Assay Detail
Binding
CHEMBL4374386
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.88 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL658 | SUFENTANIL | 4.0 | 1 | 9.40 |
| CHEMBL2355317 | — | — | 1 | 9.32 |
| CHEMBL1005 | REMIFENTANIL | 4.0 | 1 | 9.22 |
| CHEMBL2365680 | — | — | 1 | 8.96 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.91 |
| CHEMBL3302622 | — | — | 1 | 8.55 |
| CHEMBL634 | ALFENTANIL | 4.0 | 1 | 7.41 |
| CHEMBL4526998 | — | — | 1 | 7.01 |
| CHEMBL2365725 | — | — | 1 | 6.61 |
| CHEMBL4562635 | — | — | 1 | 6.53 |
| CHEMBL4446083 | — | — | 1 | 6.31 |
| CHEMBL172155 | — | — | 1 | 6.31 |
| CHEMBL330376 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL658 | SUFENTANIL | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2355317 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL1005 | REMIFENTANIL | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2365680 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL596 | FENTANYL | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL3302622 | — | IC50 | = | 2.81 | nM | 8.55 |
| CHEMBL634 | ALFENTANIL | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL4526998 | — | IC50 | = | 97.7 | nM | 7.01 |
| CHEMBL2365725 | — | IC50 | = | 245.5 | nM | 6.61 |
| CHEMBL4562635 | — | IC50 | = | 295.1 | nM | 6.53 |
| CHEMBL4446083 | — | IC50 | = | 489.0 | nM | 6.31 |
| CHEMBL172155 | — | IC50 | = | 489.7 | nM | 6.31 |
| CHEMBL330376 | — | IC50 | - | — | - |