Assay Detail
Binding
CHEMBL821941
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Binding affinity against alpha-1-adrenoceptor in rat brain homogenates [3H]-prazosin displacement.
18
Total Activities
18
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. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 9.50 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50451 | — | — | 1 | 10.10 |
| CHEMBL50979 | — | — | 1 | 9.80 |
| CHEMBL54288 | — | — | 1 | 9.74 |
| CHEMBL52155 | — | — | 1 | 9.74 |
| CHEMBL275524 | — | — | 1 | 9.72 |
| CHEMBL299584 | — | — | 1 | 9.62 |
| CHEMBL52439 | — | — | 1 | 9.59 |
| CHEMBL50137 | — | — | 1 | 9.57 |
| CHEMBL50746 | — | — | 1 | 9.57 |
| CHEMBL301614 | — | — | 1 | 9.54 |
| CHEMBL301749 | — | — | 1 | 9.51 |
| CHEMBL50084 | — | — | 1 | 9.49 |
| CHEMBL51056 | — | — | 1 | 9.44 |
| CHEMBL50473 | — | — | 1 | 9.40 |
| CHEMBL300972 | — | — | 1 | 9.33 |
| CHEMBL300632 | — | — | 1 | 9.06 |
| CHEMBL298946 | — | — | 1 | 9.04 |
| CHEMBL422581 | — | — | 1 | 8.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50451 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL50979 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL54288 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL52155 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL275524 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL299584 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL52439 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL50137 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL50746 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL301614 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL301749 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL50084 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL51056 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL50473 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL300972 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL300632 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL298946 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL422581 | — | Ki | = | 1.66 | nM | 8.78 |