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Assay Detail

CHEMBL5731958

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Binding
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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Psychotrophic agents and uses thereof
(2019)

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 -