Assay Detail
Binding
CHEMBL809524
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.23 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64115 | — | — | 1 | 8.64 |
| CHEMBL303336 | — | — | 1 | 7.92 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.77 |
| CHEMBL64047 | — | — | 1 | 7.64 |
| CHEMBL560 | — | — | 1 | 7.54 |
| CHEMBL61739 | — | — | 1 | 7.31 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.75 |
| CHEMBL292512 | — | — | 1 | 6.57 |
| CHEMBL64369 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64115 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL303336 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL64047 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL560 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL61739 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL292512 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL64369 | — | IC50 | = | 11000.0 | nM | 4.96 |