Assay Detail
Functional
CHEMBL643858
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Presynaptic antagonistic activity against alpha-1 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using methoxamine as the agonist
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 6.20 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.24 |
| CHEMBL47471 | — | — | 1 | 7.00 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.52 |
| CHEMBL50017 | — | — | 1 | 6.50 |
| CHEMBL47415 | — | — | 1 | 6.50 |
| CHEMBL9841 | — | — | 1 | 6.50 |
| CHEMBL280514 | — | — | 1 | 6.20 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 6.10 |
| CHEMBL295764 | — | — | 1 | 6.00 |
| CHEMBL45773 | — | — | 1 | 6.00 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 6.00 |
| CHEMBL295921 | — | — | 1 | 5.80 |
| CHEMBL18094 | — | — | 1 | 5.70 |
| CHEMBL298004 | — | — | 1 | 5.70 |
| CHEMBL48833 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Kd | = | 57.54 | nM | 7.24 |
| CHEMBL47471 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL15245 | YOHIMBINE | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL50017 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL47415 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL9841 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL280514 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL10316 | IDAZOXAN | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL295764 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL45773 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL10347 | RAUWOLSCINE | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL295921 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL18094 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL298004 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL48833 | — | Kd | = | 6606.93 | nM | 5.18 |