Assay Detail
Binding
CHEMBL751262
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Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | ovary |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.89 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 9.70 |
| CHEMBL109040 | — | — | 1 | 8.26 |
| CHEMBL110124 | — | — | 1 | 8.25 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.97 |
| CHEMBL110461 | — | — | 1 | 7.90 |
| CHEMBL108608 | — | — | 1 | 7.80 |
| CHEMBL107420 | — | — | 1 | 7.63 |
| CHEMBL322875 | — | — | 1 | 7.29 |
| CHEMBL320306 | — | — | 1 | 7.08 |
| CHEMBL107207 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL109040 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL110124 | — | Ki | = | 5.66 | nM | 8.25 |
| CHEMBL19019 | NALTREXONE | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL110461 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL108608 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL107420 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL322875 | — | Ki | = | 51.4 | nM | 7.29 |
| CHEMBL320306 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL107207 | — | Ki | = | 103.0 | nM | 6.99 |