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Assay Detail

CHEMBL702016

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

Functional
Antagonistic activity against Ionotropic glutamate receptor AMPA induced LDH release in cultured rat cortical neurons after 24 hr 100 uM AMPA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant activity.
Bigge CF, Malone TC, Boxer PA, Nelson CB, Ortwine DF, Schelkun RM, Retz DM, Lescosky LJ, Borosky SA, Vartanian MG.
J Med Chem (1995) 38 : 3720 -3740
PubMed 7562904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.13 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293206 1 5.60
CHEMBL222519 NBQX 1 5.52
CHEMBL331547 1 5.30
CHEMBL122054 1 5.22
CHEMBL121771 1 5.22
CHEMBL432224 1 5.10
CHEMBL122313 1 4.82
CHEMBL333463 1 4.75
CHEMBL122082 1 4.60
CHEMBL125484 1 -
CHEMBL121886 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293206 IC50 = 2500.0 nM 5.60
CHEMBL222519 NBQX IC50 = 3000.0 nM 5.52
CHEMBL331547 IC50 = 5000.0 nM 5.30
CHEMBL122054 IC50 = 6000.0 nM 5.22
CHEMBL121771 IC50 = 6000.0 nM 5.22
CHEMBL432224 IC50 = 8000.0 nM 5.10
CHEMBL122313 IC50 = 15000.0 nM 4.82
CHEMBL333463 IC50 = 18000.0 nM 4.75
CHEMBL122082 IC50 = 25000.0 nM 4.60
CHEMBL125484 IC50 > 30000.0 nM -
CHEMBL121886 IC50 > 30000.0 nM -