Assay Detail
Binding
CHEMBL4358954
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 low affinity site incubated for 45 mins by liquid scintillation spectrometry
9
Total Activities
9
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 | 9 | 5.72 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404505 | — | — | 1 | 7.94 |
| CHEMBL275970 | TRACIZOLINE | — | 1 | 6.48 |
| CHEMBL4587519 | — | — | 1 | 5.86 |
| CHEMBL2179398 | — | — | 1 | 5.45 |
| CHEMBL151697 | — | — | 1 | 5.25 |
| CHEMBL4528557 | — | — | 1 | 4.74 |
| CHEMBL4450506 | — | — | 1 | 4.29 |
| CHEMBL41103 | — | — | 1 | - |
| CHEMBL4553853 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404505 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL275970 | TRACIZOLINE | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL4587519 | — | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL2179398 | — | Ki | = | 3548.13 | nM | 5.45 |
| CHEMBL151697 | — | Ki | = | 5623.41 | nM | 5.25 |
| CHEMBL4528557 | — | Ki | = | 18197.01 | nM | 4.74 |
| CHEMBL4450506 | — | Ki | = | 51286.14 | nM | 4.29 |
| CHEMBL41103 | — | Ki | = | 151356.12 | nM | - |
| CHEMBL4553853 | — | Ki | = | 630957.34 | nM | - |