Assay Detail
Binding
CHEMBL933964
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Displacement of [3H]diprenorphine from human cloned mu opioid receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 8.08 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437983 | — | — | 1 | 9.39 |
| CHEMBL270190 | ALVIMOPAN | 4.0 | 1 | 9.33 |
| CHEMBL401615 | — | — | 1 | 9.30 |
| CHEMBL403633 | — | — | 1 | 9.20 |
| CHEMBL403190 | — | — | 1 | 8.77 |
| CHEMBL402964 | — | — | 1 | 8.72 |
| CHEMBL270187 | — | — | 1 | 8.70 |
| CHEMBL404303 | — | — | 1 | 8.57 |
| CHEMBL255354 | — | — | 1 | 8.54 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.43 |
| CHEMBL256010 | — | — | 1 | 8.33 |
| CHEMBL401789 | — | — | 1 | 8.14 |
| CHEMBL257895 | — | — | 1 | 7.96 |
| CHEMBL270401 | — | — | 1 | 7.96 |
| CHEMBL271662 | — | — | 1 | 7.82 |
| CHEMBL403324 | — | — | 1 | 7.72 |
| CHEMBL401508 | — | — | 1 | 7.70 |
| CHEMBL258294 | — | — | 1 | 7.66 |
| CHEMBL255555 | — | — | 1 | 7.64 |
| CHEMBL258115 | — | — | 1 | 7.55 |
| CHEMBL404583 | — | — | 1 | 7.50 |
| CHEMBL401716 | — | — | 1 | 7.44 |
| CHEMBL403325 | — | — | 1 | 7.24 |
| CHEMBL403191 | — | — | 1 | 7.18 |
| CHEMBL256834 | — | — | 1 | 7.18 |
| CHEMBL270833 | — | — | 1 | 7.13 |
| CHEMBL441899 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437983 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL270190 | ALVIMOPAN | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL401615 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL403633 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL403190 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL402964 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL270187 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL404303 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL255354 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL80 | NALOXONE | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL256010 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL401789 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL257895 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL270401 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL271662 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL403324 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL401508 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL258294 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL255555 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL258115 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL404583 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL401716 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL403325 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL403191 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL256834 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL270833 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL441899 | — | Ki | = | 80.0 | nM | 7.10 |