Assay Detail
Functional
CHEMBL4124269
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Agonist activity at rat mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 9.66 | 10.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126102 | — | — | 1 | 10.92 |
| CHEMBL4126050 | — | — | 1 | 10.92 |
| CHEMBL4129689 | — | — | 1 | 10.40 |
| CHEMBL4126322 | — | — | 1 | 10.00 |
| CHEMBL4128945 | — | — | 1 | 9.92 |
| CHEMBL4126470 | — | — | 1 | 9.92 |
| CHEMBL38874 | DAMGO | — | 1 | 9.59 |
| CHEMBL26575 | DELTORPHIN | — | 1 | 7.80 |
| CHEMBL4129753 | — | — | 1 | 7.46 |
| CHEMBL4129901 | — | — | 1 | - |
| CHEMBL4128530 | — | — | 1 | - |
| CHEMBL4129679 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126102 | — | EC50 | = | 0.012 | nM | 10.92 |
| CHEMBL4126050 | — | EC50 | = | 0.012 | nM | 10.92 |
| CHEMBL4129689 | — | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL4126322 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4128945 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4126470 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL38874 | DAMGO | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL26575 | DELTORPHIN | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4129753 | — | EC50 | = | 34.8 | nM | 7.46 |
| CHEMBL4129901 | — | EC50 | = | 0.006 | nM | - |
| CHEMBL4128530 | — | EC50 | = | 0.003 | nM | - |
| CHEMBL4129679 | — | EC50 | = | 0.008 | nM | - |