Assay Detail
Functional
CHEMBL647633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 24 | 7.61 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543955 | — | — | 1 | 9.55 |
| CHEMBL267375 | — | — | 1 | 9.30 |
| CHEMBL542536 | — | — | 1 | 8.70 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | 4.0 | 1 | 8.53 |
| CHEMBL544190 | — | — | 1 | 8.53 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.36 |
| CHEMBL1201274 | LEVOBETAXOLOL | 4.0 | 1 | 8.30 |
| CHEMBL7250 | — | — | 1 | 8.23 |
| CHEMBL544661 | — | — | 1 | 8.13 |
| CHEMBL6939 | — | — | 1 | 8.01 |
| CHEMBL543011 | — | — | 1 | 7.94 |
| CHEMBL543957 | — | — | 1 | 7.75 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 7.64 |
| CHEMBL552898 | — | — | 1 | 7.44 |
| CHEMBL6902 | — | — | 1 | 7.38 |
| CHEMBL543484 | — | — | 1 | 7.21 |
| CHEMBL7043 | — | — | 1 | 7.11 |
| CHEMBL423 | BETAXOLOL | 4.0 | 1 | 6.90 |
| CHEMBL6712 | — | — | 1 | 6.89 |
| CHEMBL542776 | — | — | 1 | 6.84 |
| CHEMBL542777 | — | — | 1 | 6.80 |
| CHEMBL543717 | — | — | 1 | 6.47 |
| CHEMBL6749 | — | — | 1 | 5.54 |
| CHEMBL267220 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543955 | — | Kd | = | 0.2818 | nM | 9.55 |
| CHEMBL267375 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL542536 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL1691 | BETAXOLOL HYDROCHLORIDE | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL544190 | — | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL1201274 | LEVOBETAXOLOL | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL7250 | — | Kd | = | 5.888 | nM | 8.23 |
| CHEMBL544661 | — | Kd | = | 7.413 | nM | 8.13 |
| CHEMBL6939 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL543011 | — | Kd | = | 11.48 | nM | 7.94 |
| CHEMBL543957 | — | Kd | = | 17.78 | nM | 7.75 |
| CHEMBL13 | METOPROLOL | Kd | = | 22.91 | nM | 7.64 |
| CHEMBL552898 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL6902 | — | Kd | = | 41.69 | nM | 7.38 |
| CHEMBL543484 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL7043 | — | Kd | = | 77.62 | nM | 7.11 |
| CHEMBL423 | BETAXOLOL | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL6712 | — | Kd | = | 128.82 | nM | 6.89 |
| CHEMBL542776 | — | Kd | = | 144.54 | nM | 6.84 |
| CHEMBL542777 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL543717 | — | Kd | = | 338.84 | nM | 6.47 |
| CHEMBL6749 | — | Kd | = | 2884.03 | nM | 5.54 |
| CHEMBL267220 | — | Kd | = | 7762.47 | nM | 5.11 |