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Assay Detail

CHEMBL697889

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Binding
Binding affinity was determined against ionotropic glutamate receptor AMPA in rat brain synaptic membranes using [3H]AMPA as radioligand
ChEMBL ↗
103
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
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 103 5.62 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294781 — — 2 7.70
CHEMBL222519 NBQX — 2 7.28
CHEMBL293206 — — 2 7.20
CHEMBL331547 — — 2 6.96
CHEMBL122054 — — 2 6.82
CHEMBL121771 — — 2 6.78
CHEMBL155265 DNQX — 2 6.70
CHEMBL13260 YM-90K — 2 6.70
CHEMBL122313 — — 2 6.55
CHEMBL432224 — — 2 6.55
CHEMBL333463 — — 2 6.54
CHEMBL122082 — — 2 6.27
CHEMBL330795 — — 1 6.22
CHEMBL126006 — — 2 6.13
CHEMBL331789 — — 2 5.96
CHEMBL124607 — — 2 5.89
CHEMBL121888 — — 2 5.89
CHEMBL125054 — — 2 5.87
CHEMBL341228 — — 2 5.73
CHEMBL332585 — — 2 5.72
CHEMBL122997 — — 2 5.66
CHEMBL125536 — — 2 5.60
CHEMBL125159 — — 2 5.55
CHEMBL123259 — — 2 5.55
CHEMBL123766 — — 2 5.46
CHEMBL126035 — — 2 5.37
CHEMBL123323 — — 2 5.24
CHEMBL123087 — — 2 5.19
CHEMBL333116 — — 2 5.05
CHEMBL125484 — — 2 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294781 — IC50 = 20.0 nM 7.70
CHEMBL294781 — IC50 = 20.0 nM 7.70
CHEMBL222519 NBQX IC50 = 52.0 nM 7.28
CHEMBL222519 NBQX IC50 = 52.0 nM 7.28
CHEMBL293206 — IC50 = 63.0 nM 7.20
CHEMBL293206 — IC50 = 63.0 nM 7.20
CHEMBL331547 — IC50 = 110.0 nM 6.96
CHEMBL331547 — IC50 = 110.0 nM 6.96
CHEMBL122054 — IC50 = 153.0 nM 6.82
CHEMBL122054 — IC50 = 153.0 nM 6.82
CHEMBL121771 — IC50 = 166.0 nM 6.78
CHEMBL121771 — IC50 = 166.0 nM 6.78
CHEMBL13260 YM-90K IC50 = 200.0 nM 6.70
CHEMBL13260 YM-90K IC50 = 200.0 nM 6.70
CHEMBL155265 DNQX IC50 = 200.0 nM 6.70
CHEMBL155265 DNQX IC50 = 200.0 nM 6.70
CHEMBL432224 — IC50 = 280.0 nM 6.55
CHEMBL432224 — IC50 = 280.0 nM 6.55
CHEMBL122313 — IC50 = 280.0 nM 6.55
CHEMBL122313 — IC50 = 280.0 nM 6.55
CHEMBL333463 — IC50 = 290.0 nM 6.54
CHEMBL333463 — IC50 = 290.0 nM 6.54
CHEMBL122082 — IC50 = 540.0 nM 6.27
CHEMBL122082 — IC50 = 540.0 nM 6.27
CHEMBL330795 — IC50 = 600.0 nM 6.22
CHEMBL126006 — IC50 = 740.0 nM 6.13
CHEMBL126006 — IC50 = 740.0 nM 6.13
CHEMBL331789 — IC50 = 1100.0 nM 5.96
CHEMBL331789 — IC50 = 1100.0 nM 5.96
CHEMBL124607 — IC50 = 1300.0 nM 5.89
CHEMBL121888 — IC50 = 1300.0 nM 5.89
CHEMBL121888 — IC50 = 1300.0 nM 5.89
CHEMBL124607 — IC50 = 1300.0 nM 5.89
CHEMBL125054 — IC50 = 1360.0 nM 5.87
CHEMBL125054 — IC50 = 1360.0 nM 5.87
CHEMBL341228 — IC50 = 1860.0 nM 5.73
CHEMBL341228 — IC50 = 1860.0 nM 5.73
CHEMBL332585 — IC50 = 1900.0 nM 5.72
CHEMBL332585 — IC50 = 1900.0 nM 5.72
CHEMBL122997 — IC50 = 2200.0 nM 5.66
CHEMBL122997 — IC50 = 2200.0 nM 5.66
CHEMBL125536 — IC50 = 2500.0 nM 5.60
CHEMBL125536 — IC50 = 2500.0 nM 5.60
CHEMBL125159 — IC50 = 2840.0 nM 5.55
CHEMBL125159 — IC50 = 2840.0 nM 5.55
CHEMBL123259 — IC50 = 2800.0 nM 5.55
CHEMBL123259 — IC50 = 2800.0 nM 5.55
CHEMBL123766 — IC50 = 3500.0 nM 5.46
CHEMBL123766 — IC50 = 3500.0 nM 5.46
CHEMBL126035 — IC50 = 4300.0 nM 5.37