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Assay Detail

CHEMBL3607546

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

Binding
Binding affinity to SERT in Sprague-Dawley rat brain synaptosomes assessed as induction of [3H]5-HT release by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine.
Del Bello F, Sakloth F, Partilla JS, Baumann MH, Glennon RA.
Bioorg Med Chem (2015) 23 : 5574 -5579
PubMed 26233799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.75 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43048 MIDOMAFETAMINE 3.0 1 7.21
CHEMBL3603955 1 7.04
CHEMBL3603954 1 6.93
CHEMBL3604010 METHYLONE 2.0 1 6.62
CHEMBL3604009 1 6.46
CHEMBL3603956 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43048 MIDOMAFETAMINE EC50 = 61.0 nM 7.21
CHEMBL3603955 EC50 = 91.0 nM 7.04
CHEMBL3603954 EC50 = 117.0 nM 6.93
CHEMBL3604010 METHYLONE EC50 = 242.0 nM 6.62
CHEMBL3604009 EC50 = 347.0 nM 6.46
CHEMBL3603956 EC50 = 573.0 nM 6.24