Assay Detail
Binding
CHEMBL4734036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in human brain membrane by liquid scintillation spectroscopy
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Di-aryl guanidinium derivatives: Towards improved α2-Adrenergic affinity and antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.01 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4755913 | — | — | 1 | 9.09 |
| CHEMBL75389 | — | — | 1 | 8.80 |
| CHEMBL4763113 | — | — | 1 | 8.75 |
| CHEMBL3216452 | — | — | 1 | 7.91 |
| CHEMBL4798553 | — | — | 1 | 7.47 |
| CHEMBL444295 | — | — | 1 | 7.33 |
| CHEMBL4745647 | — | — | 1 | 7.17 |
| CHEMBL451179 | — | — | 1 | 7.11 |
| CHEMBL4799288 | — | — | 1 | 7.06 |
| CHEMBL4795780 | — | — | 1 | 7.05 |
| CHEMBL4787567 | — | — | 1 | 6.92 |
| CHEMBL4790650 | — | — | 1 | 6.86 |
| CHEMBL4764564 | — | — | 1 | 6.78 |
| CHEMBL3217127 | — | — | 1 | 6.76 |
| CHEMBL3304530 | — | — | 1 | 6.63 |
| CHEMBL4744028 | — | — | 1 | 6.58 |
| CHEMBL4778444 | — | — | 1 | 6.45 |
| CHEMBL4762029 | — | — | 1 | 6.38 |
| CHEMBL4747130 | — | — | 1 | 6.36 |
| CHEMBL4795084 | — | — | 1 | 6.17 |
| CHEMBL4748073 | — | — | 1 | 6.13 |
| CHEMBL4800044 | — | — | 1 | 5.76 |
| CHEMBL4759811 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4755913 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL75389 | — | Ki | = | 1.58 | nM | 8.80 |
| CHEMBL4763113 | — | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL3216452 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL4798553 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL444295 | — | Ki | = | 46.8 | nM | 7.33 |
| CHEMBL4745647 | — | Ki | = | 67.6 | nM | 7.17 |
| CHEMBL451179 | — | Ki | = | 77.6 | nM | 7.11 |
| CHEMBL4799288 | — | Ki | = | 86.8 | nM | 7.06 |
| CHEMBL4795780 | — | Ki | = | 89.9 | nM | 7.05 |
| CHEMBL4787567 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4790650 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4764564 | — | Ki | = | 165.9 | nM | 6.78 |
| CHEMBL3217127 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL3304530 | — | Ki | = | 231.8 | nM | 6.63 |
| CHEMBL4744028 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL4778444 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4762029 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL4747130 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL4795084 | — | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL4748073 | — | Ki | = | 742.0 | nM | 6.13 |
| CHEMBL4800044 | — | Ki | = | 1745.0 | nM | 5.76 |
| CHEMBL4759811 | — | Ki | = | 2485.0 | nM | 5.61 |