Assay Detail
Binding
CHEMBL5328474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-DTG from rat liver homogenate S2R incubated for 120 mins by liquid scintillation counting method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.48 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437311 | — | — | 1 | 8.59 |
| CHEMBL5437477 | — | — | 1 | 8.11 |
| CHEMBL5433306 | — | — | 1 | 8.00 |
| CHEMBL5439863 | — | — | 1 | 7.96 |
| CHEMBL5395079 | — | — | 1 | 7.92 |
| CHEMBL5406931 | — | — | 1 | 7.92 |
| CHEMBL5406376 | — | — | 1 | 7.92 |
| CHEMBL5430002 | — | — | 1 | 7.89 |
| CHEMBL5424448 | — | — | 1 | 7.85 |
| CHEMBL5396488 | — | — | 1 | 7.75 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.75 |
| CHEMBL5421889 | — | — | 1 | 7.70 |
| CHEMBL5432579 | — | — | 1 | 7.64 |
| CHEMBL5434285 | — | — | 1 | 7.62 |
| CHEMBL5394434 | — | — | 1 | 7.40 |
| CHEMBL5420704 | — | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL5421208 | — | — | 1 | 7.07 |
| CHEMBL5434592 | — | — | 1 | 7.02 |
| CHEMBL5405188 | — | — | 1 | 7.00 |
| CHEMBL73824 | — | — | 1 | 6.69 |
| CHEMBL5408285 | — | — | 1 | 6.13 |
| CHEMBL828 | PHENOTHIAZINE | 2.0 | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437311 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL5437477 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL5433306 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5439863 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5395079 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5406931 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5406376 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5430002 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5424448 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5396488 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5421889 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5432579 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5434285 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL5394434 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5420704 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5421208 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL5434592 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL5405188 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL73824 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL5408285 | — | Ki | = | 736.0 | nM | 6.13 |
| CHEMBL828 | PHENOTHIAZINE | Ki | = | 1465.0 | nM | 5.83 |