Assay Detail
Functional
CHEMBL651634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
11
Total Activities
11
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
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 7.36 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 9.62 |
| CHEMBL1744069 | — | — | 1 | 7.86 |
| CHEMBL305153 | — | — | 1 | 7.77 |
| CHEMBL1788270 | — | — | 1 | 7.74 |
| CHEMBL26917 | — | — | 1 | 7.50 |
| CHEMBL368457 | — | — | 1 | 7.18 |
| CHEMBL2110257 | — | — | 1 | 7.13 |
| CHEMBL173976 | — | — | 1 | 7.07 |
| CHEMBL148306 | (S)-METOPROLOL | — | 1 | 7.02 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 6.79 |
| CHEMBL1741004 | (R)-METOPROLOL | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499 | TIMOLOL | Kd | = | 0.2399 | nM | 9.62 |
| CHEMBL1744069 | — | Kd | = | 13.8 | nM | 7.86 |
| CHEMBL305153 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL1788270 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL26917 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL368457 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL2110257 | — | Kd | = | 74.13 | nM | 7.13 |
| CHEMBL173976 | — | Kd | = | 85.11 | nM | 7.07 |
| CHEMBL148306 | (S)-METOPROLOL | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL13 | METOPROLOL | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL1741004 | (R)-METOPROLOL | Kd | = | 5754.4 | nM | 5.24 |