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Assay Detail

CHEMBL744184

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

Binding
Compound was evaluated for binding to Norepinephrine Transporter (NET) using [3H]desmethylimipramine as radioligand
7
Total Activities
7
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 noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
Agoston GE, Wu JH, Izenwasser S, George C, Katz J, Kline RH, Newman AH.
J Med Chem (1997) 40 : 4329 -4339
PubMed 9435902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.63 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084927 1 6.24
CHEMBL11493 1 5.88
CHEMBL12375 1 5.68
CHEMBL12227 1 5.45
CHEMBL440272 1 5.32
CHEMBL417249 1 5.23
CHEMBL317757 DIFLUOROBENZTROPINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084927 Ki = 577.0 nM 6.24
CHEMBL11493 Ki = 1330.0 nM 5.88
CHEMBL12375 Ki = 2080.0 nM 5.68
CHEMBL12227 Ki = 3520.0 nM 5.45
CHEMBL440272 Ki = 4790.0 nM 5.32
CHEMBL417249 Ki = 5920.0 nM 5.23
CHEMBL317757 DIFLUOROBENZTROPINE Ki > 8500.0 nM -