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Assay Detail

CHEMBL3387346

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

Binding
Positive allosteric modulation of AMPA receptor in rat embryonic cortex primary neuronal culture assessed as increase in AMPA-induced membrane depolarization by microplate reader
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Primary neuron
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 9 5.80 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441067 1 6.05
CHEMBL3352932 1 5.82
CHEMBL2441068 1 5.54
CHEMBL3352936 1 -
CHEMBL3352935 1 -
CHEMBL3352934 1 -
CHEMBL3352933 1 -
CHEMBL3352931 1 -
CHEMBL3352930 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441067 EC50 = 900.0 nM 6.05
CHEMBL3352932 EC50 = 1500.0 nM 5.82
CHEMBL2441068 EC50 = 2900.0 nM 5.54
CHEMBL3352936 EC50 - -
CHEMBL3352935 EC50 - -
CHEMBL3352934 EC50 - -
CHEMBL3352933 EC50 - -
CHEMBL3352931 EC50 - -
CHEMBL3352930 EC50 - -