Assay Detail
Binding
CHEMBL1040026
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Displacement of [3H]DTG from sigma2 receptor in rat cerebral cortex cell membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.96 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL570067 | — | — | 1 | 8.08 |
| CHEMBL570789 | — | — | 1 | 7.85 |
| CHEMBL38634 | — | — | 1 | 7.66 |
| CHEMBL570795 | — | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.95 |
| CHEMBL570529 | — | — | 1 | 6.76 |
| CHEMBL571418 | — | — | 1 | 6.65 |
| CHEMBL572294 | — | — | 1 | 6.64 |
| CHEMBL571659 | — | — | 1 | 6.52 |
| CHEMBL39900 | SPIPETHIANE | — | 1 | 6.40 |
| CHEMBL578825 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL570067 | — | Ki | = | 8.318 | nM | 8.08 |
| CHEMBL570789 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL38634 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL570795 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL570529 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL571418 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL572294 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL571659 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL39900 | SPIPETHIANE | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL578825 | — | Ki | = | 1548.82 | nM | 5.81 |