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Assay Detail

CHEMBL869834

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

Binding
Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells
23
Total Activities
23
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 Expert

Target

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

Publication

N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
Jonathan Fray M, Bish G, Brown AD, Fish PV, Stobie A, Wakenhut F, Whitlock GA.
Bioorg Med Chem Lett (2006) 16 : 4345 -4348
PubMed 16750359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.72 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386223 1 8.40
CHEMBL213287 1 8.27
CHEMBL1175 DULOXETINE 4.0 1 8.22
CHEMBL214240 1 8.03
CHEMBL210026 1 8.02
CHEMBL210027 1 8.00
CHEMBL210028 1 7.92
CHEMBL375131 1 7.89
CHEMBL386224 1 7.89
CHEMBL214273 1 7.89
CHEMBL214237 1 7.85
CHEMBL378418 1 7.82
CHEMBL210126 1 7.80
CHEMBL41 FLUOXETINE 4.0 1 7.80
CHEMBL214335 1 7.75
CHEMBL213754 1 7.66
CHEMBL212763 1 7.60
CHEMBL379205 1 7.42
CHEMBL213035 1 7.06
CHEMBL379536 1 6.68
CHEMBL14370 REBOXETINE 4.0 1 6.23
CHEMBL209969 1 -
CHEMBL213632 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386223 IC50 = 4.0 nM 8.40
CHEMBL213287 IC50 = 5.4 nM 8.27
CHEMBL1175 DULOXETINE IC50 = 6.0 nM 8.22
CHEMBL214240 IC50 = 9.4 nM 8.03
CHEMBL210026 IC50 = 9.5 nM 8.02
CHEMBL210027 IC50 = 10.0 nM 8.00
CHEMBL210028 IC50 = 12.0 nM 7.92
CHEMBL375131 IC50 = 13.0 nM 7.89
CHEMBL386224 IC50 = 13.0 nM 7.89
CHEMBL214273 IC50 = 13.0 nM 7.89
CHEMBL214237 IC50 = 14.0 nM 7.85
CHEMBL378418 IC50 = 15.0 nM 7.82
CHEMBL210126 IC50 = 16.0 nM 7.80
CHEMBL41 FLUOXETINE IC50 = 16.0 nM 7.80
CHEMBL214335 IC50 = 18.0 nM 7.75
CHEMBL213754 IC50 = 22.0 nM 7.66
CHEMBL212763 IC50 = 25.0 nM 7.60
CHEMBL379205 IC50 = 38.0 nM 7.42
CHEMBL213035 IC50 = 87.0 nM 7.06
CHEMBL379536 IC50 = 210.0 nM 6.68
CHEMBL14370 REBOXETINE IC50 = 590.0 nM 6.23
CHEMBL209969 IC50 > 400.0 nM -
CHEMBL213632 IC50 > 400.0 nM -