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Assay Detail

CHEMBL751182

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

Binding
Inhibitory activity evaluated by its ability to displace [3H]CPP from rat cortical membrane receptor at 10E-5 concentration of the compound
5
Total Activities
5
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 (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
Bigge CF, Johnson G, Ortwine DF, Drummond JT, Retz DM, Brahce LJ, Coughenour LL, Marcoux FW, Probert AW.
J Med Chem (1992) 35 : 1371 -1384
PubMed 1533423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.31 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29244 1 7.19
CHEMBL22304 1 7.10
CHEMBL29255 1 6.00
CHEMBL27735 1 5.64
CHEMBL28609 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29244 IC50 = 65.0 nM 7.19
CHEMBL22304 IC50 = 79.0 nM 7.10
CHEMBL29255 IC50 = 1000.0 nM 6.00
CHEMBL27735 IC50 = 2300.0 nM 5.64
CHEMBL28609 IC50 = 2400.0 nM 5.62