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Assay Detail

CHEMBL683542

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Functional
Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, kainate 1 (CHEMBL1918)
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
EC50 5 4.91 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301536 1 5.60
CHEMBL51660 1 5.21
CHEMBL52295 1 4.85
CHEMBL275040 KAINIC ACID 2.0 1 4.79
CHEMBL575060 GLUTAMIC ACID 3.0 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301536 EC50 = 2500.0 nM 5.60
CHEMBL51660 EC50 = 6200.0 nM 5.21
CHEMBL52295 EC50 = 14200.0 nM 4.85
CHEMBL275040 KAINIC ACID EC50 = 16200.0 nM 4.79
CHEMBL575060 GLUTAMIC ACID EC50 = 75000.0 nM 4.12