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Assay Detail

CHEMBL696975

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Binding
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 2 using cell membranes prepared from HEK293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor 2 (CHEMBL4016)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.
Baker SR, Bleakman D, Ezquerra J, Ballyk BA, Deverill M, Ho K, Kamboj RK, Collado I, Domínguez C, Escribano A, Mateo AI, Pedregal C, Rubio A.
Bioorg Med Chem Lett (2000) 10 : 1807 -1810
PubMed 10969973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.23 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.03
CHEMBL51660 1 5.43
CHEMBL299180 1 5.43
CHEMBL275040 KAINIC ACID 2.0 1 4.91
CHEMBL298800 1 4.35
CHEMBL51008 1 -
CHEMBL301536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 940.0 nM 6.03
CHEMBL51660 Ki = 3680.0 nM 5.43
CHEMBL299180 Ki = 3700.0 nM 5.43
CHEMBL275040 KAINIC ACID Ki = 12200.0 nM 4.91
CHEMBL298800 Ki = 44900.0 nM 4.35
CHEMBL51008 Ki = 280900.0 nM -
CHEMBL301536 Ki > 10000.0 nM -