Assay Detail
Binding
CHEMBL1040025
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Displacement of [3H](+)-pentazocine from sigma1 receptor in human Jurkat cell membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.66 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL578825 | — | — | 1 | 10.28 |
| CHEMBL570795 | — | — | 1 | 10.24 |
| CHEMBL570529 | — | — | 1 | 10.18 |
| CHEMBL571418 | — | — | 1 | 10.05 |
| CHEMBL572294 | — | — | 1 | 10.01 |
| CHEMBL570067 | — | — | 1 | 9.96 |
| CHEMBL571659 | — | — | 1 | 9.68 |
| CHEMBL570789 | — | — | 1 | 9.36 |
| CHEMBL39900 | SPIPETHIANE | — | 1 | 9.23 |
| CHEMBL38634 | — | — | 1 | 9.21 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL578825 | — | Ki | = | 0.05248 | nM | 10.28 |
| CHEMBL570795 | — | Ki | = | 0.05754 | nM | 10.24 |
| CHEMBL570529 | — | Ki | = | 0.06607 | nM | 10.18 |
| CHEMBL571418 | — | Ki | = | 0.08913 | nM | 10.05 |
| CHEMBL572294 | — | Ki | = | 0.09772 | nM | 10.01 |
| CHEMBL570067 | — | Ki | = | 0.1096 | nM | 9.96 |
| CHEMBL571659 | — | Ki | = | 0.2089 | nM | 9.68 |
| CHEMBL570789 | — | Ki | = | 0.4365 | nM | 9.36 |
| CHEMBL39900 | SPIPETHIANE | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL38634 | — | Ki | = | 0.6166 | nM | 9.21 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 7.762 | nM | 8.11 |