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Assay Detail

CHEMBL669550

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Functional
Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Dorsal root ganglion
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, kainate 1 (CHEMBL2919)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 4 5.36 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301536 1 6.10
CHEMBL51660 1 5.98
CHEMBL275040 KAINIC ACID 2.0 1 4.92
CHEMBL575060 GLUTAMIC ACID 3.0 1 4.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301536 EC50 = 800.0 nM 6.10
CHEMBL51660 EC50 = 1050.0 nM 5.98
CHEMBL275040 KAINIC ACID EC50 = 12000.0 nM 4.92
CHEMBL575060 GLUTAMIC ACID EC50 = 35200.0 nM 4.45