Assay Detail
Binding
CHEMBL4616033
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 membranes incubated for 1 hr by liquid scintillation counting method
20
Total Activities
20
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
Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.26 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.60 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.33 |
| CHEMBL4632489 | — | — | 1 | 7.72 |
| CHEMBL4646661 | — | — | 1 | 7.66 |
| CHEMBL4646941 | — | — | 1 | 7.62 |
| CHEMBL4648130 | — | — | 1 | 7.31 |
| CHEMBL4632866 | — | — | 1 | 7.30 |
| CHEMBL4640727 | — | — | 1 | 7.21 |
| CHEMBL4649845 | — | — | 1 | 7.19 |
| CHEMBL4643104 | — | — | 1 | 7.05 |
| CHEMBL4634076 | — | — | 1 | 7.03 |
| CHEMBL4644682 | — | — | 1 | 6.84 |
| CHEMBL4647577 | — | — | 1 | 6.83 |
| CHEMBL4647197 | — | — | 1 | 6.77 |
| CHEMBL4636822 | — | — | 1 | 6.60 |
| CHEMBL4632707 | — | — | 1 | 6.15 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | - |
| CHEMBL4639000 | — | — | 1 | - |
| CHEMBL4636837 | — | — | 1 | - |
| CHEMBL21708 | 4-METHYLBENZOIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL4632489 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4646661 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4646941 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4648130 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4632866 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4640727 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4649845 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL4643104 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4634076 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL4644682 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL4647577 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL4647197 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4636822 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4632707 | — | Ki | = | 711.0 | nM | 6.15 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | - | — | - | |
| CHEMBL4639000 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4636837 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL21708 | 4-METHYLBENZOIC ACID | Ki | > | 10000.0 | nM | - |