Assay Detail
Binding
CHEMBL651983
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Binding affinity determined against alpha-1 adrenergic receptor in rat cortex membranes using [3H]prazosin as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.75 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79725 | — | — | 1 | 8.92 |
| CHEMBL1159649 | — | — | 1 | 8.77 |
| CHEMBL441259 | — | — | 1 | 8.68 |
| CHEMBL82488 | — | — | 1 | 8.55 |
| CHEMBL1169435 | — | — | 1 | 8.55 |
| CHEMBL79853 | — | — | 1 | 8.52 |
| CHEMBL310744 | — | — | 1 | 8.24 |
| CHEMBL79674 | — | — | 1 | 7.92 |
| CHEMBL82523 | — | — | 1 | 7.80 |
| CHEMBL442974 | — | — | 1 | 7.80 |
| CHEMBL83617 | — | — | 1 | 7.80 |
| CHEMBL311323 | — | — | 1 | 7.77 |
| CHEMBL81703 | — | — | 1 | 7.77 |
| CHEMBL311787 | — | — | 1 | 7.70 |
| CHEMBL83112 | — | — | 1 | 7.58 |
| CHEMBL79693 | — | — | 1 | 7.52 |
| CHEMBL2112307 | — | — | 1 | 7.51 |
| CHEMBL310082 | — | — | 1 | 7.44 |
| CHEMBL84171 | — | — | 1 | 7.12 |
| CHEMBL79561 | — | — | 1 | 7.00 |
| CHEMBL311694 | — | — | 1 | 6.87 |
| CHEMBL313452 | — | — | 1 | 6.72 |
| CHEMBL83732 | — | — | 1 | 6.70 |
| CHEMBL81191 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79725 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1159649 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL441259 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL82488 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1169435 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL79853 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL310744 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL79674 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL82523 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL442974 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL83617 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL311323 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL81703 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL311787 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL83112 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL79693 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2112307 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL310082 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL84171 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL79561 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL311694 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL313452 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL83732 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL81191 | — | Ki | = | 224.0 | nM | 6.65 |