Assay Detail
Binding
CHEMBL649429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against alpha-1 adrenergic receptor by measuring displacement of [3H]prazosin from rat brain cortex membranes (in vitro).
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Studies on quinazolines. 5. 2,3-dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective alpha 1-adrenoceptor antagonists and antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 8.48 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2114071 | — | — | 1 | 10.17 |
| CHEMBL309150 | — | — | 1 | 10.15 |
| CHEMBL70872 | — | — | 1 | 9.96 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.72 |
| CHEMBL106737 | — | — | 1 | 9.68 |
| CHEMBL51433 | — | — | 1 | 9.60 |
| CHEMBL70498 | — | — | 1 | 9.47 |
| CHEMBL71470 | — | — | 1 | 9.47 |
| CHEMBL2114072 | — | — | 1 | 9.44 |
| CHEMBL304165 | — | — | 1 | 9.43 |
| CHEMBL2114069 | — | — | 1 | 9.24 |
| CHEMBL70347 | — | — | 1 | 9.17 |
| CHEMBL309149 | — | — | 1 | 8.96 |
| CHEMBL302021 | — | — | 1 | 8.89 |
| CHEMBL307961 | — | — | 1 | 8.87 |
| CHEMBL2114070 | — | — | 1 | 8.77 |
| CHEMBL71492 | — | — | 1 | 8.70 |
| CHEMBL2114065 | — | — | 1 | 8.24 |
| CHEMBL71207 | — | — | 1 | 7.98 |
| CHEMBL70928 | — | — | 1 | 7.84 |
| CHEMBL2114073 | — | — | 1 | 7.82 |
| CHEMBL70821 | — | — | 1 | 7.71 |
| CHEMBL70838 | — | — | 1 | 7.52 |
| CHEMBL304812 | — | — | 1 | 7.45 |
| CHEMBL305434 | — | — | 1 | 7.31 |
| CHEMBL306582 | — | — | 1 | 7.02 |
| CHEMBL70900 | — | — | 1 | 6.80 |
| CHEMBL308051 | — | — | 1 | 6.60 |
| CHEMBL305286 | — | — | 1 | 6.23 |
| CHEMBL68675 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2114071 | — | Ki | = | 0.068 | nM | 10.17 |
| CHEMBL309150 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL70872 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL106737 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL51433 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL70498 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL71470 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2114072 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL304165 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL2114069 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL70347 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL309149 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL302021 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL307961 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL2114070 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL71492 | — | Ki | = | 2.01 | nM | 8.70 |
| CHEMBL2114065 | — | Ki | = | 5.76 | nM | 8.24 |
| CHEMBL71207 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL70928 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL2114073 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL70821 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL70838 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL304812 | — | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL305434 | — | Ki | = | 48.8 | nM | 7.31 |
| CHEMBL306582 | — | Ki | = | 95.9 | nM | 7.02 |
| CHEMBL70900 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL308051 | — | Ki | = | 251.2 | nM | 6.60 |
| CHEMBL305286 | — | Ki | = | 586.0 | nM | 6.23 |
| CHEMBL68675 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL308089 | — | Ki | > | 10.0 | nM | - |
| CHEMBL431571 | — | Ki | > | 100.0 | nM | - |
| CHEMBL70387 | — | Ki | > | 100.0 | nM | - |
| CHEMBL68213 | — | Ki | > | 100.0 | nM | - |
| CHEMBL2114074 | — | Ki | > | 50.0 | nM | - |
| CHEMBL71603 | — | Ki | > | 100.0 | nM | - |
| CHEMBL303708 | — | Ki | > | 100.0 | nM | - |