Assay Detail
Binding
CHEMBL4356647
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
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ1 Receptor Antagonists for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 55 | 7.20 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436170 | — | — | 1 | 9.00 |
| CHEMBL4452042 | — | — | 1 | 8.52 |
| CHEMBL4516327 | — | — | 1 | 8.52 |
| CHEMBL4515812 | — | — | 1 | 8.52 |
| CHEMBL4536259 | — | — | 1 | 8.22 |
| CHEMBL4541206 | — | — | 1 | 8.15 |
| CHEMBL4584335 | — | — | 1 | 8.10 |
| CHEMBL4450665 | — | — | 1 | 8.10 |
| CHEMBL4534193 | — | — | 1 | 8.00 |
| CHEMBL4576031 | — | — | 1 | 7.96 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.92 |
| CHEMBL4439285 | — | — | 1 | 7.89 |
| CHEMBL4438550 | — | — | 1 | 7.82 |
| CHEMBL4544352 | — | — | 1 | 7.72 |
| CHEMBL4460762 | — | — | 1 | 7.55 |
| CHEMBL4522004 | — | — | 1 | 7.47 |
| CHEMBL4528962 | — | — | 1 | 7.40 |
| CHEMBL4459117 | — | — | 1 | 7.34 |
| CHEMBL4525653 | — | — | 1 | 7.34 |
| CHEMBL4463621 | — | — | 1 | 7.31 |
| CHEMBL4526087 | — | — | 1 | 7.24 |
| CHEMBL4467749 | — | — | 1 | 7.16 |
| CHEMBL4538620 | — | — | 1 | 7.05 |
| CHEMBL4473746 | — | — | 1 | 7.05 |
| CHEMBL4446209 | — | — | 1 | 7.04 |
| CHEMBL4483643 | — | — | 1 | 7.03 |
| CHEMBL4571738 | — | — | 1 | 6.93 |
| CHEMBL4535897 | — | — | 1 | 6.91 |
| CHEMBL4550656 | — | — | 1 | 6.90 |
| CHEMBL4540888 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436170 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4452042 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4515812 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4516327 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4536259 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4541206 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4584335 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4450665 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4534193 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4576031 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL656 | OXYCODONE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4439285 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4438550 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4544352 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4460762 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4522004 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4528962 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4459117 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4525653 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4463621 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4526087 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4467749 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4538620 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL4473746 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL4446209 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL4483643 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL4571738 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL4535897 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL4550656 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL4540888 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL4573960 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4461774 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL4451838 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL4470425 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL4448670 | — | Ki | = | 262.0 | nM | 6.58 |
| CHEMBL4593220 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL4439718 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL4440055 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL4461864 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL4439908 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL4445578 | — | Ki | = | 516.0 | nM | 6.29 |
| CHEMBL4592081 | — | Ki | = | 535.0 | nM | 6.27 |
| CHEMBL4446292 | — | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL4513933 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL4458456 | — | Ki | = | 636.0 | nM | 6.20 |
| CHEMBL4471711 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL4578955 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL4560624 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4463901 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4448710 | — | Ki | > | 1000.0 | nM | - |