Assay Detail
Functional
CHEMBL1671586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha1-adrenoceptor in rat anococcygeal muscle assessed as inhibition of phenylephrine-induced contraction
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 27 | 7.61 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.11 |
| CHEMBL1669507 | — | — | 1 | 8.93 |
| CHEMBL1669498 | — | — | 1 | 8.65 |
| CHEMBL1669504 | — | — | 1 | 8.58 |
| CHEMBL1669495 | — | — | 1 | 8.53 |
| CHEMBL1669509 | — | — | 1 | 8.50 |
| CHEMBL1669497 | — | — | 1 | 8.33 |
| CHEMBL1669510 | — | — | 1 | 8.21 |
| CHEMBL1669496 | — | — | 1 | 8.18 |
| CHEMBL1669508 | — | — | 1 | 8.09 |
| CHEMBL1669505 | — | — | 1 | 8.07 |
| CHEMBL1669506 | — | — | 1 | 7.91 |
| CHEMBL1669511 | — | — | 1 | 7.77 |
| CHEMBL1669503 | — | — | 1 | 7.71 |
| CHEMBL1669499 | — | — | 1 | 7.68 |
| CHEMBL1669512 | — | — | 1 | 7.47 |
| CHEMBL1669501 | — | — | 1 | 7.38 |
| CHEMBL1669502 | — | — | 1 | 6.93 |
| CHEMBL1669514 | — | — | 1 | 6.92 |
| CHEMBL1669513 | — | — | 1 | 6.90 |
| CHEMBL16459 | — | — | 1 | 6.84 |
| CHEMBL1669500 | — | — | 1 | 6.71 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | — | 1 | 6.61 |
| CHEMBL1669517 | — | — | 1 | 6.54 |
| CHEMBL1669515 | — | — | 1 | 6.41 |
| CHEMBL1669518 | — | — | 1 | 6.37 |
| CHEMBL1669516 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Kd | = | 0.7727 | nM | 9.11 |
| CHEMBL1669507 | — | Kd | = | 1.175 | nM | 8.93 |
| CHEMBL1669498 | — | Kd | = | 2.254 | nM | 8.65 |
| CHEMBL1669504 | — | Kd | = | 2.636 | nM | 8.58 |
| CHEMBL1669495 | — | Kd | = | 2.979 | nM | 8.53 |
| CHEMBL1669509 | — | Kd | = | 3.177 | nM | 8.50 |
| CHEMBL1669497 | — | Kd | = | 4.645 | nM | 8.33 |
| CHEMBL1669510 | — | Kd | = | 6.209 | nM | 8.21 |
| CHEMBL1669496 | — | Kd | = | 6.653 | nM | 8.18 |
| CHEMBL1669508 | — | Kd | = | 8.166 | nM | 8.09 |
| CHEMBL1669505 | — | Kd | = | 8.472 | nM | 8.07 |
| CHEMBL1669506 | — | Kd | = | 12.19 | nM | 7.91 |
| CHEMBL1669511 | — | Kd | = | 16.9 | nM | 7.77 |
| CHEMBL1669503 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL1669499 | — | Kd | = | 20.7 | nM | 7.68 |
| CHEMBL1669512 | — | Kd | = | 33.81 | nM | 7.47 |
| CHEMBL1669501 | — | Kd | = | 41.4 | nM | 7.38 |
| CHEMBL1669502 | — | Kd | = | 117.49 | nM | 6.93 |
| CHEMBL1669514 | — | Kd | = | 118.85 | nM | 6.92 |
| CHEMBL1669513 | — | Kd | = | 126.77 | nM | 6.90 |
| CHEMBL16459 | — | Kd | = | 142.89 | nM | 6.84 |
| CHEMBL1669500 | — | Kd | = | 195.43 | nM | 6.71 |
| CHEMBL276915 | 7-HYDROXYFLAVONE | Kd | = | 246.04 | nM | 6.61 |
| CHEMBL1669517 | — | Kd | = | 289.73 | nM | 6.54 |
| CHEMBL1669515 | — | Kd | = | 389.94 | nM | 6.41 |
| CHEMBL1669518 | — | Kd | = | 428.55 | nM | 6.37 |
| CHEMBL1669516 | — | Kd | = | 679.2 | nM | 6.17 |