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Assay Detail

CHEMBL672989

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

Binding
Ability to displace [3H]WIN-35428 from dopamine transporter on guinea pig striatal membrane.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Houlihan WJ, Ahmad UF, Koletar J, Kelly L, Brand L, Kopajtic TA.
J Med Chem (2002) 45 : 4110 -4118
PubMed 12213054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.80 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334577 1 8.68
CHEMBL337020 1 8.57
CHEMBL340281 1 8.48
CHEMBL132676 1 8.39
CHEMBL130477 1 8.38
CHEMBL424627 1 8.08
CHEMBL133646 1 7.97
CHEMBL130877 1 7.44
CHEMBL781 MAZINDOL 4.0 1 7.37
CHEMBL130593 1 6.66
CHEMBL132713 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334577 IC50 = 2.1 nM 8.68
CHEMBL337020 IC50 = 2.7 nM 8.57
CHEMBL340281 IC50 = 3.3 nM 8.48
CHEMBL132676 IC50 = 4.1 nM 8.39
CHEMBL130477 IC50 = 4.2 nM 8.38
CHEMBL424627 IC50 = 8.4 nM 8.08
CHEMBL133646 IC50 = 10.6 nM 7.97
CHEMBL130877 IC50 = 36.1 nM 7.44
CHEMBL781 MAZINDOL IC50 = 42.6 nM 7.37
CHEMBL130593 IC50 = 218.0 nM 6.66
CHEMBL132713 IC50 = 1841.0 nM 5.74