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Assay Detail

CHEMBL1013074

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

Binding
Displacement of [3H]SYM2081 from rat cloned iGluR6
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, kainate 2 (CHEMBL3607)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 4 4.92 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279561 DIHYDROKAINATE 2 4.92
CHEMBL480169 1 -
CHEMBL79140 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279561 DIHYDROKAINATE Ki = 12022.64 nM 4.92
CHEMBL279561 DIHYDROKAINATE Ki = 12300.0 nM 4.91
CHEMBL480169 Ki > 100000.0 nM -
CHEMBL79140 Ki - -