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Assay Detail

CHEMBL918082

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

Binding
Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
Cao J, Lever JR, Kopajtic T, Katz JL, Pham AT, Holmes ML, Justice JB, Newman AH.
J Med Chem (2004) 47 : 6128 -6136
PubMed 15566284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.22 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221725 1 8.25
CHEMBL330021 1 7.71
CHEMBL281594 VANOXERINE 3.0 1 7.68
CHEMBL87841 1 7.53
CHEMBL375607 1 7.18
CHEMBL222184 1 7.17
CHEMBL221767 1 7.12
CHEMBL223296 1 7.02
CHEMBL374126 1 7.00
CHEMBL221506 1 6.79
CHEMBL223134 1 6.62
CHEMBL221819 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221725 IC50 = 5.61 nM 8.25
CHEMBL330021 IC50 = 19.5 nM 7.71
CHEMBL281594 VANOXERINE IC50 = 21.1 nM 7.68
CHEMBL87841 IC50 = 29.7 nM 7.53
CHEMBL375607 IC50 = 66.0 nM 7.18
CHEMBL222184 IC50 = 68.3 nM 7.17
CHEMBL221767 IC50 = 75.4 nM 7.12
CHEMBL223296 IC50 = 95.5 nM 7.02
CHEMBL374126 IC50 = 99.8 nM 7.00
CHEMBL221506 IC50 = 163.0 nM 6.79
CHEMBL223134 IC50 = 242.0 nM 6.62
CHEMBL221819 IC50 = 282.0 nM 6.55