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Assay Detail

CHEMBL3587151

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

Binding
Inhibition of human SERT S438T mutant expressed in HEK293 GripTite cells pre-incubated for 5 mins followed by [3H]5-HT addition by [3H]5-HT uptake assay
4
Total Activities
4
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

Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram.
Kumar V, Yarravarapu N, Lapinsky DJ, Perley D, Felts B, Tomlinson MJ, Vaughan RA, Henry LK, Lever JR, Newman AH.
J Med Chem (2015) 58 : 5609 -5619
PubMed 26153715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.19 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586681 1 5.42
CHEMBL3586683 1 5.24
CHEMBL1508 ESCITALOPRAM 4.0 1 5.10
CHEMBL3586682 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586681 Ki = 3811.0 nM 5.42
CHEMBL3586683 Ki = 5697.0 nM 5.24
CHEMBL1508 ESCITALOPRAM Ki = 7879.0 nM 5.10
CHEMBL3586682 Ki = 9879.0 nM 5.00