Assay Detail
Functional
CHEMBL2051429
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Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.51 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.43 |
| CHEMBL3215668 | — | — | 1 | 7.28 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | 6.92 |
| CHEMBL3217001 | — | — | 1 | 6.77 |
| CHEMBL3216999 | — | — | 1 | 6.47 |
| CHEMBL3215667 | — | — | 1 | 6.40 |
| CHEMBL3216560 | — | — | 1 | 6.23 |
| CHEMBL1201776 | TAPENTADOL | 4.0 | 1 | 6.17 |
| CHEMBL3217211 | — | — | 1 | 6.03 |
| CHEMBL1237044 | TRAMADOL | 4.0 | 1 | 5.89 |
| CHEMBL3217000 | — | — | 1 | 5.82 |
| CHEMBL3216780 | — | — | 1 | 5.66 |
| CHEMBL3215669 | — | — | 1 | - |
| CHEMBL3215885 | — | — | 1 | - |
| CHEMBL3217210 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3215668 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3217001 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3216999 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3215667 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3216560 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1201776 | TAPENTADOL | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3217211 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1237044 | TRAMADOL | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3217000 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3216780 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3215669 | — | EC50 | - | — | - | |
| CHEMBL3215885 | — | EC50 | - | — | - | |
| CHEMBL3217210 | — | EC50 | - | — | - |