Assay Detail
Binding
CHEMBL4676429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method
29
Total Activities
29
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
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ Receptor Antagonist Clinical Candidate for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.41 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748898 | — | — | 1 | 8.70 |
| CHEMBL4789005 | — | — | 1 | 8.22 |
| CHEMBL4541206 | — | — | 1 | 8.15 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.92 |
| CHEMBL4776924 | — | — | 1 | 7.75 |
| CHEMBL4796605 | — | — | 1 | 7.70 |
| CHEMBL4756310 | — | — | 1 | 7.68 |
| CHEMBL4776743 | — | — | 1 | 7.66 |
| CHEMBL4741494 | — | — | 1 | 7.58 |
| CHEMBL4759184 | — | — | 1 | 7.48 |
| CHEMBL4755446 | — | — | 1 | 7.39 |
| CHEMBL4754130 | — | — | 1 | 7.25 |
| CHEMBL4777859 | — | — | 1 | 7.21 |
| CHEMBL4781352 | — | — | 1 | 7.19 |
| CHEMBL4753006 | — | — | 1 | 7.04 |
| CHEMBL4755342 | — | — | 1 | 6.94 |
| CHEMBL4786209 | — | — | 1 | 6.81 |
| CHEMBL4788650 | — | — | 1 | 6.79 |
| CHEMBL4461774 | — | — | 1 | 6.76 |
| CHEMBL4752386 | — | — | 1 | 6.72 |
| CHEMBL4762816 | — | — | 1 | 6.66 |
| CHEMBL4787186 | — | — | 1 | - |
| CHEMBL4761794 | — | — | 1 | - |
| CHEMBL4754601 | — | — | 1 | - |
| CHEMBL4761093 | — | — | 1 | - |
| CHEMBL4796930 | — | — | 1 | - |
| CHEMBL4751130 | — | — | 1 | - |
| CHEMBL2170062 | — | — | 1 | - |
| CHEMBL4750243 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748898 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4789005 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4541206 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL656 | OXYCODONE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4776924 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4796605 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4756310 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4776743 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4741494 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4759184 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4755446 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4754130 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL4777859 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4781352 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL4753006 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL4755342 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4786209 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL4788650 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL4461774 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL4752386 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL4762816 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL4787186 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4761794 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4754601 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4761093 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4796930 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4751130 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170062 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4750243 | — | Ki | > | 1000.0 | nM | - |