Assay Detail
Binding
CHEMBL1066832
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.58 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218166 | BIFEPRUNOX | 3.0 | 1 | 10.40 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 9.21 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.00 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.55 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.54 |
| CHEMBL88365 | — | — | 1 | 8.34 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.21 |
| CHEMBL7549 | PRECLAMOL | 2.0 | 1 | 7.76 |
| CHEMBL592377 | — | — | 1 | 7.46 |
| CHEMBL447809 | — | — | 1 | 7.16 |
| CHEMBL592618 | — | — | 1 | 6.46 |
| CHEMBL596800 | — | — | 1 | 6.41 |
| CHEMBL597413 | — | — | 1 | 6.37 |
| CHEMBL596801 | — | — | 1 | 6.18 |
| CHEMBL311730 | — | — | 1 | 6.12 |
| CHEMBL596802 | PRIDOPIDINE | 3.0 | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218166 | BIFEPRUNOX | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL53 | APOMORPHINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL59 | DOPAMINE | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL88365 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL715 | OLANZAPINE | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL7549 | PRECLAMOL | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL592377 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL447809 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL592618 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL596800 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL597413 | — | Ki | = | 431.0 | nM | 6.37 |
| CHEMBL596801 | — | Ki | = | 664.0 | nM | 6.18 |
| CHEMBL311730 | — | Ki | = | 755.0 | nM | 6.12 |
| CHEMBL596802 | PRIDOPIDINE | Ki | = | 7521.0 | nM | 5.12 |