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Assay Detail

CHEMBL1074040

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

Binding
Displacement of [I125]RTI-55 from human SERT transfected in human HEK293 cells
23
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 hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.
Marcin LR, Mattson RJ, Gao Q, Wu D, Molski TF, Mattson GK, Lodge NJ.
Bioorg Med Chem Lett (2010) 20 : 1027 -1030
PubMed 20034793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.30 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552167 1 9.89
CHEMBL196468 1 9.44
CHEMBL609908 3 9.38
CHEMBL234706 1 9.14
CHEMBL180630 1 8.70
CHEMBL599684 1 8.68
CHEMBL590487 1 8.60
CHEMBL41 FLUOXETINE 4.0 1 8.60
CHEMBL606244 1 8.41
CHEMBL592776 1 8.40
CHEMBL598042 1 8.24
CHEMBL600890 1 8.15
CHEMBL605535 1 8.12
CHEMBL600263 1 8.09
CHEMBL601503 1 7.77
CHEMBL596615 1 7.77
CHEMBL596613 1 7.75
CHEMBL591829 1 7.34
CHEMBL596614 1 7.12
CHEMBL591830 1 7.10
CHEMBL597031 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552167 IC50 = 0.13 nM 9.89
CHEMBL196468 IC50 = 0.36 nM 9.44
CHEMBL609908 IC50 = 0.42 nM 9.38
CHEMBL234706 IC50 = 0.72 nM 9.14
CHEMBL609908 IC50 = 1.1 nM 8.96
CHEMBL180630 IC50 = 2.0 nM 8.70
CHEMBL599684 IC50 = 2.1 nM 8.68
CHEMBL590487 IC50 = 2.5 nM 8.60
CHEMBL41 FLUOXETINE IC50 = 2.5 nM 8.60
CHEMBL606244 IC50 = 3.9 nM 8.41
CHEMBL592776 IC50 = 4.0 nM 8.40
CHEMBL609908 IC50 = 4.2 nM 8.38
CHEMBL598042 IC50 = 5.7 nM 8.24
CHEMBL600890 IC50 = 7.0 nM 8.15
CHEMBL605535 IC50 = 7.6 nM 8.12
CHEMBL600263 IC50 = 8.1 nM 8.09
CHEMBL601503 IC50 = 17.0 nM 7.77
CHEMBL596615 IC50 = 17.0 nM 7.77
CHEMBL596613 IC50 = 18.0 nM 7.75
CHEMBL591829 IC50 = 46.0 nM 7.34
CHEMBL596614 IC50 = 76.0 nM 7.12
CHEMBL591830 IC50 = 80.0 nM 7.10
CHEMBL597031 IC50 = 120.0 nM 6.92