Assay Detail
Binding
CHEMBL2155339
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Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.16 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215421 | — | — | 1 | 9.39 |
| CHEMBL2153557 | — | — | 1 | 9.19 |
| CHEMBL2153555 | — | — | 1 | 9.05 |
| CHEMBL2153553 | — | — | 1 | 9.04 |
| CHEMBL2153551 | — | — | 1 | 8.66 |
| CHEMBL2153556 | — | — | 1 | 8.25 |
| CHEMBL214986 | — | — | 1 | 7.95 |
| CHEMBL2153554 | — | — | 1 | 7.78 |
| CHEMBL2153558 | — | — | 1 | 7.74 |
| CHEMBL2153559 | — | — | 1 | 7.62 |
| CHEMBL2153552 | — | — | 1 | 7.18 |
| CHEMBL2153560 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215421 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL2153557 | — | Ki | = | 0.6457 | nM | 9.19 |
| CHEMBL2153555 | — | Ki | = | 0.8913 | nM | 9.05 |
| CHEMBL2153553 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL2153551 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL2153556 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL214986 | — | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL2153554 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL2153558 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL2153559 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL2153552 | — | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL2153560 | — | Ki | = | 812.83 | nM | 6.09 |