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Assay Detail

CHEMBL4041111

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

Binding
Inhibition of SERT expressed in rat brain synaptosomes assessed as decrease in incorporation of [3H]serotonin measured after 15 mins by scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
Bucki A, Marcinkowska M, Śniecikowska J, Więckowski K, Pawłowski M, Głuch-Lutwin M, Gryboś A, Siwek A, Pytka K, Jastrzębska-Więsek M, Partyka A, Wesołowska A, Mierzejewski P, Kołaczkowski M.
J Med Chem (2017) 60 : 7483 -7501
PubMed 28763213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.78 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095555 1 8.00
CHEMBL4066532 1 7.96
CHEMBL4088249 1 7.92
CHEMBL4104622 1 7.80
CHEMBL4065568 1 7.77
CHEMBL11 IMIPRAMINE 4.0 1 7.21
CHEMBL4075673 1 -
CHEMBL4080369 1 -
CHEMBL4104216 1 -
CHEMBL4095979 1 -
CHEMBL4085802 1 -
CHEMBL1112 ARIPIPRAZOLE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095555 IC50 = 10.0 nM 8.00
CHEMBL4066532 IC50 = 11.0 nM 7.96
CHEMBL4088249 IC50 = 12.0 nM 7.92
CHEMBL4104622 IC50 = 16.0 nM 7.80
CHEMBL4065568 IC50 = 17.0 nM 7.77
CHEMBL11 IMIPRAMINE IC50 = 61.0 nM 7.21
CHEMBL4075673 IC50 - -
CHEMBL4080369 IC50 - -
CHEMBL4104216 IC50 - -
CHEMBL4095979 IC50 - -
CHEMBL4085802 IC50 - -
CHEMBL1112 ARIPIPRAZOLE IC50 - -