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Assay Detail

CHEMBL3097310

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

Binding
Displacement of [3H]paroxetine from SERT in rat cortical membranes after 6 mins by liquid scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor.
Pessoa-Mahana H, González-Lira C, Fierro A, Zapata-Torres G, Pessoa-Mahana CD, Ortiz-Severin J, Iturriaga-Vásquez P, Reyes-Parada M, Silva-Matus P, Saitz-Barría C, Araya-Maturana R.
Bioorg Med Chem (2013) 21 : 7604 -7611
PubMed 24262884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.47 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL549 CITALOPRAM 4.0 1 8.52
CHEMBL3092348 1 7.89
CHEMBL3092343 1 7.85
CHEMBL3092342 1 7.58
CHEMBL3092347 1 7.43
CHEMBL3092346 1 7.41
CHEMBL3092344 1 7.37
CHEMBL3092345 1 7.21
CHEMBL3092350 1 7.06
CHEMBL3092349 1 7.01
CHEMBL3092351 1 6.86
CHEMBL56 8-OH-DPAT 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL549 CITALOPRAM IC50 = 3.0 nM 8.52
CHEMBL3092348 IC50 = 13.0 nM 7.89
CHEMBL3092343 IC50 = 14.0 nM 7.85
CHEMBL3092342 IC50 = 26.0 nM 7.58
CHEMBL3092347 IC50 = 37.0 nM 7.43
CHEMBL3092346 IC50 = 39.0 nM 7.41
CHEMBL3092344 IC50 = 43.0 nM 7.37
CHEMBL3092345 IC50 = 61.0 nM 7.21
CHEMBL3092350 IC50 = 87.0 nM 7.06
CHEMBL3092349 IC50 = 98.0 nM 7.01
CHEMBL3092351 IC50 = 137.0 nM 6.86
CHEMBL56 8-OH-DPAT IC50 - -