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Assay Detail

CHEMBL1064061

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

Binding
Displacement of [125I]nisoxetine from human NET expressed in HEK293 cells
3
Total Activities
3
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

Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Denhart DJ, Deskus JA, Ditta JL, Gao Q, Dalton King H, Kozlowski ES, Meng Z, LaPaglia MA, Mattson GK, Molski TF, Taber MT, Lodge NJ, Mattson RJ, Macor JE.
Bioorg Med Chem Lett (2009) 19 : 4031 -4033
PubMed 19560923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.52 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234706 1 6.41
CHEMBL552167 1 5.10
CHEMBL196468 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234706 IC50 = 390.0 nM 6.41
CHEMBL552167 IC50 = 7900.0 nM 5.10
CHEMBL196468 IC50 = 9200.0 nM 5.04