Assay Detail
Functional
CHEMBL4356649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 55 | 7.10 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436170 | — | — | 1 | 9.70 |
| CHEMBL4452042 | — | — | 1 | 9.00 |
| CHEMBL4515812 | — | — | 1 | 9.00 |
| CHEMBL4584335 | — | — | 1 | 8.40 |
| CHEMBL4536259 | — | — | 1 | 8.40 |
| CHEMBL4516327 | — | — | 1 | 8.40 |
| CHEMBL4438550 | — | — | 1 | 7.96 |
| CHEMBL4534193 | — | — | 1 | 7.89 |
| CHEMBL4541206 | — | — | 1 | 7.85 |
| CHEMBL4450665 | — | — | 1 | 7.80 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.77 |
| CHEMBL4544352 | — | — | 1 | 7.60 |
| CHEMBL4460762 | — | — | 1 | 7.60 |
| CHEMBL4576031 | — | — | 1 | 7.58 |
| CHEMBL4439285 | — | — | 1 | 7.50 |
| CHEMBL4463621 | — | — | 1 | 7.21 |
| CHEMBL4522004 | — | — | 1 | 7.19 |
| CHEMBL4525653 | — | — | 1 | 7.16 |
| CHEMBL4528962 | — | — | 1 | 6.97 |
| CHEMBL4459117 | — | — | 1 | 6.90 |
| CHEMBL4526087 | — | — | 1 | 6.84 |
| CHEMBL4446209 | — | — | 1 | 6.74 |
| CHEMBL4535897 | — | — | 1 | 6.73 |
| CHEMBL4461774 | — | — | 1 | 6.71 |
| CHEMBL4483643 | — | — | 1 | 6.70 |
| CHEMBL4538620 | — | — | 1 | 6.66 |
| CHEMBL4473746 | — | — | 1 | 6.64 |
| CHEMBL4470425 | — | — | 1 | 6.64 |
| CHEMBL4467749 | — | — | 1 | 6.58 |
| CHEMBL4550656 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436170 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4452042 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4515812 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4584335 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4536259 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4516327 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4438550 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4534193 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4541206 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4450665 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL656 | OXYCODONE | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4544352 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4460762 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4576031 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4439285 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4463621 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4522004 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4525653 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4528962 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4459117 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4526087 | — | EC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4446209 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4535897 | — | EC50 | = | 186.0 | nM | 6.73 |
| CHEMBL4461774 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4483643 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4538620 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL4470425 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4473746 | — | EC50 | = | 229.0 | nM | 6.64 |
| CHEMBL4467749 | — | EC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4550656 | — | EC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4451838 | — | EC50 | = | 342.0 | nM | 6.47 |
| CHEMBL4448670 | — | EC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4573960 | — | EC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4439718 | — | EC50 | = | 527.0 | nM | 6.28 |
| CHEMBL4439908 | — | EC50 | = | 523.0 | nM | 6.28 |
| CHEMBL4440055 | — | EC50 | = | 627.0 | nM | 6.20 |
| CHEMBL4593220 | — | EC50 | = | 721.0 | nM | 6.14 |
| CHEMBL4540888 | — | EC50 | = | 767.0 | nM | 6.12 |
| CHEMBL4571738 | — | EC50 | = | 853.0 | nM | 6.07 |
| CHEMBL4445578 | — | EC50 | = | 1424.0 | nM | 5.85 |
| CHEMBL4578955 | — | EC50 | = | 1987.0 | nM | 5.70 |
| CHEMBL4446292 | — | EC50 | = | 3044.0 | nM | 5.52 |
| CHEMBL4463901 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4513933 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4560624 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4448710 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4457602 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4471711 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4592081 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4458456 | — | EC50 | > | 1000.0 | nM | - |