Assay Detail
Binding
CHEMBL4045546
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 analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.15 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4075349 | — | — | 1 | 7.32 |
| CHEMBL4088218 | — | — | 1 | 7.10 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL4065052 | — | — | 1 | 6.91 |
| CHEMBL1289403 | — | — | 1 | 6.74 |
| CHEMBL1289626 | — | — | 1 | 6.71 |
| CHEMBL319706 | (S)-IFENPRODIL | — | 1 | - |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4075349 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4088218 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4065052 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1289403 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL1289626 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL319706 | (S)-IFENPRODIL | Ki | - | — | - | |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - |