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Assay Detail

CHEMBL752467

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

Binding
Inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor
88
Total Activities
86
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

CoMFA and homology-based models of the glycine binding site of N-methyl-d-aspartate receptor.
Tikhonova IG, Baskin II, Palyulin VA, Zefirov NS.
J Med Chem (2003) 46 : 1609 -1616
PubMed 12699379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 88 6.04 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297881 1 8.33
CHEMBL289832 LICOSTINEL 2.0 1 8.23
CHEMBL288855 1 8.15
CHEMBL42426 1 8.06
CHEMBL40623 1 7.92
CHEMBL40976 1 7.64
CHEMBL40652 1 7.54
CHEMBL41460 1 7.54
CHEMBL43846 1 7.52
CHEMBL42915 1 7.48
CHEMBL42146 1 7.43
CHEMBL41691 1 7.35
CHEMBL295154 1 7.28
CHEMBL42248 1 7.19
CHEMBL288839 1 7.14
CHEMBL291149 1 7.09
CHEMBL291148 1 7.02
CHEMBL41291 1 6.96
CHEMBL40745 1 6.89
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE 2 6.89
CHEMBL42466 1 6.82
CHEMBL295995 1 6.82
CHEMBL41295 1 6.80
CHEMBL40708 1 6.77
CHEMBL291161 1 6.66
CHEMBL42176 1 6.66
CHEMBL282003 1 6.55
CHEMBL41340 1 6.54
CHEMBL41341 1 6.40
CHEMBL42329 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297881 IC50 = 4.7 nM 8.33
CHEMBL289832 LICOSTINEL IC50 = 5.9 nM 8.23
CHEMBL288855 IC50 = 7.0 nM 8.15
CHEMBL42426 IC50 = 8.7 nM 8.06
CHEMBL40623 IC50 = 12.0 nM 7.92
CHEMBL40976 IC50 = 23.0 nM 7.64
CHEMBL40652 IC50 = 29.0 nM 7.54
CHEMBL41460 IC50 = 29.0 nM 7.54
CHEMBL43846 IC50 = 30.0 nM 7.52
CHEMBL42915 IC50 = 33.0 nM 7.48
CHEMBL42146 IC50 = 37.0 nM 7.43
CHEMBL41691 IC50 = 45.0 nM 7.35
CHEMBL295154 IC50 = 53.0 nM 7.28
CHEMBL42248 IC50 = 64.0 nM 7.19
CHEMBL288839 IC50 = 73.0 nM 7.14
CHEMBL291149 IC50 = 82.0 nM 7.09
CHEMBL291148 IC50 = 95.0 nM 7.02
CHEMBL41291 IC50 = 110.0 nM 6.96
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE IC50 = 130.0 nM 6.89
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE IC50 = 130.0 nM 6.89
CHEMBL40745 IC50 = 130.0 nM 6.89
CHEMBL42466 IC50 = 150.0 nM 6.82
CHEMBL295995 IC50 = 150.0 nM 6.82
CHEMBL41295 IC50 = 160.0 nM 6.80
CHEMBL40708 IC50 = 170.0 nM 6.77
CHEMBL42176 IC50 = 220.0 nM 6.66
CHEMBL291161 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
CHEMBL41399 IC50 = 640.0 nM 6.19
CHEMBL289779 IC50 = 730.0 nM 6.14
CHEMBL288384 IC50 = 780.0 nM 6.11
CHEMBL291169 IC50 = 910.0 nM 6.04
CHEMBL553334 IC50 = 1000.0 nM 6.00
CHEMBL42071 IC50 = 1400.0 nM 5.85
CHEMBL42482 IC50 = 1400.0 nM 5.85
CHEMBL42350 IC50 = 1500.0 nM 5.82
CHEMBL295178 IC50 = 1500.0 nM 5.82
CHEMBL44260 IC50 = 1800.0 nM 5.75
CHEMBL21641 IC50 = 1800.0 nM 5.75
CHEMBL42694 IC50 = 1800.0 nM 5.75
CHEMBL40649 IC50 = 1900.0 nM 5.72
CHEMBL296068 IC50 = 2100.0 nM 5.68
CHEMBL290747 IC50 = 2800.0 nM 5.55
CHEMBL297310 IC50 = 2900.0 nM 5.54
CHEMBL41180 IC50 = 3000.0 nM 5.52
CHEMBL296521 IC50 = 3100.0 nM 5.51
CHEMBL295084 IC50 = 3300.0 nM 5.48