Assay Detail
Binding
CHEMBL2155338
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Displacement of [3H]prazosin from human cloned alpha1B 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 | 7.44 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153555 | — | — | 1 | 8.66 |
| CHEMBL2153557 | — | — | 1 | 8.62 |
| CHEMBL2153553 | — | — | 1 | 8.56 |
| CHEMBL215421 | — | — | 1 | 8.24 |
| CHEMBL2153551 | — | — | 1 | 7.51 |
| CHEMBL2153556 | — | — | 1 | 7.47 |
| CHEMBL214986 | — | — | 1 | 7.14 |
| CHEMBL2153554 | — | — | 1 | 7.10 |
| CHEMBL2153558 | — | — | 1 | 6.99 |
| CHEMBL2153552 | — | — | 1 | 6.40 |
| CHEMBL2153559 | — | — | 1 | 6.35 |
| CHEMBL2153560 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153555 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL2153557 | — | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL2153553 | — | Ki | = | 2.754 | nM | 8.56 |
| CHEMBL215421 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL2153551 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL2153556 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL214986 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL2153554 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL2153558 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL2153552 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL2153559 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL2153560 | — | Ki | = | 645.65 | nM | 6.19 |