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Assay Detail

CHEMBL1013549

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

Binding
Displacement of [3H]WIN-35428 from DAT
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter.
Jin C, Navarro HA, Carroll FI.
J Med Chem (2008) 51 : 8048 -8056
PubMed 19053748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.68 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457865 1 9.09
CHEMBL459332 1 8.60
CHEMBL514424 1 8.48
CHEMBL457635 1 8.22
CHEMBL457655 1 8.22
CHEMBL512202 1 8.19
CHEMBL458080 1 8.15
CHEMBL455937 1 7.89
CHEMBL515988 1 7.85
CHEMBL516933 1 7.82
CHEMBL458072 1 7.80
CHEMBL461241 1 7.75
CHEMBL457866 1 7.38
CHEMBL513090 1 7.33
CHEMBL529437 COCAINE HYDROCHLORIDE 4.0 1 7.05
CHEMBL458282 1 7.04
CHEMBL458488 1 7.04
CHEMBL459333 1 6.99
CHEMBL457415 1 6.77
CHEMBL457416 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457865 IC50 = 0.82 nM 9.09
CHEMBL459332 IC50 = 2.5 nM 8.60
CHEMBL514424 IC50 = 3.3 nM 8.48
CHEMBL457635 IC50 = 6.0 nM 8.22
CHEMBL457655 IC50 = 6.0 nM 8.22
CHEMBL512202 IC50 = 6.5 nM 8.19
CHEMBL458080 IC50 = 7.0 nM 8.15
CHEMBL455937 IC50 = 13.0 nM 7.89
CHEMBL515988 IC50 = 14.0 nM 7.85
CHEMBL516933 IC50 = 15.0 nM 7.82
CHEMBL458072 IC50 = 16.0 nM 7.80
CHEMBL461241 IC50 = 18.0 nM 7.75
CHEMBL457866 IC50 = 42.0 nM 7.38
CHEMBL513090 IC50 = 47.0 nM 7.33
CHEMBL529437 COCAINE HYDROCHLORIDE IC50 = 89.1 nM 7.05
CHEMBL458282 IC50 = 92.0 nM 7.04
CHEMBL458488 IC50 = 92.0 nM 7.04
CHEMBL459333 IC50 = 102.0 nM 6.99
CHEMBL457415 IC50 = 170.0 nM 6.77
CHEMBL457416 IC50 = 1300.0 nM 5.89