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Assay Detail

CHEMBL670035

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

Binding
Inhibition of [3H]WIN-35428 binding to Dopamine transporter
12
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
Holmquist CR, Keverline-Frantz KI, Abraham P, Boja JW, Kuhar MJ, Carroll FI.
J Med Chem (1996) 39 : 4139 -4141
PubMed 8863789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.85 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306208 2 8.95
CHEMBL14391 2 8.90
CHEMBL82027 2 8.77
CHEMBL2079586 2 7.85
CHEMBL1790051 2 7.64
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL340560 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306208 IC50 = 1.12 nM 8.95
CHEMBL14391 IC50 = 1.26 nM 8.90
CHEMBL82027 IC50 = 1.71 nM 8.77
CHEMBL306208 IC50 = 2.4 nM 8.62
CHEMBL14391 IC50 = 2.85 nM 8.54
CHEMBL82027 IC50 = 10.2 nM 7.99
CHEMBL2079586 IC50 = 14.0 nM 7.85
CHEMBL2079586 IC50 = 21.0 nM 7.68
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL1790051 IC50 = 101.0 nM 7.00
CHEMBL340560 IC50 = 6160.0 nM 5.21