Assay Detail
Binding
CHEMBL3411418
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Displacement of [125I] PIC from I1 imidazoline receptor in rat PC12 cells after 45 mins by gamma counting
27
Total Activities
27
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
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.98 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2058635 | — | — | 1 | 9.70 |
| CHEMBL3408293 | — | — | 1 | 9.66 |
| CHEMBL2058631 | — | — | 1 | 9.03 |
| CHEMBL3408294 | — | — | 1 | 8.55 |
| CHEMBL3408289 | — | — | 1 | 8.55 |
| CHEMBL3408291 | — | — | 1 | 8.49 |
| CHEMBL268734 | — | — | 1 | 8.28 |
| CHEMBL3408298 | — | — | 1 | 8.22 |
| CHEMBL3408297 | — | — | 1 | 8.19 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.85 |
| CHEMBL3408292 | — | — | 1 | 7.72 |
| CHEMBL3408285 | — | — | 1 | 7.72 |
| CHEMBL3408284 | — | — | 1 | 7.57 |
| CHEMBL3408290 | — | — | 1 | 7.38 |
| CHEMBL3408283 | — | — | 1 | 7.16 |
| CHEMBL3408286 | — | — | 1 | 7.14 |
| CHEMBL19236 | MOXONIDINE | 4.0 | 1 | 7.11 |
| CHEMBL289480 | RILMENIDINE | 4.0 | 1 | 7.08 |
| CHEMBL288139 | — | — | 1 | 6.27 |
| CHEMBL3408288 | — | — | 1 | - |
| CHEMBL3408279 | — | — | 1 | - |
| CHEMBL3408287 | — | — | 1 | - |
| CHEMBL3408295 | — | — | 1 | - |
| CHEMBL3408296 | — | — | 1 | - |
| CHEMBL3408282 | — | — | 1 | - |
| CHEMBL3408281 | — | — | 1 | - |
| CHEMBL3408280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2058635 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3408293 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2058631 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL3408294 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3408289 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3408291 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL268734 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3408298 | — | Ki | = | 6.03 | nM | 8.22 |
| CHEMBL3408297 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL134 | CLONIDINE | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL3408292 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3408285 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3408284 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3408290 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3408283 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3408286 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL19236 | MOXONIDINE | Ki | = | 77.8 | nM | 7.11 |
| CHEMBL289480 | RILMENIDINE | Ki | = | 83.1 | nM | 7.08 |
| CHEMBL288139 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL3408288 | — | Ki | - | — | - | |
| CHEMBL3408279 | — | Ki | - | — | - | |
| CHEMBL3408287 | — | Ki | - | — | - | |
| CHEMBL3408295 | — | Ki | - | — | - | |
| CHEMBL3408296 | — | Ki | - | — | - | |
| CHEMBL3408282 | — | Ki | - | — | - | |
| CHEMBL3408281 | — | Ki | - | — | - | |
| CHEMBL3408280 | — | Ki | - | — | - |