Assay Detail
Binding
CHEMBL3863083
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Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.37 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 10.15 |
| CHEMBL3947830 | — | — | 1 | 7.96 |
| CHEMBL3894175 | — | — | 1 | 7.47 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 7.29 |
| CHEMBL3895815 | — | — | 1 | 7.08 |
| CHEMBL3939560 | — | — | 1 | 7.00 |
| CHEMBL3956998 | — | — | 1 | 6.92 |
| CHEMBL3986337 | — | — | 1 | 6.85 |
| CHEMBL3937911 | — | — | 1 | 6.83 |
| CHEMBL3968662 | — | — | 1 | 6.79 |
| CHEMBL3948333 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3947830 | — | EC50 | = | 11.1 | nM | 7.96 |
| CHEMBL3894175 | — | EC50 | = | 34.1 | nM | 7.47 |
| CHEMBL611 | TERAZOSIN | EC50 | = | 51.89 | nM | 7.29 |
| CHEMBL3895815 | — | EC50 | = | 84.2 | nM | 7.08 |
| CHEMBL3939560 | — | EC50 | = | 99.7 | nM | 7.00 |
| CHEMBL3956998 | — | EC50 | = | 120.6 | nM | 6.92 |
| CHEMBL3986337 | — | EC50 | = | 140.1 | nM | 6.85 |
| CHEMBL3937911 | — | EC50 | = | 148.2 | nM | 6.83 |
| CHEMBL3968662 | — | EC50 | = | 160.7 | nM | 6.79 |
| CHEMBL3948333 | — | EC50 | = | 191.6 | nM | 6.72 |