Assay Detail
Binding
CHEMBL809168
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In vitro binding affinity at Sigma opioid receptor type 1 on guinea pig brain membranes by [3H]pentazocine displacement.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 9 | 8.54 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL541091 | — | — | 1 | 9.15 |
| CHEMBL540331 | — | — | 1 | 8.80 |
| CHEMBL127899 | — | — | 1 | 8.74 |
| CHEMBL128860 | — | — | 1 | 8.72 |
| CHEMBL553962 | — | — | 1 | 8.66 |
| CHEMBL128799 | — | — | 1 | 8.39 |
| CHEMBL128717 | — | — | 1 | 8.25 |
| CHEMBL341003 | — | — | 1 | 8.09 |
| CHEMBL339638 | — | — | 1 | 8.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL541091 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL540331 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL127899 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL128860 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL553962 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL128799 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL128717 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL341003 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL339638 | — | IC50 | = | 8.1 | nM | 8.09 |