Assay Detail
Binding
CHEMBL4358952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]clonidine from I1IR in human brain frontal cortex in presence of adrenaline incubated for 45 mins by liquid scintillation spectrometry
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.47 | 8.45 |
| Ki | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19236 | MOXONIDINE | 4.0 | 1 | 8.45 |
| CHEMBL4536304 | — | — | 1 | 8.09 |
| CHEMBL4434967 | — | — | 1 | 7.98 |
| CHEMBL4535472 | — | — | 1 | 7.54 |
| CHEMBL4590209 | — | — | 1 | 7.19 |
| CHEMBL4482861 | — | — | 1 | 6.74 |
| CHEMBL4459090 | — | — | 1 | 6.19 |
| CHEMBL4438158 | — | — | 1 | 5.87 |
| CHEMBL4546903 | — | — | 1 | 5.47 |
| CHEMBL4438801 | — | — | 1 | 5.26 |
| CHEMBL4483022 | — | — | 1 | 5.14 |
| CHEMBL4467833 | — | — | 1 | 5.13 |
| CHEMBL4469237 | — | — | 1 | 5.12 |
| CHEMBL4534152 | — | — | 1 | - |
| CHEMBL4450506 | — | — | 2 | - |
| CHEMBL4439953 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19236 | MOXONIDINE | IC50 | = | 3.548 | nM | 8.45 |
| CHEMBL4536304 | — | IC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4434967 | — | IC50 | = | 10.47 | nM | 7.98 |
| CHEMBL4535472 | — | IC50 | = | 28.84 | nM | 7.54 |
| CHEMBL4590209 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL4482861 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL4459090 | — | IC50 | = | 645.65 | nM | 6.19 |
| CHEMBL4438158 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL4546903 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL4438801 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL4483022 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4467833 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL4469237 | — | IC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL4450506 | — | IC50 | = | 912010.84 | nM | - |
| CHEMBL4450506 | — | Ki | = | 912000.0 | nM | - |
| CHEMBL4534152 | — | IC50 | = | 602559.59 | nM | - |
| CHEMBL4439953 | — | IC50 | > | 1000000.0 | nM | - |