Assay Detail
Binding
CHEMBL651635
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In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| 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 | 6.10 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 9.62 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.52 |
| CHEMBL3085291 | — | — | 1 | 8.05 |
| CHEMBL366769 | — | — | 1 | 7.48 |
| CHEMBL2096752 | — | — | 1 | 7.24 |
| CHEMBL423 | BETAXOLOL | 4.0 | 1 | 6.98 |
| CHEMBL11171 | — | — | 1 | 6.88 |
| CHEMBL173424 | — | — | 1 | 6.84 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 6.79 |
| CHEMBL427297 | — | — | 1 | 6.25 |
| CHEMBL174783 | — | — | 1 | 6.21 |
| CHEMBL2096750 | — | — | 1 | 6.06 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | 5.93 |
| CHEMBL366389 | — | — | 1 | 5.89 |
| CHEMBL434360 | — | — | 1 | 5.60 |
| CHEMBL6995 | PRACTOLOL | 4.0 | 1 | 5.35 |
| CHEMBL1788320 | — | — | 1 | 5.13 |
| CHEMBL177765 | — | — | 1 | 4.91 |
| CHEMBL366573 | — | — | 1 | 4.57 |
| CHEMBL2096751 | — | — | 1 | 4.53 |
| CHEMBL173629 | — | — | 1 | 4.46 |
| CHEMBL177860 | — | — | 1 | 4.44 |
| CHEMBL174259 | — | — | 1 | 4.34 |
| CHEMBL11671 | — | — | 1 | 4.32 |
| CHEMBL172431 | — | — | 1 | - |
| CHEMBL174106 | — | — | 1 | - |
| CHEMBL2093062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | Kd | = | 0.2399 | nM | 9.62 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 3.02 | nM | 8.52 |
| CHEMBL3085291 | — | Kd | = | 8.913 | nM | 8.05 |
| CHEMBL366769 | — | Kd | = | 33.11 | nM | 7.48 |
| CHEMBL2096752 | — | Kd | = | 57.54 | nM | 7.24 |
| CHEMBL423 | BETAXOLOL | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL11171 | — | Kd | = | 131.83 | nM | 6.88 |
| CHEMBL173424 | — | Kd | = | 144.54 | nM | 6.84 |
| CHEMBL13 | METOPROLOL | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL427297 | — | Kd | = | 562.34 | nM | 6.25 |
| CHEMBL174783 | — | Kd | = | 616.6 | nM | 6.21 |
| CHEMBL2096750 | — | Kd | = | 870.96 | nM | 6.06 |
| CHEMBL24 | ATENOLOL | Kd | = | 1174.9 | nM | 5.93 |
| CHEMBL366389 | — | Kd | = | 1288.25 | nM | 5.89 |
| CHEMBL434360 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL6995 | PRACTOLOL | Kd | = | 4466.84 | nM | 5.35 |
| CHEMBL1788320 | — | Kd | = | 7413.1 | nM | 5.13 |
| CHEMBL177765 | — | Kd | = | 12302.69 | nM | 4.91 |
| CHEMBL366573 | — | Kd | = | 26915.35 | nM | 4.57 |
| CHEMBL2096751 | — | Kd | = | 29512.09 | nM | 4.53 |
| CHEMBL173629 | — | Kd | = | 34673.69 | nM | 4.46 |
| CHEMBL177860 | — | Kd | = | 36307.81 | nM | 4.44 |
| CHEMBL174259 | — | Kd | = | 45708.82 | nM | 4.34 |
| CHEMBL11671 | — | Kd | = | 47863.01 | nM | 4.32 |
| CHEMBL172431 | — | Kd | = | 107151.93 | nM | - |
| CHEMBL174106 | — | Kd | = | 186208.71 | nM | - |
| CHEMBL2093062 | — | Kd | > | 316227.77 | nM | - |