Assay Detail
Binding
CHEMBL1785973
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor PCP binding site in guinea pig brain by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| 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 of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA and σ receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.53 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.46 |
| CHEMBL1783450 | — | — | 1 | 7.72 |
| CHEMBL1783458 | — | — | 1 | 7.57 |
| CHEMBL1783463 | — | — | 1 | 6.79 |
| CHEMBL1783426 | — | — | 1 | 6.78 |
| CHEMBL1783460 | — | — | 1 | 6.78 |
| CHEMBL1783464 | — | — | 1 | 6.76 |
| CHEMBL1783454 | — | — | 1 | 6.50 |
| CHEMBL1783461 | — | — | 1 | 6.49 |
| CHEMBL1783448 | — | — | 1 | 6.35 |
| CHEMBL1783457 | — | — | 1 | 6.29 |
| CHEMBL1783453 | — | — | 1 | 6.18 |
| CHEMBL1783456 | — | — | 1 | 6.07 |
| CHEMBL1783455 | — | — | 1 | 6.02 |
| CHEMBL1783462 | — | — | 1 | 5.91 |
| CHEMBL1783459 | — | — | 1 | 5.90 |
| CHEMBL1783449 | — | — | 1 | 5.78 |
| CHEMBL1783465 | — | — | 1 | 5.19 |
| CHEMBL1783451 | — | — | 1 | - |
| CHEMBL1783452 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1783450 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1783458 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL1783463 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL1783426 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL1783460 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL1783464 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL1783454 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL1783461 | — | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL1783448 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL1783457 | — | Ki | = | 511.0 | nM | 6.29 |
| CHEMBL1783453 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL1783456 | — | Ki | = | 856.0 | nM | 6.07 |
| CHEMBL1783455 | — | Ki | = | 955.0 | nM | 6.02 |
| CHEMBL1783462 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL1783459 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL1783449 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL1783465 | — | Ki | = | 6450.0 | nM | 5.19 |
| CHEMBL1783451 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1783452 | — | Ki | > | 10000.0 | nM | - |