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Assay Detail

CHEMBL752331

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

Binding
Affinity for N-methyl-D-aspartate glutamate receptor 1 in rat brain synaptic membranes, using [3H]glycine as radioligand
ChEMBL ↗
64
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗
Type SINGLE PROTEIN
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 64 5.66 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293206 — — 2 6.43
CHEMBL126006 — — 2 6.21
CHEMBL331547 — — 2 6.07
CHEMBL122054 — — 2 6.03
CHEMBL122313 — — 2 6.03
CHEMBL123766 — — 2 6.00
CHEMBL122997 — — 2 5.89
CHEMBL432224 — — 2 5.89
CHEMBL121771 — — 2 5.85
CHEMBL125054 — — 2 5.85
CHEMBL125159 — — 2 5.40
CHEMBL341228 — — 2 5.37
CHEMBL333463 — — 2 5.31
CHEMBL122082 — — 2 5.30
CHEMBL123259 — — 2 4.70
CHEMBL330790 — — 2 4.30
CHEMBL123087 — — 2 -
CHEMBL123323 — — 2 -
CHEMBL125484 — — 2 -
CHEMBL338173 — — 2 -
CHEMBL124607 — — 2 -
CHEMBL121887 — — 2 -
CHEMBL122228 — — 2 -
CHEMBL331789 — — 2 -
CHEMBL222519 NBQX — 2 -
CHEMBL121886 — — 2 -
CHEMBL331725 — — 2 -
CHEMBL125536 — — 2 -
CHEMBL123228 — — 2 -
CHEMBL332585 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293206 — IC50 = 370.0 nM 6.43
CHEMBL293206 — IC50 = 370.0 nM 6.43
CHEMBL126006 — IC50 = 620.0 nM 6.21
CHEMBL126006 — IC50 = 620.0 nM 6.21
CHEMBL331547 — IC50 = 860.0 nM 6.07
CHEMBL331547 — IC50 = 860.0 nM 6.07
CHEMBL122313 — IC50 = 930.0 nM 6.03
CHEMBL122054 — IC50 = 930.0 nM 6.03
CHEMBL122054 — IC50 = 930.0 nM 6.03
CHEMBL122313 — IC50 = 930.0 nM 6.03
CHEMBL123766 — IC50 = 1000.0 nM 6.00
CHEMBL123766 — IC50 = 1000.0 nM 6.00
CHEMBL122997 — IC50 = 1300.0 nM 5.89
CHEMBL432224 — IC50 = 1300.0 nM 5.89
CHEMBL122997 — IC50 = 1300.0 nM 5.89
CHEMBL432224 — IC50 = 1300.0 nM 5.89
CHEMBL125054 — IC50 = 1400.0 nM 5.85
CHEMBL121771 — IC50 = 1400.0 nM 5.85
CHEMBL121771 — IC50 = 1400.0 nM 5.85
CHEMBL125054 — IC50 = 1400.0 nM 5.85
CHEMBL125159 — IC50 = 4000.0 nM 5.40
CHEMBL125159 — IC50 = 4000.0 nM 5.40
CHEMBL341228 — IC50 = 4300.0 nM 5.37
CHEMBL341228 — IC50 = 4300.0 nM 5.37
CHEMBL333463 — IC50 = 4900.0 nM 5.31
CHEMBL333463 — IC50 = 4900.0 nM 5.31
CHEMBL122082 — IC50 = 5000.0 nM 5.30
CHEMBL122082 — IC50 = 5000.0 nM 5.30
CHEMBL123259 — IC50 = 20000.0 nM 4.70
CHEMBL123259 — IC50 = 20000.0 nM 4.70
CHEMBL330790 — IC50 = 50000.0 nM 4.30
CHEMBL330790 — IC50 = 50000.0 nM 4.30
CHEMBL122228 — IC50 > 10000.0 nM -
CHEMBL122228 — IC50 > 10000.0 nM -
CHEMBL125484 — IC50 > 10000.0 nM -
CHEMBL124607 — IC50 > 100000.0 nM -
CHEMBL123087 — IC50 > 100000.0 nM -
CHEMBL125536 — IC50 > 10000.0 nM -
CHEMBL331789 — IC50 > 10000.0 nM -
CHEMBL123323 — IC50 > 10000.0 nM -
CHEMBL123228 — IC50 > 100000.0 nM -
CHEMBL338173 — IC50 > 100000.0 nM -
CHEMBL332585 — IC50 > 10000.0 nM -
CHEMBL121888 — IC50 = 267000.0 nM -
CHEMBL332585 — IC50 > 10000.0 nM -
CHEMBL125536 — IC50 > 10000.0 nM -
CHEMBL121888 — IC50 = 267000.0 nM -
CHEMBL122811 — IC50 > 100000.0 nM -
CHEMBL122811 — IC50 > 100000.0 nM -
CHEMBL123228 — IC50 > 100000.0 nM -