Assay Detail
Binding
CHEMBL3801477
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Displacement of [3H]spiperone from human D2S 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 | 6.50 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269004 | — | — | 1 | 8.15 |
| CHEMBL3800341 | — | — | 1 | 7.77 |
| CHEMBL3798017 | (R)-Carvedilol | — | 1 | 7.58 |
| CHEMBL301559 | — | — | 1 | 7.40 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 7.32 |
| CHEMBL3797758 | — | — | 1 | 7.32 |
| CHEMBL3799125 | — | — | 1 | 7.31 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | 7.22 |
| CHEMBL3798748 | — | — | 1 | 7.19 |
| CHEMBL3800303 | — | — | 1 | 7.17 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 7.16 |
| CHEMBL3797205 | — | — | 1 | 7.02 |
| CHEMBL3800636 | — | — | 1 | 6.92 |
| CHEMBL3799455 | — | — | 1 | 6.80 |
| CHEMBL3799593 | — | — | 1 | 6.70 |
| CHEMBL3797876 | — | — | 1 | 6.37 |
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | 6.04 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 5.89 |
| CHEMBL3799427 | — | — | 1 | 5.77 |
| CHEMBL3800468 | — | — | 1 | 5.64 |
| CHEMBL3800400 | — | — | 1 | 5.50 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 4.92 |
| CHEMBL1256786 | FORMOTEROL | 4.0 | 1 | 4.89 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 4.50 |
| CHEMBL160519 | PROCATEROL | 3.0 | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269004 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3800341 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL301559 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL59 | DOPAMINE | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL3797758 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL3799125 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL301265 | PRAMIPEXOLE | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3798748 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3800303 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL240773 | QUINPIROLE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3797205 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL3800636 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3799455 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3799593 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3797876 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL679 | EPINEPHRINE | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3799427 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL3800468 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL3800400 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL434 | ISOPROTERENOL | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1256786 | FORMOTEROL | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1263 | SALMETEROL | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL160519 | PROCATEROL | Ki | = | 86000.0 | nM | 4.07 |