Assay Detail
Binding
CHEMBL2026134
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Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in Sf9 cells
24
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| 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 | 8.91 | 9.59 |
| Ki | 8 | 8.51 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024516 | — | — | 1 | 9.59 |
| CHEMBL2024514 | — | — | 1 | 9.54 |
| CHEMBL2024520 | — | — | 1 | 9.49 |
| CHEMBL2024518 | — | — | 1 | 9.47 |
| CHEMBL2024513 | — | — | 1 | 9.39 |
| CHEMBL2024677 | — | — | 1 | 9.36 |
| CHEMBL2024515 | — | — | 1 | 9.32 |
| CHEMBL2024519 | — | — | 1 | 9.21 |
| CHEMBL2024675 | — | — | 1 | 9.18 |
| CHEMBL2024509 | — | — | 1 | 9.05 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 8.80 |
| CHEMBL2024522 | — | — | 1 | 8.80 |
| CHEMBL2024506 | — | — | 1 | 8.72 |
| CHEMBL2024508 | — | — | 1 | 8.72 |
| CHEMBL2024507 | — | — | 1 | 8.48 |
| CHEMBL2024676 | — | — | 1 | 8.48 |
| CHEMBL2024510 | — | — | 1 | 8.32 |
| CHEMBL2024523 | — | — | 1 | 8.30 |
| CHEMBL2024512 | — | — | 1 | 8.29 |
| CHEMBL2021954 | — | — | 1 | 8.28 |
| CHEMBL2024525 | — | — | 1 | 8.27 |
| CHEMBL2024511 | — | — | 1 | 7.96 |
| CHEMBL2024524 | — | — | 1 | 7.88 |
| CHEMBL2024521 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024516 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2024514 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL2024520 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL2024518 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL2024513 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL2024677 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL2024515 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL2024519 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL2024675 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL2024509 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2024522 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2024506 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2024508 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2024507 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2024676 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2024510 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2024523 | — | Ki | = | 4.95 | nM | 8.30 |
| CHEMBL2024512 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2021954 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL2024525 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2024511 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2024524 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL2024521 | — | Ki | = | 15.9 | nM | 7.80 |