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Assay Detail

CHEMBL872738

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

Binding
In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay
29
Total Activities
29
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

5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, Schmutz M.
Bioorg Med Chem Lett (2002) 12 : 1099 -1102
PubMed 11909726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.76 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12513 1 9.10
CHEMBL12804 1 9.00
CHEMBL12242 1 8.92
CHEMBL537478 1 8.82
CHEMBL273662 1 8.82
CHEMBL274422 1 8.82
CHEMBL269683 1 8.77
CHEMBL536107 1 8.70
CHEMBL552664 1 8.52
CHEMBL557993 1 8.39
CHEMBL12256 1 8.13
CHEMBL273636 1 8.10
CHEMBL275906 1 8.09
CHEMBL268920 1 8.01
CHEMBL275966 1 7.77
CHEMBL12414 1 7.57
CHEMBL273686 1 7.51
CHEMBL276670 1 7.42
CHEMBL543722 1 7.40
CHEMBL543489 1 7.22
CHEMBL543252 1 7.19
CHEMBL536106 1 7.10
CHEMBL12301 1 6.92
CHEMBL12546 1 6.89
CHEMBL12733 1 6.80
CHEMBL12706 1 6.60
CHEMBL268714 1 6.43
CHEMBL273889 1 6.07
CHEMBL12728 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12513 IC50 = 0.8 nM 9.10
CHEMBL12804 IC50 = 1.0 nM 9.00
CHEMBL12242 IC50 = 1.2 nM 8.92
CHEMBL537478 IC50 = 1.5 nM 8.82
CHEMBL273662 IC50 = 1.5 nM 8.82
CHEMBL274422 IC50 = 1.5 nM 8.82
CHEMBL269683 IC50 = 1.7 nM 8.77
CHEMBL536107 IC50 = 2.0 nM 8.70
CHEMBL552664 IC50 = 3.0 nM 8.52
CHEMBL557993 IC50 = 4.1 nM 8.39
CHEMBL12256 IC50 = 7.4 nM 8.13
CHEMBL273636 IC50 = 8.0 nM 8.10
CHEMBL275906 IC50 = 8.1 nM 8.09
CHEMBL268920 IC50 = 9.7 nM 8.01
CHEMBL275966 IC50 = 17.0 nM 7.77
CHEMBL12414 IC50 = 27.0 nM 7.57
CHEMBL273686 IC50 = 31.0 nM 7.51
CHEMBL276670 IC50 = 38.0 nM 7.42
CHEMBL543722 IC50 = 40.0 nM 7.40
CHEMBL543489 IC50 = 60.0 nM 7.22
CHEMBL543252 IC50 = 65.0 nM 7.19
CHEMBL536106 IC50 = 80.0 nM 7.10
CHEMBL12301 IC50 = 120.0 nM 6.92
CHEMBL12546 IC50 = 130.0 nM 6.89
CHEMBL12733 IC50 = 160.0 nM 6.80
CHEMBL12706 IC50 = 250.0 nM 6.60
CHEMBL268714 IC50 = 370.0 nM 6.43
CHEMBL273889 IC50 = 860.0 nM 6.07
CHEMBL12728 IC50 = 1100.0 nM 5.96