Assay Detail
Binding
CHEMBL965020
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ditolylguanidine from sigma 2 receptor in rat liver membrane by liquid scintillation analyzer
7
Total Activities
7
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
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.55 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.47 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.19 |
| CHEMBL477036 | — | — | 1 | 6.75 |
| CHEMBL513224 | — | — | 1 | 6.43 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.41 |
| CHEMBL518434 | — | — | 1 | 5.04 |
| CHEMBL477037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL477036 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL513224 | — | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL60859 | BMY-14802 | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL518434 | — | Ki | = | 9010.0 | nM | 5.04 |
| CHEMBL477037 | — | Ki | > | 10000.0 | nM | - |