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Assay Detail

CHEMBL1011735

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

Binding
Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells
8
Total Activities
8
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

Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.
Cashman JR, Voelker T, Johnson R, Janowsky A.
Bioorg Med Chem (2009) 17 : 337 -343
PubMed 19014888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.35 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41 FLUOXETINE 4.0 1 8.96
CHEMBL446084 1 7.58
CHEMBL465123 SEPROXETINE 2.0 1 7.30
CHEMBL499461 1 7.19
CHEMBL370805 COCAINE 4.0 1 6.56
CHEMBL454507 1 6.52
CHEMBL313041 1 -
CHEMBL480988 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41 FLUOXETINE Ki = 1.1 nM 8.96
CHEMBL446084 Ki = 26.0 nM 7.58
CHEMBL465123 SEPROXETINE Ki = 50.0 nM 7.30
CHEMBL499461 Ki = 65.0 nM 7.19
CHEMBL370805 COCAINE Ki = 276.0 nM 6.56
CHEMBL454507 Ki = 300.0 nM 6.52
CHEMBL313041 Ki > 100000.0 nM -
CHEMBL480988 Ki > 100000.0 nM -