Assay Detail
Binding
CHEMBL643945
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Ability to displace beta ([125I]-iodo-4-hydroxyphenyl) ethylamino methyl tetralone from human cloned Alpha-1d adrenergic receptor stably expressed in HEK cells.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.86 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.70 |
| CHEMBL311247 | — | — | 1 | 7.80 |
| CHEMBL83272 | — | — | 1 | 7.60 |
| CHEMBL311890 | — | — | 1 | 7.39 |
| CHEMBL309518 | — | — | 1 | 7.23 |
| CHEMBL83592 | — | — | 1 | 7.15 |
| CHEMBL81006 | — | — | 1 | 7.14 |
| CHEMBL83340 | — | — | 1 | 7.12 |
| CHEMBL82877 | — | — | 1 | 7.12 |
| CHEMBL313990 | — | — | 1 | 7.07 |
| CHEMBL432947 | — | — | 1 | 6.87 |
| CHEMBL420578 | — | — | 1 | 6.65 |
| CHEMBL83226 | — | — | 1 | 6.46 |
| CHEMBL83041 | — | — | 1 | 6.19 |
| CHEMBL309949 | — | — | 1 | 6.05 |
| CHEMBL82056 | — | — | 1 | 5.99 |
| CHEMBL311014 | — | — | 1 | 5.56 |
| CHEMBL311290 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL311247 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL83272 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL311890 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL309518 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL83592 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL81006 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL83340 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL82877 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL313990 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL432947 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL420578 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL83226 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL83041 | — | Ki | = | 644.0 | nM | 6.19 |
| CHEMBL309949 | — | Ki | = | 894.0 | nM | 6.05 |
| CHEMBL82056 | — | Ki | = | 1019.0 | nM | 5.99 |
| CHEMBL311014 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL311290 | — | Ki | = | 3429.0 | nM | 5.46 |