Assay Detail
Binding
CHEMBL654957
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 27 | 8.05 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 9.44 |
| CHEMBL173424 | — | — | 1 | 9.07 |
| CHEMBL1788320 | — | — | 1 | 9.07 |
| CHEMBL3085291 | — | — | 1 | 9.05 |
| CHEMBL11171 | — | — | 1 | 8.92 |
| CHEMBL366769 | — | — | 1 | 8.80 |
| CHEMBL423 | BETAXOLOL | 4.0 | 1 | 8.76 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.76 |
| CHEMBL2096752 | — | — | 1 | 8.72 |
| CHEMBL11671 | — | — | 1 | 8.36 |
| CHEMBL366389 | — | — | 1 | 8.27 |
| CHEMBL177765 | — | — | 1 | 8.22 |
| CHEMBL2096750 | — | — | 1 | 8.21 |
| CHEMBL434360 | — | — | 1 | 8.20 |
| CHEMBL177860 | — | — | 1 | 8.04 |
| CHEMBL173629 | — | — | 1 | 7.97 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 7.83 |
| CHEMBL2096751 | — | — | 1 | 7.68 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | 7.62 |
| CHEMBL174106 | — | — | 1 | 7.62 |
| CHEMBL2093062 | — | — | 1 | 7.27 |
| CHEMBL174783 | — | — | 1 | 7.22 |
| CHEMBL427297 | — | — | 1 | 7.22 |
| CHEMBL366573 | — | — | 1 | 7.22 |
| CHEMBL6995 | PRACTOLOL | 4.0 | 1 | 6.98 |
| CHEMBL174259 | — | — | 1 | 6.73 |
| CHEMBL172431 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | Kd | = | 0.3631 | nM | 9.44 |
| CHEMBL173424 | — | Kd | = | 0.8511 | nM | 9.07 |
| CHEMBL1788320 | — | Kd | = | 0.8511 | nM | 9.07 |
| CHEMBL3085291 | — | Kd | = | 0.8913 | nM | 9.05 |
| CHEMBL11171 | — | Kd | = | 1.202 | nM | 8.92 |
| CHEMBL366769 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL423 | BETAXOLOL | Kd | = | 1.738 | nM | 8.76 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 1.738 | nM | 8.76 |
| CHEMBL2096752 | — | Kd | = | 1.905 | nM | 8.72 |
| CHEMBL11671 | — | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL366389 | — | Kd | = | 5.37 | nM | 8.27 |
| CHEMBL177765 | — | Kd | = | 6.026 | nM | 8.22 |
| CHEMBL2096750 | — | Kd | = | 6.166 | nM | 8.21 |
| CHEMBL434360 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL177860 | — | Kd | = | 9.12 | nM | 8.04 |
| CHEMBL173629 | — | Kd | = | 10.72 | nM | 7.97 |
| CHEMBL13 | METOPROLOL | Kd | = | 14.79 | nM | 7.83 |
| CHEMBL2096751 | — | Kd | = | 20.89 | nM | 7.68 |
| CHEMBL24 | ATENOLOL | Kd | = | 23.99 | nM | 7.62 |
| CHEMBL174106 | — | Kd | = | 23.99 | nM | 7.62 |
| CHEMBL2093062 | — | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL174783 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL427297 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL366573 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL6995 | PRACTOLOL | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL174259 | — | Kd | = | 186.21 | nM | 6.73 |
| CHEMBL172431 | — | Kd | = | 676.08 | nM | 6.17 |