Assay Detail
Functional
CHEMBL4308247
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Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay
9
Total Activities
9
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
β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.34 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38874 | DAMGO | — | 1 | 9.10 |
| CHEMBL4468844 | — | — | 1 | 8.23 |
| CHEMBL4471584 | — | — | 1 | 8.12 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 7.97 |
| CHEMBL4458454 | — | — | 1 | 7.11 |
| CHEMBL4550454 | — | — | 1 | 7.05 |
| CHEMBL4516683 | — | — | 1 | 6.99 |
| CHEMBL4441320 | — | — | 1 | 6.98 |
| CHEMBL4537210 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38874 | DAMGO | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4468844 | — | IC50 | = | 5.888 | nM | 8.23 |
| CHEMBL4471584 | — | IC50 | = | 7.586 | nM | 8.12 |
| CHEMBL596 | FENTANYL | IC50 | = | 10.72 | nM | 7.97 |
| CHEMBL4458454 | — | IC50 | = | 77.62 | nM | 7.11 |
| CHEMBL4550454 | — | IC50 | = | 89.13 | nM | 7.05 |
| CHEMBL4516683 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL4441320 | — | IC50 | = | 104.71 | nM | 6.98 |
| CHEMBL4537210 | — | IC50 | = | 31622.78 | nM | 4.50 |