Assay Detail
Binding
CHEMBL1023943
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.48 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473783 | — | — | 1 | 10.00 |
| CHEMBL474565 | — | — | 1 | 8.54 |
| CHEMBL472979 | — | — | 1 | 8.44 |
| CHEMBL515571 | — | — | 1 | 8.41 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.24 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 7.82 |
| CHEMBL473976 | — | — | 1 | 7.64 |
| CHEMBL514488 | — | — | 1 | 7.52 |
| CHEMBL474175 | — | — | 1 | 7.48 |
| CHEMBL472984 | — | — | 1 | 7.21 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.75 |
| CHEMBL473975 | — | — | 1 | 6.59 |
| CHEMBL474567 | — | — | 1 | 6.41 |
| CHEMBL474182 | — | — | 1 | 5.98 |
| CHEMBL474566 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473783 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL474565 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL472979 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL515571 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL473976 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL514488 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL474175 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL472984 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL473975 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL474567 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL474182 | — | Ki | = | 1057.0 | nM | 5.98 |
| CHEMBL474566 | — | Ki | = | 6230.0 | nM | 5.21 |