Assay Detail
Binding
CHEMBL754005
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Inhibition of total opioid receptor by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.93 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 8.89 |
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.82 |
| CHEMBL140050 | ETORPHINE | 2.0 | 1 | 8.77 |
| CHEMBL2092986 | — | — | 1 | 8.66 |
| CHEMBL143815 | — | — | 1 | 8.62 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.24 |
| CHEMBL343167 | — | — | 1 | 7.99 |
| CHEMBL76023 | — | — | 1 | 7.96 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.96 |
| CHEMBL140278 | — | — | 1 | 7.89 |
| CHEMBL143416 | — | — | 1 | 7.85 |
| CHEMBL407685 | — | — | 1 | 7.66 |
| CHEMBL140044 | — | — | 1 | 7.57 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.37 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.33 |
| CHEMBL344420 | — | — | 1 | 7.10 |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 7.05 |
| CHEMBL140145 | — | — | 1 | 6.96 |
| CHEMBL140855 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL140050 | ETORPHINE | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2092986 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL143815 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL343167 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL76023 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL140278 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL143416 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL407685 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL140044 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL80 | NALOXONE | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL567175 | NALTRINDOLE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL344420 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL963 | OXYMORPHONE | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL140145 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL140855 | — | IC50 | > | 3000.0 | nM | - |