Assay Detail
Binding
CHEMBL5381022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-5-HT from 5HT2B receptor in HEK293 cell membranes by scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dopamine D<sub>3</sub>/D<sub>2</sub> Receptor Ligands Based on Cariprazine for the Treatment of Psychostimulant Use Disorders That May Be Dual Diagnosed with Affective Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.36 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 9.82 |
| CHEMBL5404054 | — | — | 1 | 8.90 |
| CHEMBL5431103 | — | — | 1 | 8.83 |
| CHEMBL5408223 | — | — | 1 | 8.77 |
| CHEMBL5429826 | — | — | 1 | 8.70 |
| CHEMBL5424897 | — | — | 1 | 8.24 |
| CHEMBL5437660 | — | — | 1 | 8.21 |
| CHEMBL5409134 | — | — | 1 | 8.14 |
| CHEMBL5434229 | — | — | 1 | 7.95 |
| CHEMBL5436641 | — | — | 1 | 7.73 |
| CHEMBL5403268 | — | — | 1 | 7.53 |
| CHEMBL5427695 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 0.151 | nM | 9.82 |
| CHEMBL5404054 | — | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL5431103 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL5408223 | — | Ki | = | 1.71 | nM | 8.77 |
| CHEMBL5429826 | — | Ki | = | 1.99 | nM | 8.70 |
| CHEMBL5424897 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL5437660 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL5409134 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL5434229 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL5436641 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL5403268 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL5427695 | — | Ki | = | 34.2 | nM | 7.47 |