Assay Detail
Binding
CHEMBL5035603
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Displacement of [3H]DAMGO from MOR in Sprague-Dawley rat brain membranes measured after 90 mins by scintillation counting method
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of bifunctional piperidinamide derivatives as σ<sub>1</sub>R Antagonists/MOR agonists for treating neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 7.38 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5082165 | — | — | 1 | 9.66 |
| CHEMBL5094445 | — | — | 1 | 8.96 |
| CHEMBL5086596 | — | — | 1 | 8.48 |
| CHEMBL4788719 | — | — | 1 | 8.43 |
| CHEMBL5075339 | — | — | 1 | 8.43 |
| CHEMBL5087973 | — | — | 1 | 8.37 |
| CHEMBL5079619 | — | — | 1 | 8.36 |
| CHEMBL5087044 | — | — | 1 | 8.30 |
| CHEMBL5094800 | — | — | 1 | 8.21 |
| CHEMBL5094951 | — | — | 1 | 8.03 |
| CHEMBL5082953 | — | — | 1 | 7.68 |
| CHEMBL5093427 | — | — | 1 | 7.58 |
| CHEMBL5086252 | — | — | 1 | 7.47 |
| CHEMBL5080562 | — | — | 1 | 7.46 |
| CHEMBL5078411 | — | — | 1 | 7.15 |
| CHEMBL5078652 | — | — | 1 | 7.04 |
| CHEMBL5092506 | — | — | 1 | 7.04 |
| CHEMBL5079004 | — | — | 1 | 6.94 |
| CHEMBL5081685 | — | — | 1 | 6.72 |
| CHEMBL5092130 | — | — | 1 | 6.45 |
| CHEMBL5079832 | — | — | 1 | 6.22 |
| CHEMBL5079255 | — | — | 1 | 6.13 |
| CHEMBL5078787 | — | — | 1 | 6.07 |
| CHEMBL5081955 | — | — | 1 | 6.05 |
| CHEMBL5092754 | — | — | 1 | 6.04 |
| CHEMBL5087369 | — | — | 1 | 6.02 |
| CHEMBL5078392 | — | — | 1 | 6.01 |
| CHEMBL5080342 | — | — | 1 | - |
| CHEMBL5090778 | — | — | 1 | - |
| CHEMBL5084297 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5082165 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL5094445 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL5086596 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4788719 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL5075339 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL5087973 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL5079619 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL5087044 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5094800 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL5094951 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL5082953 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL5093427 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL5086252 | — | Ki | = | 33.6 | nM | 7.47 |
| CHEMBL5080562 | — | Ki | = | 34.3 | nM | 7.46 |
| CHEMBL5078411 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL5078652 | — | Ki | = | 90.2 | nM | 7.04 |
| CHEMBL5092506 | — | Ki | = | 90.3 | nM | 7.04 |
| CHEMBL5079004 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL5081685 | — | Ki | = | 189.7 | nM | 6.72 |
| CHEMBL5092130 | — | Ki | = | 359.2 | nM | 6.45 |
| CHEMBL5079832 | — | Ki | = | 608.2 | nM | 6.22 |
| CHEMBL5079255 | — | Ki | = | 739.1 | nM | 6.13 |
| CHEMBL5078787 | — | Ki | = | 861.7 | nM | 6.07 |
| CHEMBL5081955 | — | Ki | = | 893.2 | nM | 6.05 |
| CHEMBL5092754 | — | Ki | = | 906.3 | nM | 6.04 |
| CHEMBL5087369 | — | Ki | = | 960.1 | nM | 6.02 |
| CHEMBL5078392 | — | Ki | = | 968.8 | nM | 6.01 |
| CHEMBL5087716 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5087894 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5077650 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5085473 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5092251 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5086128 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5092876 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5089128 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5075068 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5075572 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5084297 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5090778 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5080342 | — | Ki | > | 1000.0 | nM | - |