Assay Detail
Binding
CHEMBL803917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against [3H]- (+)-3-PPP binding to sigma receptor in guinea pig brain membrane homogenates
4
Total Activities
4
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 | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of N,N'-di-o-tolylguanidine analogues, high-affinity ligands for the haloperidol-sensitive sigma receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.05 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL78637 | — | — | 1 | 7.38 |
| CHEMBL312318 | — | — | 1 | 7.18 |
| CHEMBL543121 | — | — | 1 | 6.84 |
| CHEMBL312806 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL78637 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL312318 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL543121 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL312806 | — | IC50 | = | 163.0 | nM | 6.79 |