Assay Detail
Binding
CHEMBL5236912
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Partial agonist activity at human D2 receptor assessed as inhibition constant
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent and Subtype-Selective Dopamine D<sub>2</sub> Receptor Biased Partial Agonists Discovered via an Ugi-Based Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.32 | 9.47 |
| K | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 9.47 |
| CHEMBL4445841 | — | — | 1 | 7.92 |
| CHEMBL5272965 | — | — | 1 | 7.57 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | - |
| CHEMBL5289063 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL4445841 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5272965 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL2028019 | CARIPRAZINE | K | = | 0.49 | nM | - |
| CHEMBL5289063 | — | K | = | 46.0 | nM | - |