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Assay Detail

CHEMBL675903

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

Binding
Inhibitory activity against Dopamine transporter using 0.5 nM [3H]WIN-35428 as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.
Chang AC, Burgess JP, Mascarella SW, Abraham P, Kuhar MJ, Carroll FI.
J Med Chem (1997) 40 : 1247 -1251
PubMed 9111298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.66 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790051 1 7.64
CHEMBL3085557 1 7.55
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL21362 1 6.26
CHEMBL3084343 1 5.90
CHEMBL610898 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL3085557 IC50 = 28.0 nM 7.55
CHEMBL370805 COCAINE IC50 = 89.0 nM 7.05
CHEMBL21362 IC50 = 550.0 nM 6.26
CHEMBL3084343 IC50 = 1270.0 nM 5.90
CHEMBL610898 IC50 = 2860.0 nM 5.54