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Assay Detail

CHEMBL680698

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

Binding
Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2
8
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Excitatory amino acid transporter 2 (CHEMBL4973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers.
Shimamoto K, Shigeri Y, Yasuda-Kamatani Y, Lebrun B, Yumoto N, Nakajima T.
Bioorg Med Chem Lett (2000) 10 : 2407 -2410
PubMed 11078189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.34 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790042 1 5.89
CHEMBL1790044 1 5.70
CHEMBL1790043 1 5.66
CHEMBL79140 4 5.42
CHEMBL475341 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790042 IC50 = 1300.0 nM 5.89
CHEMBL1790044 IC50 = 2000.0 nM 5.70
CHEMBL1790043 IC50 = 2200.0 nM 5.66
CHEMBL79140 IC50 = 3800.0 nM 5.42
CHEMBL475341 IC50 = 7000.0 nM 5.16
CHEMBL79140 IC50 = 64000.0 nM 4.19
CHEMBL79140 IC50 = 221000.0 nM -
CHEMBL79140 IC50 = 164000.0 nM -