Assay Detail
Binding
CHEMBL971388
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Displacement of [3H]spiperone from rat dopamine D2L 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 | 6.54 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468833 | — | — | 1 | 7.46 |
| CHEMBL468017 | — | — | 3 | 7.36 |
| CHEMBL513352 | — | — | 1 | 7.09 |
| CHEMBL156639 | — | — | 1 | 6.85 |
| CHEMBL468016 | — | — | 3 | 6.78 |
| CHEMBL467767 | — | — | 1 | 6.72 |
| CHEMBL285755 | — | — | 1 | 6.70 |
| CHEMBL468015 | — | — | 3 | 6.61 |
| CHEMBL467540 | — | — | 1 | 6.58 |
| CHEMBL466561 | — | — | 1 | 6.13 |
| CHEMBL468022 | — | — | 1 | 6.11 |
| CHEMBL469182 | — | — | 1 | 6.09 |
| CHEMBL469181 | — | — | 1 | 6.04 |
| CHEMBL468834 | — | — | 1 | 5.74 |
| CHEMBL467768 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468833 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL468017 | — | Ki | = | 44.2 | nM | 7.36 |
| CHEMBL468017 | — | Ki | = | 56.8 | nM | 7.25 |
| CHEMBL468017 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL513352 | — | Ki | = | 81.2 | nM | 7.09 |
| CHEMBL156639 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL468016 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL467767 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL285755 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL468015 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL468016 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL467540 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL468016 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL468015 | — | Ki | = | 639.0 | nM | 6.19 |
| CHEMBL466561 | — | Ki | = | 746.0 | nM | 6.13 |
| CHEMBL468022 | — | Ki | = | 769.0 | nM | 6.11 |
| CHEMBL469182 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL469181 | — | Ki | = | 915.0 | nM | 6.04 |
| CHEMBL468834 | — | Ki | = | 1835.0 | nM | 5.74 |
| CHEMBL468015 | — | Ki | = | 1979.0 | nM | 5.70 |
| CHEMBL467768 | — | Ki | = | 2570.0 | nM | 5.59 |