Assay Detail
Functional
CHEMBL2423628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
11
Total Activities
11
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
Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide opening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.92 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38874 | DAMGO | — | 1 | 7.82 |
| CHEMBL2418739 | — | — | 1 | 7.70 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.30 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 6.30 |
| CHEMBL2418738 | — | — | 1 | 5.70 |
| CHEMBL2418745 | — | — | 1 | 5.50 |
| CHEMBL2418743 | — | — | 1 | 5.50 |
| CHEMBL2418744 | — | — | 1 | 5.30 |
| CHEMBL2418741 | — | — | 1 | 4.80 |
| CHEMBL2418740 | — | — | 1 | 4.80 |
| CHEMBL2418742 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38874 | DAMGO | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2418739 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL70 | MORPHINE | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL656 | OXYCODONE | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2418738 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2418745 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2418743 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2418744 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2418741 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2418740 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2418742 | — | EC50 | = | 40000.0 | nM | 4.40 |