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Assay Detail

CHEMBL867291

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

Binding
Displacement of [3H]WIN-35428 from human DAT
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.
Carroll FI, Blough BE, Huang X, Nie Z, Mascarella SW, Deschamps J, Navarro HA.
J Med Chem (2006) 49 : 4589 -4594
PubMed 16854064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.78 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214209 1 8.42
CHEMBL1790051 1 7.64
CHEMBL385359 1 7.16
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL211372 1 6.89
CHEMBL380056 1 6.82
CHEMBL379333 1 6.80
CHEMBL378243 1 6.77
CHEMBL378483 1 6.54
CHEMBL379755 1 6.41
CHEMBL386978 1 6.39
CHEMBL379181 1 6.31
CHEMBL211494 1 6.05
CHEMBL212328 1 5.72
CHEMBL211396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214209 IC50 = 3.8 nM 8.42
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL385359 IC50 = 70.0 nM 7.16
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL211372 IC50 = 130.0 nM 6.89
CHEMBL380056 IC50 = 150.0 nM 6.82
CHEMBL379333 IC50 = 160.0 nM 6.80
CHEMBL378243 IC50 = 170.0 nM 6.77
CHEMBL378483 IC50 = 290.0 nM 6.54
CHEMBL379755 IC50 = 390.0 nM 6.41
CHEMBL386978 IC50 = 410.0 nM 6.39
CHEMBL379181 IC50 = 490.0 nM 6.31
CHEMBL211494 IC50 = 890.0 nM 6.05
CHEMBL212328 IC50 = 1920.0 nM 5.72
CHEMBL211396 IC50 > 2000.0 nM -