Assay Detail
Functional
CHEMBL647015
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Antagonistic Alpha-1 adrenergic receptor activity against phenylephrine-induced contraction of rabbit prostate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 7.24 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288360 | — | — | 1 | 8.00 |
| CHEMBL36927 | — | — | 1 | 7.80 |
| CHEMBL41685 | — | — | 1 | 7.80 |
| CHEMBL287716 | — | — | 1 | 7.70 |
| CHEMBL39209 | — | — | 1 | 7.60 |
| CHEMBL39419 | — | — | 1 | 7.50 |
| CHEMBL41202 | — | — | 1 | 7.20 |
| CHEMBL279229 | URAPIDIL | 3.0 | 1 | 7.10 |
| CHEMBL39842 | — | — | 1 | 7.00 |
| CHEMBL40847 | — | — | 1 | 6.80 |
| CHEMBL41413 | — | — | 1 | 6.80 |
| CHEMBL289397 | — | — | 1 | 6.80 |
| CHEMBL289613 | — | — | 1 | 6.70 |
| CHEMBL39559 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288360 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL36927 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL41685 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL287716 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL39209 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL39419 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL41202 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL279229 | URAPIDIL | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL39842 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL40847 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL41413 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL289397 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL289613 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL39559 | — | Kd | = | 251.19 | nM | 6.60 |