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Assay Detail

CHEMBL3387343

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

Binding
Binding affinity to GluA2-LBD-L483Y-N754S complex (unknown origin) by isothermal titration calorimetry
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Positive allosteric modulators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors belonging to 4-cyclopropyl-3,4-dihydro-2h-1,2,4-pyridothiadiazine dioxides and diversely chloro-substituted 4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides.
Francotte P, Nørholm AB, Deva T, Olsen L, Frydenvang K, Goffin E, Fraikin P, de Tullio P, Challal S, Thomas JY, Iop F, Louis C, Botez-Pop I, Lestage P, Danober L, Kastrup JS, Pirotte B.
J Med Chem (2014) 57 : 9539 -9553
PubMed 25375781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.57 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441067 1 6.46
CHEMBL411612 1 5.25
CHEMBL103741 1 5.01
CHEMBL99732 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441067 Kd = 350.0 nM 6.46
CHEMBL411612 Kd = 5600.0 nM 5.25
CHEMBL103741 Kd = 9800.0 nM 5.01
CHEMBL99732 Kd = 1200000.0 nM -