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Assay Detail

CHEMBL948896

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

Binding
Inhibition of [3H]5HT uptake at human 5HT transporter expressed in HEK293 cells
30
Total Activities
30
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

1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Whitlock GA, Blagg J, Fish PV.
Bioorg Med Chem Lett (2008) 18 : 596 -599
PubMed 18240382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.71 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402057 1 8.40
CHEMBL401878 1 8.30
CHEMBL404258 1 8.22
CHEMBL256819 1 8.22
CHEMBL401819 1 8.15
CHEMBL402345 1 8.10
CHEMBL247733 1 8.05
CHEMBL403090 1 8.00
CHEMBL258062 1 7.96
CHEMBL438889 1 7.92
CHEMBL401877 1 7.92
CHEMBL404754 1 7.89
CHEMBL256818 1 7.89
CHEMBL257481 1 7.89
CHEMBL403441 1 7.89
CHEMBL404317 1 7.85
CHEMBL258060 1 7.80
CHEMBL272493 1 7.77
CHEMBL403071 1 7.75
CHEMBL257423 1 7.75
CHEMBL255957 1 7.66
CHEMBL258063 1 7.55
CHEMBL256817 1 7.50
CHEMBL258271 1 7.43
CHEMBL256816 1 7.25
CHEMBL407815 1 7.14
CHEMBL257424 1 6.62
CHEMBL402851 1 6.55
CHEMBL256058 1 6.18
CHEMBL256168 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402057 IC50 = 4.0 nM 8.40
CHEMBL401878 IC50 = 5.0 nM 8.30
CHEMBL404258 IC50 = 6.0 nM 8.22
CHEMBL256819 IC50 = 6.0 nM 8.22
CHEMBL401819 IC50 = 7.0 nM 8.15
CHEMBL402345 IC50 = 8.0 nM 8.10
CHEMBL247733 IC50 = 9.0 nM 8.05
CHEMBL403090 IC50 = 10.0 nM 8.00
CHEMBL258062 IC50 = 11.0 nM 7.96
CHEMBL438889 IC50 = 12.0 nM 7.92
CHEMBL401877 IC50 = 12.0 nM 7.92
CHEMBL404754 IC50 = 13.0 nM 7.89
CHEMBL256818 IC50 = 13.0 nM 7.89
CHEMBL257481 IC50 = 13.0 nM 7.89
CHEMBL403441 IC50 = 13.0 nM 7.89
CHEMBL404317 IC50 = 14.0 nM 7.85
CHEMBL258060 IC50 = 16.0 nM 7.80
CHEMBL272493 IC50 = 17.0 nM 7.77
CHEMBL403071 IC50 = 18.0 nM 7.75
CHEMBL257423 IC50 = 18.0 nM 7.75
CHEMBL255957 IC50 = 22.0 nM 7.66
CHEMBL258063 IC50 = 28.0 nM 7.55
CHEMBL256817 IC50 = 32.0 nM 7.50
CHEMBL258271 IC50 = 37.0 nM 7.43
CHEMBL256816 IC50 = 56.0 nM 7.25
CHEMBL407815 IC50 = 73.0 nM 7.14
CHEMBL257424 IC50 = 238.0 nM 6.62
CHEMBL402851 IC50 = 282.0 nM 6.55
CHEMBL256058 IC50 = 660.0 nM 6.18
CHEMBL256168 IC50 - -