Assay Detail
Binding
CHEMBL4481035
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Benzimidazolone-based selective σ2 receptor ligands: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.21 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4531345 | — | — | 1 | 9.18 |
| CHEMBL4542088 | — | — | 1 | 8.74 |
| CHEMBL4584941 | — | — | 1 | 8.69 |
| CHEMBL4537047 | — | — | 1 | 8.67 |
| CHEMBL4563981 | — | — | 1 | 8.59 |
| CHEMBL4577544 | — | — | 1 | 8.37 |
| CHEMBL4589807 | — | — | 1 | 8.34 |
| CHEMBL4580186 | — | — | 1 | 8.12 |
| CHEMBL4520061 | — | — | 1 | 7.74 |
| CHEMBL4573555 | — | — | 1 | 7.54 |
| CHEMBL4525954 | — | — | 1 | 7.49 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4531345 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL4542088 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL4584941 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL4537047 | — | Ki | = | 2.15 | nM | 8.67 |
| CHEMBL4563981 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4577544 | — | Ki | = | 4.27 | nM | 8.37 |
| CHEMBL4589807 | — | Ki | = | 4.55 | nM | 8.34 |
| CHEMBL4580186 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL4520061 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL4573555 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL4525954 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 80.6 | nM | 7.09 |