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Assay Detail

CHEMBL902423

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

Binding
Inhibition of [3H]NA from human NET expressed in HEK293 cells
19
Total Activities
19
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 Intermediate

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.
Fish PV, Fray MJ, Stobie A, Wakenhut F, Whitlock GA.
Bioorg Med Chem Lett (2007) 17 : 2022 -2025
PubMed 17267217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.97 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391806 1 8.52
CHEMBL247340 1 8.40
CHEMBL440230 1 8.30
CHEMBL245880 1 8.30
CHEMBL247341 1 8.30
CHEMBL397392 1 8.15
CHEMBL247733 1 8.15
CHEMBL392016 1 8.10
CHEMBL442272 1 8.05
CHEMBL246920 1 8.05
CHEMBL247538 1 7.96
CHEMBL245482 1 7.92
CHEMBL245687 1 7.92
CHEMBL245492 1 7.89
CHEMBL395931 1 7.82
CHEMBL1175 DULOXETINE 4.0 1 7.72
CHEMBL391143 1 7.70
CHEMBL246519 1 7.40
CHEMBL395408 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391806 IC50 = 3.0 nM 8.52
CHEMBL247340 IC50 = 4.0 nM 8.40
CHEMBL440230 IC50 = 5.0 nM 8.30
CHEMBL245880 IC50 = 5.0 nM 8.30
CHEMBL247341 IC50 = 5.0 nM 8.30
CHEMBL397392 IC50 = 7.0 nM 8.15
CHEMBL247733 IC50 = 7.0 nM 8.15
CHEMBL392016 IC50 = 8.0 nM 8.10
CHEMBL442272 IC50 = 9.0 nM 8.05
CHEMBL246920 IC50 = 9.0 nM 8.05
CHEMBL247538 IC50 = 11.0 nM 7.96
CHEMBL245482 IC50 = 12.0 nM 7.92
CHEMBL245687 IC50 = 12.0 nM 7.92
CHEMBL245492 IC50 = 13.0 nM 7.89
CHEMBL395931 IC50 = 15.0 nM 7.82
CHEMBL1175 DULOXETINE IC50 = 19.0 nM 7.72
CHEMBL391143 IC50 = 20.0 nM 7.70
CHEMBL246519 IC50 = 40.0 nM 7.40
CHEMBL395408 IC50 = 144.0 nM 6.84