Assay Detail
Binding
CHEMBL4307197
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
17
Total Activities
17
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
Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.08 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4449269 | — | — | 1 | 7.80 |
| CHEMBL4459690 | — | — | 1 | 7.75 |
| CHEMBL4446466 | — | — | 1 | 7.72 |
| CHEMBL4446431 | — | — | 1 | 7.70 |
| CHEMBL4581662 | — | — | 1 | 7.68 |
| CHEMBL4451677 | — | — | 1 | 7.46 |
| CHEMBL4533030 | — | — | 1 | 7.22 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL4439170 | — | — | 1 | 6.94 |
| CHEMBL4453315 | — | — | 1 | 6.92 |
| CHEMBL4445874 | — | — | 1 | 6.90 |
| CHEMBL4463741 | — | — | 1 | 6.75 |
| CHEMBL4567801 | — | — | 1 | 6.42 |
| CHEMBL4454333 | — | — | 1 | 6.08 |
| CHEMBL4442750 | — | — | 1 | 6.03 |
| CHEMBL4446009 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4449269 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4459690 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4446466 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4446431 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4581662 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4451677 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4533030 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4439170 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL4453315 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4445874 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4463741 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL4567801 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL4454333 | — | Ki | = | 829.0 | nM | 6.08 |
| CHEMBL4442750 | — | Ki | = | 944.0 | nM | 6.03 |
| CHEMBL4446009 | — | Ki | = | 1600.0 | nM | 5.80 |