Assay Detail
Binding
CHEMBL896183
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 membrane
15
Total Activities
15
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 | Intermediate |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.49 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL537177 | — | — | 1 | 9.46 |
| CHEMBL538089 | — | — | 1 | 9.05 |
| CHEMBL535856 | — | — | 1 | 8.80 |
| CHEMBL535857 | — | — | 1 | 8.50 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.49 |
| CHEMBL535634 | — | — | 1 | 8.26 |
| CHEMBL541390 | — | — | 1 | 8.17 |
| CHEMBL535410 | — | — | 1 | 7.35 |
| CHEMBL535636 | — | — | 1 | 6.94 |
| CHEMBL538091 | — | — | 1 | 6.86 |
| CHEMBL555969 | — | — | 1 | 6.76 |
| CHEMBL537696 | — | — | 1 | 6.47 |
| CHEMBL558572 | — | — | 1 | 6.13 |
| CHEMBL536759 | — | — | 1 | 5.70 |
| CHEMBL536305 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL537177 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL538089 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL535856 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL535857 | — | Ki | = | 3.16 | nM | 8.50 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.24 | nM | 8.49 |
| CHEMBL535634 | — | Ki | = | 5.48 | nM | 8.26 |
| CHEMBL541390 | — | Ki | = | 6.78 | nM | 8.17 |
| CHEMBL535410 | — | Ki | = | 44.9 | nM | 7.35 |
| CHEMBL535636 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL538091 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL555969 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL537696 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL558572 | — | Ki | = | 733.0 | nM | 6.13 |
| CHEMBL536759 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL536305 | — | Ki | = | 3450.0 | nM | 5.46 |