Assay Detail
Binding
CHEMBL617482
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Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserin from rat prefrontal cerebral cortex mambranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.48 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL152997 | — | — | 1 | 8.28 |
| CHEMBL356250 | — | — | 1 | 8.10 |
| CHEMBL346203 | — | — | 1 | 7.99 |
| CHEMBL150578 | — | — | 1 | 7.84 |
| CHEMBL654 | MIRTAZAPINE | 4.0 | 1 | 7.83 |
| CHEMBL423034 | — | — | 1 | 7.79 |
| CHEMBL357308 | — | — | 1 | 7.76 |
| CHEMBL153685 | — | — | 1 | 7.72 |
| CHEMBL153391 | — | — | 1 | 7.64 |
| CHEMBL150333 | — | — | 1 | 7.62 |
| CHEMBL348235 | — | — | 1 | 7.55 |
| CHEMBL151043 | — | — | 1 | 7.40 |
| CHEMBL357341 | — | — | 1 | 7.35 |
| CHEMBL421787 | — | — | 1 | 7.27 |
| CHEMBL153684 | — | — | 1 | 7.27 |
| CHEMBL153716 | — | — | 1 | 7.26 |
| CHEMBL348005 | — | — | 1 | 6.85 |
| CHEMBL152083 | — | — | 1 | 6.83 |
| CHEMBL348492 | — | — | 1 | 6.71 |
| CHEMBL356403 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL152997 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL356250 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL346203 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL150578 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL654 | MIRTAZAPINE | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL423034 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL357308 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL153685 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL153391 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL150333 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL348235 | — | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL151043 | — | Ki | = | 40.2 | nM | 7.40 |
| CHEMBL357341 | — | Ki | = | 44.4 | nM | 7.35 |
| CHEMBL421787 | — | Ki | = | 53.8 | nM | 7.27 |
| CHEMBL153684 | — | Ki | = | 53.3 | nM | 7.27 |
| CHEMBL153716 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL348005 | — | Ki | = | 139.9 | nM | 6.85 |
| CHEMBL152083 | — | Ki | = | 149.1 | nM | 6.83 |
| CHEMBL348492 | — | Ki | = | 193.7 | nM | 6.71 |
| CHEMBL356403 | — | Ki | = | 360.2 | nM | 6.44 |