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Assay Detail

CHEMBL781144

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

Functional
Concentration of compound that inhibits by 50% LDH released by 24 hr application of 500 uM kainate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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 10 5.15 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 5.70
CHEMBL293206 1 5.40
CHEMBL122054 1 5.16
CHEMBL121771 1 5.16
CHEMBL331547 1 5.16
CHEMBL333463 1 5.05
CHEMBL432224 1 4.96
CHEMBL122082 1 4.58
CHEMBL121886 1 -
CHEMBL125484 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX IC50 = 2000.0 nM 5.70
CHEMBL293206 IC50 = 4000.0 nM 5.40
CHEMBL122054 IC50 = 7000.0 nM 5.16
CHEMBL121771 IC50 = 7000.0 nM 5.16
CHEMBL331547 IC50 = 7000.0 nM 5.16
CHEMBL333463 IC50 = 9000.0 nM 5.05
CHEMBL432224 IC50 = 11000.0 nM 4.96
CHEMBL122082 IC50 = 26000.0 nM 4.58
CHEMBL121886 IC50 > 30000.0 nM -
CHEMBL125484 IC50 > 30000.0 nM -