Assay Detail
Binding
CHEMBL850001
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Ratio of mu/delta-opioid receptors Binding affinity
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 | 9.01 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 10.70 |
| CHEMBL109040 | — | — | 1 | 10.10 |
| CHEMBL108608 | — | — | 1 | 9.40 |
| CHEMBL107420 | — | — | 1 | 9.22 |
| CHEMBL110124 | — | — | 1 | 9.10 |
| CHEMBL320306 | — | — | 1 | 8.82 |
| CHEMBL107207 | — | — | 1 | 8.49 |
| CHEMBL110461 | — | — | 1 | 8.46 |
| CHEMBL322875 | — | — | 1 | 8.31 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL109040 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL108608 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL107420 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL110124 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL320306 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL107207 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL110461 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL322875 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 31.5 | nM | 7.50 |