Assay Detail
Binding
CHEMBL3296644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RX821002 from alpha2-adrenergic receptor in prefrontal cortex of human brain after 30 mins by liquid scintillation spectrometric analysis
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Prefrontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Guanidine-based α2-adrenoceptor ligands: Towards selective antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 5.87 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256176 | — | — | 1 | 8.72 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | 4.0 | 1 | 7.68 |
| CHEMBL3289551 | — | — | 1 | 7.10 |
| CHEMBL3289540 | — | — | 1 | 6.85 |
| CHEMBL3289532 | — | — | 1 | 6.67 |
| CHEMBL3289521 | — | — | 1 | 6.58 |
| CHEMBL3289522 | — | — | 1 | 6.41 |
| CHEMBL3289531 | — | — | 1 | 6.29 |
| CHEMBL3289537 | — | — | 1 | 6.17 |
| CHEMBL3289548 | — | — | 1 | 6.16 |
| CHEMBL3289543 | — | — | 1 | 6.00 |
| CHEMBL3289530 | — | — | 1 | 5.97 |
| CHEMBL3289536 | — | — | 1 | 5.95 |
| CHEMBL3289547 | — | — | 1 | 5.88 |
| CHEMBL3289533 | — | — | 1 | 5.83 |
| CHEMBL3289529 | — | — | 1 | 5.82 |
| CHEMBL3289550 | — | — | 1 | 5.77 |
| CHEMBL3289526 | — | — | 1 | 5.76 |
| CHEMBL3289527 | — | — | 1 | 5.73 |
| CHEMBL3289549 | — | — | 1 | 5.66 |
| CHEMBL3289523 | — | — | 1 | 5.65 |
| CHEMBL3289545 | — | — | 1 | 5.63 |
| CHEMBL3289546 | — | — | 1 | 5.58 |
| CHEMBL3289542 | — | — | 1 | 5.48 |
| CHEMBL3289535 | — | — | 1 | 5.37 |
| CHEMBL3289534 | — | — | 1 | 5.36 |
| CHEMBL3289520 | — | — | 1 | 5.31 |
| CHEMBL3289538 | — | — | 1 | 5.08 |
| CHEMBL3289524 | — | — | 1 | 4.93 |
| CHEMBL3289544 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256176 | — | Ki | = | 1.905 | nM | 8.72 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL3289551 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3289540 | — | Ki | = | 141.25 | nM | 6.85 |
| CHEMBL3289532 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL3289521 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL3289522 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL3289531 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL3289537 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL3289548 | — | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL3289543 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3289530 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL3289536 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL3289547 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL3289533 | — | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL3289529 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL3289550 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL3289526 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL3289527 | — | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL3289549 | — | Ki | = | 2187.76 | nM | 5.66 |
| CHEMBL3289523 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL3289545 | — | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL3289546 | — | Ki | = | 2630.27 | nM | 5.58 |
| CHEMBL3289542 | — | Ki | = | 3311.31 | nM | 5.48 |
| CHEMBL3289535 | — | Ki | = | 4265.8 | nM | 5.37 |
| CHEMBL3289534 | — | Ki | = | 4365.16 | nM | 5.36 |
| CHEMBL3289520 | — | Ki | = | 4897.79 | nM | 5.31 |
| CHEMBL3289538 | — | Ki | = | 8317.64 | nM | 5.08 |
| CHEMBL3289524 | — | Ki | = | 11748.98 | nM | 4.93 |
| CHEMBL3289544 | — | Ki | = | 12302.69 | nM | 4.91 |
| CHEMBL3289541 | — | Ki | = | 14125.38 | nM | 4.85 |
| CHEMBL3289539 | — | Ki | = | 15135.61 | nM | 4.82 |
| CHEMBL3289525 | — | Ki | = | 18620.87 | nM | 4.73 |
| CHEMBL3289528 | — | Ki | = | 19054.61 | nM | 4.72 |