Assay Detail
Binding
CHEMBL2155386
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Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in rat hippocampal membranes after 30 mins by liquid scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Subcellular | Membrane |
| 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 | 8.09 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153553 | — | — | 1 | 9.07 |
| CHEMBL2153551 | — | — | 1 | 9.00 |
| CHEMBL2153557 | — | — | 1 | 8.85 |
| CHEMBL2153555 | — | — | 1 | 8.77 |
| CHEMBL215421 | — | — | 1 | 8.61 |
| CHEMBL2153554 | — | — | 1 | 7.89 |
| CHEMBL2153552 | — | — | 1 | 7.76 |
| CHEMBL2153556 | — | — | 1 | 7.76 |
| CHEMBL2153559 | — | — | 1 | 7.54 |
| CHEMBL2153558 | — | — | 1 | 7.50 |
| CHEMBL214986 | — | — | 1 | 7.39 |
| CHEMBL2153560 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153553 | — | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL2153551 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2153557 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL2153555 | — | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL215421 | — | Ki | = | 2.455 | nM | 8.61 |
| CHEMBL2153554 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL2153552 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL2153556 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL2153559 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL2153558 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL214986 | — | Ki | = | 40.74 | nM | 7.39 |
| CHEMBL2153560 | — | Ki | = | 123.03 | nM | 6.91 |