Assay Detail
Functional
CHEMBL648808
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity at Alpha-1 adrenergic receptor was performed on ring segments of rabbit thoracic aorta contracted by noradrenaline.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Thoracic aorta |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
New (2-methoxyphenyl)piperazine derivatives as 5-HT1A receptor ligands with reduced alpha 1-adrenergic activity. Synthesis and structure-affinity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 8.31 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.42 |
| CHEMBL8618 | NAN-190 | — | 1 | 9.18 |
| CHEMBL23449 | — | — | 1 | 9.16 |
| CHEMBL23315 | — | — | 1 | 8.16 |
| CHEMBL23505 | — | — | 1 | 7.72 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 6.24 |
| CHEMBL22482 | — | — | 1 | - |
| CHEMBL282453 | — | — | 1 | - |
| CHEMBL23946 | — | — | 1 | - |
| CHEMBL23877 | — | — | 1 | - |
| CHEMBL23847 | — | — | 1 | - |
| CHEMBL276953 | — | — | 1 | - |
| CHEMBL25654 | — | — | 1 | - |
| CHEMBL23266 | — | — | 1 | - |
| CHEMBL22600 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Kd | = | 0.3802 | nM | 9.42 |
| CHEMBL8618 | NAN-190 | Kd | = | 0.6607 | nM | 9.18 |
| CHEMBL23449 | — | Kd | = | 0.6918 | nM | 9.16 |
| CHEMBL23315 | — | Kd | = | 6.918 | nM | 8.16 |
| CHEMBL23505 | — | Kd | = | 19.05 | nM | 7.72 |
| CHEMBL49 | BUSPIRONE | Kd | = | 575.44 | nM | 6.24 |
| CHEMBL22482 | — | Kd | > | 100.0 | nM | - |
| CHEMBL282453 | — | Kd | > | 100.0 | nM | - |
| CHEMBL23946 | — | Kd | > | 100.0 | nM | - |
| CHEMBL23877 | — | Kd | > | 100.0 | nM | - |
| CHEMBL23847 | — | Kd | > | 100.0 | nM | - |
| CHEMBL276953 | — | Kd | > | 100.0 | nM | - |
| CHEMBL25654 | — | Kd | > | 100.0 | nM | - |
| CHEMBL23266 | — | Kd | > | 100.0 | nM | - |
| CHEMBL22600 | — | Kd | > | 100.0 | nM | - |