Assay Detail
Binding
CHEMBL3100691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis
12
Total Activities
12
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
From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.76 | 8.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 8.99 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.89 |
| CHEMBL3099037 | — | — | 1 | 7.22 |
| CHEMBL3099036 | — | — | 1 | 7.11 |
| CHEMBL3099035 | — | — | 1 | 6.99 |
| CHEMBL3099053 | — | — | 1 | 6.73 |
| CHEMBL3099052 | — | — | 1 | 6.25 |
| CHEMBL3099034 | — | — | 1 | 5.72 |
| CHEMBL3099050 | — | — | 1 | 5.57 |
| CHEMBL3099051 | — | — | 1 | 5.51 |
| CHEMBL518480 | — | — | 1 | 5.33 |
| CHEMBL456206 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3099037 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3099036 | — | Ki | = | 78.5 | nM | 7.11 |
| CHEMBL3099035 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL3099053 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL3099052 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL3099034 | — | Ki | = | 1910.0 | nM | 5.72 |
| CHEMBL3099050 | — | Ki | = | 2680.0 | nM | 5.57 |
| CHEMBL3099051 | — | Ki | = | 3080.0 | nM | 5.51 |
| CHEMBL518480 | — | Ki | = | 4734.0 | nM | 5.33 |
| CHEMBL456206 | — | Ki | > | 5000.0 | nM | - |