Assay Detail
Binding
CHEMBL3367283
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 cortex membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Pyridine analogues of spirocyclic σ₁ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.03 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064198 | — | — | 1 | 9.51 |
| CHEMBL521657 | — | — | 1 | 9.49 |
| CHEMBL138083 | — | — | 1 | 9.16 |
| CHEMBL141209 | — | — | 1 | 8.89 |
| CHEMBL577956 | — | — | 1 | 8.64 |
| CHEMBL494870 | — | — | 1 | 8.37 |
| CHEMBL3309614 | — | — | 1 | 8.34 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL3309265 | — | — | 1 | 7.96 |
| CHEMBL148289 | — | — | 1 | 7.80 |
| CHEMBL3309615 | — | — | 1 | 7.72 |
| CHEMBL3309610 | — | — | 1 | 7.64 |
| CHEMBL3309608 | — | — | 1 | 7.36 |
| CHEMBL3309611 | — | — | 1 | 7.36 |
| CHEMBL2064190 | — | — | 1 | 7.19 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL3309609 | — | — | 1 | 6.92 |
| CHEMBL3309612 | — | — | 1 | 6.75 |
| CHEMBL3309613 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064198 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL521657 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL138083 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL141209 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL577956 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL494870 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3309614 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3309265 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL148289 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3309615 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3309610 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3309608 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3309611 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2064190 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3309609 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3309612 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL3309613 | — | Ki | > | 1000.0 | nM | - |