Assay Detail
Binding
CHEMBL3815884
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | PC-12 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.33 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2058635 | — | — | 1 | 9.75 |
| CHEMBL360803 | PI-CLONIDINE | — | 1 | 9.10 |
| CHEMBL266155 | BENAZOLINE | — | 1 | 8.89 |
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 8.25 |
| CHEMBL289480 | RILMENIDINE | 4.0 | 1 | 7.90 |
| CHEMBL1162356 | — | — | 1 | 7.55 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2058635 | — | Ki | = | 0.1778 | nM | 9.75 |
| CHEMBL360803 | PI-CLONIDINE | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL266155 | BENAZOLINE | Ki | = | 1.288 | nM | 8.89 |
| CHEMBL17860 | LOFEXIDINE | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL289480 | RILMENIDINE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1162356 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL134 | CLONIDINE | Ki | = | 125.89 | nM | 6.90 |