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Assay Detail

CHEMBL675909

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

Binding
Inhibitory activity against radioligand [3H]WIN-35428 binding at the dopamine transporter
9
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 (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes.
Jiang S, Chang AC, Abraham P, Kuhar MJ, Carroll FI.
Bioorg Med Chem Lett (1998) 8 : 3689 -3692
PubMed 9934496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.34 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82027 1 8.77
CHEMBL123058 2 8.71
CHEMBL3084336 2 7.90
CHEMBL1790051 1 7.64
CHEMBL3085511 2 7.55
CHEMBL370805 COCAINE 4.0 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82027 IC50 = 1.71 nM 8.77
CHEMBL123058 IC50 = 1.96 nM 8.71
CHEMBL3084336 IC50 = 12.6 nM 7.90
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL3085511 IC50 = 28.0 nM 7.55
CHEMBL370805 COCAINE IC50 = 89.0 nM 7.05
CHEMBL123058 IC50 = 429.0 nM 6.37
CHEMBL3084336 IC50 = 690.0 nM 6.16
CHEMBL3085511 IC50 = 1270.0 nM 5.90