Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5137236

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

Binding
Displacement of [3H]-citalopram from SERT in Sprague-Dawley rat brainstem incubated for 60 mins by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.
Camacho-Hernandez GA, Casiraghi A, Rudin D, Luethi D, Ku TC, Guthrie DA, Straniero V, Valoti E, Schütz GJ, Sitte HH, Newman AH.
RSC Med Chem (2021) 12 : 1174 -1186
PubMed 34355183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.49 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196760 1 7.80
CHEMBL5188712 1 6.11
CHEMBL299233 TALOPRAM 2.0 1 6.10
CHEMBL5176356 1 5.94
CHEMBL295467 NISOXETINE 2.0 1 -
CHEMBL5170876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196760 Ki = 16.0 nM 7.80
CHEMBL5188712 Ki = 785.0 nM 6.11
CHEMBL299233 TALOPRAM Ki = 795.0 nM 6.10
CHEMBL5176356 Ki = 1144.0 nM 5.94
CHEMBL295467 NISOXETINE Ki - -
CHEMBL5170876 Ki > 10000.0 nM -