Assay Detail
Binding
CHEMBL850000
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Ratio of kappa/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 |
Target
Opioid receptors; delta & kappa (CHEMBL2095151) ↗| Type | SELECTIVITY GROUP |
| Organism | Homo sapiens |
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 | 9.22 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL110124 | — | — | 1 | 10.70 |
| CHEMBL107420 | — | — | 1 | 10.52 |
| CHEMBL109040 | — | — | 1 | 10.40 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 10.40 |
| CHEMBL107207 | — | — | 1 | 9.52 |
| CHEMBL108608 | — | — | 1 | 8.66 |
| CHEMBL320306 | — | — | 1 | 8.54 |
| CHEMBL110461 | — | — | 1 | 8.12 |
| CHEMBL322875 | — | — | 1 | 8.07 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL110124 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL107420 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL109040 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL107207 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL108608 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL320306 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL110461 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL322875 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 50.5 | nM | 7.30 |