Assay Detail
Binding
CHEMBL4274854
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.46 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL4288091 | — | — | 1 | 6.67 |
| CHEMBL4276754 | — | — | 1 | 6.58 |
| CHEMBL4284692 | — | — | 1 | 6.58 |
| CHEMBL4284122 | — | — | 1 | 6.03 |
| CHEMBL4280186 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4288091 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL4276754 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL4284692 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL4284122 | — | Ki | = | 942.0 | nM | 6.03 |
| CHEMBL4280186 | — | Ki | = | 992.0 | nM | 6.00 |