Assay Detail
Binding
CHEMBL5731958
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Dopamine D2 Receptors (Cell-Based Assay): The ability of Compound 102 to bind dopamine D2 receptors was measured in a cell-based assay. Dopamine D2 receptor cells were seeded in a half a black, clear-bottomed 96 well plate. At a density of 15,000 cells/well to a volume of 25 μL and were left to incubate overnight. Calcium 5 dye in HEPES buffered HBSS (Hanks' balanced salt solution) was prepared and 10 μL was added to each well and the mixture was left to sit at 37° C. for 1 hour. After equilibration, 5 μL of the test compound and controls were added to the wells and incubated at room temperature for 10 minutes. Fluorescence was measured every 1.52 seconds. After 20 seconds 10 μL of dopamine (at EC80 concentration) was added and the fluorescence monitored for 2 minutes with excitation at 452 nm and emission at 525 nm.
12
Total Activities
4
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Psychotrophic agents and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.62 | 8.82 |
| kon | 4 | - | - |
| k_off | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL243712 | AMISULPRIDE | 4.0 | 3 | 8.82 |
| CHEMBL85 | RISPERIDONE | 4.0 | 3 | 8.44 |
| CHEMBL4594422 | LB-102 | 2.0 | 3 | 8.05 |
| CHEMBL42 | CLOZAPINE | 4.0 | 3 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL243712 | AMISULPRIDE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4594422 | LB-102 | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4594422 | LB-102 | kon | = | - | — | - |
| CHEMBL4594422 | LB-102 | k_off | = | - | s-1 | - |
| CHEMBL85 | RISPERIDONE | kon | = | - | — | - |
| CHEMBL85 | RISPERIDONE | k_off | = | - | s-1 | - |
| CHEMBL243712 | AMISULPRIDE | kon | = | - | — | - |
| CHEMBL243712 | AMISULPRIDE | k_off | = | - | s-1 | - |
| CHEMBL42 | CLOZAPINE | kon | = | - | — | - |
| CHEMBL42 | CLOZAPINE | k_off | = | - | s-1 | - |