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Assay Detail

CHEMBL748198

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

Binding
Tested for the inhibitory activity by the inhibition of excitatory L-[3H]Glutamate binding to NMDA recognition sites
7
Total Activities
7
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

Enzymatic asymmetric synthesis of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a potent, selective and competitive NMDA antagonist
Hamilton G, Huang Z, Patch R, Narayanan B, Ferkany J
Bioorg Med Chem Lett (1993) 3 : 27 -32
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.05 7.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29811 CGP-37849 1 7.59
CHEMBL47277 1 6.49
CHEMBL107660 1 6.22
CHEMBL322304 1 5.80
CHEMBL108823 1 5.59
CHEMBL108096 1 5.50
CHEMBL107961 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29811 CGP-37849 IC50 = 25.7 nM 7.59
CHEMBL47277 IC50 = 321.0 nM 6.49
CHEMBL107660 IC50 = 607.0 nM 6.22
CHEMBL322304 IC50 = 1600.0 nM 5.80
CHEMBL108823 IC50 = 2589.0 nM 5.59
CHEMBL108096 IC50 = 3132.0 nM 5.50
CHEMBL107961 IC50 = 6458.0 nM 5.19