Assay Detail
Binding
CHEMBL3299604
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]BE2254 from human alpha1a receptor expressed in HEK293 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
High affinity ligands and potent antagonists for the α1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.71 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3298750 | — | — | 1 | 9.49 |
| CHEMBL3298023 | — | — | 1 | 9.04 |
| CHEMBL3297829 | — | — | 1 | 9.03 |
| CHEMBL3298024 | — | — | 1 | 9.00 |
| CHEMBL3298745 | — | — | 1 | 8.96 |
| CHEMBL3298749 | — | — | 1 | 8.96 |
| CHEMBL3298746 | — | — | 1 | 8.83 |
| CHEMBL220221 | — | — | 1 | 8.83 |
| CHEMBL3298017 | — | — | 1 | 8.79 |
| CHEMBL3298019 | — | — | 1 | 8.77 |
| CHEMBL220781 | — | — | 1 | 8.48 |
| CHEMBL3298021 | — | — | 1 | 8.47 |
| CHEMBL3298022 | — | — | 1 | 8.45 |
| CHEMBL3298020 | — | — | 1 | 8.41 |
| CHEMBL3298748 | — | — | 1 | 8.28 |
| CHEMBL3298018 | — | — | 1 | 8.16 |
| CHEMBL3298747 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3298750 | — | Ki | = | 0.3236 | nM | 9.49 |
| CHEMBL3298023 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL3297829 | — | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL3298024 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3298745 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL3298749 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL3298746 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL220221 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL3298017 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL3298019 | — | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL220781 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL3298021 | — | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL3298022 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL3298020 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL3298748 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL3298018 | — | Ki | = | 6.918 | nM | 8.16 |
| CHEMBL3298747 | — | Ki | = | 7.079 | nM | 8.15 |