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Assay Detail

CHEMBL1647124

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

Binding
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
32
Total Activities
31
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 pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Shao L, Wang F, Malcolm SC, Ma J, Hewitt MC, Campbell UC, Bush LR, Spicer NA, Engel SR, Saraswat LD, Hardy LW, Koch P, Schreiber R, Spear KL, Varney MA.
Bioorg Med Chem (2011) 19 : 663 -676
PubMed 21093273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.42 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642904 1 9.00
CHEMBL1642912 1 9.00
CHEMBL1642902 1 8.70
CHEMBL809 SERTRALINE 4.0 1 8.52
CHEMBL1642900 1 8.52
CHEMBL41 FLUOXETINE 4.0 1 8.28
CHEMBL1642894 1 8.22
CHEMBL1642898 1 8.15
CHEMBL1642896 1 8.10
CHEMBL1642906 1 8.05
CHEMBL592374 AMITIFADINE 2.0 2 7.92
CHEMBL1642909 1 7.80
CHEMBL1642903 1 7.72
CHEMBL1642901 1 7.70
CHEMBL1642908 1 7.64
CHEMBL1642914 1 7.38
CHEMBL1642890 1 7.34
CHEMBL1642907 1 7.27
CHEMBL1642905 1 7.21
CHEMBL1642913 1 7.10
CHEMBL1642892 1 7.08
CHEMBL1642893 1 6.97
CHEMBL1642899 1 6.97
CHEMBL1642897 1 6.97
CHEMBL1642895 1 6.90
CHEMBL1642910 1 6.51
CHEMBL1642911 1 6.01
CHEMBL1642891 1 5.74
CHEMBL1642915 1 5.71
CHEMBL1642916 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642912 IC50 = 1.0 nM 9.00
CHEMBL1642904 IC50 = 1.0 nM 9.00
CHEMBL1642902 IC50 = 2.0 nM 8.70
CHEMBL809 SERTRALINE IC50 = 3.0 nM 8.52
CHEMBL1642900 IC50 = 3.0 nM 8.52
CHEMBL41 FLUOXETINE IC50 = 5.2 nM 8.28
CHEMBL1642894 IC50 = 6.0 nM 8.22
CHEMBL1642898 IC50 = 7.0 nM 8.15
CHEMBL1642896 IC50 = 8.0 nM 8.10
CHEMBL1642906 IC50 = 9.0 nM 8.05
CHEMBL592374 AMITIFADINE IC50 = 12.0 nM 7.92
CHEMBL592374 AMITIFADINE IC50 = 14.0 nM 7.85
CHEMBL1642909 IC50 = 16.0 nM 7.80
CHEMBL1642903 IC50 = 19.0 nM 7.72
CHEMBL1642901 IC50 = 20.0 nM 7.70
CHEMBL1642908 IC50 = 23.0 nM 7.64
CHEMBL1642914 IC50 = 42.0 nM 7.38
CHEMBL1642890 IC50 = 46.0 nM 7.34
CHEMBL1642907 IC50 = 54.0 nM 7.27
CHEMBL1642905 IC50 = 61.0 nM 7.21
CHEMBL1642913 IC50 = 79.0 nM 7.10
CHEMBL1642892 IC50 = 84.0 nM 7.08
CHEMBL1642899 IC50 = 108.0 nM 6.97
CHEMBL1642897 IC50 = 107.0 nM 6.97
CHEMBL1642893 IC50 = 108.0 nM 6.97
CHEMBL1642895 IC50 = 125.0 nM 6.90
CHEMBL1642910 IC50 = 311.0 nM 6.51
CHEMBL1642911 IC50 = 970.0 nM 6.01
CHEMBL1642891 IC50 = 1830.0 nM 5.74
CHEMBL1642915 IC50 = 1956.0 nM 5.71
CHEMBL1642916 IC50 = 2495.0 nM 5.60
CHEMBL1642917 IC50 = 2827.0 nM 5.55