Assay Detail
Binding
CHEMBL1023944
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Displacement of [3H]DTG from sigma 2 receptor in rat liver membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 18 | 6.79 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473989 | — | — | 1 | 8.23 |
| CHEMBL473990 | — | — | 1 | 8.23 |
| CHEMBL274010 | — | — | 1 | 8.07 |
| CHEMBL474565 | — | — | 1 | 6.94 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.89 |
| CHEMBL515571 | — | — | 1 | 6.77 |
| CHEMBL514488 | — | — | 1 | 6.73 |
| CHEMBL473976 | — | — | 1 | 6.67 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.63 |
| CHEMBL472979 | — | — | 1 | 6.61 |
| CHEMBL472984 | — | — | 1 | 6.52 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 6.49 |
| CHEMBL474175 | — | — | 1 | 6.47 |
| CHEMBL473975 | — | — | 1 | 6.42 |
| CHEMBL473783 | — | — | 1 | 6.37 |
| CHEMBL474182 | — | — | 1 | 5.89 |
| CHEMBL474566 | — | — | 1 | 5.54 |
| CHEMBL474567 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473989 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL473990 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL274010 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL474565 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL515571 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL514488 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL473976 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL472979 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL472984 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL474175 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL473975 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL473783 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL474182 | — | Ki | = | 1292.0 | nM | 5.89 |
| CHEMBL474566 | — | Ki | = | 2881.0 | nM | 5.54 |
| CHEMBL474567 | — | Ki | > | 10000.0 | nM | - |