Assay Detail
Binding
CHEMBL4015812
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5-HT2AR expressed in HEK293T 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 |
| Cell Type | HEK-293T |
| 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 | 6.26 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165126 | — | — | 1 | 8.70 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.44 |
| CHEMBL4064186 | — | — | 1 | 7.41 |
| CHEMBL4091933 | — | — | 1 | 6.80 |
| CHEMBL4061986 | — | — | 1 | 6.70 |
| CHEMBL4072780 | — | — | 1 | 6.37 |
| CHEMBL4083727 | — | — | 1 | 6.32 |
| CHEMBL4100183 | — | — | 1 | 5.89 |
| CHEMBL4068702 | — | — | 1 | 5.82 |
| CHEMBL4064742 | — | — | 1 | 5.70 |
| CHEMBL4083239 | — | — | 1 | 5.66 |
| CHEMBL4084690 | — | — | 1 | 5.64 |
| CHEMBL4073330 | — | — | 1 | 5.55 |
| CHEMBL4102628 | — | — | 1 | 5.47 |
| CHEMBL4092441 | — | — | 1 | 5.44 |
| CHEMBL4070604 | — | — | 1 | 5.38 |
| CHEMBL4091507 | — | — | 1 | 5.05 |
| CHEMBL4099666 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165126 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4064186 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4091933 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4061986 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4072780 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL4083727 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL4100183 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4068702 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4064742 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4083239 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4084690 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL4073330 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL4102628 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL4092441 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL4070604 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL4091507 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL4099666 | — | Ki | > | 20000.0 | nM | - |