Assay Detail
Functional
CHEMBL655646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
7
Total Activities
7
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
Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 5.93 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 7.90 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 6.14 |
| CHEMBL543955 | — | — | 1 | 6.02 |
| CHEMBL6939 | — | — | 1 | 5.54 |
| CHEMBL542776 | — | — | 1 | 5.42 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | 4.0 | 1 | 5.40 |
| CHEMBL6995 | PRACTOLOL | 4.0 | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL13 | METOPROLOL | Kd | = | 724.44 | nM | 6.14 |
| CHEMBL543955 | — | Kd | = | 954.99 | nM | 6.02 |
| CHEMBL6939 | — | Kd | = | 2884.03 | nM | 5.54 |
| CHEMBL542776 | — | Kd | = | 3801.89 | nM | 5.42 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | Kd | = | 3981.07 | nM | 5.40 |
| CHEMBL6995 | PRACTOLOL | Kd | = | 8317.64 | nM | 5.08 |