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Assay Detail

CHEMBL803036

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

Binding
Inhibitory activity against serotonin transporter (SERT) labeled with [3H]-citalopram in rat brain striatal membrane.
10
Total Activities
10
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

Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-[2-(diphenylmethoxy)ethyl]-1-(3-phenylpropyl)piperidine analogues.
Dutta AK, Coffey LL, Reith ME.
J Med Chem (1998) 41 : 699 -705
PubMed 9513598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.78 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112928 1 7.12
CHEMBL164303 1 7.07
CHEMBL281594 VANOXERINE 3.0 1 7.06
CHEMBL161437 1 6.74
CHEMBL349023 1 6.71
CHEMBL2112929 1 6.69
CHEMBL350057 1 6.65
CHEMBL2112930 1 6.63
CHEMBL137718 1 6.57
CHEMBL2112927 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112928 IC50 = 75.8 nM 7.12
CHEMBL164303 IC50 = 85.7 nM 7.07
CHEMBL281594 VANOXERINE IC50 = 86.6 nM 7.06
CHEMBL161437 IC50 = 180.4 nM 6.74
CHEMBL349023 IC50 = 194.1 nM 6.71
CHEMBL2112929 IC50 = 205.2 nM 6.69
CHEMBL350057 IC50 = 223.4 nM 6.65
CHEMBL2112930 IC50 = 231.8 nM 6.63
CHEMBL137718 IC50 = 271.2 nM 6.57
CHEMBL2112927 IC50 = 290.8 nM 6.54