Assay Detail
Binding
CHEMBL846626
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes
6
Total Activities
6
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 | 6 | 7.06 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.40 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.82 |
| CHEMBL275528 | PHENCYCLIDINE | 2.0 | 1 | 6.25 |
| CHEMBL415284 | NALORPHINE | 2.0 | 1 | 5.75 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | - |
| CHEMBL80 | NALOXONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL275528 | PHENCYCLIDINE | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL415284 | NALORPHINE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL53 | APOMORPHINE | IC50 | > | 31000.0 | nM | - |
| CHEMBL80 | NALOXONE | IC50 | > | 100000.0 | nM | - |