Assay Detail
Binding
CHEMBL645480
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Displacement of clonidine from Alpha-2 adrenergic receptor of rat cortical membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 5.99 | 6.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1788222 | — | — | 1 | 6.74 |
| CHEMBL302021 | — | — | 1 | 6.64 |
| CHEMBL106737 | — | — | 1 | 6.23 |
| CHEMBL1744044 | — | — | 1 | 6.01 |
| CHEMBL51433 | — | — | 1 | 5.80 |
| CHEMBL1788223 | — | — | 1 | 5.46 |
| CHEMBL2092927 | — | — | 1 | 5.05 |
| CHEMBL2092926 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1788222 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL302021 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL106737 | — | Ki | = | 593.0 | nM | 6.23 |
| CHEMBL1744044 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL51433 | — | Ki | = | 1599.0 | nM | 5.80 |
| CHEMBL1788223 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL2092927 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL2092926 | — | Ki | > | 10000.0 | nM | - |