Assay Detail
Functional
CHEMBL4124270
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Agonist activity at rat delta-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 | 8.15 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26575 | DELTORPHIN | — | 1 | 10.00 |
| CHEMBL4129679 | — | — | 1 | 8.95 |
| CHEMBL4126050 | — | — | 1 | 8.62 |
| CHEMBL4128530 | — | — | 1 | 8.36 |
| CHEMBL4126470 | — | — | 1 | 8.31 |
| CHEMBL4129901 | — | — | 1 | 8.24 |
| CHEMBL4126102 | — | — | 1 | 8.15 |
| CHEMBL4126322 | — | — | 1 | 7.71 |
| CHEMBL4128945 | — | — | 1 | 7.57 |
| CHEMBL4129689 | — | — | 1 | 7.31 |
| CHEMBL38874 | DAMGO | — | 1 | 7.31 |
| CHEMBL4129753 | — | — | 1 | 7.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26575 | DELTORPHIN | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4129679 | — | EC50 | = | 1.13 | nM | 8.95 |
| CHEMBL4126050 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4128530 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4126470 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4129901 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4126102 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4126322 | — | EC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4128945 | — | EC50 | = | 26.8 | nM | 7.57 |
| CHEMBL4129689 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL38874 | DAMGO | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4129753 | — | EC50 | = | 56.0 | nM | 7.25 |