Assay Detail
Binding
CHEMBL620706
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Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | C6 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.92 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33884 | — | — | 1 | 10.00 |
| CHEMBL121913 | — | — | 1 | 9.00 |
| CHEMBL331396 | — | — | 1 | 8.85 |
| CHEMBL121776 | — | — | 1 | 8.85 |
| CHEMBL332553 | — | — | 1 | 8.82 |
| CHEMBL330848 | — | — | 1 | 8.70 |
| CHEMBL334325 | — | — | 1 | 8.52 |
| CHEMBL122914 | — | — | 1 | 8.46 |
| CHEMBL286136 | — | — | 1 | 8.25 |
| CHEMBL125926 | — | — | 1 | 8.04 |
| CHEMBL125716 | — | — | 1 | 8.01 |
| CHEMBL2112621 | — | — | 1 | 7.94 |
| CHEMBL123377 | — | — | 1 | 7.84 |
| CHEMBL421256 | — | — | 1 | 7.78 |
| CHEMBL339936 | — | — | 1 | 7.75 |
| CHEMBL122818 | — | — | 1 | 7.64 |
| CHEMBL333028 | — | — | 1 | 7.64 |
| CHEMBL121766 | — | — | 1 | 7.19 |
| CHEMBL127876 | — | — | 1 | 6.79 |
| CHEMBL331264 | — | — | 1 | 6.70 |
| CHEMBL420166 | — | — | 1 | 6.62 |
| CHEMBL125670 | — | — | 1 | 6.53 |
| CHEMBL124485 | — | — | 1 | 6.15 |
| CHEMBL125005 | — | — | 1 | - |
| CHEMBL338136 | — | — | 1 | - |
| CHEMBL122973 | — | — | 1 | - |
| CHEMBL126098 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33884 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL121913 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL331396 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL121776 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL332553 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL330848 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL334325 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL122914 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL286136 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL125926 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL125716 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL2112621 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL123377 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL421256 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL339936 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL122818 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL333028 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL121766 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL127876 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL331264 | — | Ki | = | 199.2 | nM | 6.70 |
| CHEMBL420166 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL125670 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL124485 | — | Ki | = | 715.0 | nM | 6.15 |
| CHEMBL125005 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL338136 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL122973 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL126098 | — | Ki | > | 1000.0 | nM | - |