Assay Detail
Binding
CHEMBL4182984
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 cortex 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.11 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4218465 | — | — | 1 | 8.00 |
| CHEMBL4204621 | — | — | 1 | 7.34 |
| CHEMBL4206913 | — | — | 1 | 7.07 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL1289626 | — | — | 1 | 6.71 |
| CHEMBL4205955 | — | — | 1 | 6.58 |
| CHEMBL3753409 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4218465 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4204621 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4206913 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL1289626 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL4205955 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL3753409 | — | Ki | = | 676.0 | nM | 6.17 |