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Assay Detail

CHEMBL807133

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

Binding
Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand
10
Total Activities
9
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

High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo.
Ghorai SK, Cook C, Davis M, Venkataraman SK, George C, Beardsley PM, Reith ME, Dutta AK.
J Med Chem (2003) 46 : 1220 -1228
PubMed 12646032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.79 6.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 6.88
CHEMBL370805 COCAINE 4.0 1 6.13
CHEMBL20432 1 5.96
CHEMBL21115 2 5.74
CHEMBL20648 1 5.72
CHEMBL20127 1 5.48
CHEMBL21213 1 5.44
CHEMBL20710 1 5.11
CHEMBL20362 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE IC50 = 132.0 nM 6.88
CHEMBL370805 COCAINE IC50 = 737.0 nM 6.13
CHEMBL20432 IC50 = 1110.0 nM 5.96
CHEMBL21115 IC50 = 1830.0 nM 5.74
CHEMBL20648 IC50 = 1920.0 nM 5.72
CHEMBL21115 IC50 = 2360.0 nM 5.63
CHEMBL20127 IC50 = 3310.0 nM 5.48
CHEMBL21213 IC50 = 3600.0 nM 5.44
CHEMBL20710 IC50 = 7750.0 nM 5.11
CHEMBL20362 IC50 = 178000.0 nM -