Assay Detail
Binding
CHEMBL643720
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Inhibition of Alpha-1 adrenergic receptor in rat cortex membrane
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.52 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344178 | — | — | 1 | 9.70 |
| CHEMBL137903 | — | — | 1 | 8.85 |
| CHEMBL343364 | — | — | 1 | 8.80 |
| CHEMBL137598 | — | — | 1 | 8.70 |
| CHEMBL342200 | — | — | 1 | 8.49 |
| CHEMBL430717 | — | — | 1 | 8.40 |
| CHEMBL136684 | — | — | 1 | 8.39 |
| CHEMBL123128 | — | — | 1 | 8.34 |
| CHEMBL335731 | — | — | 1 | 8.22 |
| CHEMBL434228 | — | — | 1 | 8.14 |
| CHEMBL424658 | — | — | 1 | 7.82 |
| CHEMBL343283 | — | — | 1 | 7.77 |
| CHEMBL342671 | — | — | 1 | 7.50 |
| CHEMBL136482 | — | — | 1 | 7.40 |
| CHEMBL136561 | — | — | 1 | 7.35 |
| CHEMBL137679 | — | — | 1 | 7.31 |
| CHEMBL136588 | — | — | 1 | 7.16 |
| CHEMBL136123 | — | — | 1 | 7.07 |
| CHEMBL337371 | — | — | 1 | 6.96 |
| CHEMBL136458 | — | — | 1 | 6.91 |
| CHEMBL136067 | — | — | 1 | 6.59 |
| CHEMBL136060 | — | — | 1 | 6.47 |
| CHEMBL1226 | AMINODIMETHOXYQUINAZOLINYLPIPERAZINE | — | 1 | 6.47 |
| CHEMBL435591 | — | — | 1 | 5.93 |
| CHEMBL136375 | — | — | 1 | 5.50 |
| CHEMBL136627 | — | — | 1 | 5.29 |
| CHEMBL136426 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344178 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL137903 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL343364 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL137598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL342200 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL430717 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL136684 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL123128 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL335731 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL434228 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL424658 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL343283 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL342671 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL136482 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL136561 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL137679 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL136588 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL136123 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL337371 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL136458 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL136067 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL136060 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1226 | AMINODIMETHOXYQUINAZOLINYLPIPERAZINE | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL435591 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL136375 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL136627 | — | IC50 | = | 5080.0 | nM | 5.29 |
| CHEMBL136426 | — | IC50 | > | 1000.0 | nM | - |