 7.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2371282 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL60444 | — | Ki | = | 1.69 | nM | 8.77 |
| CHEMBL436434 | — | Ki | = | 5.78 | nM | 8.24 |
| CHEMBL2371283 | — | Ki | = | 10.4 | nM | 7.98 |