Assay Detail
Binding
CHEMBL5133628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from Dunkin-Hartley guinea pig brain cortex Sigma 1 receptor incubated for 150 mins by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.35 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.59 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | — | 1 | 8.57 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.37 |
| CHEMBL4080696 | — | — | 1 | 8.22 |
| CHEMBL73824 | — | — | 1 | 7.85 |
| CHEMBL5192985 | — | — | 1 | 7.24 |
| CHEMBL5205647 | — | — | 1 | 7.03 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 6.91 |
| CHEMBL5198792 | — | — | 1 | 6.90 |
| CHEMBL5178450 | — | — | 1 | 6.81 |
| CHEMBL5194022 | — | — | 1 | 6.76 |
| CHEMBL5203238 | — | — | 1 | 6.17 |
| CHEMBL5190377 | — | — | 1 | 6.08 |
| CHEMBL335258 | TEREPHTHALAMIC ACID | — | 1 | - |
| CHEMBL3596572 | — | — | 1 | - |
| CHEMBL5194121 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4080696 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL73824 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5192985 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL5205647 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL5198792 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL5178450 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL5194022 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL5203238 | — | Ki | = | 668.0 | nM | 6.17 |
| CHEMBL5190377 | — | Ki | = | 837.0 | nM | 6.08 |
| CHEMBL335258 | TEREPHTHALAMIC ACID | Ki | > | 10000.0 | nM | - |
| CHEMBL3596572 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5194121 | — | Ki | > | 5000.0 | nM | - |