Assay Detail
Functional
CHEMBL1798146
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Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
3
Total Activities
3
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
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands for α₁-adrenoceptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.03 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1796033 | — | — | 1 | 8.60 |
| CHEMBL1796050 | — | — | 1 | 8.00 |
| CHEMBL1796046 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1796033 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1796050 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1796046 | — | Ki | = | 31.62 | nM | 7.50 |