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Assay Detail

CHEMBL779502

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

Functional
Inhibition of NMDA-induced depolarizations in rat cortical wedges.
14
Total Activities
14
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

Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
Fray MJ, Bull DJ, Carr CL, Gautier EC, Mowbray CE, Stobie A.
J Med Chem (2001) 44 : 1951 -1962
PubMed 11384240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.29 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303539 1 7.06
CHEMBL293831 1 7.05
CHEMBL450325 1 7.05
CHEMBL61364 1 6.82
CHEMBL299281 1 6.54
CHEMBL59894 1 6.46
CHEMBL61720 1 6.46
CHEMBL62164 1 6.38
CHEMBL58446 1 6.19
CHEMBL289832 LICOSTINEL 2.0 1 5.96
CHEMBL58182 1 5.96
CHEMBL304436 1 5.89
CHEMBL59251 1 5.39
CHEMBL283819 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303539 EC50 = 88.0 nM 7.06
CHEMBL293831 EC50 = 90.0 nM 7.05
CHEMBL450325 EC50 = 90.0 nM 7.05
CHEMBL61364 EC50 = 150.0 nM 6.82
CHEMBL299281 EC50 = 290.0 nM 6.54
CHEMBL59894 EC50 = 350.0 nM 6.46
CHEMBL61720 EC50 = 350.0 nM 6.46
CHEMBL62164 EC50 = 420.0 nM 6.38
CHEMBL58446 EC50 = 640.0 nM 6.19
CHEMBL289832 LICOSTINEL EC50 = 1100.0 nM 5.96
CHEMBL58182 EC50 = 1090.0 nM 5.96
CHEMBL304436 EC50 = 1300.0 nM 5.89
CHEMBL59251 EC50 = 4100.0 nM 5.39
CHEMBL283819 EC50 = 16000.0 nM 4.80