Assay Detail
Functional
CHEMBL754922
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Agonistic activity towards Opioid receptor kappa 1
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| EC50 | 9 | 7.18 | 8.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.73 |
| CHEMBL110124 | — | — | 1 | 8.47 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.30 |
| CHEMBL109040 | — | — | 1 | 7.76 |
| CHEMBL107420 | — | — | 1 | 7.08 |
| CHEMBL108608 | — | — | 1 | 6.49 |
| CHEMBL107207 | — | — | 1 | 6.06 |
| CHEMBL322875 | — | — | 1 | 6.03 |
| CHEMBL110461 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | EC50 | = | 1.86 | nM | 8.73 |
| CHEMBL110124 | — | EC50 | = | 3.38 | nM | 8.47 |
| CHEMBL567175 | NALTRINDOLE | EC50 | = | 4.95 | nM | 8.30 |
| CHEMBL109040 | — | EC50 | = | 17.5 | nM | 7.76 |
| CHEMBL107420 | — | EC50 | = | 82.4 | nM | 7.08 |
| CHEMBL108608 | — | EC50 | = | 323.0 | nM | 6.49 |
| CHEMBL107207 | — | EC50 | = | 866.0 | nM | 6.06 |
| CHEMBL322875 | — | EC50 | = | 945.0 | nM | 6.03 |
| CHEMBL110461 | — | EC50 | = | 2046.0 | nM | 5.69 |