Assay Detail
Functional
CHEMBL644565
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Antagonistic activity against Alpha-1 adrenergic receptor in the epidermal portion of the rat vas deferens
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Vas deferens |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 5.28 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 7.94 |
| CHEMBL31836 | PIPEROXAN | 2.0 | 1 | 6.40 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 6.27 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.21 |
| CHEMBL1203725 | — | — | 1 | 5.00 |
| CHEMBL1204368 | — | — | 1 | 5.00 |
| CHEMBL1203742 | — | — | 1 | 4.33 |
| CHEMBL161519 | — | — | 1 | 4.30 |
| CHEMBL1237158 | — | — | 1 | 4.22 |
| CHEMBL1203739 | — | — | 1 | 4.20 |
| CHEMBL1203715 | — | — | 1 | 4.20 |
| CHEMBL1237152 | — | — | 1 | - |
| CHEMBL434858 | — | — | 1 | - |
| CHEMBL1203743 | — | — | 1 | - |
| CHEMBL578481 | IMILOXAN HYDROCHLORIDE | -1.0 | 1 | - |
| CHEMBL1203729 | — | — | 1 | - |
| CHEMBL162087 | — | — | 1 | - |
| CHEMBL1203727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597 | PHENTOLAMINE | Kd | = | 11.48 | nM | 7.94 |
| CHEMBL31836 | PIPEROXAN | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL10347 | RAUWOLSCINE | Kd | = | 537.03 | nM | 6.27 |
| CHEMBL15245 | YOHIMBINE | Kd | = | 616.6 | nM | 6.21 |
| CHEMBL1203725 | — | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL1204368 | — | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL1203742 | — | Kd | = | 46773.51 | nM | 4.33 |
| CHEMBL161519 | — | Kd | = | 50118.72 | nM | 4.30 |
| CHEMBL1237158 | — | Kd | = | 60255.96 | nM | 4.22 |
| CHEMBL1203739 | — | Kd | = | 63095.73 | nM | 4.20 |
| CHEMBL1203715 | — | Kd | = | 63095.73 | nM | 4.20 |
| CHEMBL1237152 | — | Kd | > | 100000.0 | nM | - |
| CHEMBL434858 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1203743 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL578481 | IMILOXAN HYDROCHLORIDE | Kd | > | 100000.0 | nM | - |
| CHEMBL1203729 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL162087 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1203727 | — | Kd | > | 31622.78 | nM | - |