Assay Detail
Binding
CHEMBL1930737
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 without cerebellum
19
Total Activities
19
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
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities as σ₁ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.82 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929282 | — | — | 1 | 9.85 |
| CHEMBL1929279 | — | — | 1 | 9.68 |
| CHEMBL1929281 | — | — | 1 | 9.42 |
| CHEMBL1929287 | — | — | 1 | 8.99 |
| CHEMBL1929275 | — | — | 1 | 8.76 |
| CHEMBL128358 | — | — | 1 | 8.67 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.50 |
| CHEMBL1929430 | — | — | 1 | 7.85 |
| CHEMBL1929276 | — | — | 1 | 7.57 |
| CHEMBL1929286 | — | — | 1 | 7.38 |
| CHEMBL1929284 | — | — | 1 | 7.29 |
| CHEMBL1929278 | — | — | 1 | 7.28 |
| CHEMBL1929277 | — | — | 1 | 7.20 |
| CHEMBL1929285 | — | — | 1 | 6.47 |
| CHEMBL1929429 | — | — | 1 | 6.34 |
| CHEMBL1929428 | — | — | 1 | 6.25 |
| CHEMBL1929283 | — | — | 1 | 5.43 |
| CHEMBL1929288 | — | — | 1 | - |
| CHEMBL1929289 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929282 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL1929279 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL1929281 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL1929287 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL1929275 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL128358 | — | Ki | = | 2.12 | nM | 8.67 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.16 | nM | 8.50 |
| CHEMBL1929430 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL1929276 | — | Ki | = | 27.1 | nM | 7.57 |
| CHEMBL1929286 | — | Ki | = | 41.6 | nM | 7.38 |
| CHEMBL1929284 | — | Ki | = | 50.9 | nM | 7.29 |
| CHEMBL1929278 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL1929277 | — | Ki | = | 63.5 | nM | 7.20 |
| CHEMBL1929285 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL1929429 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL1929428 | — | Ki | = | 566.0 | nM | 6.25 |
| CHEMBL1929283 | — | Ki | = | 3690.0 | nM | 5.43 |
| CHEMBL1929288 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1929289 | — | Ki | > | 10000.0 | nM | - |