Assay Detail
Binding
CHEMBL4685219
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cortex |
| 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
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.47 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4746028 | — | — | 1 | 8.72 |
| CHEMBL4740593 | — | — | 1 | 8.22 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4754021 | — | — | 1 | 7.77 |
| CHEMBL4778291 | — | — | 1 | 7.66 |
| CHEMBL4800530 | — | — | 1 | 7.51 |
| CHEMBL4745685 | — | — | 1 | 7.36 |
| CHEMBL4759924 | — | — | 1 | 7.34 |
| CHEMBL4745317 | — | — | 1 | 7.29 |
| CHEMBL4758763 | — | — | 1 | 7.29 |
| CHEMBL55317 | — | — | 1 | 7.24 |
| CHEMBL25858 | — | — | 1 | 7.23 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL4759856 | — | — | 1 | 6.78 |
| CHEMBL4744736 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4746028 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4740593 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4754021 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4778291 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4800530 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4745685 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4759924 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4745317 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4758763 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL55317 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL25858 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4759856 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL4744736 | — | Ki | = | 285.0 | nM | 6.54 |