Assay Detail
Functional
CHEMBL3801486
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Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 14 | 7.44 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3800341 | — | — | 1 | 8.59 |
| CHEMBL3797205 | — | — | 1 | 8.14 |
| CHEMBL3799455 | — | — | 1 | 7.77 |
| CHEMBL3797758 | — | — | 1 | 7.60 |
| CHEMBL3798748 | — | — | 1 | 7.01 |
| CHEMBL3800636 | — | — | 1 | 6.96 |
| CHEMBL3797876 | — | — | 1 | 6.77 |
| CHEMBL3800303 | — | — | 1 | 6.70 |
| CHEMBL3800400 | — | — | 1 | - |
| CHEMBL3800468 | — | — | 1 | - |
| CHEMBL3799427 | — | — | 1 | - |
| CHEMBL3799593 | — | — | 1 | - |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | - |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3800341 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3797205 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3799455 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3797758 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3798748 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3800636 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3797876 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3800303 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3800400 | — | EC50 | - | — | - | |
| CHEMBL3800468 | — | EC50 | - | — | - | |
| CHEMBL3799427 | — | EC50 | - | — | - | |
| CHEMBL3799593 | — | EC50 | - | — | - | |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 1.6 | nM | - |
| CHEMBL434 | ISOPROTERENOL | EC50 | - | — | - |