Assay Detail
Binding
CHEMBL1798144
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Displacement of [125I]BE-2254 from human adrenergic Alpha-1B receptor expressed in HEK293 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 24 | 6.74 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301707 | — | — | 1 | 8.74 |
| CHEMBL1796033 | — | — | 1 | 7.62 |
| CHEMBL1796034 | — | — | 1 | 7.52 |
| CHEMBL1796046 | — | — | 1 | 7.25 |
| CHEMBL1796050 | — | — | 1 | 7.14 |
| CHEMBL1796036 | — | — | 1 | 7.01 |
| CHEMBL1796035 | — | — | 1 | 6.97 |
| CHEMBL1796030 | — | — | 1 | 6.95 |
| CHEMBL1796031 | — | — | 1 | 6.95 |
| CHEMBL1796037 | — | — | 1 | 6.95 |
| CHEMBL1796039 | — | — | 1 | 6.90 |
| CHEMBL1796042 | — | — | 1 | 6.89 |
| CHEMBL1796044 | — | — | 1 | 6.89 |
| CHEMBL1796040 | — | — | 1 | 6.87 |
| CHEMBL1796047 | — | — | 1 | 6.82 |
| CHEMBL1796045 | — | — | 1 | 6.71 |
| CHEMBL1796043 | — | — | 1 | 6.68 |
| CHEMBL1796049 | — | — | 1 | 6.63 |
| CHEMBL1796041 | — | — | 1 | 6.61 |
| CHEMBL1796032 | — | — | 1 | 6.48 |
| CHEMBL1796029 | — | — | 1 | 5.65 |
| CHEMBL1796048 | — | — | 1 | 5.30 |
| CHEMBL1796028 | — | — | 1 | 5.13 |
| CHEMBL1796038 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301707 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL1796033 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL1796034 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL1796046 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL1796050 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL1796036 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL1796035 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL1796030 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL1796031 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL1796037 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL1796039 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1796042 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1796044 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1796040 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL1796047 | — | Ki | = | 151.36 | nM | 6.82 |
| CHEMBL1796045 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL1796043 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL1796049 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL1796041 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL1796032 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL1796029 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL1796048 | — | Ki | = | 5011.87 | nM | 5.30 |
| CHEMBL1796028 | — | Ki | = | 7413.1 | nM | 5.13 |
| CHEMBL1796038 | — | Ki | = | 10000.0 | nM | 5.00 |