Assay Detail
Binding
CHEMBL2155385
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from human cloned alpha1D 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 | 8.14 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153553 | — | — | 1 | 9.43 |
| CHEMBL2153557 | — | — | 1 | 9.31 |
| CHEMBL215421 | — | — | 1 | 9.29 |
| CHEMBL2153555 | — | — | 1 | 9.15 |
| CHEMBL2153556 | — | — | 1 | 8.40 |
| CHEMBL2153558 | — | — | 1 | 8.13 |
| CHEMBL2153551 | — | — | 1 | 8.05 |
| CHEMBL214986 | — | — | 1 | 7.98 |
| CHEMBL2153554 | — | — | 1 | 7.78 |
| CHEMBL2153559 | — | — | 1 | 7.10 |
| CHEMBL2153560 | — | — | 1 | 6.58 |
| CHEMBL2153552 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153553 | — | Ki | = | 0.3715 | nM | 9.43 |
| CHEMBL2153557 | — | Ki | = | 0.4898 | nM | 9.31 |
| CHEMBL215421 | — | Ki | = | 0.5129 | nM | 9.29 |
| CHEMBL2153555 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL2153556 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL2153558 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL2153551 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL214986 | — | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL2153554 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL2153559 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL2153560 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL2153552 | — | Ki | = | 323.59 | nM | 6.49 |