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Assay Detail

CHEMBL1001387

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

Binding
Displacement of [3H]nisoxetine from human NET expressed in HEK293 cells
6
Total Activities
6
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 Autocuration

Target

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

Publication

3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.
Funke U, Fischer S, Hiller A, Scheunemann M, Deuther-Conrad W, Brust P, Steinbach J.
Bioorg Med Chem Lett (2008) 18 : 4727 -4730
PubMed 18644726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.45 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293583 1 7.01
CHEMBL477587 1 6.99
CHEMBL55505 1 6.74
CHEMBL449277 1 6.11
CHEMBL294481 1 5.99
CHEMBL54465 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293583 Ki = 96.7 nM 7.01
CHEMBL477587 Ki = 102.0 nM 6.99
CHEMBL55505 Ki = 184.0 nM 6.74
CHEMBL449277 Ki = 772.0 nM 6.11
CHEMBL294481 Ki = 1020.0 nM 5.99
CHEMBL54465 Ki = 1430.0 nM 5.84