Assay Detail
Binding
CHEMBL803922
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards sigma receptor in guinea pig brain membranes using [3H]DTG as radioligand
23
Total Activities
23
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
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.69 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85879 | — | — | 1 | 8.59 |
| CHEMBL112574 | — | — | 1 | 8.55 |
| CHEMBL112125 | — | — | 1 | 8.54 |
| CHEMBL112037 | — | — | 1 | 8.40 |
| CHEMBL114477 | — | — | 1 | 8.27 |
| CHEMBL111896 | — | — | 1 | 8.17 |
| CHEMBL113293 | — | — | 1 | 8.12 |
| CHEMBL113621 | — | — | 1 | 7.98 |
| CHEMBL325262 | — | — | 1 | 7.72 |
| CHEMBL114510 | — | — | 1 | 7.13 |
| CHEMBL19351 | — | — | 1 | 6.90 |
| CHEMBL278509 | — | — | 1 | 6.26 |
| CHEMBL114478 | — | — | 1 | 5.94 |
| CHEMBL274866 | — | — | 1 | 5.87 |
| CHEMBL277120 | — | — | 1 | 5.57 |
| CHEMBL59517 | — | — | 1 | 5.23 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 5.21 |
| CHEMBL113600 | — | — | 1 | 4.98 |
| CHEMBL113624 | — | — | 1 | 4.95 |
| CHEMBL9666 | — | — | 1 | 4.95 |
| CHEMBL9434 | PHENYLPIPERAZINE | — | 1 | 4.94 |
| CHEMBL334036 | — | — | 1 | 4.84 |
| CHEMBL724 | 2-PIPERAZIN-1-YL-PYRIMIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85879 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL112574 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL112125 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL112037 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL114477 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL111896 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL113293 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL113621 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL325262 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL114510 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL19351 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL278509 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL114478 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL274866 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL277120 | — | Ki | = | 2720.0 | nM | 5.57 |
| CHEMBL59517 | — | Ki | = | 5850.0 | nM | 5.23 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | Ki | = | 6150.0 | nM | 5.21 |
| CHEMBL113600 | — | Ki | = | 10480.0 | nM | 4.98 |
| CHEMBL113624 | — | Ki | = | 11360.0 | nM | 4.95 |
| CHEMBL9666 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL9434 | PHENYLPIPERAZINE | Ki | = | 11440.0 | nM | 4.94 |
| CHEMBL334036 | — | Ki | = | 14280.0 | nM | 4.84 |
| CHEMBL724 | 2-PIPERAZIN-1-YL-PYRIMIDINE | Ki | > | 10000.0 | nM | - |