Assay Detail
Binding
CHEMBL4481034
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins 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 non-opioid intracellular receptor 1 (CHEMBL3602) ↗| 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 | 6.66 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.47 |
| CHEMBL4563981 | — | — | 1 | 7.30 |
| CHEMBL4580186 | — | — | 1 | 7.14 |
| CHEMBL4520061 | — | — | 1 | 6.84 |
| CHEMBL4573555 | — | — | 1 | 6.78 |
| CHEMBL4542088 | — | — | 1 | 6.56 |
| CHEMBL4537047 | — | — | 1 | 6.52 |
| CHEMBL4584941 | — | — | 1 | 6.44 |
| CHEMBL4589807 | — | — | 1 | 6.14 |
| CHEMBL4531345 | — | — | 1 | 6.12 |
| CHEMBL4525954 | — | — | 1 | 6.00 |
| CHEMBL4577544 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.35 | nM | 8.47 |
| CHEMBL4563981 | — | Ki | = | 50.22 | nM | 7.30 |
| CHEMBL4580186 | — | Ki | = | 72.3 | nM | 7.14 |
| CHEMBL4520061 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4573555 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL4542088 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL4537047 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL4584941 | — | Ki | = | 366.0 | nM | 6.44 |
| CHEMBL4589807 | — | Ki | = | 724.0 | nM | 6.14 |
| CHEMBL4531345 | — | Ki | = | 752.0 | nM | 6.12 |
| CHEMBL4525954 | — | Ki | = | 988.0 | nM | 6.00 |
| CHEMBL4577544 | — | Ki | = | 2274.0 | nM | 5.64 |