Assay Detail
Binding
CHEMBL807589
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Evaluated for the binding affinity towards sigma 2 receptor by displacing the radioligand [3H]DTG in guinea-pig brain cortex.
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
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 | 8.16 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129145 | — | — | 1 | 10.80 |
| CHEMBL337974 | — | — | 1 | 10.52 |
| CHEMBL128997 | — | — | 1 | 9.36 |
| CHEMBL129091 | — | — | 1 | 9.00 |
| CHEMBL341472 | — | — | 1 | 8.96 |
| CHEMBL129654 | — | — | 1 | 8.96 |
| CHEMBL129655 | — | — | 1 | 8.96 |
| CHEMBL129092 | — | — | 1 | 8.35 |
| CHEMBL129200 | — | — | 1 | 8.34 |
| CHEMBL128442 | — | — | 1 | 8.26 |
| CHEMBL129551 | — | — | 1 | 8.00 |
| CHEMBL128996 | — | — | 1 | 7.06 |
| CHEMBL338465 | — | — | 1 | 7.00 |
| CHEMBL129075 | — | — | 1 | 6.96 |
| CHEMBL127006 | — | — | 3 | 6.96 |
| CHEMBL128358 | — | — | 1 | 6.89 |
| CHEMBL339206 | — | — | 1 | 6.87 |
| CHEMBL128125 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129145 | — | IC50 | = | 0.016 | nM | 10.80 |
| CHEMBL337974 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL128997 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL129091 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL129654 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL129655 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL341472 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL129092 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL129200 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL128442 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL129551 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL128996 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL338465 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL129075 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL127006 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL127006 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL128358 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL339206 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL127006 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL128125 | — | IC50 | = | 0.008 | nM | - |