Assay Detail
Binding
CHEMBL860170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.74 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL545278 | — | — | 1 | 10.52 |
| CHEMBL539333 | — | — | 1 | 9.62 |
| CHEMBL540818 | — | — | 1 | 9.52 |
| CHEMBL537177 | — | — | 1 | 9.46 |
| CHEMBL544343 | — | — | 1 | 9.44 |
| CHEMBL540573 | — | — | 1 | 9.38 |
| CHEMBL559377 | — | — | 1 | 9.30 |
| CHEMBL545508 | — | — | 1 | 9.18 |
| CHEMBL537842 | — | — | 1 | 9.00 |
| CHEMBL190883 | — | — | 1 | 8.99 |
| CHEMBL535366 | — | — | 1 | 8.94 |
| CHEMBL538566 | — | — | 1 | 8.93 |
| CHEMBL558980 | — | — | 1 | 8.92 |
| CHEMBL552542 | — | — | 1 | 8.87 |
| CHEMBL535363 | — | — | 1 | 8.85 |
| CHEMBL536483 | — | — | 1 | 8.83 |
| CHEMBL559178 | — | — | 1 | 8.82 |
| CHEMBL534695 | — | — | 1 | 8.75 |
| CHEMBL542701 | — | — | 1 | 8.74 |
| CHEMBL540563 | — | — | 1 | 8.65 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.55 |
| CHEMBL554663 | — | — | 1 | 8.48 |
| CHEMBL539545 | — | — | 1 | 8.21 |
| CHEMBL538772 | — | — | 1 | 8.15 |
| CHEMBL553091 | — | — | 1 | 8.11 |
| CHEMBL554450 | — | — | 1 | 7.65 |
| CHEMBL537399 | — | — | 1 | 6.75 |
| CHEMBL540361 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL545278 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL539333 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL540818 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL537177 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL544343 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL540573 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL559377 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL545508 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL537842 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL190883 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL535366 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL538566 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL558980 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL552542 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL535363 | — | Ki | = | 1.43 | nM | 8.85 |
| CHEMBL536483 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL559178 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL534695 | — | Ki | = | 1.78 | nM | 8.75 |
| CHEMBL542701 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL540563 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL554663 | — | Ki | = | 3.32 | nM | 8.48 |
| CHEMBL539545 | — | Ki | = | 6.16 | nM | 8.21 |
| CHEMBL538772 | — | Ki | = | 7.05 | nM | 8.15 |
| CHEMBL553091 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL554450 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL537399 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL540361 | — | Ki | = | 1060.0 | nM | 5.97 |