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Assay Detail

CHEMBL756266

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

Binding
Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Houlihan WJ, Kelly L, Pankuch J, Koletar J, Brand L, Janowsky A, Kopajtic TA.
J Med Chem (2002) 45 : 4097 -4109
PubMed 12213053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.37 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336100 1 9.05
CHEMBL336940 1 8.17
CHEMBL781 MAZINDOL 4.0 1 7.75
CHEMBL130477 1 7.75
CHEMBL132082 1 7.64
CHEMBL132954 1 7.64
CHEMBL132955 1 7.40
CHEMBL133043 1 7.08
CHEMBL133902 1 7.00
CHEMBL336613 1 6.77
CHEMBL130668 1 6.42
CHEMBL370805 COCAINE 4.0 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336100 Ki = 0.9 nM 9.05
CHEMBL336940 Ki = 6.8 nM 8.17
CHEMBL781 MAZINDOL Ki = 18.0 nM 7.75
CHEMBL130477 Ki = 18.0 nM 7.75
CHEMBL132082 Ki = 23.0 nM 7.64
CHEMBL132954 Ki = 23.1 nM 7.64
CHEMBL132955 Ki = 40.0 nM 7.40
CHEMBL133043 Ki = 84.0 nM 7.08
CHEMBL133902 Ki = 100.0 nM 7.00
CHEMBL336613 Ki = 170.0 nM 6.77
CHEMBL130668 Ki = 380.0 nM 6.42
CHEMBL370805 COCAINE Ki = 1940.0 nM 5.71