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Assay Detail

CHEMBL830129

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

Binding
In vitro inhibition of [3H]nisoxetine binding to norepinephrine transporter expressed in human kidney cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
Jarkas N, McConathy J, Voll RJ, Goodman MM.
J Med Chem (2005) 48 : 4254 -4265
PubMed 15974579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.80 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190700 1 8.30
CHEMBL2113055 1 7.43
CHEMBL22183 1 7.21
CHEMBL413562 1 6.97
CHEMBL2113054 1 6.72
CHEMBL187935 1 6.71
CHEMBL363396 1 6.66
CHEMBL190703 1 6.57
CHEMBL190937 1 6.52
CHEMBL189367 1 6.43
CHEMBL189375 1 6.35
CHEMBL362783 1 6.32
CHEMBL23034 1 6.16
CHEMBL188964 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190700 Ki = 4.95 nM 8.30
CHEMBL2113055 Ki = 37.52 nM 7.43
CHEMBL22183 Ki = 61.0 nM 7.21
CHEMBL413562 Ki = 108.0 nM 6.97
CHEMBL2113054 Ki = 191.0 nM 6.72
CHEMBL187935 Ki = 194.0 nM 6.71
CHEMBL363396 Ki = 219.0 nM 6.66
CHEMBL190703 Ki = 269.0 nM 6.57
CHEMBL190937 Ki = 303.0 nM 6.52
CHEMBL189367 Ki = 370.0 nM 6.43
CHEMBL189375 Ki = 445.36 nM 6.35
CHEMBL362783 Ki = 483.55 nM 6.32
CHEMBL23034 Ki = 699.0 nM 6.16
CHEMBL188964 Ki > 5000.0 nM -