Assay Detail
Binding
CHEMBL651981
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat brain homogenate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.21 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL69584 | — | — | 1 | 7.06 |
| CHEMBL351989 | — | — | 1 | 6.31 |
| CHEMBL159742 | — | — | 1 | 6.18 |
| CHEMBL351612 | — | — | 1 | 6.01 |
| CHEMBL349833 | — | — | 1 | 6.00 |
| CHEMBL345438 | — | — | 1 | 6.00 |
| CHEMBL354699 | — | — | 1 | 5.98 |
| CHEMBL68191 | — | — | 1 | 5.90 |
| CHEMBL351963 | — | — | 1 | 5.87 |
| CHEMBL439646 | — | — | 1 | 5.76 |
| CHEMBL352207 | — | — | 1 | 5.64 |
| CHEMBL67414 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL69584 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL351989 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL159742 | — | Ki | = | 653.0 | nM | 6.18 |
| CHEMBL351612 | — | Ki | = | 983.0 | nM | 6.01 |
| CHEMBL349833 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL345438 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL354699 | — | Ki | = | 1056.0 | nM | 5.98 |
| CHEMBL68191 | — | Ki | = | 1265.0 | nM | 5.90 |
| CHEMBL351963 | — | Ki | = | 1361.0 | nM | 5.87 |
| CHEMBL439646 | — | Ki | = | 1735.0 | nM | 5.76 |
| CHEMBL352207 | — | Ki | = | 2284.0 | nM | 5.64 |
| CHEMBL67414 | — | Ki | = | 2678.0 | nM | 5.57 |