Assay Detail
Binding
CHEMBL754932
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Inhibition of [3H][p-Cl-Phe-]DPDE binding to rat brain homogenate delta-opioid receptor
12
Total Activities
11
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
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.49 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32202 | — | — | 1 | 9.33 |
| CHEMBL317956 | DELTORPHIN C | — | 2 | 9.22 |
| CHEMBL289006 | — | — | 1 | 9.06 |
| CHEMBL286629 | — | — | 1 | 8.66 |
| CHEMBL2372214 | — | — | 1 | 8.47 |
| CHEMBL288317 | — | — | 1 | 8.43 |
| CHEMBL2372212 | — | — | 1 | 8.32 |
| CHEMBL2372209 | — | — | 1 | 8.29 |
| CHEMBL2372208 | — | — | 1 | 8.24 |
| CHEMBL2372213 | — | — | 1 | 8.00 |
| CHEMBL284621 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32202 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL289006 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL286629 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2372214 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL288317 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2372212 | — | IC50 | = | 4.83 | nM | 8.32 |
| CHEMBL2372209 | — | IC50 | = | 5.11 | nM | 8.29 |
| CHEMBL2372208 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2372213 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL284621 | — | IC50 | = | 210.0 | nM | 6.68 |