Assay Detail
Binding
CHEMBL4734202
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 membrane incubated for 120 mins by liquid scintillation counting method
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| 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
Novel σ antagonists designed for tumor therapy: Structure - activity relationships of aminoethyl substituted cyclohexanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.06 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4758825 | — | — | 2 | 9.21 |
| CHEMBL4756284 | — | — | 1 | 8.89 |
| CHEMBL4793113 | — | — | 1 | 8.85 |
| CHEMBL4746722 | — | — | 2 | 8.74 |
| CHEMBL4741910 | — | — | 1 | 8.70 |
| CHEMBL4757626 | — | — | 1 | 8.52 |
| CHEMBL4747167 | — | — | 1 | 8.44 |
| CHEMBL4751986 | — | — | 1 | 8.38 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4741498 | — | — | 1 | 8.00 |
| CHEMBL4749981 | — | — | 1 | 7.89 |
| CHEMBL4754878 | — | — | 1 | 7.85 |
| CHEMBL4797217 | — | — | 1 | 7.80 |
| CHEMBL4754558 | — | — | 1 | 7.37 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL4758163 | — | — | 1 | 6.86 |
| CHEMBL4792725 | — | — | 1 | 6.78 |
| CHEMBL4795923 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4758825 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL4756284 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4793113 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4746722 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4758825 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4741910 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4746722 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL4757626 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4747167 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4751986 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4741498 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4749981 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4754878 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4797217 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4754558 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4758163 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4792725 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL4795923 | — | Ki | = | 603.0 | nM | 6.22 |