Assay Detail
Binding
CHEMBL2026138
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Displacement of [3H]-prazosin from adrenergic alpha-1 receptor in rat cerebral cortical membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.98 | 7.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024676 | — | — | 1 | 7.53 |
| CHEMBL2024675 | — | — | 1 | 7.46 |
| CHEMBL2024522 | — | — | 1 | 7.34 |
| CHEMBL2024523 | — | — | 1 | 7.14 |
| CHEMBL2024524 | — | — | 1 | 6.97 |
| CHEMBL2024525 | — | — | 1 | 6.81 |
| CHEMBL2024521 | — | — | 1 | 6.69 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 6.67 |
| CHEMBL2024677 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024676 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL2024675 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL2024522 | — | Ki | = | 45.9 | nM | 7.34 |
| CHEMBL2024523 | — | Ki | = | 72.9 | nM | 7.14 |
| CHEMBL2024524 | — | Ki | = | 106.4 | nM | 6.97 |
| CHEMBL2024525 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL2024521 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL2024677 | — | Ki | = | 667.0 | nM | 6.18 |