Assay Detail
Binding
CHEMBL4768236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-diprenorphin from human mu opioid receptor expressed in CHO cell membrane incubated for 150 mins by liquid scintillation counting method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.29 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789321 | — | — | 1 | 8.68 |
| CHEMBL4788719 | — | — | 1 | 8.43 |
| CHEMBL4776178 | — | — | 1 | 8.25 |
| CHEMBL4778918 | — | — | 1 | 7.78 |
| CHEMBL4785048 | — | — | 1 | 7.71 |
| CHEMBL4797982 | — | — | 1 | 7.69 |
| CHEMBL4783182 | — | — | 1 | 7.58 |
| CHEMBL4789528 | — | — | 1 | 7.55 |
| CHEMBL4797005 | — | — | 1 | 7.37 |
| CHEMBL4787348 | — | — | 1 | 7.13 |
| CHEMBL4790304 | — | — | 1 | 7.11 |
| CHEMBL4777042 | — | — | 1 | 7.11 |
| CHEMBL4777040 | — | — | 1 | 7.09 |
| CHEMBL4788466 | — | — | 1 | 7.09 |
| CHEMBL4792476 | — | — | 1 | 6.83 |
| CHEMBL4779284 | — | — | 1 | 6.78 |
| CHEMBL4790216 | — | — | 1 | 6.62 |
| CHEMBL4783373 | — | — | 1 | 6.60 |
| CHEMBL4792467 | — | — | 1 | 6.24 |
| CHEMBL4797585 | — | — | 1 | 6.16 |
| CHEMBL4788563 | — | — | 1 | - |
| CHEMBL4781647 | — | — | 1 | - |
| CHEMBL4794751 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789321 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4788719 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4776178 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL4778918 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL4785048 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL4797982 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL4783182 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4789528 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL4797005 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL4787348 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL4790304 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4777042 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4777040 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL4788466 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL4792476 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL4779284 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL4790216 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL4783373 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL4792467 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL4797585 | — | Ki | = | 694.0 | nM | 6.16 |
| CHEMBL4788563 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL4781647 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL4794751 | — | Ki | > | 2000.0 | nM | - |