Assay Detail
Functional
CHEMBL751917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonistic activity towards Opioid receptor delta 1
10
Total Activities
10
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 | 10 | 7.56 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 9.96 |
| CHEMBL109040 | — | — | 1 | 8.38 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.26 |
| CHEMBL110461 | — | — | 1 | 7.66 |
| CHEMBL108608 | — | — | 1 | 7.37 |
| CHEMBL110124 | — | — | 1 | 7.14 |
| CHEMBL322875 | — | — | 1 | 7.04 |
| CHEMBL107207 | — | — | 1 | 6.68 |
| CHEMBL320306 | — | — | 1 | 6.66 |
| CHEMBL107420 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL109040 | — | EC50 | = | 4.19 | nM | 8.38 |
| CHEMBL19019 | NALTREXONE | EC50 | = | 5.44 | nM | 8.26 |
| CHEMBL110461 | — | EC50 | = | 21.8 | nM | 7.66 |
| CHEMBL108608 | — | EC50 | = | 42.6 | nM | 7.37 |
| CHEMBL110124 | — | EC50 | = | 72.3 | nM | 7.14 |
| CHEMBL322875 | — | EC50 | = | 90.1 | nM | 7.04 |
| CHEMBL107207 | — | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL320306 | — | EC50 | = | 221.0 | nM | 6.66 |
| CHEMBL107420 | — | EC50 | = | 368.0 | nM | 6.43 |