Assay Detail
Binding
CHEMBL2026135
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Displacement of [3H]spiperone from dopamine D2 receptor in rat striatal membranes
24
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| IC50 | 16 | 7.55 | 8.64 |
| Ki | 8 | 7.27 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024514 | — | — | 1 | 8.64 |
| CHEMBL2024515 | — | — | 1 | 8.27 |
| CHEMBL2024513 | — | — | 1 | 8.23 |
| CHEMBL2024516 | — | — | 1 | 8.15 |
| CHEMBL2024675 | — | — | 1 | 8.09 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 7.80 |
| CHEMBL2024518 | — | — | 1 | 7.77 |
| CHEMBL2024677 | — | — | 1 | 7.70 |
| CHEMBL2024522 | — | — | 1 | 7.70 |
| CHEMBL2024512 | — | — | 1 | 7.60 |
| CHEMBL2024520 | — | — | 1 | 7.54 |
| CHEMBL2024506 | — | — | 1 | 7.41 |
| CHEMBL2024519 | — | — | 1 | 7.37 |
| CHEMBL2024523 | — | — | 1 | 7.27 |
| CHEMBL2024507 | — | — | 1 | 7.19 |
| CHEMBL2024510 | — | — | 1 | 7.18 |
| CHEMBL2021954 | — | — | 1 | 7.07 |
| CHEMBL2024521 | — | — | 1 | 7.03 |
| CHEMBL2024525 | — | — | 1 | 6.97 |
| CHEMBL2024676 | — | — | 1 | 6.96 |
| CHEMBL2024509 | — | — | 1 | 6.87 |
| CHEMBL2024508 | — | — | 1 | 6.84 |
| CHEMBL2024511 | — | — | 1 | 6.80 |
| CHEMBL2024524 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024514 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2024515 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2024513 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL2024516 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2024675 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2024518 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL2024677 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL2024522 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL2024512 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2024520 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2024506 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2024519 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL2024523 | — | Ki | = | 53.4 | nM | 7.27 |
| CHEMBL2024507 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2024510 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2021954 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2024521 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2024525 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL2024676 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2024509 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2024508 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL2024511 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2024524 | — | Ki | = | 392.0 | nM | 6.41 |