Assay Detail
Functional
CHEMBL933966
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human cloned mu opioid receptor assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 29 | 8.04 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403633 | — | — | 1 | 8.92 |
| CHEMBL401615 | — | — | 1 | 8.92 |
| CHEMBL437983 | — | — | 1 | 8.85 |
| CHEMBL403190 | — | — | 1 | 8.82 |
| CHEMBL270190 | ALVIMOPAN | 4.0 | 1 | 8.77 |
| CHEMBL255354 | — | — | 1 | 8.52 |
| CHEMBL401789 | — | — | 1 | 8.42 |
| CHEMBL270401 | — | — | 1 | 8.28 |
| CHEMBL401508 | — | — | 1 | 8.26 |
| CHEMBL270187 | — | — | 1 | 8.21 |
| CHEMBL271662 | — | — | 1 | 8.17 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.14 |
| CHEMBL401716 | — | — | 1 | 8.11 |
| CHEMBL404303 | — | — | 1 | 8.10 |
| CHEMBL256010 | — | — | 1 | 8.00 |
| CHEMBL403325 | — | — | 1 | 8.00 |
| CHEMBL257895 | — | — | 1 | 7.89 |
| CHEMBL256834 | — | — | 1 | 7.85 |
| CHEMBL258294 | — | — | 1 | 7.80 |
| CHEMBL402964 | — | — | 1 | 7.68 |
| CHEMBL255555 | — | — | 1 | 7.60 |
| CHEMBL441899 | — | — | 1 | 7.55 |
| CHEMBL270833 | — | — | 1 | 7.44 |
| CHEMBL258115 | — | — | 1 | 7.37 |
| CHEMBL403191 | — | — | 1 | 7.20 |
| CHEMBL404583 | — | — | 1 | 7.16 |
| CHEMBL403324 | — | — | 1 | 6.96 |
| CHEMBL270403 | — | — | 1 | - |
| CHEMBL255761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403633 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL401615 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL437983 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL403190 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL270190 | ALVIMOPAN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL255354 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL401789 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL270401 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL401508 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL270187 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL271662 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL80 | NALOXONE | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL401716 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL404303 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL256010 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL403325 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL257895 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL256834 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL258294 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL402964 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL255555 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL441899 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL270833 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL258115 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL403191 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL404583 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL403324 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL270403 | — | IC50 | - | — | - | |
| CHEMBL255761 | — | IC50 | - | — | - |