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Assay Detail

CHEMBL5584715

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

Binding
Inhibition of human SERT expressed in HEK293 cells assessed as reduction in 5-HT reuptake incubated for 30 mins by fluorescent dye uptake assay
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 serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT<sub>1A</sub>/5-HT<sub>7</sub>.
Wu J, Zhang Z, Zhang Q, Li J.
Bioorg Med Chem (2024) 104 : 117698 -117698
PubMed 38552597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.30 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5598106 1 9.07
CHEMBL5597217 1 9.07
CHEMBL5598295 1 8.72
CHEMBL549 CITALOPRAM 4.0 1 8.04
CHEMBL4434876 1 6.60
CHEMBL5597179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5598106 IC50 = 0.85 nM 9.07
CHEMBL5597217 IC50 = 0.85 nM 9.07
CHEMBL5598295 IC50 = 1.9 nM 8.72
CHEMBL549 CITALOPRAM IC50 = 9.2 nM 8.04
CHEMBL4434876 IC50 = 251.1 nM 6.60
CHEMBL5597179 IC50 > 10000.0 nM -