Assay Detail
Binding
CHEMBL4349903
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.67 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL3355379 | — | — | 1 | 7.05 |
| CHEMBL113830 | (S,R)-IFENPRODIL | — | 1 | 6.90 |
| CHEMBL4472450 | — | — | 1 | 6.79 |
| CHEMBL4521578 | — | — | 1 | 6.56 |
| CHEMBL4553195 | — | — | 1 | 6.47 |
| CHEMBL4463826 | — | — | 1 | 6.25 |
| CHEMBL4441512 | — | — | 1 | 6.15 |
| CHEMBL4464273 | — | — | 1 | 6.15 |
| CHEMBL4439555 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3355379 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL113830 | (S,R)-IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4472450 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL4521578 | — | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL4553195 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4463826 | — | Ki | = | 565.0 | nM | 6.25 |
| CHEMBL4441512 | — | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL4464273 | — | Ki | = | 715.0 | nM | 6.15 |
| CHEMBL4439555 | — | Ki | = | 705.0 | nM | 6.15 |