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Assay Detail

CHEMBL947040

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

Binding
Displacement of [3H]citalopram from human SERT expressed in HEK293 cells
7
Total Activities
7
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 serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter.
Zeng F, Jarkas N, Stehouwer JS, Voll RJ, Owens MJ, Kilts CD, Nemeroff CB, Goodman MM.
Bioorg Med Chem (2008) 16 : 783 -793
PubMed 17983754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.76 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181188 1 8.01
CHEMBL272003 1 7.04
CHEMBL411262 1 6.92
CHEMBL223166 1 6.73
CHEMBL270099 1 6.30
CHEMBL272002 1 6.21
CHEMBL411263 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181188 Ki = 9.69 nM 8.01
CHEMBL272003 Ki = 90.88 nM 7.04
CHEMBL411262 Ki = 121.0 nM 6.92
CHEMBL223166 Ki = 185.0 nM 6.73
CHEMBL270099 Ki = 498.0 nM 6.30
CHEMBL272002 Ki = 614.0 nM 6.21
CHEMBL411263 Ki = 733.0 nM 6.13