Assay Detail
Binding
CHEMBL858016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Sigma-1 binding assay was performed using [3H](+)-pentazocine to label sigma-1 binding sites, in guinea pig cerebral cortex
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.21 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308633 | — | — | 1 | 8.30 |
| CHEMBL77925 | — | — | 1 | 8.24 |
| CHEMBL76256 | — | — | 1 | 8.19 |
| CHEMBL274490 | — | — | 1 | 8.17 |
| CHEMBL78272 | — | — | 1 | 8.11 |
| CHEMBL76944 | — | — | 1 | 8.02 |
| CHEMBL308085 | — | — | 1 | 7.21 |
| CHEMBL311578 | — | — | 1 | 7.15 |
| CHEMBL440689 | — | — | 1 | 7.05 |
| CHEMBL80422 | — | — | 1 | 6.63 |
| CHEMBL80582 | — | — | 1 | 6.59 |
| CHEMBL75625 | — | — | 1 | 6.54 |
| CHEMBL76556 | — | — | 1 | 6.47 |
| CHEMBL307850 | — | — | 1 | 6.34 |
| CHEMBL76807 | — | — | 1 | 6.29 |
| CHEMBL76002 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308633 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL77925 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL76256 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL274490 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL78272 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL76944 | — | Ki | = | 9.55 | nM | 8.02 |
| CHEMBL308085 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL311578 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL440689 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL80422 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL80582 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL75625 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL76556 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL307850 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL76807 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL76002 | — | Ki | = | 758.58 | nM | 6.12 |