Assay Detail
Binding
CHEMBL4254057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes in presence of (+)-pentazocine by radioligand binding assay
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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (σ2) receptor and P-gp protein in the cytotoxic action: In vitro and in vivo activity in pancreatic tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.48 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4292641 | — | — | 1 | 7.82 |
| CHEMBL4290541 | — | — | 1 | 7.47 |
| CHEMBL4285825 | — | — | 1 | 7.45 |
| CHEMBL4284762 | — | — | 1 | 7.19 |
| CHEMBL4277892 | — | — | 1 | - |
| CHEMBL4282423 | — | — | 1 | - |
| CHEMBL4293027 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4292641 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4290541 | — | Ki | = | 34.1 | nM | 7.47 |
| CHEMBL4285825 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL4284762 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL4277892 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4282423 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4293027 | — | Ki | > | 10000.0 | nM | - |