Assay Detail
Functional
CHEMBL950286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human mu opioid receptor by [35S]GTPgammaS binding assay
15
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ke | 8 | - | - |
| Kd | 7 | 9.68 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 2 | 10.30 |
| CHEMBL411916 | — | — | 2 | 9.78 |
| CHEMBL410526 | — | — | 2 | 9.78 |
| CHEMBL406116 | — | — | 2 | 9.68 |
| CHEMBL982 | NALMEFENE | 4.0 | 2 | 9.53 |
| CHEMBL443326 | — | — | 2 | 9.34 |
| CHEMBL409036 | — | — | 2 | 9.33 |
| CHEMBL412050 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL410526 | — | Kd | = | 0.166 | nM | 9.78 |
| CHEMBL411916 | — | Kd | = | 0.166 | nM | 9.78 |
| CHEMBL406116 | — | Kd | = | 0.2089 | nM | 9.68 |
| CHEMBL982 | NALMEFENE | Kd | = | 0.2951 | nM | 9.53 |
| CHEMBL443326 | — | Kd | = | 0.4571 | nM | 9.34 |
| CHEMBL409036 | — | Kd | = | 0.4677 | nM | 9.33 |
| CHEMBL19019 | NALTREXONE | Ke | = | 0.05 | nM | - |
| CHEMBL443326 | — | Ke | = | 0.41 | nM | - |
| CHEMBL412050 | — | Ke | = | 0.15 | nM | - |
| CHEMBL411916 | — | Ke | = | 0.14 | nM | - |
| CHEMBL410526 | — | Ke | = | 0.17 | nM | - |
| CHEMBL409036 | — | Ke | = | 0.37 | nM | - |
| CHEMBL406116 | — | Ke | = | 0.16 | nM | - |
| CHEMBL982 | NALMEFENE | Ke | = | 0.34 | nM | - |