Assay Detail
Binding
CHEMBL753523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of opioid receptor kappa 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 | 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 | 7.69 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.92 |
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 8.74 |
| CHEMBL140050 | ETORPHINE | 2.0 | 1 | 8.47 |
| CHEMBL2092986 | — | — | 1 | 8.44 |
| CHEMBL143815 | — | — | 1 | 8.31 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 8.22 |
| CHEMBL407685 | — | — | 1 | 8.08 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.02 |
| CHEMBL343167 | — | — | 1 | 7.72 |
| CHEMBL140278 | — | — | 1 | 7.70 |
| CHEMBL76023 | — | — | 1 | 7.68 |
| CHEMBL143416 | — | — | 1 | 7.38 |
| CHEMBL140044 | — | — | 1 | 7.33 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.30 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.00 |
| CHEMBL344420 | — | — | 1 | 6.76 |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 6.20 |
| CHEMBL140145 | — | — | 1 | 6.06 |
| CHEMBL140855 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL281786 | DIPRENORPHINE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL140050 | ETORPHINE | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2092986 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL143815 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL407685 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL343167 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL140278 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL76023 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL143416 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL140044 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL80 | NALOXONE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL567175 | NALTRINDOLE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL344420 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL963 | OXYMORPHONE | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL140145 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL140855 | — | IC50 | > | 3000.0 | nM | - |