Assay Detail
Binding
CHEMBL4393065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed in HEK293 cell membranes after 120 mins by microbeta scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.04 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3359239 | — | — | 1 | 8.96 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.51 |
| CHEMBL2203551 | — | — | 1 | 8.39 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.15 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.82 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL2338343 | — | — | 1 | 7.52 |
| CHEMBL3417063 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3359239 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2203551 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2338343 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3417063 | — | Ki | = | 61.0 | nM | 7.21 |