Assay Detail
Binding
CHEMBL4706006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EST64454: a Highly Soluble σ Receptor Antagonist Clinical Candidate for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.81 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790686 | — | — | 1 | 8.70 |
| CHEMBL4760287 | — | — | 1 | 8.70 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.70 |
| CHEMBL4759343 | — | — | 1 | 8.52 |
| CHEMBL4762627 | — | — | 1 | 8.30 |
| CHEMBL4792105 | — | — | 1 | 8.22 |
| CHEMBL4776009 | — | — | 1 | 8.05 |
| CHEMBL4795798 | — | — | 1 | 8.05 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 7.92 |
| CHEMBL4792110 | — | — | 1 | 7.85 |
| CHEMBL4782656 | — | — | 1 | 7.82 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL4743610 | — | — | 1 | 7.66 |
| CHEMBL4757975 | — | — | 1 | 7.24 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.23 |
| CHEMBL4786808 | — | — | 1 | 6.68 |
| CHEMBL4795269 | — | — | 1 | 6.62 |
| CHEMBL4799271 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790686 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4760287 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4759343 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4762627 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4792105 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4776009 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4795798 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4792110 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4782656 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4743610 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4757975 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4786808 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4795269 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4799271 | — | Ki | = | 278.0 | nM | 6.56 |