Assay Detail
Binding
CHEMBL5733909
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: Serotonin, 5HT2A :Materials and Methods: Receptor Source: Human Cortex Radioligand: [3H]-Ketanserin (60-90 Ci/mmol) Control Compound: Ketanserin Incubation Conditions: The reactions were carried out in 50 mM TRIS-HCl (pH 7.6) at room temperature for 90 minutes. The reaction was terminated by rapid vacuum filtration onto glass fiber filters. Radioactivity trapped onto the filters was determined and compared to control values in order to ascertain any interactions of test compounds with the serotonin-5HT2A binding site
12
Total Activities
2
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Arylpiperazine derivatives and methods of utilizing same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| kon | 4 | - | - |
| k_off | 4 | - | - |
| IC50 | 2 | 6.74 | 6.89 |
| Ki | 2 | 7.08 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5095172 | BRILAROXAZINE | 3.0 | 6 | 7.23 |
| CHEMBL6004129 | — | — | 6 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5095172 | BRILAROXAZINE | Ki | = | 58.5 | nM | 7.23 |
| CHEMBL6004129 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL5095172 | BRILAROXAZINE | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL6004129 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL6004129 | — | kon | = | - | — | - |
| CHEMBL6004129 | — | k_off | = | - | s-1 | - |
| CHEMBL6004129 | — | kon | = | - | — | - |
| CHEMBL6004129 | — | k_off | = | - | s-1 | - |
| CHEMBL5095172 | BRILAROXAZINE | kon | = | - | — | - |
| CHEMBL5095172 | BRILAROXAZINE | k_off | = | - | s-1 | - |
| CHEMBL5095172 | BRILAROXAZINE | kon | = | - | — | - |
| CHEMBL5095172 | BRILAROXAZINE | k_off | = | - | s-1 | - |