Assay Detail
Binding
CHEMBL5733907
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: Dopamine, D2S: Materials and Methods: Receptor Source: Human recombinant expressed in CHO cells Radioligand: [3H]Spiperone (20-60 Ci/mmol) Control Compound: Haloperidol Incubation Conditions: The reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 120 mM NaCl, 5 mM KCl, 5 mM MgCl2, 1 mM EDTA for 60 minutes at 25 C. 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 dopamineD2 short 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 | 8.86 | 9.01 |
| Ki | 2 | 9.37 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6004129 | — | — | 6 | 9.52 |
| CHEMBL5095172 | BRILAROXAZINE | 3.0 | 6 | 9.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6004129 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5095172 | BRILAROXAZINE | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL6004129 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5095172 | BRILAROXAZINE | IC50 | = | 1.96 | nM | 8.71 |
| 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 | - |