Assay Detail
Binding
CHEMBL804880
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.03 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299499 | — | — | 1 | 8.55 |
| CHEMBL442356 | — | — | 1 | 8.49 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.30 |
| CHEMBL55970 | — | — | 1 | 8.21 |
| CHEMBL55873 | — | — | 1 | 8.15 |
| CHEMBL54407 | — | — | 1 | 8.15 |
| CHEMBL293059 | — | — | 1 | 8.10 |
| CHEMBL55769 | — | — | 1 | 8.10 |
| CHEMBL292450 | — | — | 1 | 8.05 |
| CHEMBL292668 | — | — | 1 | 8.00 |
| CHEMBL413257 | — | — | 1 | 7.89 |
| CHEMBL301623 | — | — | 1 | 7.77 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.55 |
| CHEMBL276500 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299499 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL442356 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL55970 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL55873 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL54407 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL293059 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL55769 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL292450 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL292668 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL413257 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL301623 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL276500 | — | IC50 | = | 76.0 | nM | 7.12 |