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Assay Detail

CHEMBL5165150

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

Binding
Inhibition of SERT (unknown origin) expressed in human HEK293 cells
36
Total Activities
36
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

Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression.
Zhang C, Wang L, Xu Y, Huang Y, Huang J, Zhu J, Wang W, Li W, Sun A, Li X, Zhang H, Li J.
Eur J Med Chem (2022) 236 : 114347 -114347
PubMed 35430560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.84 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.40
CHEMBL5176363 1 8.36
CHEMBL5191418 1 8.36
CHEMBL5180472 1 8.34
CHEMBL5181226 1 8.30
CHEMBL5184959 1 8.19
CHEMBL5170075 1 8.17
CHEMBL5175011 1 8.13
CHEMBL5208902 1 8.11
CHEMBL5183093 1 8.09
CHEMBL5201565 1 7.95
CHEMBL5207117 1 7.93
CHEMBL5170676 1 7.86
CHEMBL5183581 1 7.85
CHEMBL5180815 1 7.82
CHEMBL5173093 1 7.72
CHEMBL5203206 1 7.51
CHEMBL5200156 1 7.38
CHEMBL5204395 1 7.34
CHEMBL5194592 1 7.24
CHEMBL5188606 1 7.18
CHEMBL5192104 1 7.17
CHEMBL5170867 1 5.92
CHEMBL5178292 1 -
CHEMBL5172714 1 -
CHEMBL3989929 AZELIRAGON 3.0 1 -
CHEMBL5178447 1 -
CHEMBL5204858 1 -
CHEMBL5199141 1 -
CHEMBL5174761 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE IC50 = 0.4 nM 9.40
CHEMBL5176363 IC50 = 4.36 nM 8.36
CHEMBL5191418 IC50 = 4.4 nM 8.36
CHEMBL5180472 IC50 = 4.6 nM 8.34
CHEMBL5181226 IC50 = 4.97 nM 8.30
CHEMBL5184959 IC50 = 6.42 nM 8.19
CHEMBL5170075 IC50 = 6.71 nM 8.17
CHEMBL5175011 IC50 = 7.47 nM 8.13
CHEMBL5208902 IC50 = 7.77 nM 8.11
CHEMBL5183093 IC50 = 8.23 nM 8.09
CHEMBL5201565 IC50 = 11.16 nM 7.95
CHEMBL5207117 IC50 = 11.67 nM 7.93
CHEMBL5170676 IC50 = 13.83 nM 7.86
CHEMBL5183581 IC50 = 14.17 nM 7.85
CHEMBL5180815 IC50 = 15.05 nM 7.82
CHEMBL5173093 IC50 = 18.9 nM 7.72
CHEMBL5203206 IC50 = 31.09 nM 7.51
CHEMBL5200156 IC50 = 41.58 nM 7.38
CHEMBL5204395 IC50 = 45.83 nM 7.34
CHEMBL5194592 IC50 = 57.73 nM 7.24
CHEMBL5188606 IC50 = 65.58 nM 7.18
CHEMBL5192104 IC50 = 67.83 nM 7.17
CHEMBL5170867 IC50 = 1206.0 nM 5.92
CHEMBL5170035 IC50 > 100.0 nM -
CHEMBL5177452 IC50 > 100.0 nM -
CHEMBL5206806 IC50 > 100.0 nM -
CHEMBL5208411 IC50 > 100.0 nM -
CHEMBL5196372 IC50 > 100.0 nM -
CHEMBL5172417 IC50 > 100.0 nM -
CHEMBL5174761 IC50 > 100.0 nM -
CHEMBL5199141 IC50 > 100.0 nM -
CHEMBL5204858 IC50 > 100.0 nM -
CHEMBL5178447 IC50 > 100.0 nM -
CHEMBL3989929 AZELIRAGON IC50 > 3000.0 nM -
CHEMBL5172714 IC50 > 100.0 nM -
CHEMBL5178292 IC50 > 100.0 nM -