Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1013069

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

Binding
Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells
22
Total Activities
11
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 3 (CHEMBL2721)
Type SINGLE PROTEIN
Organism Homo sapiens

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 22 5.67 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 2 7.29
CHEMBL446256 2 6.00
CHEMBL480169 2 5.52
CHEMBL518313 2 5.52
CHEMBL482080 2 5.52
CHEMBL500448 2 5.52
CHEMBL494878 2 -
CHEMBL500042 2 -
CHEMBL479804 2 -
CHEMBL482081 2 -
CHEMBL479797 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 51.0 nM 7.29
CHEMBL446256 Ki = 1000.0 nM 6.00
CHEMBL480169 Ki = 3000.0 nM 5.52
CHEMBL518313 Ki = 3000.0 nM 5.52
CHEMBL500448 Ki = 3000.0 nM 5.52
CHEMBL482080 Ki = 3000.0 nM 5.52
CHEMBL575060 GLUTAMIC ACID Ki = 50118.72 nM 4.30
CHEMBL480169 Ki = 3162277.66 nM -
CHEMBL518313 Ki = 3162277.66 nM -
CHEMBL494878 Ki > 3000.0 nM -
CHEMBL494878 Ki > 3162277.66 nM -
CHEMBL500042 Ki > 3000.0 nM -
CHEMBL500042 Ki > 3162277.66 nM -
CHEMBL479804 Ki > 3000.0 nM -
CHEMBL479804 Ki > 3162277.66 nM -
CHEMBL482080 Ki > 3162277.66 nM -
CHEMBL482081 Ki > 3000.0 nM -
CHEMBL482081 Ki > 3162277.66 nM -
CHEMBL479797 Ki > 3000.0 nM -
CHEMBL479797 Ki > 3162277.66 nM -
CHEMBL446256 Ki = 3162277.66 nM -
CHEMBL500448 Ki = 3162277.66 nM -