Assay Detail
Binding
CHEMBL676300
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Tested for in vitro binding affinity against cloned mammalian dopamine autoreceptor (DA) receptors expressed in CHO-K1 cells [3H]-spiperone as radioligand
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| 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 | 19 | 6.75 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328119 | — | — | 1 | 7.72 |
| CHEMBL327263 | — | — | 2 | 7.66 |
| CHEMBL92682 | — | — | 1 | 7.21 |
| CHEMBL93534 | — | — | 1 | 7.17 |
| CHEMBL90359 | — | — | 1 | 7.17 |
| CHEMBL92578 | — | — | 1 | 7.08 |
| CHEMBL328785 | — | — | 1 | 7.07 |
| CHEMBL92630 | — | — | 1 | 7.04 |
| CHEMBL92938 | — | — | 1 | 6.86 |
| CHEMBL92817 | — | — | 1 | 6.77 |
| CHEMBL2111566 | — | — | 2 | 6.76 |
| CHEMBL328431 | — | — | 1 | 6.47 |
| CHEMBL93283 | — | — | 1 | 6.47 |
| CHEMBL93234 | — | — | 1 | 6.24 |
| CHEMBL315890 | — | — | 1 | 6.11 |
| CHEMBL328448 | — | — | 1 | 5.95 |
| CHEMBL93701 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328119 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL327263 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL92682 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL93534 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL90359 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL92578 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL328785 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL92630 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL92938 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL92817 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2111566 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL328431 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL93283 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL93234 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL327263 | — | Ki | = | 587.0 | nM | 6.23 |
| CHEMBL315890 | — | Ki | = | 777.0 | nM | 6.11 |
| CHEMBL328448 | — | Ki | = | 1136.0 | nM | 5.95 |
| CHEMBL93701 | — | Ki | = | 3113.0 | nM | 5.51 |
| CHEMBL2111566 | — | Ki | > | 500.0 | nM | - |