Assay Detail
Binding
CHEMBL809837
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity at Sigma opioid receptors on guinea pig brain membranes by [3H]3-PPP displacement.
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.59 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521582 | — | — | 1 | 8.89 |
| CHEMBL553962 | — | — | 1 | 8.82 |
| CHEMBL540331 | — | — | 1 | 8.74 |
| CHEMBL128860 | — | — | 1 | 8.68 |
| CHEMBL128799 | — | — | 1 | 8.35 |
| CHEMBL128717 | — | — | 1 | 8.24 |
| CHEMBL127899 | — | — | 1 | 8.10 |
| CHEMBL339638 | — | — | 1 | 8.05 |
| CHEMBL341003 | — | — | 1 | 8.02 |
| CHEMBL545760 | — | — | 1 | 8.00 |
| CHEMBL127720 | — | — | 1 | 7.92 |
| CHEMBL421446 | — | — | 1 | 7.89 |
| CHEMBL340587 | — | — | 1 | 7.54 |
| CHEMBL542786 | — | — | 1 | 7.47 |
| CHEMBL543896 | — | — | 1 | 6.96 |
| CHEMBL11311 | — | — | 1 | 6.96 |
| CHEMBL538845 | — | — | 1 | 6.89 |
| CHEMBL340275 | — | — | 1 | 6.82 |
| CHEMBL128254 | — | — | 1 | 6.80 |
| CHEMBL339253 | — | — | 1 | 6.77 |
| CHEMBL128999 | — | — | 1 | 6.77 |
| CHEMBL128944 | — | — | 1 | 6.64 |
| CHEMBL553841 | — | — | 1 | 6.48 |
| CHEMBL338781 | — | — | 1 | 6.38 |
| CHEMBL538290 | — | — | 1 | - |
| CHEMBL341508 | — | — | 1 | - |
| CHEMBL128998 | — | — | 1 | - |
| CHEMBL542784 | — | — | 1 | - |
| CHEMBL541091 | — | — | 1 | - |
| CHEMBL555052 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521582 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL553962 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL540331 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL128860 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL128799 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL128717 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL127899 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL339638 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL341003 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL545760 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL127720 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL421446 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL340587 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL542786 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL543896 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL11311 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL538845 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL340275 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL128254 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL339253 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL128999 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL128944 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL553841 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL338781 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL538290 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL341508 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL128998 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL542784 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL541091 | — | IC50 | - | nM | - | |
| CHEMBL555052 | — | IC50 | > | 1000.0 | nM | - |