Assay Detail
Binding
CHEMBL617438
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Binding affinity towards 5-hydroxytryptamine 2 receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]ketanserin as radioligand
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.38 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6616 | — | — | 1 | 7.72 |
| CHEMBL69700 | — | — | 1 | 7.62 |
| CHEMBL292821 | — | — | 1 | 7.47 |
| CHEMBL6607 | BROLAMFETAMINE | 2.0 | 1 | 7.39 |
| CHEMBL8214 | — | — | 1 | 7.24 |
| CHEMBL317634 | — | — | 1 | 7.19 |
| CHEMBL8569 | — | — | 1 | 7.16 |
| CHEMBL351858 | — | — | 1 | 7.10 |
| CHEMBL8600 | DOM | — | 1 | 7.00 |
| CHEMBL8224 | — | — | 1 | 7.00 |
| CHEMBL468880 | — | — | 1 | 6.84 |
| CHEMBL161905 | — | — | 1 | 6.24 |
| CHEMBL60146 | — | — | 1 | 6.08 |
| CHEMBL162122 | — | — | 1 | 6.08 |
| CHEMBL163985 | — | — | 1 | 5.99 |
| CHEMBL8389 | — | — | 1 | 5.90 |
| CHEMBL166040 | — | — | 1 | 5.84 |
| CHEMBL6731 | TENAMFETAMINE | 2.0 | 2 | 5.66 |
| CHEMBL8225 | — | — | 1 | 5.66 |
| CHEMBL273251 | — | — | 1 | 5.61 |
| CHEMBL18762 | — | — | 1 | 5.61 |
| CHEMBL163814 | — | — | 1 | 5.60 |
| CHEMBL8642 | — | — | 1 | 5.28 |
| CHEMBL30336 | — | — | 1 | 4.78 |
| CHEMBL282734 | — | — | 1 | - |
| CHEMBL161985 | — | — | 1 | - |
| CHEMBL162209 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6616 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL69700 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL292821 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL6607 | BROLAMFETAMINE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL8214 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL317634 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL8569 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL351858 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL8600 | DOM | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL8224 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL468880 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL161905 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL162122 | — | Ki | = | 825.0 | nM | 6.08 |
| CHEMBL60146 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL163985 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL8389 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL166040 | — | Ki | = | 1435.0 | nM | 5.84 |
| CHEMBL6731 | TENAMFETAMINE | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL8225 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL273251 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL18762 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL163814 | — | Ki | = | 2525.0 | nM | 5.60 |
| CHEMBL6731 | TENAMFETAMINE | Ki | = | 3425.0 | nM | 5.46 |
| CHEMBL8642 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL30336 | — | Ki | = | 16500.0 | nM | 4.78 |
| CHEMBL282734 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL162209 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL161985 | — | Ki | > | 10000.0 | nM | - |