Assay Detail
Functional
CHEMBL921450
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Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
29
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 6.84 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260720 | — | — | 1 | 8.52 |
| CHEMBL326702 | — | — | 1 | 8.05 |
| CHEMBL406316 | — | — | 1 | 7.85 |
| CHEMBL257978 | DABUZALGRON | 2.0 | 1 | 7.60 |
| CHEMBL404566 | — | — | 1 | 7.50 |
| CHEMBL402388 | — | — | 1 | 7.50 |
| CHEMBL255938 | — | — | 1 | 7.48 |
| CHEMBL256982 | — | — | 1 | 7.37 |
| CHEMBL256983 | — | — | 1 | 7.28 |
| CHEMBL257800 | — | — | 1 | 7.16 |
| CHEMBL257799 | — | — | 1 | 7.11 |
| CHEMBL260009 | — | — | 1 | 6.96 |
| CHEMBL257977 | — | — | 3 | 6.85 |
| CHEMBL256984 | — | — | 1 | 6.78 |
| CHEMBL407308 | — | — | 1 | 6.77 |
| CHEMBL406348 | — | — | 1 | 6.56 |
| CHEMBL402003 | — | — | 1 | 6.49 |
| CHEMBL258007 | — | — | 1 | 6.42 |
| CHEMBL260116 | — | — | 1 | 6.37 |
| CHEMBL255937 | — | — | 1 | 6.35 |
| CHEMBL258178 | — | — | 1 | 6.33 |
| CHEMBL260575 | — | — | 1 | 5.94 |
| CHEMBL257801 | — | — | 1 | 5.87 |
| CHEMBL260576 | — | — | 1 | 5.69 |
| CHEMBL257976 | — | — | 1 | 5.66 |
| CHEMBL261304 | — | — | 1 | - |
| CHEMBL260789 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260720 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL326702 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL406316 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL257978 | DABUZALGRON | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL404566 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL402388 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL255938 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL256982 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL256983 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL257800 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL257799 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL260009 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL257977 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL256984 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL407308 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL257977 | — | EC50 | = | 234.0 | nM | 6.63 |
| CHEMBL406348 | — | EC50 | = | 278.0 | nM | 6.56 |
| CHEMBL402003 | — | EC50 | = | 322.0 | nM | 6.49 |
| CHEMBL258007 | — | EC50 | = | 385.0 | nM | 6.42 |
| CHEMBL260116 | — | EC50 | = | 426.0 | nM | 6.37 |
| CHEMBL255937 | — | EC50 | = | 451.0 | nM | 6.35 |
| CHEMBL258178 | — | EC50 | = | 473.0 | nM | 6.33 |
| CHEMBL260575 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL257801 | — | EC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL260576 | — | EC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL257977 | — | EC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL257976 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL260789 | — | EC50 | > | 1300.0 | nM | - |
| CHEMBL261304 | — | EC50 | > | 2900.0 | nM | - |