Assay Detail
ADMET
CHEMBL3863085
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Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence of coelenterazine H by luminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 7.42 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 9.89 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.76 |
| CHEMBL3937911 | — | — | 1 | 7.90 |
| CHEMBL3895815 | — | — | 1 | 7.85 |
| CHEMBL3956998 | — | — | 1 | 7.81 |
| CHEMBL3947830 | — | — | 1 | 7.38 |
| CHEMBL3894175 | — | — | 1 | 6.98 |
| CHEMBL3948333 | — | — | 1 | 6.34 |
| CHEMBL3986337 | — | — | 1 | 6.29 |
| CHEMBL3939560 | — | — | 1 | 6.22 |
| CHEMBL3968662 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL611 | TERAZOSIN | EC50 | = | 1.73 | nM | 8.76 |
| CHEMBL3937911 | — | EC50 | = | 12.65 | nM | 7.90 |
| CHEMBL3895815 | — | EC50 | = | 14.15 | nM | 7.85 |
| CHEMBL3956998 | — | EC50 | = | 15.5 | nM | 7.81 |
| CHEMBL3947830 | — | EC50 | = | 42.1 | nM | 7.38 |
| CHEMBL3894175 | — | EC50 | = | 104.8 | nM | 6.98 |
| CHEMBL3948333 | — | EC50 | = | 461.1 | nM | 6.34 |
| CHEMBL3986337 | — | EC50 | = | 514.8 | nM | 6.29 |
| CHEMBL3939560 | — | EC50 | = | 608.4 | nM | 6.22 |
| CHEMBL3968662 | — | EC50 | = | 598.6 | nM | 6.22 |