Assay Detail
Binding
CHEMBL5110290
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzylaminofentanyl derivates: Discovery of bifunctional μ opioid and σ<sub>1</sub> receptor ligands as novel analgesics with reduced adverse effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 45 | 7.17 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789321 | — | — | 1 | 8.72 |
| CHEMBL38874 | DAMGO | — | 1 | 8.49 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.48 |
| CHEMBL94350 | — | — | 1 | 8.41 |
| CHEMBL5179132 | — | — | 1 | 8.19 |
| CHEMBL5183712 | — | — | 1 | 8.10 |
| CHEMBL5181954 | — | — | 1 | 7.94 |
| CHEMBL5179531 | — | — | 1 | 7.82 |
| CHEMBL5208537 | — | — | 1 | 7.76 |
| CHEMBL5195239 | — | — | 1 | 7.73 |
| CHEMBL5087973 | — | — | 1 | 7.71 |
| CHEMBL5174391 | — | — | 1 | 7.65 |
| CHEMBL5179109 | — | — | 1 | 7.57 |
| CHEMBL5181914 | — | — | 1 | 7.48 |
| CHEMBL4461774 | — | — | 1 | 7.24 |
| CHEMBL5173931 | — | — | 1 | 7.23 |
| CHEMBL5190421 | — | — | 1 | 7.23 |
| CHEMBL316632 | — | — | 1 | 7.21 |
| CHEMBL5187961 | — | — | 1 | 7.19 |
| CHEMBL5204518 | — | — | 1 | 7.05 |
| CHEMBL4781352 | — | — | 1 | 6.93 |
| CHEMBL5202810 | — | — | 1 | 6.80 |
| CHEMBL5187144 | — | — | 1 | 6.77 |
| CHEMBL5208375 | — | — | 1 | 6.65 |
| CHEMBL5176125 | — | — | 1 | 6.63 |
| CHEMBL5187189 | — | — | 1 | 6.62 |
| CHEMBL5208252 | — | — | 1 | 6.59 |
| CHEMBL5186423 | — | — | 1 | 6.57 |
| CHEMBL5192862 | — | — | 1 | 6.46 |
| CHEMBL5204271 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789321 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL38874 | DAMGO | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL596 | FENTANYL | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL94350 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5179132 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5183712 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL5181954 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL5179531 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL5208537 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL5195239 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL5087973 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL5174391 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL5179109 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5181914 | — | Ki | = | 33.4 | nM | 7.48 |
| CHEMBL4461774 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL5173931 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5190421 | — | Ki | = | 58.5 | nM | 7.23 |
| CHEMBL316632 | — | Ki | = | 61.7 | nM | 7.21 |
| CHEMBL5187961 | — | Ki | = | 64.6 | nM | 7.19 |
| CHEMBL5204518 | — | Ki | = | 88.7 | nM | 7.05 |
| CHEMBL4781352 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL5202810 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL5187144 | — | Ki | = | 169.7 | nM | 6.77 |
| CHEMBL5208375 | — | Ki | = | 224.4 | nM | 6.65 |
| CHEMBL5176125 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL5187189 | — | Ki | = | 237.5 | nM | 6.62 |
| CHEMBL5208252 | — | Ki | = | 259.1 | nM | 6.59 |
| CHEMBL5186423 | — | Ki | = | 271.3 | nM | 6.57 |
| CHEMBL5192862 | — | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL5204271 | — | Ki | = | 365.2 | nM | 6.44 |
| CHEMBL5179620 | — | Ki | = | 376.3 | nM | 6.42 |
| CHEMBL4439908 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL5169886 | — | Ki | = | 453.3 | nM | 6.34 |
| CHEMBL5188409 | — | Ki | = | 555.3 | nM | 6.25 |
| CHEMBL172155 | — | Ki | = | 572.2 | nM | 6.24 |
| CHEMBL5198980 | — | Ki | = | 837.1 | nM | 6.08 |
| CHEMBL5182393 | — | Ki | = | 1259.4 | nM | 5.90 |
| CHEMBL5182558 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5186562 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5201601 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5192526 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5196794 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5191081 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5204843 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5182504 | — | Ki | > | 1000.0 | nM | - |