Assay Detail
Binding
CHEMBL846484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes
7
Total Activities
7
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
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.27 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60859 | BMY-14802 | — | 1 | 7.15 |
| CHEMBL415284 | NALORPHINE | 2.0 | 1 | 6.13 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.11 |
| CHEMBL279676 | TENOCYCLIDINE | 2.0 | 1 | 5.69 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | - |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | - |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60859 | BMY-14802 | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL415284 | NALORPHINE | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL279676 | TENOCYCLIDINE | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL3 | NICOTINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL284237 | DIZOCILPINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL26 | SULPIRIDE | IC50 | > | 10000.0 | nM | - |