Assay Detail
Binding
CHEMBL645692
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Binding affinity towards alpha-1 adrenergic receptors in rat brain synaptosomal preparations
9
Total Activities
9
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
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.34 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275045 | — | — | 1 | 9.15 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.00 |
| CHEMBL10085 | MAZAPERTINE | 2.0 | 1 | 8.89 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.85 |
| CHEMBL10417 | — | — | 1 | 8.52 |
| CHEMBL416703 | — | — | 1 | 8.40 |
| CHEMBL428175 | RWJ-25730 | — | 1 | 8.09 |
| CHEMBL10105 | — | — | 1 | 7.50 |
| CHEMBL10327 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275045 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL10085 | MAZAPERTINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL42 | CLOZAPINE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL10417 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL416703 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL428175 | RWJ-25730 | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL10105 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL10327 | — | Ki | = | 220.0 | nM | 6.66 |