Assay Detail
Functional
CHEMBL653375
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Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Role of the (acyloxy)methyl moiety in eliciting the adrenergic beta-blocking activity of 3-(acyloxy)propanolamines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 5.29 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL266548 | — | — | 1 | 6.90 |
| CHEMBL156603 | — | — | 1 | 6.34 |
| CHEMBL156147 | — | — | 1 | 5.80 |
| CHEMBL6995 | PRACTOLOL | 4.0 | 1 | 5.78 |
| CHEMBL156682 | — | — | 1 | 5.10 |
| CHEMBL156683 | — | — | 1 | 4.96 |
| CHEMBL449651 | — | — | 1 | 4.94 |
| CHEMBL157557 | — | — | 1 | 4.91 |
| CHEMBL156271 | — | — | 1 | 4.57 |
| CHEMBL156304 | — | — | 1 | 4.55 |
| CHEMBL289093 | BUTOXAMINE | 2.0 | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL266548 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL156603 | — | Kd | = | 457.09 | nM | 6.34 |
| CHEMBL156147 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL6995 | PRACTOLOL | Kd | = | 1659.59 | nM | 5.78 |
| CHEMBL156682 | — | Kd | = | 7943.28 | nM | 5.10 |
| CHEMBL156683 | — | Kd | = | 10964.78 | nM | 4.96 |
| CHEMBL449651 | — | Kd | = | 11481.54 | nM | 4.94 |
| CHEMBL157557 | — | Kd | = | 12302.69 | nM | 4.91 |
| CHEMBL156271 | — | Kd | = | 26915.35 | nM | 4.57 |
| CHEMBL156304 | — | Kd | = | 28183.83 | nM | 4.55 |
| CHEMBL289093 | BUTOXAMINE | Kd | = | 44668.36 | nM | 4.35 |