Assay Detail
Binding
CHEMBL972419
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Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat liver homogenates by solid scintillation analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.44 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.38 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL466289 | — | — | 1 | 6.88 |
| CHEMBL468929 | — | — | 1 | 6.57 |
| CHEMBL466096 | — | — | 1 | 6.38 |
| CHEMBL511587 | — | — | 1 | 6.02 |
| CHEMBL468930 | — | — | 1 | 6.01 |
| CHEMBL138809 | — | — | 1 | 5.89 |
| CHEMBL513470 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL466289 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL468929 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL466096 | — | Ki | = | 414.0 | nM | 6.38 |
| CHEMBL511587 | — | Ki | = | 946.0 | nM | 6.02 |
| CHEMBL468930 | — | Ki | = | 971.0 | nM | 6.01 |
| CHEMBL138809 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL513470 | — | Ki | = | 1920.0 | nM | 5.72 |