Assay Detail
Binding
CHEMBL755008
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Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO 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 | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 8.36 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140050 | ETORPHINE | 2.0 | 1 | 9.32 |
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.15 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.14 |
| CHEMBL143815 | — | — | 1 | 9.12 |
| CHEMBL2092986 | — | — | 1 | 9.00 |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 8.85 |
| CHEMBL343167 | — | — | 1 | 8.82 |
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.74 |
| CHEMBL140278 | — | — | 1 | 8.66 |
| CHEMBL140145 | — | — | 1 | 8.62 |
| CHEMBL76023 | — | — | 1 | 8.60 |
| CHEMBL143416 | — | — | 1 | 8.55 |
| CHEMBL140044 | — | — | 1 | 8.55 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.05 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.75 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.43 |
| CHEMBL407685 | — | — | 1 | 7.33 |
| CHEMBL344420 | — | — | 1 | 7.02 |
| CHEMBL140855 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140050 | ETORPHINE | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL281786 | DIPRENORPHINE | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL143815 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL2092986 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL963 | OXYMORPHONE | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL343167 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL140278 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL140145 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL76023 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL143416 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL140044 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL80 | NALOXONE | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL567175 | NALTRINDOLE | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL407685 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL344420 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL140855 | — | IC50 | = | 840.0 | nM | 6.08 |