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Assay Detail

CHEMBL1019480

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]dopamine from human recombinant DAT expressed in HEK293 cells by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
Cashman JR, Voelker T, Zhang HT, O'Donnell JM.
J Med Chem (2009) 52 : 1530 -1539
PubMed 19256502 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.21 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 1 6.52
CHEMBL505431 1 5.45
CHEMBL451500 1 5.27
CHEMBL450907 1 4.77
CHEMBL41 FLUOXETINE 4.0 1 4.71
CHEMBL464422 1 4.55
CHEMBL313041 1 -
CHEMBL463431 1 -
CHEMBL473966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE IC50 = 303.0 nM 6.52
CHEMBL505431 IC50 = 3556.0 nM 5.45
CHEMBL451500 IC50 = 5340.0 nM 5.27
CHEMBL450907 IC50 = 16987.0 nM 4.77
CHEMBL41 FLUOXETINE IC50 = 19500.0 nM 4.71
CHEMBL464422 IC50 = 27850.0 nM 4.55
CHEMBL313041 IC50 > 100000.0 nM -
CHEMBL463431 IC50 > 100000.0 nM -
CHEMBL473966 IC50 > 100000.0 nM -