Assay Detail
Binding
CHEMBL5381009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human D3 receptor in HEK293 cell membranes measured after 60 mins by scintillation counting method
35
Total Activities
35
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 | 35 | 8.92 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5431103 | — | — | 1 | 9.85 |
| CHEMBL5425134 | — | — | 1 | 9.74 |
| CHEMBL5433284 | — | — | 1 | 9.68 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 9.66 |
| CHEMBL5408223 | — | — | 1 | 9.60 |
| CHEMBL5417351 | — | — | 1 | 9.59 |
| CHEMBL5404807 | — | — | 1 | 9.54 |
| CHEMBL5415846 | — | — | 1 | 9.54 |
| CHEMBL5395965 | — | — | 1 | 9.51 |
| CHEMBL5404054 | — | — | 1 | 9.47 |
| CHEMBL5398100 | — | — | 1 | 9.44 |
| CHEMBL5440422 | — | — | 1 | 9.24 |
| CHEMBL5429048 | — | — | 1 | 9.23 |
| CHEMBL5437660 | — | — | 1 | 9.19 |
| CHEMBL5429826 | — | — | 1 | 9.18 |
| CHEMBL5424897 | — | — | 1 | 9.14 |
| CHEMBL5409755 | — | — | 1 | 9.11 |
| CHEMBL5438081 | — | — | 1 | 9.02 |
| CHEMBL5436641 | — | — | 1 | 9.00 |
| CHEMBL5400528 | — | — | 1 | 8.99 |
| CHEMBL5427065 | — | — | 1 | 8.99 |
| CHEMBL5434229 | — | — | 1 | 8.97 |
| CHEMBL5403268 | — | — | 1 | 8.88 |
| CHEMBL5421925 | — | — | 1 | 8.88 |
| CHEMBL5409134 | — | — | 1 | 8.75 |
| CHEMBL5436957 | — | — | 1 | 8.73 |
| CHEMBL3085821 | — | — | 1 | 8.67 |
| CHEMBL5402212 | — | — | 1 | 8.62 |
| CHEMBL5435745 | — | — | 1 | 8.46 |
| CHEMBL5427695 | — | — | 1 | 8.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5431103 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL5425134 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL5433284 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL5408223 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL5417351 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL5404807 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL5415846 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL5395965 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL5404054 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL5398100 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL5440422 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL5429048 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL5437660 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL5429826 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL5424897 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL5409755 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL5438081 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL5436641 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5400528 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL5427065 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL5434229 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL5403268 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL5421925 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL5409134 | — | Ki | = | 1.76 | nM | 8.75 |
| CHEMBL5436957 | — | Ki | = | 1.86 | nM | 8.73 |
| CHEMBL3085821 | — | Ki | = | 2.13 | nM | 8.67 |
| CHEMBL5402212 | — | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL5435745 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL5427695 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL5399129 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL5421827 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL5420316 | — | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL5424241 | — | Ki | = | 38.8 | nM | 7.41 |
| CHEMBL5426620 | — | Ki | = | 50.7 | nM | 7.29 |