Assay Detail
Binding
CHEMBL803918
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against [3H]-DTG in guinea pig brain membrane homogenates
8
Total Activities
8
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 | 8 | 7.26 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310003 | — | — | 1 | 8.30 |
| CHEMBL81773 | — | — | 1 | 8.11 |
| CHEMBL78637 | — | — | 1 | 7.16 |
| CHEMBL312318 | — | — | 1 | 7.05 |
| CHEMBL543121 | — | — | 1 | 6.62 |
| CHEMBL312806 | — | — | 1 | 6.29 |
| CHEMBL311074 | — | — | 1 | - |
| CHEMBL79616 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310003 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL81773 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL78637 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL312318 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL543121 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL312806 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL311074 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL79616 | — | IC50 | > | 100000.0 | nM | - |