Assay Detail
Binding
CHEMBL3636228
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method in the presence of pentazocine
27
Total Activities
27
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
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.47 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.22 |
| CHEMBL3633403 | — | — | 1 | 8.13 |
| CHEMBL3633402 | — | — | 1 | 7.43 |
| CHEMBL3633393 | — | — | 1 | 6.81 |
| CHEMBL3633401 | — | — | 1 | 6.72 |
| CHEMBL3633404 | — | — | 1 | 6.53 |
| CHEMBL3633571 | — | — | 1 | 6.50 |
| CHEMBL3633400 | — | — | 1 | 6.30 |
| CHEMBL3633394 | — | — | 1 | 6.27 |
| CHEMBL3633395 | — | — | 1 | 6.26 |
| CHEMBL3633396 | — | — | 1 | 6.22 |
| CHEMBL3633391 | — | — | 1 | 5.85 |
| CHEMBL3633397 | — | — | 1 | 5.82 |
| CHEMBL3633398 | — | — | 1 | 5.57 |
| CHEMBL3633572 | — | — | 1 | 5.52 |
| CHEMBL3633399 | — | — | 1 | 5.31 |
| CHEMBL3633206 | — | — | 1 | - |
| CHEMBL3633389 | — | — | 1 | - |
| CHEMBL3633390 | — | — | 1 | - |
| CHEMBL3633388 | — | — | 1 | - |
| CHEMBL3633387 | — | — | 1 | - |
| CHEMBL3633211 | — | — | 1 | - |
| CHEMBL3633210 | — | — | 1 | - |
| CHEMBL3633209 | — | — | 1 | - |
| CHEMBL3633208 | — | — | 1 | - |
| CHEMBL3633392 | — | — | 1 | - |
| CHEMBL3633207 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 6.03 | nM | 8.22 |
| CHEMBL3633403 | — | Ki | = | 7.37 | nM | 8.13 |
| CHEMBL3633402 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3633393 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL3633401 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL3633404 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL3633571 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL3633400 | — | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL3633394 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL3633395 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL3633396 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL3633391 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL3633397 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3633398 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL3633572 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3633399 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL3633206 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633389 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633390 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633388 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633387 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633211 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633210 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633209 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633208 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633392 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3633207 | — | Ki | > | 10000.0 | nM | - |