Assay Detail
Binding
CHEMBL3299605
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]BE2254 from human alpha1b 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 | 8.04 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3298750 | — | — | 1 | 9.08 |
| CHEMBL3298019 | — | — | 1 | 8.78 |
| CHEMBL3297829 | — | — | 1 | 8.72 |
| CHEMBL3298749 | — | — | 1 | 8.57 |
| CHEMBL3298017 | — | — | 1 | 8.19 |
| CHEMBL3298023 | — | — | 1 | 8.19 |
| CHEMBL3298018 | — | — | 1 | 8.13 |
| CHEMBL3298024 | — | — | 1 | 8.12 |
| CHEMBL220781 | — | — | 1 | 8.05 |
| CHEMBL3298745 | — | — | 1 | 8.00 |
| CHEMBL220221 | — | — | 1 | 7.76 |
| CHEMBL3298022 | — | — | 1 | 7.72 |
| CHEMBL3298746 | — | — | 1 | 7.55 |
| CHEMBL3298021 | — | — | 1 | 7.52 |
| CHEMBL3298747 | — | — | 1 | 7.47 |
| CHEMBL3298748 | — | — | 1 | 7.44 |
| CHEMBL3298020 | — | — | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3298750 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL3298019 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL3297829 | — | Ki | = | 1.905 | nM | 8.72 |
| CHEMBL3298749 | — | Ki | = | 2.692 | nM | 8.57 |
| CHEMBL3298017 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL3298023 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL3298018 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL3298024 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL220781 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL3298745 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL220221 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL3298022 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL3298746 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL3298021 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL3298747 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL3298748 | — | Ki | = | 36.31 | nM | 7.44 |
| CHEMBL3298020 | — | Ki | = | 38.9 | nM | 7.41 |