Assay Detail
Binding
CHEMBL648587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at Alpha-1 adrenergic receptor in rat brain homogenates by [3H]- prazosin displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Expert |
Target
Alpha adrenergic receptor 1A and 1B (CHEMBL2111476) ↗| Type | SELECTIVITY GROUP |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.06 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL69584 | — | — | 1 | 7.06 |
| CHEMBL302075 | — | — | 1 | 6.49 |
| CHEMBL302340 | — | — | 1 | 6.09 |
| CHEMBL68191 | — | — | 1 | 5.90 |
| CHEMBL305276 | — | — | 1 | 5.70 |
| CHEMBL67222 | — | — | 1 | 5.70 |
| CHEMBL305061 | — | — | 1 | 5.69 |
| CHEMBL67414 | — | — | 1 | 5.57 |
| CHEMBL63209 | — | — | 1 | 5.54 |
| CHEMBL66957 | — | — | 1 | 5.51 |
| CHEMBL67042 | — | — | 1 | 5.02 |
| CHEMBL67429 | — | — | 1 | - |
| CHEMBL68190 | — | — | 1 | - |
| CHEMBL304777 | — | — | 1 | - |
| CHEMBL303406 | — | — | 1 | - |
| CHEMBL304584 | — | — | 1 | - |
| CHEMBL303692 | — | — | 1 | - |
| CHEMBL305453 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL69584 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL302075 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL302340 | — | Ki | = | 815.0 | nM | 6.09 |
| CHEMBL68191 | — | Ki | = | 1265.0 | nM | 5.90 |
| CHEMBL305276 | — | Ki | = | 2003.0 | nM | 5.70 |
| CHEMBL67222 | — | Ki | = | 2003.0 | nM | 5.70 |
| CHEMBL305061 | — | Ki | = | 2038.0 | nM | 5.69 |
| CHEMBL67414 | — | Ki | = | 2678.0 | nM | 5.57 |
| CHEMBL63209 | — | Ki | = | 2878.0 | nM | 5.54 |
| CHEMBL66957 | — | Ki | = | 3120.0 | nM | 5.51 |
| CHEMBL67042 | — | Ki | = | 9591.0 | nM | 5.02 |
| CHEMBL67429 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL68190 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL304777 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL303406 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL304584 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL303692 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL305453 | — | Ki | > | 10000.0 | nM | - |