Assay Detail
Binding
CHEMBL809700
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Binding affinity for Sigma opioid receptor type 2 in guinea pig brain homogenate with 4 nM [3H]-(+)-DTG
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Phenytoin derivatives as potent ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.42 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304506 | — | — | 1 | 8.52 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.22 |
| CHEMBL303408 | — | — | 1 | 8.08 |
| CHEMBL71104 | — | — | 1 | 7.96 |
| CHEMBL302096 | — | — | 1 | 7.72 |
| CHEMBL73169 | — | — | 1 | 7.60 |
| CHEMBL308433 | — | — | 1 | 7.37 |
| CHEMBL69972 | — | — | 1 | 7.31 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.16 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.79 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 6.25 |
| CHEMBL65951 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304506 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL303408 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL71104 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL302096 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL73169 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL308433 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL69972 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL60859 | BMY-14802 | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL65951 | — | Ki | = | 842.0 | nM | 6.08 |