Assay Detail
Binding
CHEMBL873113
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for the binding affinity towards sigma 1 receptor by displacing the radioligand [3H]-SKF- 10047 in whole rat brain membrane.
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.46 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL127006 | — | — | 3 | 10.05 |
| CHEMBL337974 | — | — | 1 | 9.21 |
| CHEMBL128442 | — | — | 1 | 9.16 |
| CHEMBL341472 | — | — | 1 | 9.00 |
| CHEMBL129092 | — | — | 1 | 8.16 |
| CHEMBL129200 | — | — | 1 | 8.03 |
| CHEMBL129075 | — | — | 1 | 7.66 |
| CHEMBL128997 | — | — | 1 | 7.59 |
| CHEMBL338465 | — | — | 1 | 7.39 |
| CHEMBL339206 | — | — | 1 | 6.60 |
| CHEMBL128358 | — | — | 1 | 6.01 |
| CHEMBL128125 | — | — | 1 | 5.82 |
| CHEMBL129145 | — | — | 1 | 5.67 |
| CHEMBL129091 | — | — | 1 | 5.33 |
| CHEMBL129551 | — | — | 1 | 5.23 |
| CHEMBL129655 | — | — | 1 | 5.03 |
| CHEMBL128996 | — | — | 1 | - |
| CHEMBL129654 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL127006 | — | IC50 | = | 0.089 | nM | 10.05 |
| CHEMBL127006 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL337974 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL128442 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL127006 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL341472 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL129092 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL129200 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL129075 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL128997 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL338465 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL339206 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL128358 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL128125 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL129145 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL129091 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL129551 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL129655 | — | IC50 | = | 9450.0 | nM | 5.03 |
| CHEMBL128996 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL129654 | — | IC50 | > | 10000.0 | nM | - |