Assay Detail
Binding
CHEMBL3801474
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Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.08 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3799125 | — | — | 1 | 10.47 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 9.74 |
| CHEMBL3798748 | — | — | 1 | 9.60 |
| CHEMBL3800400 | — | — | 1 | 9.32 |
| CHEMBL3798017 | (R)-Carvedilol | — | 1 | 9.06 |
| CHEMBL3800341 | — | — | 1 | 8.55 |
| CHEMBL3799455 | — | — | 1 | 8.20 |
| CHEMBL3797205 | — | — | 1 | 7.89 |
| CHEMBL3800303 | — | — | 1 | 7.75 |
| CHEMBL3800468 | — | — | 1 | 7.64 |
| CHEMBL1256786 | FORMOTEROL | 4.0 | 1 | 7.58 |
| CHEMBL160519 | PROCATEROL | 3.0 | 1 | 7.48 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 7.34 |
| CHEMBL3799427 | — | — | 1 | 7.33 |
| CHEMBL3800636 | — | — | 1 | 7.28 |
| CHEMBL3797876 | — | — | 1 | 7.01 |
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | 6.44 |
| CHEMBL3797758 | — | — | 1 | 6.21 |
| CHEMBL3799593 | — | — | 1 | 6.07 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 5.48 |
| CHEMBL269004 | — | — | 1 | 4.40 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 4.21 |
| CHEMBL301559 | — | — | 1 | 4.07 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 4.00 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3799125 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL1263 | SALMETEROL | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL3798748 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3800400 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL3800341 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3799455 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3797205 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3800303 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3800468 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1256786 | FORMOTEROL | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL160519 | PROCATEROL | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL434 | ISOPROTERENOL | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3799427 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL3800636 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL3797876 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL679 | EPINEPHRINE | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL3797758 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL3799593 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL269004 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL59 | DOPAMINE | Ki | = | 61000.0 | nM | 4.21 |
| CHEMBL301559 | — | Ki | = | 86000.0 | nM | 4.07 |
| CHEMBL240773 | QUINPIROLE | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL301265 | PRAMIPEXOLE | Ki | = | 100000.0 | nM | 4.00 |