Assay Detail
Binding
CHEMBL649224
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Binding affinity against alpha-2 adrenergic receptor by measuring displacement of [3H]clonidine from rat brain cortex membranes (in vitro).
24
Total Activities
24
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 | 24 | 5.93 | 6.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70872 | — | — | 1 | 6.94 |
| CHEMBL70498 | — | — | 1 | 6.65 |
| CHEMBL2114065 | — | — | 1 | 6.52 |
| CHEMBL70928 | — | — | 1 | 6.41 |
| CHEMBL2114069 | — | — | 1 | 6.41 |
| CHEMBL70347 | — | — | 1 | 6.33 |
| CHEMBL309150 | — | — | 1 | 6.33 |
| CHEMBL106737 | — | — | 1 | 6.23 |
| CHEMBL2114071 | — | — | 1 | 6.09 |
| CHEMBL307961 | — | — | 1 | 6.02 |
| CHEMBL2114070 | — | — | 1 | 6.02 |
| CHEMBL2114072 | — | — | 1 | 5.85 |
| CHEMBL51433 | — | — | 1 | 5.80 |
| CHEMBL70838 | — | — | 1 | 5.77 |
| CHEMBL304165 | — | — | 1 | 5.76 |
| CHEMBL71470 | — | — | 1 | 5.75 |
| CHEMBL309149 | — | — | 1 | 5.50 |
| CHEMBL71207 | — | — | 1 | 5.48 |
| CHEMBL302021 | — | — | 1 | 5.46 |
| CHEMBL71492 | — | — | 1 | 5.41 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 5.32 |
| CHEMBL304812 | — | — | 1 | 5.30 |
| CHEMBL305434 | — | — | 1 | 5.08 |
| CHEMBL68675 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70872 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL70498 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL2114065 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL70928 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL2114069 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL70347 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL309150 | — | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL106737 | — | Ki | = | 593.0 | nM | 6.23 |
| CHEMBL2114071 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL307961 | — | Ki | = | 952.0 | nM | 6.02 |
| CHEMBL2114070 | — | Ki | = | 962.0 | nM | 6.02 |
| CHEMBL2114072 | — | Ki | = | 1419.0 | nM | 5.85 |
| CHEMBL51433 | — | Ki | = | 1599.0 | nM | 5.80 |
| CHEMBL70838 | — | Ki | = | 1694.0 | nM | 5.77 |
| CHEMBL304165 | — | Ki | = | 1740.0 | nM | 5.76 |
| CHEMBL71470 | — | Ki | = | 1778.0 | nM | 5.75 |
| CHEMBL309149 | — | Ki | = | 3166.0 | nM | 5.50 |
| CHEMBL71207 | — | Ki | = | 3334.0 | nM | 5.48 |
| CHEMBL302021 | — | Ki | = | 3450.0 | nM | 5.46 |
| CHEMBL71492 | — | Ki | = | 3860.0 | nM | 5.41 |
| CHEMBL2 | PRAZOSIN | Ki | = | 4830.0 | nM | 5.32 |
| CHEMBL304812 | — | Ki | = | 5011.0 | nM | 5.30 |
| CHEMBL305434 | — | Ki | = | 8356.0 | nM | 5.08 |
| CHEMBL68675 | — | Ki | > | 10000.0 | nM | - |