Assay Detail
Binding
CHEMBL971387
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Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells
21
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.83 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL467540 | — | — | 1 | 9.04 |
| CHEMBL156639 | — | — | 1 | 8.81 |
| CHEMBL468017 | — | — | 3 | 8.74 |
| CHEMBL285755 | — | — | 1 | 8.63 |
| CHEMBL468015 | — | — | 3 | 8.38 |
| CHEMBL468016 | — | — | 3 | 8.29 |
| CHEMBL468833 | — | — | 1 | 8.15 |
| CHEMBL468022 | — | — | 1 | 7.91 |
| CHEMBL513352 | — | — | 1 | 7.46 |
| CHEMBL467767 | — | — | 1 | 7.39 |
| CHEMBL468834 | — | — | 1 | 7.33 |
| CHEMBL469181 | — | — | 1 | 6.81 |
| CHEMBL466561 | — | — | 1 | 6.80 |
| CHEMBL467768 | — | — | 1 | 6.73 |
| CHEMBL469182 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL467540 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL156639 | — | Ki | = | 1.56 | nM | 8.81 |
| CHEMBL468017 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL468017 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL285755 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL468015 | — | Ki | = | 4.15 | nM | 8.38 |
| CHEMBL468016 | — | Ki | = | 5.09 | nM | 8.29 |
| CHEMBL468015 | — | Ki | = | 5.96 | nM | 8.22 |
| CHEMBL468016 | — | Ki | = | 7.01 | nM | 8.15 |
| CHEMBL468833 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL468017 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL468022 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL513352 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL467767 | — | Ki | = | 40.7 | nM | 7.39 |
| CHEMBL468015 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL468834 | — | Ki | = | 46.7 | nM | 7.33 |
| CHEMBL468016 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL469181 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL466561 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL467768 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL469182 | — | Ki | = | 254.0 | nM | 6.59 |