Assay Detail
Binding
CHEMBL676706
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Tested for affinity against striatal dopamine autoreceptor (DA) D2 receptors using [3H]spiperone as radioligand in rats.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.16 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328119 | — | — | 1 | 7.40 |
| CHEMBL327263 | — | — | 2 | 7.19 |
| CHEMBL92682 | — | — | 1 | 7.09 |
| CHEMBL93701 | — | — | 1 | 7.04 |
| CHEMBL328785 | — | — | 1 | 6.41 |
| CHEMBL90359 | — | — | 1 | 6.39 |
| CHEMBL92817 | — | — | 1 | 6.27 |
| CHEMBL93283 | — | — | 1 | 6.15 |
| CHEMBL92938 | — | — | 1 | 6.07 |
| CHEMBL93234 | — | — | 1 | 6.03 |
| CHEMBL92578 | — | — | 1 | 5.95 |
| CHEMBL329139 | — | — | 1 | 5.93 |
| CHEMBL92630 | — | — | 1 | 5.88 |
| CHEMBL315890 | — | — | 1 | 5.83 |
| CHEMBL328431 | — | — | 1 | 5.20 |
| CHEMBL94224 | — | — | 1 | 4.93 |
| CHEMBL328448 | — | — | 1 | 4.93 |
| CHEMBL2111566 | — | — | 2 | - |
| CHEMBL93534 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328119 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL327263 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL92682 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL93701 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL328785 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL90359 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL92817 | — | Ki | = | 533.0 | nM | 6.27 |
| CHEMBL93283 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL92938 | — | Ki | = | 849.0 | nM | 6.07 |
| CHEMBL93234 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL92578 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL329139 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL92630 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL315890 | — | Ki | = | 1490.0 | nM | 5.83 |
| CHEMBL328431 | — | Ki | = | 6250.0 | nM | 5.20 |
| CHEMBL328448 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL94224 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL327263 | — | Ki | > | 453.0 | nM | - |
| CHEMBL2111566 | — | Ki | > | 172.0 | nM | - |
| CHEMBL2111566 | — | Ki | > | 172.0 | nM | - |
| CHEMBL93534 | — | Ki | > | 172.0 | nM | - |