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Assay Detail

CHEMBL832636

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

Binding
Inhibition of [3H]citalopram binding to human serotonin transporter (hSERT)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters.
Meltzer PC, Pham-Huu DP, Madras BK.
Bioorg Med Chem Lett (2004) 14 : 6007 -6010
PubMed 15546718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.45 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185169 1 6.16
CHEMBL365092 1 5.89
CHEMBL169429 1 5.72
CHEMBL186242 1 5.44
CHEMBL187211 1 5.32
CHEMBL364146 1 5.06
CHEMBL363510 1 4.55
CHEMBL186501 1 -
CHEMBL186447 1 -
CHEMBL187695 1 -
CHEMBL184867 1 -
CHEMBL361493 1 -
CHEMBL185792 1 -
CHEMBL186488 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185169 IC50 = 700.0 nM 6.16
CHEMBL365092 IC50 = 1300.0 nM 5.89
CHEMBL169429 IC50 = 1900.0 nM 5.72
CHEMBL186242 IC50 = 3600.0 nM 5.44
CHEMBL187211 IC50 = 4800.0 nM 5.32
CHEMBL364146 IC50 = 8700.0 nM 5.06
CHEMBL363510 IC50 = 28000.0 nM 4.55
CHEMBL186501 IC50 > 10000.0 nM -
CHEMBL186447 IC50 > 10000.0 nM -
CHEMBL187695 IC50 > 25000.0 nM -
CHEMBL184867 IC50 > 10000.0 nM -
CHEMBL361493 IC50 > 50000.0 nM -
CHEMBL185792 IC50 > 60000.0 nM -
CHEMBL186488 IC50 > 30000.0 nM -