Assay Detail
Binding
CHEMBL5733908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: Serotonin, 5HT1A:Receptor Source: Human recombinant expressed in HEK-293 cellsRadioligand: [3H]-8-OH-DPAT (221 Ci/mmol)Control Compound: 8-OH-DPATIncubation Conditions: The reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 10 mM MgSO4, 0.5 mM EDTA and 0.1% Ascorbic acid at room temperature for 1 hour. 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 cloned serotonin-5HT1A 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 | 8.83 | 9.01 |
| Ki | 2 | 9.01 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6004129 | — | — | 6 | 9.19 |
| CHEMBL5095172 | BRILAROXAZINE | 3.0 | 6 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6004129 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL6004129 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5095172 | BRILAROXAZINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5095172 | BRILAROXAZINE | IC50 | = | 2.25 | nM | 8.65 |
| 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 | - |