Assay Detail
Functional
CHEMBL4685304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effect on MOR/DOR in Wistar rat brain membranes measured after 60 mins by [35S]GTPgammaS binding based liquid scintillation counting analysis
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Opioid receptors; mu & delta (CHEMBL2095155) ↗| Type | SELECTIVITY GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.65 | 9.02 |
| pEC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4751305 | — | — | 1 | 9.02 |
| CHEMBL4762529 | — | — | 1 | 8.99 |
| CHEMBL4776706 | — | — | 1 | 8.71 |
| CHEMBL4753839 | — | — | 1 | 8.01 |
| CHEMBL4745764 | — | — | 1 | 7.77 |
| CHEMBL4787652 | — | — | 1 | 7.09 |
| CHEMBL4764372 | — | — | 1 | 6.94 |
| CHEMBL4758369 | — | — | 1 | 6.39 |
| CHEMBL4758814 | — | — | 1 | 5.96 |
| CHEMBL4754079 | — | — | 1 | - |
| CHEMBL4752367 | — | — | 1 | - |
| CHEMBL4746512 | — | — | 1 | - |
| CHEMBL4761619 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4751305 | — | EC50 | = | 0.955 | nM | 9.02 |
| CHEMBL4762529 | — | EC50 | = | 1.023 | nM | 8.99 |
| CHEMBL4776706 | — | EC50 | = | 1.95 | nM | 8.71 |
| CHEMBL4753839 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL4745764 | — | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL4787652 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL4764372 | — | EC50 | = | 114.82 | nM | 6.94 |
| CHEMBL4758369 | — | EC50 | = | 407.38 | nM | 6.39 |
| CHEMBL4758814 | — | EC50 | = | 1096.48 | nM | 5.96 |
| CHEMBL4754079 | — | pEC50 | - | — | - | |
| CHEMBL4752367 | — | pEC50 | - | — | - | |
| CHEMBL4746512 | — | pEC50 | - | — | - | |
| CHEMBL4761619 | — | pEC50 | - | — | - |