Assay Detail
Binding
CHEMBL649435
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Binding affinity for alpha-1 adrenergic receptor by displacement of [3H]-prazosin from rat brain homogenate preparation
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.04 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.82 |
| CHEMBL148457 | — | — | 1 | 9.82 |
| CHEMBL147255 | — | — | 1 | 9.82 |
| CHEMBL147393 | — | — | 1 | 9.32 |
| CHEMBL149047 | — | — | 1 | 9.28 |
| CHEMBL150112 | — | — | 1 | 9.21 |
| CHEMBL149262 | — | — | 1 | 9.17 |
| CHEMBL149187 | — | — | 1 | 9.00 |
| CHEMBL149828 | — | — | 1 | 8.99 |
| CHEMBL149997 | — | — | 1 | 8.94 |
| CHEMBL149481 | — | — | 1 | 8.89 |
| CHEMBL146844 | — | — | 1 | 8.85 |
| CHEMBL149452 | — | — | 1 | 8.74 |
| CHEMBL150919 | — | — | 1 | 8.67 |
| CHEMBL150239 | — | — | 1 | 8.66 |
| CHEMBL149253 | — | — | 1 | 8.45 |
| CHEMBL147019 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL148457 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL147255 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL147393 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL149047 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL150112 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL149262 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL149187 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL149828 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL149997 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL149481 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL146844 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL149452 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL150919 | — | Ki | = | 2.12 | nM | 8.67 |
| CHEMBL150239 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL149253 | — | Ki | = | 3.52 | nM | 8.45 |
| CHEMBL147019 | — | Ki | = | 10.0 | nM | 8.00 |