Assay Detail
Binding
CHEMBL648042
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Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain
12
Total Activities
12
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
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.45 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.13 |
| CHEMBL35057 | TIOSPIRONE | 2.0 | 1 | 8.82 |
| CHEMBL37633 | — | — | 1 | 8.68 |
| CHEMBL284847 | — | — | 1 | 8.64 |
| CHEMBL35743 | — | — | 1 | 8.52 |
| CHEMBL35085 | — | — | 1 | 8.38 |
| CHEMBL287605 | — | — | 1 | 8.35 |
| CHEMBL35565 | — | — | 1 | 8.29 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.25 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL35040 | — | — | 1 | 8.19 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL35057 | TIOSPIRONE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL37633 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL284847 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL35743 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL35085 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL287605 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL35565 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL42 | CLOZAPINE | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL35040 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 11.0 | nM | 7.96 |