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Assay Detail

CHEMBL746729

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

Binding
Inhibition of [3H]- DCKA binding to NMDA receptor of rat brain membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes: novel and highly potent antagonists for NMDA receptor glycine site.
Cai SX, Zhou ZL, Huang JC, Whittemore ER, Egbuwoku ZO, Lü Y, Hawkinson JE, Woodward RM, Weber E, Keana JF.
J Med Chem (1996) 39 : 3248 -3255
PubMed 8765507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.47 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288855 1 8.15
CHEMBL40623 1 7.92
CHEMBL43846 1 7.52
CHEMBL42915 1 7.48
CHEMBL42146 1 7.43
CHEMBL295154 1 7.28
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE 1 6.89
CHEMBL40708 1 6.77
CHEMBL282003 1 6.55
CHEMBL42329 1 6.20
CHEMBL289779 1 6.14
CHEMBL291169 1 6.04
CHEMBL42071 1 5.85
CHEMBL21641 1 5.75
CHEMBL296068 1 5.68
CHEMBL291170 1 5.48
CHEMBL43318 1 5.47
CHEMBL42057 1 5.36
CHEMBL282672 1 5.01
CHEMBL43918 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288855 IC50 = 7.0 nM 8.15
CHEMBL40623 IC50 = 12.0 nM 7.92
CHEMBL43846 IC50 = 30.0 nM 7.52
CHEMBL42915 IC50 = 33.0 nM 7.48
CHEMBL42146 IC50 = 37.0 nM 7.43
CHEMBL295154 IC50 = 53.0 nM 7.28
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE IC50 = 130.0 nM 6.89
CHEMBL40708 IC50 = 170.0 nM 6.77
CHEMBL282003 IC50 = 280.0 nM 6.55
CHEMBL42329 IC50 = 630.0 nM 6.20
CHEMBL289779 IC50 = 730.0 nM 6.14
CHEMBL291169 IC50 = 910.0 nM 6.04
CHEMBL42071 IC50 = 1400.0 nM 5.85
CHEMBL21641 IC50 = 1800.0 nM 5.75
CHEMBL296068 IC50 = 2100.0 nM 5.68
CHEMBL291170 IC50 = 3300.0 nM 5.48
CHEMBL43318 IC50 = 3400.0 nM 5.47
CHEMBL42057 IC50 = 4400.0 nM 5.36
CHEMBL282672 IC50 = 9800.0 nM 5.01
CHEMBL43918 IC50 > 100000.0 nM -