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Assay Detail

CHEMBL780513

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

Functional
Evaluated for inhibition of norepinephrine, biogenic amine reuptake in synaptosomal rat brain preparations
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition
Meyer MD, Hancock AA, Tietje K, Sippy kB, Giardina WJ, Kerwin JF
Bioorg Med Chem Lett (1995) 5 : 2287 -2292
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.17 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490 PAROXETINE 4.0 1 6.80
CHEMBL75342 1 6.32
CHEMBL268258 1 6.06
CHEMBL41 FLUOXETINE 4.0 1 5.48
CHEMBL10347 RAUWOLSCINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490 PAROXETINE IC50 = 160.0 nM 6.80
CHEMBL75342 IC50 = 476.0 nM 6.32
CHEMBL268258 IC50 = 865.0 nM 6.06
CHEMBL41 FLUOXETINE IC50 = 3280.0 nM 5.48
CHEMBL10347 RAUWOLSCINE IC50 > 10000.0 nM -