Assay Detail
Binding
CHEMBL4015806
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from human D2LR expressed in CHO cell membranes by radioligand binding assay
18
Total Activities
18
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
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D2R Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.08 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 9.28 |
| CHEMBL2165126 | — | — | 1 | 9.28 |
| CHEMBL4072780 | — | — | 1 | 9.06 |
| CHEMBL4083239 | — | — | 1 | 9.05 |
| CHEMBL4102628 | — | — | 1 | 8.80 |
| CHEMBL4064742 | — | — | 1 | 8.80 |
| CHEMBL4100183 | — | — | 1 | 8.70 |
| CHEMBL4091933 | — | — | 1 | 8.54 |
| CHEMBL4064186 | — | — | 1 | 8.47 |
| CHEMBL4099666 | — | — | 1 | 8.32 |
| CHEMBL4092441 | — | — | 1 | 8.08 |
| CHEMBL4061986 | — | — | 1 | 7.48 |
| CHEMBL4073330 | — | — | 1 | 7.40 |
| CHEMBL4091507 | — | — | 1 | 7.11 |
| CHEMBL4084690 | — | — | 1 | 7.00 |
| CHEMBL4083727 | — | — | 1 | 6.96 |
| CHEMBL4068702 | — | — | 1 | 6.70 |
| CHEMBL4070604 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL2165126 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL4072780 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL4083239 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL4102628 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4064742 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4100183 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4091933 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4064186 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4099666 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4092441 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL4061986 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4073330 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4091507 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4084690 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4083727 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4068702 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4070604 | — | Ki | = | 350.0 | nM | 6.46 |