Assay Detail
Binding
CHEMBL933967
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Displacement of [3H]diprenorphine from human cloned kappa opioid receptor
21
Total Activities
21
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 | 21 | 6.44 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.04 |
| CHEMBL403633 | — | — | 1 | 7.17 |
| CHEMBL404303 | — | — | 1 | 7.08 |
| CHEMBL270190 | ALVIMOPAN | 4.0 | 1 | 7.00 |
| CHEMBL402964 | — | — | 1 | 6.80 |
| CHEMBL437983 | — | — | 1 | 6.70 |
| CHEMBL270833 | — | — | 1 | 6.64 |
| CHEMBL270187 | — | — | 1 | 6.62 |
| CHEMBL403190 | — | — | 1 | 6.60 |
| CHEMBL271662 | — | — | 1 | 6.34 |
| CHEMBL256010 | — | — | 1 | 6.29 |
| CHEMBL255555 | — | — | 1 | 6.26 |
| CHEMBL401615 | — | — | 1 | 6.24 |
| CHEMBL403325 | — | — | 1 | 6.16 |
| CHEMBL270401 | — | — | 1 | 6.14 |
| CHEMBL255354 | — | — | 1 | 6.04 |
| CHEMBL441899 | — | — | 1 | 5.96 |
| CHEMBL403191 | — | — | 1 | 5.92 |
| CHEMBL404583 | — | — | 1 | 5.85 |
| CHEMBL258294 | — | — | 1 | 5.66 |
| CHEMBL258115 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80 | NALOXONE | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL403633 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL404303 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL270190 | ALVIMOPAN | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL402964 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL437983 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL270833 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL270187 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL403190 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL271662 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL256010 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL255555 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL401615 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL403325 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL270401 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL255354 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL441899 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL403191 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL404583 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL258294 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL258115 | — | Ki | = | 2200.0 | nM | 5.66 |