Assay Detail
Binding
CHEMBL4315424
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 membranes incubated for 120 mins by solid scintillation counting method
9
Total Activities
9
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
Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.99 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4448528 | — | — | 1 | 7.48 |
| CHEMBL4473586 | — | — | 1 | 7.41 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL4536973 | — | — | 1 | 6.85 |
| CHEMBL4561134 | — | — | 1 | 6.80 |
| CHEMBL4550150 | — | — | 1 | 6.37 |
| CHEMBL4453563 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4448528 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4473586 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4536973 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4561134 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4550150 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL4453563 | — | Ki | = | 1300.0 | nM | 5.89 |