Assay Detail
Binding
CHEMBL839748
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for recombinant human mu-opioid receptor was determined by using [3H]- diprenophine radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.15 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL364625 | — | — | 1 | 9.96 |
| CHEMBL421665 | FLUPERAMIDE | 2.0 | 1 | 9.96 |
| CHEMBL186795 | — | — | 1 | 9.80 |
| CHEMBL186300 | — | — | 1 | 9.64 |
| CHEMBL186938 | — | — | 1 | 9.52 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 9.28 |
| CHEMBL322515 | — | — | 1 | 9.00 |
| CHEMBL111233 | — | — | 1 | 8.60 |
| CHEMBL325536 | — | — | 1 | 8.40 |
| CHEMBL186426 | — | — | 1 | 7.43 |
| CHEMBL109509 | — | — | 1 | 6.98 |
| CHEMBL187648 | — | — | 1 | 6.48 |
| CHEMBL187038 | — | — | 1 | 6.31 |
| CHEMBL184689 | — | — | 1 | 5.83 |
| CHEMBL184496 | — | — | 1 | 5.09 |
| CHEMBL185706 | — | — | 1 | - |
| CHEMBL187083 | — | — | 1 | - |
| CHEMBL321685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL364625 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL421665 | FLUPERAMIDE | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL186795 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL186300 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL186938 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL322515 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL111233 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL325536 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL186426 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL109509 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL187648 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL187038 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL184689 | — | Ki | = | 1461.0 | nM | 5.83 |
| CHEMBL184496 | — | Ki | = | 8128.0 | nM | 5.09 |
| CHEMBL185706 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL187083 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL321685 | — | Ki | > | 10000.0 | nM | - |