Assay Detail
Functional
CHEMBL3801484
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Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
12
Total Activities
12
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 | 12 | 6.33 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3800400 | — | — | 1 | 8.21 |
| CHEMBL3798748 | — | — | 1 | 8.15 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 7.06 |
| CHEMBL3797876 | — | — | 1 | 6.92 |
| CHEMBL3797758 | — | — | 1 | 6.14 |
| CHEMBL3800468 | — | — | 1 | 6.08 |
| CHEMBL3797205 | — | — | 1 | 6.00 |
| CHEMBL3799593 | — | — | 1 | 5.85 |
| CHEMBL3799427 | — | — | 1 | 5.58 |
| CHEMBL3800303 | — | — | 1 | 5.29 |
| CHEMBL3800636 | — | — | 1 | 4.33 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3800400 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3798748 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL434 | ISOPROTERENOL | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3797876 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3797758 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3800468 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL3797205 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3799593 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3799427 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3800303 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3800636 | — | EC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL240773 | QUINPIROLE | EC50 | - | — | - |