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Assay Detail

CHEMBL745939

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.
32
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)-ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors.
Cai SX, Zhou ZL, Huang JC, Whittemore ER, Egbuwoku ZO, Hawkinson JE, Woodward RM, Weber E, Keana JF.
J Med Chem (1996) 39 : 4682 -4686
PubMed 8917657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.29 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288855 1 8.15
CHEMBL40623 1 7.92
CHEMBL291161 1 7.66
CHEMBL43846 2 7.52
CHEMBL42915 1 7.48
CHEMBL42146 1 7.43
CHEMBL295154 1 7.28
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE 1 6.89
CHEMBL42176 1 6.66
CHEMBL282003 1 6.55
CHEMBL41340 1 6.54
CHEMBL41341 1 6.40
CHEMBL42329 1 6.20
CHEMBL289779 1 6.14
CHEMBL291169 1 6.04
CHEMBL42071 1 5.85
CHEMBL21641 2 5.75
CHEMBL296068 1 5.68
CHEMBL291170 1 5.48
CHEMBL43318 1 5.47
CHEMBL42057 1 5.36
CHEMBL282672 1 5.01
CHEMBL296577 1 4.47
CHEMBL298232 1 4.40
CHEMBL288904 1 4.21
CHEMBL44079 1 -
CHEMBL41538 1 -
CHEMBL296558 1 -
CHEMBL295179 1 -
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
CHEMBL291161 IC50 = 22.0 nM 7.66
CHEMBL43846 IC50 = 30.0 nM 7.52
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
CHEMBL42176 IC50 = 220.0 nM 6.66
CHEMBL282003 IC50 = 280.0 nM 6.55
CHEMBL41340 IC50 = 290.0 nM 6.54
CHEMBL41341 IC50 = 400.0 nM 6.40
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
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
CHEMBL296577 IC50 = 34000.0 nM 4.47
CHEMBL298232 IC50 = 40000.0 nM 4.40
CHEMBL288904 IC50 = 61000.0 nM 4.21
CHEMBL41538 IC50 > 100000.0 nM -
CHEMBL44079 IC50 > 100000.0 nM -
CHEMBL296558 IC50 > 100000.0 nM -
CHEMBL295179 IC50 > 100000.0 nM -
CHEMBL43918 IC50 > 100000.0 nM -