Assay Detail
Binding
CHEMBL5236915
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Partial agonist activity at human D2 receptor assessed as increase in cAMP accumulation
4
Total Activities
4
Compounds Tested
1
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 |
|---|---|---|---|
| EC50 | 4 | 7.86 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 9.74 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.42 |
| CHEMBL5272965 | — | — | 1 | 7.21 |
| CHEMBL5289063 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5272965 | — | EC50 | = | 61.7 | nM | 7.21 |
| CHEMBL5289063 | — | EC50 | = | 90.0 | nM | 7.05 |