Assay Detail
Functional
CHEMBL4734035
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at adrenergic alpha 2 receptor in human brain membrane assessed as inhibition of UK14304-induced stimulation of [35S]GTPgammaS binding by liquid scintillation spectroscopy (Rvb = 1.77 +/- 0.16 uM)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 9 | 4.64 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787567 | — | — | 1 | 5.38 |
| CHEMBL4795780 | — | — | 1 | 4.99 |
| CHEMBL4763113 | — | — | 1 | 4.94 |
| CHEMBL3216452 | — | — | 1 | 4.70 |
| CHEMBL4755913 | — | — | 1 | 4.52 |
| CHEMBL4745647 | — | — | 1 | 4.51 |
| CHEMBL4799288 | — | — | 1 | 4.40 |
| CHEMBL4798553 | — | — | 1 | 4.28 |
| CHEMBL10332 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787567 | — | EC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL4795780 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL4763113 | — | EC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL3216452 | — | EC50 | = | 20200.0 | nM | 4.70 |
| CHEMBL4755913 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4745647 | — | EC50 | = | 30800.0 | nM | 4.51 |
| CHEMBL4799288 | — | EC50 | = | 39900.0 | nM | 4.40 |
| CHEMBL4798553 | — | EC50 | = | 52300.0 | nM | 4.28 |
| CHEMBL10332 | — | EC50 | = | 87200.0 | nM | 4.06 |