Assay Detail
Binding
CHEMBL4358950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
39
Total Activities
38
Compounds Tested
1
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 |
|---|---|---|---|
| Ki | 39 | 6.62 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4482861 | — | — | 1 | 10.38 |
| CHEMBL4536304 | — | — | 1 | 10.27 |
| CHEMBL4438801 | — | — | 1 | 10.18 |
| CHEMBL4483022 | — | — | 1 | 9.49 |
| CHEMBL4535472 | — | — | 1 | 9.01 |
| CHEMBL4439953 | — | — | 1 | 8.49 |
| CHEMBL4467833 | — | — | 1 | 8.35 |
| CHEMBL4438158 | — | — | 1 | 8.11 |
| CHEMBL4450506 | — | — | 2 | 7.28 |
| CHEMBL4568994 | — | — | 1 | 7.20 |
| CHEMBL4554450 | — | — | 1 | 6.77 |
| CHEMBL4454147 | — | — | 1 | 6.77 |
| CHEMBL404505 | — | — | 1 | 6.64 |
| CHEMBL4456882 | — | — | 1 | 6.22 |
| CHEMBL4528557 | — | — | 1 | 6.15 |
| CHEMBL4459090 | — | — | 1 | 5.93 |
| CHEMBL4587519 | — | — | 1 | 5.85 |
| CHEMBL4587003 | — | — | 1 | 5.65 |
| CHEMBL4533687 | — | — | 1 | 5.43 |
| CHEMBL4475933 | — | — | 1 | 5.34 |
| CHEMBL151697 | — | — | 1 | 5.17 |
| CHEMBL4459403 | — | — | 1 | 5.16 |
| CHEMBL4590209 | — | — | 1 | 5.12 |
| CHEMBL4546903 | — | — | 1 | 5.02 |
| CHEMBL4476557 | — | — | 1 | 4.73 |
| CHEMBL4534152 | — | — | 1 | 4.59 |
| CHEMBL41103 | — | — | 1 | 4.37 |
| CHEMBL275970 | TRACIZOLINE | — | 1 | 4.33 |
| CHEMBL4445396 | — | — | 1 | 4.31 |
| CHEMBL2179398 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4482861 | — | Ki | = | 0.04169 | nM | 10.38 |
| CHEMBL4536304 | — | Ki | = | 0.0537 | nM | 10.27 |
| CHEMBL4438801 | — | Ki | = | 0.06607 | nM | 10.18 |
| CHEMBL4483022 | — | Ki | = | 0.3236 | nM | 9.49 |
| CHEMBL4535472 | — | Ki | = | 0.9772 | nM | 9.01 |
| CHEMBL4439953 | — | Ki | = | 3.236 | nM | 8.49 |
| CHEMBL4467833 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL4438158 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL4450506 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4568994 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4554450 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL4454147 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL404505 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL4450506 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL4456882 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL4528557 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL4459090 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL4587519 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL4587003 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL4533687 | — | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL4475933 | — | Ki | = | 4570.88 | nM | 5.34 |
| CHEMBL151697 | — | Ki | = | 6760.83 | nM | 5.17 |
| CHEMBL4459403 | — | Ki | = | 6918.31 | nM | 5.16 |
| CHEMBL4590209 | — | Ki | = | 7585.78 | nM | 5.12 |
| CHEMBL4546903 | — | Ki | = | 9549.93 | nM | 5.02 |
| CHEMBL4476557 | — | Ki | = | 18620.87 | nM | 4.73 |
| CHEMBL4534152 | — | Ki | = | 25703.96 | nM | 4.59 |
| CHEMBL41103 | — | Ki | = | 42657.95 | nM | 4.37 |
| CHEMBL275970 | TRACIZOLINE | Ki | = | 46773.51 | nM | 4.33 |
| CHEMBL4445396 | — | Ki | = | 48977.88 | nM | 4.31 |
| CHEMBL2179398 | — | Ki | = | 2238721.14 | nM | - |
| CHEMBL4543019 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4465834 | — | Ki | = | 416869.38 | nM | - |
| CHEMBL4584406 | — | Ki | = | 141253.75 | nM | - |
| CHEMBL4527478 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4469237 | — | Ki | = | 114815.36 | nM | - |
| CHEMBL4434967 | — | Ki | = | 169824.37 | nM | - |
| CHEMBL4553853 | — | Ki | = | 363078.05 | nM | - |
| CHEMBL4531381 | — | Ki | > | 1000000.0 | nM | - |