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Assay Detail

CHEMBL5382774

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

Binding
Inhibition of human EAAT1 transfected in African green monkey COS-1 cells assessed as reduction in [14C]glutamate uptake
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Excitatory amino acid transporter 1 (CHEMBL3085)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Medicinal Chemistry Perspective on Excitatory Amino Acid Transporter 2 Dysfunction in Neurodegenerative Diseases.
Fontana IC, Souza DG, Souza DO, Gee A, Zimmer ER, Bongarzone S.
J Med Chem (2023) 66 : 2330 -2346
PubMed 36787643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.30 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1257519 1 7.66
CHEMBL5423219 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1257519 IC50 = 22.0 nM 7.66
CHEMBL5423219 IC50 = 116.0 nM 6.94