Assay Detail
Functional
CHEMBL651252
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 rat atria
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 6 | 8.16 | 9.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543955 | — | — | 1 | 9.56 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | 4.0 | 1 | 8.53 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.36 |
| CHEMBL6939 | — | — | 1 | 8.01 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 7.64 |
| CHEMBL542776 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543955 | — | Kd | = | 0.2754 | nM | 9.56 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL6939 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL13 | METOPROLOL | Kd | = | 22.91 | nM | 7.64 |
| CHEMBL542776 | — | Kd | = | 144.54 | nM | 6.84 |