Assay Detail
Binding
CHEMBL3405641
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Antagonist activity at alpha-1B adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
7
Total Activities
7
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
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 7.70 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 9.30 |
| CHEMBL3400597 | — | — | 1 | 8.60 |
| CHEMBL3400593 | — | — | 1 | 8.46 |
| CHEMBL3400596 | — | — | 1 | 7.33 |
| CHEMBL3400594 | — | — | 1 | 6.88 |
| CHEMBL3400595 | — | — | 1 | 6.78 |
| CHEMBL3400598 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611 | TERAZOSIN | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3400597 | — | EC50 | = | 2.53 | nM | 8.60 |
| CHEMBL3400593 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3400596 | — | EC50 | = | 46.9 | nM | 7.33 |
| CHEMBL3400594 | — | EC50 | = | 131.1 | nM | 6.88 |
| CHEMBL3400595 | — | EC50 | = | 165.3 | nM | 6.78 |
| CHEMBL3400598 | — | EC50 | = | 288.7 | nM | 6.54 |