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Assay Detail

CHEMBL5614961

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

Binding
Inhibition of human SERT expressed in HEK293 cells incubated for 30 mins
21
Total Activities
21
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 and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile.
Zheng J, Zhou L, Gong X, Yang F, Cheng J, Ma R, Wu C, Xu Z, Zhu W, He Y, Shen J.
Eur J Med Chem (2024) 275 : 116564 -116564
PubMed 38875810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.16 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.17
CHEMBL5618995 1 8.70
CHEMBL5620090 1 8.52
CHEMBL5618877 1 7.92
CHEMBL5619646 1 7.47
CHEMBL5619208 1 7.40
CHEMBL5619328 1 7.32
CHEMBL5619931 1 7.19
CHEMBL5620043 1 7.14
CHEMBL5618922 1 7.10
CHEMBL5620117 1 6.97
CHEMBL5620061 1 6.86
CHEMBL5618136 1 6.84
CHEMBL5619007 1 6.82
CHEMBL5618693 1 6.45
CHEMBL5619076 1 6.33
CHEMBL5618780 1 5.58
CHEMBL5618601 1 5.17
CHEMBL5620209 1 -
CHEMBL5619978 1 -
CHEMBL5619395 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE IC50 = 0.67 nM 9.17
CHEMBL5618995 IC50 = 2.0 nM 8.70
CHEMBL5620090 IC50 = 3.0 nM 8.52
CHEMBL5618877 IC50 = 12.0 nM 7.92
CHEMBL5619646 IC50 = 34.0 nM 7.47
CHEMBL5619208 IC50 = 39.7 nM 7.40
CHEMBL5619328 IC50 = 48.0 nM 7.32
CHEMBL5619931 IC50 = 65.0 nM 7.19
CHEMBL5620043 IC50 = 72.0 nM 7.14
CHEMBL5618922 IC50 = 80.0 nM 7.10
CHEMBL5620117 IC50 = 107.0 nM 6.97
CHEMBL5620061 IC50 = 139.0 nM 6.86
CHEMBL5618136 IC50 = 146.0 nM 6.84
CHEMBL5619007 IC50 = 152.0 nM 6.82
CHEMBL5618693 IC50 = 359.0 nM 6.45
CHEMBL5619076 IC50 = 467.0 nM 6.33
CHEMBL5618780 IC50 = 2642.0 nM 5.58
CHEMBL5618601 IC50 = 6757.0 nM 5.17
CHEMBL5620209 IC50 > 30000.0 nM -
CHEMBL5619978 IC50 > 30000.0 nM -
CHEMBL5619395 IC50 > 30000.0 nM -