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Assay Detail

CHEMBL4723562

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

Binding
Inhibition of SERT (unknown origin)
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Ye N,Qin W,Tian S,Xu Q,Wold EA,Zhou J,Zhen XC
J Med Chem (2020) 63 : 15187 -15217
PubMed 33111525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.53 9.72
Ki 1 8.80 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL809 SERTRALINE 4.0 1 9.72
CHEMBL549 CITALOPRAM 4.0 1 8.80
CHEMBL41 FLUOXETINE 4.0 1 8.45
CHEMBL814 FLUVOXAMINE 4.0 1 8.42
CHEMBL11 IMIPRAMINE 4.0 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL809 SERTRALINE IC50 = 0.19 nM 9.72
CHEMBL549 CITALOPRAM Ki = 1.6 nM 8.80
CHEMBL41 FLUOXETINE IC50 = 3.58 nM 8.45
CHEMBL814 FLUVOXAMINE IC50 = 3.8 nM 8.42
CHEMBL11 IMIPRAMINE IC50 = 29.0 nM 7.54