Assay Detail
Functional
CHEMBL868153
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Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.73 | 10.40 |
| Kd | 1 | 10.10 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378501 | CYANOPINDOLOL | — | 1 | 10.40 |
| CHEMBL210309 | — | — | 1 | 10.10 |
| CHEMBL280822 | CGP-20712A | — | 1 | 8.70 |
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 7.80 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 7.50 |
| CHEMBL207802 | LK-204545 | — | 1 | 7.10 |
| CHEMBL208185 | — | — | 1 | 7.00 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378501 | CYANOPINDOLOL | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL210309 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL280822 | CGP-20712A | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL499 | TIMOLOL | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL207802 | LK-204545 | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL208185 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL13 | METOPROLOL | Ki | = | 2511.89 | nM | 5.60 |