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Assay Detail

CHEMBL873243

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

Binding
Activity towards Serotonin transporter was determined by the ability to inhibit [3H]5-HT uptake in rat synaptosomes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological evaluation of ring-methylated derivatives of 3,4-(methylenedioxy)amphetamine (MDA).
Parker MA, Marona-Lewicka D, Kurrasch D, Shulgin AT, Nichols DE.
J Med Chem (1998) 41 : 1001 -1005
PubMed 9526575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.82 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6467 4-METHYLTHIOAMPHETAMINE 1 7.13
CHEMBL6842 1 7.09
CHEMBL6368 p-IODOAMPHETAMINE 1 7.09
CHEMBL6391 1 7.03
CHEMBL6330 1 6.97
CHEMBL6731 TENAMFETAMINE 2.0 1 6.32
CHEMBL6376 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6467 4-METHYLTHIOAMPHETAMINE IC50 = 74.0 nM 7.13
CHEMBL6842 IC50 = 82.0 nM 7.09
CHEMBL6368 p-IODOAMPHETAMINE IC50 = 82.0 nM 7.09
CHEMBL6391 IC50 = 93.0 nM 7.03
CHEMBL6330 IC50 = 107.0 nM 6.97
CHEMBL6731 TENAMFETAMINE IC50 = 478.0 nM 6.32
CHEMBL6376 IC50 = 783.0 nM 6.11