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Assay Detail

CHEMBL1013071

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

Binding
Displacement of CGP-39653 from KA receptor in rat synaptosomes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
Sagot E, Jensen AA, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Assaf Z, Aboab B, Bolte J, Gefflaut T, Bunch L.
J Med Chem (2008) 51 : 4085 -4092
PubMed 18578477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.22 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279561 DIHYDROKAINATE 1 5.22
CHEMBL480169 1 -
CHEMBL79140 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279561 DIHYDROKAINATE IC50 = 6000.0 nM 5.22
CHEMBL480169 IC50 > 100000.0 nM -
CHEMBL79140 IC50 = 550000.0 nM -