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Assay Detail

CHEMBL4219694

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

Binding
Binding affinity to human SERT expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting
5
Total Activities
4
Compounds Tested
2
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

Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.
Subbaiah MAM.
J Med Chem (2018) 61 : 2133 -2165
PubMed 28731336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.06 8.68
Kd 1 6.68 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4227444 2 8.68
CHEMBL4226233 1 8.22
CHEMBL637 VENLAFAXINE 4.0 1 7.41
CHEMBL4228171 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4227444 Ki = 2.1 nM 8.68
CHEMBL4226233 Ki = 6.0 nM 8.22
CHEMBL4227444 Ki = 12.0 nM 7.92
CHEMBL637 VENLAFAXINE Ki = 39.0 nM 7.41
CHEMBL4228171 Kd = 210.0 nM 6.68