Assay Detail
Binding
CHEMBL648031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was tested for its binding affinity for alpha-1 adrenergic receptor site by displacement of [3H]clonidine at 10e-6 M concentration
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.50 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.72 |
| CHEMBL154624 | — | — | 2 | 9.15 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 3 | 8.96 |
| CHEMBL262745 | — | — | 1 | 8.80 |
| CHEMBL154882 | — | — | 1 | 8.52 |
| CHEMBL154212 | — | — | 1 | 8.43 |
| CHEMBL155264 | — | — | 1 | 8.42 |
| CHEMBL154844 | — | — | 1 | 8.19 |
| CHEMBL154686 | — | — | 1 | 8.19 |
| CHEMBL424516 | — | — | 1 | 8.19 |
| CHEMBL155532 | — | — | 1 | 8.17 |
| CHEMBL154088 | — | — | 1 | 8.11 |
| CHEMBL153815 | — | — | 1 | 7.90 |
| CHEMBL154119 | — | — | 1 | 7.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL154624 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL262745 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL154624 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL154882 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL154212 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL155264 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL154686 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL424516 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL154844 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL155532 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL154088 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL153815 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL154119 | — | Ki | = | 13.3 | nM | 7.88 |