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Assay Detail

CHEMBL806548

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

Binding
IC50 value was evaluated using [3H]citalopram (radioligand) on serotonin transporter in rat striatum.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.
Dutta AK, Xu C, Reith ME.
J Med Chem (1998) 41 : 3293 -3297
PubMed 9703474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.43 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 7.06
CHEMBL34032 1 6.70
CHEMBL110530 1 6.23
CHEMBL20648 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE IC50 = 87.0 nM 7.06
CHEMBL34032 IC50 = 198.0 nM 6.70
CHEMBL110530 IC50 = 585.0 nM 6.23
CHEMBL20648 IC50 = 1920.0 nM 5.72