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Assay Detail

CHEMBL2317645

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

Binding
Inhibition of human EAAT2 expressed in HEK293 cells by [3H]-D-Asp uptake assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
Assaf Z, Larsen AP, Venskutonytė R, Han L, Abrahamsen B, Nielsen B, Gajhede M, Kastrup JS, Jensen AA, Pickering DS, Frydenvang K, Gefflaut T, Bunch L.
J Med Chem (2013) 56 : 1614 -1628
PubMed 23414088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.62 4.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2312682 1 4.62
CHEMBL2312686 1 -
CHEMBL2312685 1 -
CHEMBL2312684 1 -
CHEMBL2312683 1 -
CHEMBL2312681 1 -
CHEMBL2312403 1 -
CHEMBL2312402 1 -
CHEMBL2312400 1 -
CHEMBL2312399 1 -
CHEMBL2312397 1 -
CHEMBL2312396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2312682 IC50 = 24000.0 nM 4.62
CHEMBL2312686 IC50 > 300000.0 nM -
CHEMBL2312685 IC50 > 1000000.0 nM -
CHEMBL2312684 IC50 > 1000000.0 nM -
CHEMBL2312683 IC50 = 700000.0 nM -
CHEMBL2312681 IC50 = 300000.0 nM -
CHEMBL2312403 IC50 = 1000000.0 nM -
CHEMBL2312402 IC50 = 300000.0 nM -
CHEMBL2312400 IC50 > 300000.0 nM -
CHEMBL2312399 IC50 > 300000.0 nM -
CHEMBL2312397 IC50 > 300000.0 nM -
CHEMBL2312396 IC50 > 300000.0 nM -