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Assay Detail

CHEMBL964690

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
9
Total Activities
9
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

Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
Ben-Daniel R, Deuther-Conrad W, Scheunemann M, Steinbach J, Brust P, Mishani E.
Bioorg Med Chem (2008) 16 : 6364 -6370
PubMed 18487050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.80 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490 PAROXETINE 4.0 1 9.38
CHEMBL43048 MIDOMAFETAMINE 3.0 1 9.14
CHEMBL482903 1 8.39
CHEMBL549 CITALOPRAM 4.0 1 8.36
CHEMBL520301 1 8.19
CHEMBL503609 1 7.94
CHEMBL519819 1 6.67
CHEMBL520970 1 6.43
CHEMBL483316 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490 PAROXETINE Ki = 0.42 nM 9.38
CHEMBL43048 MIDOMAFETAMINE Ki = 0.73 nM 9.14
CHEMBL482903 Ki = 4.11 nM 8.39
CHEMBL549 CITALOPRAM Ki = 4.38 nM 8.36
CHEMBL520301 Ki = 6.46 nM 8.19
CHEMBL503609 Ki = 11.4 nM 7.94
CHEMBL519819 Ki = 213.0 nM 6.67
CHEMBL520970 Ki = 374.0 nM 6.43
CHEMBL483316 Ki = 1910.0 nM 5.72