Assay Detail
Binding
CHEMBL4616034
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.71 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.80 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 7.75 |
| CHEMBL4646941 | — | — | 1 | 7.72 |
| CHEMBL4634076 | — | — | 1 | 7.16 |
| CHEMBL4647577 | — | — | 1 | 7.12 |
| CHEMBL4636822 | — | — | 1 | 7.05 |
| CHEMBL4649845 | — | — | 1 | 7.03 |
| CHEMBL4640727 | — | — | 1 | 6.90 |
| CHEMBL4632866 | — | — | 1 | 6.85 |
| CHEMBL4644682 | — | — | 1 | 6.64 |
| CHEMBL4646661 | — | — | 1 | 6.57 |
| CHEMBL4632489 | — | — | 1 | 6.50 |
| CHEMBL4648130 | — | — | 1 | 6.48 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 5.83 |
| CHEMBL4647197 | — | — | 1 | 5.60 |
| CHEMBL4632707 | — | — | 1 | 5.58 |
| CHEMBL4643104 | — | — | 1 | 5.57 |
| CHEMBL4639000 | — | — | 1 | - |
| CHEMBL4636837 | — | — | 1 | - |
| CHEMBL21708 | 4-METHYLBENZOIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4646941 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4634076 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4647577 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4636822 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4649845 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL4640727 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL4632866 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL4644682 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL4646661 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL4632489 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL4648130 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 1465.0 | nM | 5.83 |
| CHEMBL4647197 | — | Ki | = | 2514.0 | nM | 5.60 |
| CHEMBL4632707 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL4643104 | — | Ki | = | 2673.0 | nM | 5.57 |
| CHEMBL4639000 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4636837 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL21708 | 4-METHYLBENZOIC ACID | Ki | > | 10000.0 | nM | - |