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Assay Detail

CHEMBL987974

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Binding
Inhibition of [3H]DA reuptake at human dopamine transporter expressed in HEK293 cells
4
Total Activities
4
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

Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines.
Middleton DS, Andrews M, Glossop P, Gymer G, Hepworth D, Jessiman A, Johnson PS, MacKenny M, Stobie A, Tang K, Morgan P, Jones B.
Bioorg Med Chem Lett (2008) 18 : 5303 -5306
PubMed 18782666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.01 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510484 1 5.05
CHEMBL479410 1 4.96
CHEMBL523146 1 -
CHEMBL491408 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510484 IC50 = 9000.0 nM 5.05
CHEMBL479410 IC50 = 11000.0 nM 4.96
CHEMBL523146 IC50 > 10000.0 nM -
CHEMBL491408 IC50 > 10000.0 nM -