Assay Detail
Functional
CHEMBL4676428
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Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 |
|---|---|---|---|
| EC50 | 29 | 7.08 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748898 | — | — | 1 | 8.70 |
| CHEMBL4789005 | — | — | 1 | 8.15 |
| CHEMBL4776743 | — | — | 1 | 8.00 |
| CHEMBL4541206 | — | — | 1 | 7.85 |
| CHEMBL4756310 | — | — | 1 | 7.80 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.77 |
| CHEMBL4759184 | — | — | 1 | 7.68 |
| CHEMBL4796605 | — | — | 1 | 7.66 |
| CHEMBL4776924 | — | — | 1 | 7.62 |
| CHEMBL4741494 | — | — | 1 | 7.31 |
| CHEMBL4781352 | — | — | 1 | 7.28 |
| CHEMBL4777859 | — | — | 1 | 7.28 |
| CHEMBL4754130 | — | — | 1 | 7.25 |
| CHEMBL4755446 | — | — | 1 | 7.19 |
| CHEMBL4788650 | — | — | 1 | 6.97 |
| CHEMBL4755342 | — | — | 1 | 6.76 |
| CHEMBL4461774 | — | — | 1 | 6.71 |
| CHEMBL4753006 | — | — | 1 | 6.50 |
| CHEMBL4762816 | — | — | 1 | 6.36 |
| CHEMBL4752386 | — | — | 1 | 6.30 |
| CHEMBL4751130 | — | — | 1 | 6.21 |
| CHEMBL4786209 | — | — | 1 | 6.10 |
| CHEMBL4761093 | — | — | 1 | 6.04 |
| CHEMBL4750243 | — | — | 1 | 5.82 |
| CHEMBL4761794 | — | — | 1 | 5.75 |
| CHEMBL4787186 | — | — | 1 | - |
| CHEMBL4754601 | — | — | 1 | - |
| CHEMBL4796930 | — | — | 1 | - |
| CHEMBL2170062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748898 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4789005 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4776743 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4541206 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4756310 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL656 | OXYCODONE | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4759184 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4796605 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4776924 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4741494 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4781352 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4777859 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4754130 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4755446 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4788650 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4755342 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4461774 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4753006 | — | EC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4762816 | — | EC50 | = | 442.0 | nM | 6.36 |
| CHEMBL4752386 | — | EC50 | = | 505.0 | nM | 6.30 |
| CHEMBL4751130 | — | EC50 | = | 624.0 | nM | 6.21 |
| CHEMBL4786209 | — | EC50 | = | 787.0 | nM | 6.10 |
| CHEMBL4761093 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4750243 | — | EC50 | = | 1498.0 | nM | 5.82 |
| CHEMBL4761794 | — | EC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL4787186 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4754601 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4796930 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL2170062 | — | EC50 | > | 10000.0 | nM | - |