Assay Detail
Binding
CHEMBL4374384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.17 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330376 | — | — | 1 | 7.16 |
| CHEMBL172155 | — | — | 1 | 6.49 |
| CHEMBL2365680 | — | — | 1 | 6.33 |
| CHEMBL2355317 | — | — | 1 | 6.30 |
| CHEMBL2365725 | — | — | 1 | 5.93 |
| CHEMBL658 | SUFENTANIL | 4.0 | 1 | 5.68 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 5.30 |
| CHEMBL634 | ALFENTANIL | 4.0 | 1 | - |
| CHEMBL1005 | REMIFENTANIL | 4.0 | 1 | - |
| CHEMBL4562635 | — | — | 1 | - |
| CHEMBL4446083 | — | — | 1 | - |
| CHEMBL4526998 | — | — | 1 | - |
| CHEMBL3302622 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330376 | — | IC50 | = | 69.4 | nM | 7.16 |
| CHEMBL172155 | — | IC50 | = | 322.1 | nM | 6.49 |
| CHEMBL2365680 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL2355317 | — | IC50 | = | 495.3 | nM | 6.30 |
| CHEMBL2365725 | — | IC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL658 | SUFENTANIL | IC50 | = | 2077.0 | nM | 5.68 |
| CHEMBL596 | FENTANYL | IC50 | = | 4973.0 | nM | 5.30 |
| CHEMBL634 | ALFENTANIL | IC50 | > | 10000.0 | nM | - |
| CHEMBL1005 | REMIFENTANIL | IC50 | > | 10000.0 | nM | - |
| CHEMBL4562635 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4446083 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4526998 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3302622 | — | IC50 | > | 10000.0 | nM | - |