Assay Detail
Binding
CHEMBL648631
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylamino methyl tetralone from human cloned Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells
11
Total Activities
11
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 | 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 | 11 | 8.25 | 10.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83272 | — | — | 1 | 10.08 |
| CHEMBL311890 | — | — | 1 | 9.92 |
| CHEMBL83226 | — | — | 1 | 9.89 |
| CHEMBL311247 | — | — | 1 | 9.55 |
| CHEMBL432947 | — | — | 1 | 8.92 |
| CHEMBL83041 | — | — | 1 | 8.51 |
| CHEMBL420578 | — | — | 1 | 7.70 |
| CHEMBL309949 | — | — | 1 | 7.05 |
| CHEMBL82056 | — | — | 1 | 6.83 |
| CHEMBL311014 | — | — | 1 | 6.30 |
| CHEMBL311290 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83272 | — | Ki | = | 0.084 | nM | 10.08 |
| CHEMBL311890 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL83226 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL311247 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL432947 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL83041 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL420578 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL309949 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL82056 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL311014 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL311290 | — | Ki | = | 1033.0 | nM | 5.99 |