Assay Detail
Binding
CHEMBL754078
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Displacement of [3H]bremazocine from opioid receptor of guinea pig membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.34 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2367604 | — | — | 1 | 8.64 |
| CHEMBL2367645 | — | — | 1 | 8.54 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.24 |
| CHEMBL312039 | — | — | 1 | 8.17 |
| CHEMBL2367762 | — | — | 1 | 8.13 |
| CHEMBL2367764 | — | — | 1 | 7.92 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.64 |
| CHEMBL2367603 | — | — | 1 | 7.08 |
| CHEMBL2367758 | — | — | 1 | 7.05 |
| CHEMBL2367761 | — | — | 1 | 6.42 |
| CHEMBL2367760 | — | — | 1 | 6.21 |
| CHEMBL2367759 | — | — | 1 | 5.75 |
| CHEMBL311708 | — | — | 1 | 5.66 |
| CHEMBL2367757 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2367604 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2367645 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL312039 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2367762 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2367764 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL80 | NALOXONE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2367603 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2367758 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2367761 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2367760 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2367759 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL311708 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2367757 | — | IC50 | > | 3000.0 | nM | - |