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Assay Detail

CHEMBL974566

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

Binding
Inhibition of [14C]glutamate uptake at human EAAT3 expressed in african green monkey COS1 cells
3
Total Activities
3
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 3 (CHEMBL2721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and preliminary pharmacological evaluation of novel derivatives of L-beta-threo-benzylaspartate as inhibitors of the neuronal glutamate transporter EAAT3.
Mavencamp TL, Rhoderick JF, Bridges RJ, Esslinger CS.
Bioorg Med Chem (2008) 16 : 7740 -7748
PubMed 18650095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.22 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790042 1 5.32
CHEMBL1790043 1 5.19
CHEMBL79140 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790042 IC50 = 4800.0 nM 5.32
CHEMBL1790043 IC50 = 6500.0 nM 5.19
CHEMBL79140 IC50 = 7000.0 nM 5.16