Assay Detail
Binding
CHEMBL4358953
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at high affinity site incubated for 45 mins by liquid scintillation spectrometry
18
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Ki | 18 | 7.94 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404505 | — | — | 2 | 9.89 |
| CHEMBL151697 | — | — | 3 | 9.52 |
| CHEMBL4587519 | — | — | 1 | 8.95 |
| CHEMBL4450506 | — | — | 1 | 8.61 |
| CHEMBL275970 | TRACIZOLINE | — | 2 | 8.48 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.74 |
| CHEMBL2179398 | — | — | 3 | 7.72 |
| CHEMBL4528557 | — | — | 1 | 7.53 |
| CHEMBL41103 | — | — | 3 | 6.89 |
| CHEMBL4553853 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404505 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL404505 | — | Ki | = | 0.1349 | nM | 9.87 |
| CHEMBL151697 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL151697 | — | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL4587519 | — | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL4450506 | — | Ki | = | 2.455 | nM | 8.61 |
| CHEMBL275970 | TRACIZOLINE | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL275970 | TRACIZOLINE | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL2179398 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL2179398 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4528557 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL41103 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL41103 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL4553853 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL2179398 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL151697 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL41103 | — | Ki | = | 151000.0 | nM | - |